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Kinase products by group:AGC Group ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .4
CAMK Group ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .7
CK1 Group.... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .9
CMGC Group ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10
STE Group ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 14
TK Group ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15
TKL Group ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19
Other Protein Kinases ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 21
Atypical Kinases ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 22
Lipid Kinases ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 23
Broad Spectrum Kinase Inhibitors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 24
Phosphatases ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 25
Greater CelandineChelidonium majusA source of Chelerythrine
KinasesProduct Listing | Edition 2
High Performance Life Science Reagents
Tocris Product Listing Series
2 |
PROTEIN KINASES
AGC Group (Protein Kinases A, G and C) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .4
Akt/PKB ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 4
PDK1 ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 4
PKA ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 5
PKC ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 5
PKG ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 6
ROCK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 6
RSK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 6
SGK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 6
CAMK Group (Calcium/Calmodulin-dependent Kinases) . . . . . . . . .7
AMPK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 7
CaMK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 7
Chk ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 7
DAPK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 8
MK2 ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 8
MLCK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 8
Mnk ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 8
Pim ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 8
PKD ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 8
CK1 Group (Casein Kinase 1) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 9
CK1 ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 9
CMGC Group (CDK, MAPK, GSK-3 and Clk) . . . . . . . . . . . . . . . . . . . . . . . 10
CDK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10
CK2 ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 11
Clk ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 11
ERK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 11
GSK-3 ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 11
JNK/c-Jun ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 12
p38 MAPK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 12
STE Group (Homologs of Yeast STE7, STE11 and STE20). . . . 14
ASK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 14
MEK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 14
PAK.... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 14
TK Group (Tyrosine Kinases) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15
Abl .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15
BTK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15
EGFR ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15
FAK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 16
FGFR ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 16FLT3 ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 16IRs and IGFRs ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 16JAK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 17MET Receptor .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 17PDGFR ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 17Src ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 18Syk ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 18Trk Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 18VEGFR ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 18Other RTKs ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 18Multi-TK Inhibitors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 18
TKL Group (Tyrosine Kinase-like) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19BMP and Other Activin Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19LRRK2 ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19Raf .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19RIPK1 ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19TAK1.... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19TGF-b Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19
Other Protein Kinases . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 21Aurora Kinase ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 21CaMKK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 21IKK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 21Mps1 ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 21PLK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 21
ATYPICAL & LIPID KINASES
Atypical Kinases . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 22ATM and ATR ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 22DNA-PK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 22eEF-2 Kinase ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 22mTOR ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 22
Lipid Kinases . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 23CerK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 23DGK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 23PI 3-K ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 23SphK ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 23
OTHER
Broad Spectrum Kinase Inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 24
Phosphatases. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 25
ContentsThis listing contains over 300 products from Tocris, including a wide range of protein kinase inhibitors divided into their respective kinome groups: AGC, CAMK, CK1, CMGC, STE, TK and TKL. Atypical, lipid and broad spectrum kinase inibitors are also listed, alongside phosphatase inhibitors.
KINASES
www.tocris.com | 3
IntroductionKinases act as integral mediators of signal transduction. They modify their substrate(s) by adding phosphate groups from ATP. There are over 500 known kinases, encoded by ~1.7% of all human genes. They constitute the second largest set of drug targets after G-protein-coupled receptors. The structural and functional relationships of the known protein kinases – the ‘kinome’ – are represented below (Figure 1). Key kinases within each kinome group are highlighted; inhibitors, activators and substrates for these kinases may be found within this product listing, alongside products targeting lipid kinases and phosphatases.
Phosphorylation is an important post-translational modification, affecting not only the activity of the modified substrate, but also its intracellular location, degradation and interaction with other molecules. Kinases are involved in a variety of cellular processes, such as control of the cell cycle and cell proliferation, induction of apoptosis, and regulation of cell metabolism.
Tocris has a unique collection of kinase products, from established standards to exclusive licensed compounds. For more information, please visit www.tocris.com.
STE Group
CK1 Group
AGC Group
CAMK Group
CMGC Group
Other Protein Kinases
Lyn
Lck Abl
EphB4
FAK
IGF1RTRK
FGFR
PDGFR
EGFR
JAK
RIPK1
LRRK2
TGFβRIBMPR1
MEKK
ASK
PAK
MEK
Wee1
IKKCAMKK
PLK
Aurora
RSK
Akt/PKB SGK
PKC
PKA
ROCK
CAMK2
MNKPKD
DAPK
MLCK
Pim
CHK1
CK2
CLK2 GSK3
p38
JNK CDK
TK Group
TKL Group
Adapted from Manning et al (2002) Science 298 1912.
Figure 1 | A representation of the human protein kinome
Tocris Product Listing Series
4 |
AGC GroupThe AGC group is named after three of its substituents – cAMP-dependent (protein kinase A, PKA), c-GMP-dependent (PKG) and protein kinase C (PKC). Members of this group preferentially phosphorylate serine/threonine residues close to arginine and lysine, the basic residues.
Highly Potent, Selective PDK1 Inhibitor
GSK 2334470 Cat. No. 4143
NO
NH N N
NHMe
NH
N
NH2
OHN
N
N
N
N O
N
H2N
O
O
N
O
GSK 2334470 is a potent 3-phosphoinositide-dependent protein kinase (PDK1) inhibitor (IC50 ~ 10 nM). The compound exhibits no effects on other kinases including Aurora, ROCK, p38 MAPK and PI 3-K. GSK 2334470 suppresses T-loop phosphorylation and subsequent activation of PDK1 substrates S6K1, SGK and RSK in HEK293, U87 and mouse embryonic fibroblast cell lines; it exhibits limited inhibitory effect on Akt activation.
(Sold for research purposes under agreement from GlaxoSmithKline)
Potent and Selective ROCK Inhibitor
GSK 269962 Cat. No. 4009
NO
NH N N
NHMe
NH
N
NH2
OHN
N
N
N
N O
N
H2N
O
O
N
O
GSK 269962 is a potent Rho kinase (ROCK) inhibitor (IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively). The compound displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases. GSK 269962 induces vasorelaxation in preconstricted rat aorta (IC50 = 35 nM) and lowers blood pressure in a rat model of hypertension.
(Sold for research purposes under agreement from GlaxoSmithKline)
Category Cat. No. Product Name Description Unit Size USD
Akt/PKB (Protein Kinase B)
Inhibitors 3897 API-1 Selective Akt/PKB inhibitor. Antitumor 10 mg 269
2151 API-2 Selective inhibitor of Akt/PKB signaling. Antitumor and antiviral 10 mg 245
2558 10-DEBC Selective Akt/PKB inhibitor 10 mg
50 mg
115
439
2926 FPA 124 Akt/PKB inhibitor 10 mg
50 mg
155
619
4144 GSK 690693 Akt kinase inhibitor. Antitumor 10 mg
50 mg
245
1029
4398 SC 66 Allosteric Akt inhibitor 10 mg
50 mg
79
325
Substrates 1353 Akt/SKG Substrate Peptide Akt/PKB substrate (synthetic) 1 mg 155
PDK1 (3-phosphoinositide-dependent Kinase 1)
Activators 4087 PS 48 PDK1 activator 10 mg
50 mg
105
409
Inhibitors 3606 BAG 956 Dual PDK1 and PI 3-kinase inhibitor 10 mg
50 mg
209
875
4318 BX 795 PDK1 inhibitor 10 mg
50 mg
179
759
4143 GSK 2334470 Highly potent, selective PDK1 inhibitor 10 mg
50 mg
199
845
KINASES
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AGC Group – continued
NN
NH
OH Me
O
HOO
O
KT 5720 (1288)Selective protein kinase A inhibitor
HN OO
NH
NMe2N
GF 109203X (0741)Protein kinase C inhibitor
Myr-Ser-Ile-Tyr-Arg-Arg-Gly-Ala-Arg-Arg-Trp-Arg-Lys-Leu
ZIP (2549)Cell permeable inhibitior of atypical PKC
isozyme PKMζ
NNN
N
NHN
CF3
PF 4708671 (4032)S6K1 inhibitor
N NH
CO2H
GSK 650394 (3572)Serum- and glucocorticoid-regulated kinase (SGK) inhibitor
Key AGC Kinase Inhibitors
Category Cat. No. Product Name Description Unit Size USD
PKA (Protein Kinase A)
Activators 1140 8-Bromo-cAMP Cell permeable cAMP analog; activates PKA 10 mg
50 mg
59
205
1333 cAMPS-Sp Cell permeable cAMP analog; activates PKA 1 mg 125
Inhibitors 1337 cAMPS-Rp cAMP antagonist; inhibits PKA activation 1 mg 125
2910 H 89 Protein kinase A inhibitor 1 mg
10 mg
50 mg
69
169
675
1288 KT 5720 Selective protein kinase A inhibitor 100 µg 165
1904 PKA inhibitor fragment (6-22) amide Potent protein kinase A inhibitor 1 mg 155
2546 PKI 14-22 amide, myristoylated Cell permeable protein kinase A inhibitor 1 mg 115
PKC (Protein Kinase C)
Activators 2383 Bryostatin 1 Protein kinase C activator 10 µg 125
3091 FR 236924 Selective PKCe activator 10 mg 145
3651 (-)-Indolactam V Protein kinase C activator 1 mg 239
4054 PEP 005 Protein kinase C activator 1 mg 179
4153 Phorbol 12,13-dibutyrate Protein kinase C activator 1 mg 55
1201 Phorbol 12-myristate 13-acetate Protein kinase C activator 1 mg
5 mg
59
205
1887 PKC Fragment (530-558) Potent activator of protein kinase C 1 mg 189
1790 Pseudo RACK1 PKC activator peptide (attached to cell permeable vector) 1 mg 279
Inhibitors 4128 Bisindolylmaleimide II Potent PKC inhibitor and nicotinic receptor antagonist 10 mg
50 mg
169
795
0543 C-1 Protein kinase C inhibitor 10 mg
50 mg
125
559
1626 Calphostin C Potent, selective and photo-dependent PKC inhibitor 100 µg 165
2442 CGP 53353 Selective inhibitor of PKCbII 10 mg 209
1330 Chelerythrine Cell permeable protein kinase C inhibitor 5 mg 125
0749 Dihydrosphingosine Protein kinase C inhibitor 10 mg 125
Tocris Product Listing Series
6 |
AGC Group – continued
Category Cat. No. Product Name Description Unit Size USD
0741 GF 109203X Protein kinase C inhibitor 1 mg
10 mg
79
169
2253 Go 6976 Potent protein kinase C inhibitor; selective for α and b isozymes 1 mg 189
2285 Go 6983 Broad spectrum PKC inhibitor 1 mg
10 mg
95
209
2287 K-252c Protein kinase C inhibitor 1 mg 145
1193 Melittin Inhibits protein kinase C and cAMP-dependent protein kinase 500 µg 125
0609 (±)-Palmitoylcarnitine Protein kinase C inhibitor 50 mg 105
4058 PKC (19-36) Pseudosubstrate peptide; inhibitor of PKC 1 mg 119
2992 PKC 412 Protein kinase C inhibitor 1 mg 155
1792 PKC b pseudosubstrate Selective cell-permeable PKC inhibitor peptide (attached to vector) 1 mg 279
1791 PKC z pseudosubstrate PKC z inhibitor peptide (attached to cell permeable vector) 1 mg 279
1587 Ro 32-0432 Potent, orally active PKC inhibitor 1 mg 179
1610 Rottlerin Reported PKCd inhibitor 10 mg
50 mg
79
325
0633 D-erythro-Sphingosine (synthetic) Protein kinase C inhibitor 10 mg 79
2549 ZIP Cell permeable inhibitor of atypical PKC isozyme PKMz 1 mg 179
3290 ZIP, Biotinylated Biotinylated peptide for ZIP (Cat. No. 2549) 1 mg 229
3215 ZIP (Scrambled) Control peptide for ZIP (Cat. No. 2549) 1 mg 179
PKG (Protein Kinase G)
Inhibitors 3028 Rp-8-Br-PET-cGMPS Protein kinase G inhibitor 560 µg 169
1289 KT 5823 Selective protein kinase G inhibitor 100 µg 165
ROCK (Rho-kinases)
Inhibitors 0541 Fasudil Inhibitor of cyclic nucleotide dependent- and Rho-kinases 10 mg
50 mg
125
525
4009 GSK 269962 Potent and selective ROCK inhibitor 10 mg
50 mg
219
909
3726 GSK 429286 Selective Rho-kinase (ROCK) inhibitor 1 mg
10 mg
50 mg
85
225
945
2485 Glycyl-H 1152 Selective Rho-kinase (ROCK) inhibitor. More selective analog of H 1152 (Cat. No. 2414)
1 mg 219
2414 H 1152 Selective Rho-kinase (ROCK) inhibitor 1 mg 179
4118 SB 772077B Potent Rho-kinase inhibitor; vasodilator 10 mg
50 mg
225
945
3667 SR 3677 Potent, selective Rho-kinase (ROCK) inhibitor 10 mg
50 mg
209
875
1254 Y-27632 Selective p160ROCK inhibitor 1 mg
10 mg
50 mg
85
225
945
RSK (Ribosomal S6 Protein Kinase)
Inhibitors 4037 BRD 7389 p90 ribosomal S6 kinase inhibitor 10 mg
50 mg
169
675
4032 PF 4708671 S6K1 inhibitor 10 mg
50 mg
179
819
2250 SL 0101-1 Selective p90 ribosomal S6 kinase (RSK) inhibitor 1 mg 265
SGK (Serum- and Glucocorticoid-regulated Kinase)
Inhibitors 3572 GSK 650394 Serum- and glucocorticoid-regulated kinase (SGK) inhibitor 10 mg
50 mg
179
735
KINASES
www.tocris.com | 7
CAMK GroupThe CAMK group of protein kinases contains kinases that are primarily regulated by calcium/calmodulin signaling. Members include calcium/calmodulin-dependent protein kinase (CaMK), AMPK and Pim kinase. Like AGC kinases, these kinases tend to modify substrates containing basic residues.
Potent AMPK Activator
A 769662 Cat. No. 3336
SNH
OH
O
HOCN
N
NN
N
ON
A 769662 is a potent, reversible AMP-activated protein kinase (AMPK activator (EC50 = 0.8 μM) that displays selectivity towards b1 subunit-containing heterotrimers. The compound inhibits fatty acid synthesis (IC50 = 3.2 μM) and decreases plasma glucose and triglyceride levels in vivo.
Selective AMPK Activator
Dorsomorphin Cat. No. 3093
SNH
OH
O
HOCN
N
NN
N
ON
Dorsomorphin is a selective inhibitor of AMP-activated protein kinase (AMPK) (Ki = 109 nM). The compound displays no significant activity on several structurally related kinases, including ZAPK, SYK, PKCθ, PKA and JAK3. Dorsomorphin inhibits AMPK activation induced by AICAR (Cat. No. 2840) and metformin (Cat. No. 2684); it also inhibits bone morphogenic protein (BMP) type I receptors (ALK2, ALK3 and ALK6).
Category Cat. No. Product Name Description Unit Size USD
AMPK (AMP-activated Protein Kinase)
Activators 3336 A 769662 Potent AMPK activator 10 mg
50 mg
169
705
2840 AICAR AMPK activator 50 mg 99
3713 Cryptotanshinone Activates AMPK. Also displays multiple other activities 10 mg
50 mg
115
469
2864 Metformin Activator of LKB1/AMPK; antidiabetic agent 100 mg 59
4039 PT 1 AMPK activator 10 mg
50 mg
175
735
Inhibitors 3093 Dorsomorphin Selective AMPK inhibitor 10 mg
50 mg
169
705
CaMK (Calmodulin-dependent Kinase)
Inhibitors 2457 Arcyriaflavin A Potent CaM Kinase II and cdk4/cyclin D1 inhibitor. Antiviral agent 10 mg 179
1688 Autocamtide-2-related inhibitory peptide
Selective CaM kinase II inhibitor 1 mg 209
1277 KN-62 CaM kinase II inhibitor 1 mg 125
1278 KN-93 CaM kinase II inhibitor. Also K+ channel blocker (KV) 1 mg 169
Chk (Checkpoint Kinases)
Activators 4502 DIM Activates Chk2; induces G2/M cell cycle arrest 50 mg 39
Inhibitors 3034 NSC 109555 Selective Chk2 inhibitor 10 mg
50 mg
145
645
2694 PD 407824 Selective inhibitor of Chk1 and Wee1 1 mg
10 mg
95
209
4277 PF 477736 Selective Chk1 inhibitor 10 mg
50 mg
219
909
2560 SB 218078 Inhibitor of checkpoint kinase 1 (Chk1) 1 mg
10 mg
105
245
3038 TCS 2312 Potent Chk1 inhibitor 1 mg 169
Tocris Product Listing Series
8 |
CAMK Group – continued
SB 218078 (2560) Chk1 inhibitor
NN
HN OO
O
PF 477737 (4277) Selective Chk1 inhibitor
N
HN
NH
NH
O
NHO
NN
2
NSC 109555 (3034) Selective Chk2 inhibitor
NH
NH
O
NNH
NHHN
NHN
N NH 22
CGP 57380 (2731) Selective inhibitor of Mnk1
N
N NH
N
HN
F
NH2
N
NO
O
N
NH2
O
NH2
A 484954 (4483)CaM kinase III (eEF-2 kinase) inhibitor
N
S NH
HN
O
N
PF 3644022 (4279)Potent MK2 inhibitor
Key CAMK Group Inhibitors
Category Cat. No. Product Name Description Unit Size USD
DAPK (Death Associated Protein Kinase)
Inhibitors 4301 TC-DAPK 6 Potent and selective inhibitor of DAPK1 10 mg
50 mg
89
355
Substrates 1458 DAPK Substrate Peptide Death associated protein kinase substrate (synthetic) 1 mg 125
MK2 (MAPK-activated Protein Kinase 2)
Inhibitors 4279 PF 3644022 Potent MK2 inhibitor 10 mg 235
3140 PHA 767491 MK2 inhibitor. Also inhibits cdc7/cdk9 10 mg
50 mg
125
495
MLCK (Myosin Light Chain Kinase)
Inhibitors 4310 ML 7 Selective inhibitor of myosin light chain kinase 10 mg
50 mg
105
409
0431 ML 9 Myosin light chain kinase inhibitor 10 mg
50 mg
125
495
1885 MLCK inhibitor peptide 18 Selective inhibitor of myosin light chain kinase 1 mg 95
0369 W-7 Myosin light chain kinase inhibitor. Calmodulin antagonist 100 mg 115
Mnk (MAPK-interacting Kinase)
Inhibitors 4500 Cercosporamide Potent Mnk2 inhibitor; also inhibits JAK3 500 µg 169
2731 CGP 57380 Selective inhibitor of Mnk1 1 mg
10 mg
50 mg
79
179
735
Pim Kinase
Inhibitors 3589 PIM-1 Inhibitor 2 Pim-1 kinase inhibitor 10 mg
50 mg
125
525
4592 R8-T198wt Pim-1 kinase inhibitor 1 mg 85
2979 TCS PIM-1 1 Selective, ATP-competitive Pim-1 kinase inhibitor 10 mg
50 mg
135
595
3714 TCS PIM-1 4a Selective, ATP-competitive Pim kinase inhibitor 10 mg
50 mg
105
409
PKD (Protein Kinase D)
Inhibitors 4644 CID 2011756 Pan protein kinase D (PKD) inhibitor; cell permeable 10 mg
50 mg
189
819
3327 CID 755673 Selective protein kinase D inhibitor 10 mg 199
3962 kb NB 142-70 Selective PKD inhibitor; analog of CID 755673 (Cat. No. 3327) 10 mg
50 mg
199
845
KINASES
www.tocris.com | 9
CK1 GroupThe casein kinase 1 (CK1) family is a small group of serine/threonine kinases that play an important role in a variety of signal transduction pathways, including Wnt signaling, DNA repair and control of cell differentiation and proliferation. Deregulation of CK1 has been linked to cancer, Alzheimer’s and Parkinson’s disease.
Licensing at TocrisTocris Bioscience has a long tradition of working with scientists to bring new discoveries out of the laboratory and into the commercial arena. We work in partnership with many scientists within both Universities and pharmaceutical companies to bring life science tools to the global research community.
Tocris policy has always been to never knowingly infringe third party intellectual property. It is our intention to remain a responsible and ethical supplier, and work with the scientific community.
Our ExpertiseOur licensing department has significant experience of drafting contracts and has successfully executed licenses with a multitude of licensors, including:
• Large multi-disciplinary licensing departments
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• Individual researchers
Contact UsTo discuss licensing opportunities, please contact our licensing team at licensing@tocris.co.uk
D 4476 (2902)Selective CK1 inhibitor. Also inhibits TGF-βRI
PF 4800567 (4281)Selective CK1ε inhibitor
NH
N
N
O
NH2
O
O
N
N
NN
NH2
O
O Cl
N
N
N
N
NH2
F
PF 670462 (3316)Selective CK1ε and CK1δ inhibitor
Box 3: CK1 Group Inhibitors
Category Cat. No. Product Name Description Unit Size USD
CK1 (Casein Kinase 1)
Inhibitors 3605 (R)-CR8 Dual cdk/CK1 inhibitor 10 mg
50 mg
209
875
2902 D 4476 Selective CK1 inhibitor. Also inhibits TGF-bRI 10 mg
50 mg
179
759
3610 (R)-DRF053 Dual CK1/cdk inhibitor 10 mg
50 mg
209
875
4281 PF 4800567 Selective CK1e inhibitor 10 mg
50 mg
179
759
3316 PF 670462 Potent and selective CK1e and CK1d inhibitor 10 mg
50 mg
179
735
Tocris Product Listing Series
10 |
CMGC GroupCMGC kinases include: cyclin-dependent kinases (Cdks); mitogen-activated protein kinases (MAPKs); glycogen synthase kinase 3 (GSK-3); and Cdc2-like kinases (Clks), all of which are key components of signaling cascades. The MAPK pathway in particular is one of the best-studied mammalian signaling cascades.
KH CB19 (4262)Selective, potent inhibitor of Clk1 and Clk4
PHA 767491 (3140)Dual cdc7/cdk9 inhibitor. Also inhibits MK2
Ro 3306 (4181)Cdk1 inhibitor
N
Cl
Cl
CO2Et
CNH2N
HN
HN
N
O
S
NO
NH
N
S
Key Cdk and Clk Inhibitors
Category Cat. No. Product Name Description Unit Size USD
Cdk (Cyclin-dependent Kinase)
Inhibitors 2072 Aminopurvalanol A Cyclin-dependent kinase inhibitor 10 mg
50 mg
179
819
2457 Arcyriaflavin A Potent cdk4/cyclin D1 and CaM Kinase II inhibitor. Antiviral agent 10 mg 179
3968 AZD 5438 Potent cdk 1, 2 and 9 inhibitor 10 mg
50 mg
199
845
3605 (R)-CR8 Dual cdk1/cdk5 inhibitor. Also inhibits CK1 10 mg
50 mg
209
875
3610 (R)-DRF053 Dual cdk1/cdk5 inhibitor. Also inhibits CK1 10 mg
50 mg
209
875
1398 Kenpaullone Potent cdk inhibitor. Also inhibits GSK-3 10 mg 155
2152 NSC 625987 Cdk4 inhibitor 10 mg
50 mg
145
645
3135 NU 2058 Cdk1 and cdk2 inhibitor 10 mg
50 mg
135
595
3301 NU 6140 Cdk2 inhibitor 10 mg
50 mg
179
735
1284 Olomoucine Cdk inhibitor 5 mg
25 mg
125
559
4786 PD 0332991 Potent, selective cdk4/6 inhibitor; brain penetrant 10 mg
50 mg
199
845
3140 PHA 767491 Dual cdc7/cdk9 inhibitor. Also inhibits MK2 10 mg
50 mg
125
495
1580 Purvalanol A Cdk inhibitor 10 mg
50 mg
179
819
1581 Purvalanol B Cdk inhibitor 10 mg
50 mg
179
819
4181 Ro 3306 Cdk1 inhibitor 10 mg
50 mg
179
759
2609 Ryuvidine Cdk4 inhibitor 10 mg
50 mg
169
675
4075 SNS 032 Potent cdk2, cdk7 and cdk9 inhibitor 10 mg
50 mg
199
845
2907 SU 9516 Potent cdk2 inhibitor 10 mg
50 mg
125
495
KINASES
www.tocris.com | 11
CMGC Group – continued
N
HN
HN
O
NF3C
OMe
A 1070722 (4431)Highly potent, selective GSK-3 inhibitor
N
N
HN
N
HN
HN
NCN
ClCl
CHIR 99021 (4423)Highly selective GSK-3 inhibitor
HN
NMe
OO
Cl
Cl
SB 216763 (1616)Potent, selective GSK-3 inhibitor
Key GSK-3 Inhibitors
Category Cat. No. Product Name Description Unit Size USD
CK2 (Casein Kinase 2)
Inhibitors 3058 Ellagic acid Selective inhibitor of CK2. Also inhibits glutathione S-transferase 50 mg 65
2275 TBB Selective cell permeable CK2 inhibitor 10 mg
50 mg
79
295
3675 TMCB Dual kinase inhibitor; inhibits CK2 and ERK8 10 mg
50 mg
115
439
4432 TTP 22 High affinity, selective CK2 inhibitor 10 mg
50 mg
155
619
Clk (Cdc2-like Kinase)
Inhibitors 4262 KH CB19 Selective, potent inhibitor of Clk1 and 4 1 mg 79
4336 TG 003 Potent, ATP-competitive inhibitor of Clk-family kinases 10 mg
50 mg
169
705
ERK (Extracellular Signal-regulated Kinase)
Inhibitors 3706 FR 180204 Selective ERK inhibitor 10 mg
50 mg
219
909
4433 Pluripotin Dual ERK1/RasGAP inhibitor. Maintains ESC self-renewal 1 mg 85
4465 TCS ERK 11e Potent and selective ERK2 inhibitor 10 mg 225
3675 TMCB Dual-kinase inhibitor; inhibits CK2 and ERK8 10 mg
50 mg
115
439
4132 XMD 8-92 Selective ERK5/BMK1 inhibitor 10 mg
50 mg
199
845
GSK-3 (Glycogen Synthase Kinase 3)
Inhibitors 4083 3F8 Potent and selective GSK-3b inhibitor 10 mg
50 mg
155
619
4431 A 1070722 Highly potent, selective GSK-3 inhibitor 10 mg
50 mg
169
675
3966 AR-A 014418 Selective GSK-3 inhibitor 10 mg
50 mg
145
645
3194 BIO Potent, selective GSK-3 inhibitor 10 mg
50 mg
135
595
3874 BIO-acetoxime Selective GSK-3α/b inhibitor 1 mg
10 mg
115
245
4423 CHIR 99021 Highly selective GSK-3 inhibitor 10 mg
50 mg
199
819
2235 L803 Substrate-competitive inhibitor of GSK-3 1 mg 155
2256 L803-mts Selective inhibitor of GSK-3 1 mg 189
3873 MeBIO Inactive analog of BIO (Cat. No. 3194) 10 mg 135
1937 NSC 693868 GSK-3 inhibitor. Also inhibits cdks 10 mg
50 mg
169
789
1616 SB 216763 Potent, selective GSK-3 inhibitor 1 mg
10 mg
50 mg
69
145
645
1617 SB 415286 Potent, selective GSK-3 inhibitor 10 mg
50 mg
169
675
Tocris Product Listing Series
12 |
Potent and Selective ERK2 Inhibitor
TCS ERK 11e Cat. No. 4465
N N
HNO
NH
Cl
HO
HN
Cl
F
O
N NH
TCS ERK 11e
SP 600125
NQDI 1
NH
O
O
EtO2C
TCS ERK 11e is a potent and selective extracellular signal-related kinase 2 (ERK2) inhibitor (Ki values are <2, 395, 540 and 852 nM for ERK2, GSK-3, Aurora Kinase A and Cdk2 respectively). The compound potently blocks proliferation of HT29 cells (IC50 = 48 nM) and is orally bioavailable.
Novel and Selective JNK Inhibitor
SP 600125 Cat. No. 1496
N N
HNO
NH
Cl
HO
HN
Cl
F
O
N NH
TCS ERK 11e
SP 600125
NQDI 1
NH
O
O
EtO2C
SP 600125 is a selective inhibitor of c-Jun N-terminal kinase (JNK). The compound competitively and reversibly inhibits JNK1, 2 and 3 (IC50 = 40 - 90 nM) with negligible activity at ERK2, p38b and a range of enzymes (IC50 >10 μM). SP 600125 is active in vivo and protects renal tubular epithelial cells against ischemia/reperfusion-induced apoptosis. This compound is also available as part of the MAPK Inhibitor Tocriset™.
Category Cat. No. Product Name Description Unit Size USD
4353 TC-G 24 Potent and selective GSK-3b inhibitor 10 mg
50 mg
169
705
3869 TCS 2002 Potent GSK-3b inhibitor 10 mg
50 mg
169
789
4221 TCS 21311 GSK-3b inhibitor. Also inhibits PKC and JAK3 10 mg
50 mg
209
875
3835 TWS 119 GSK-3b inhibitor; induces neuronal differentiation in ESCs 10 mg 179
JNK (c-Jun N-terminal Kinase)
Activators 1290 Anisomycin Activates JNK/SAPK/p38 MAP kinase 10 mg
50 mg
79
295
Inhibitors 2651 AEG 3482 Inhibitor of JNK signaling 10 mg
50 mg
115
439
3314 BI 78D3 Selective, competitive JNK inhibitor 10 mg
50 mg
169
675
1989 c-JUN peptide Peptide inhibitor of JNK/c-Jun interaction 1 mg 189
1496 SP 600125 Novel and selective JNK inhibitor 10 mg
50 mg
99
389
3607 SU 3327 Selective JNK inhibitor 10 mg
50 mg
135
595
2827 TCS JNK 5a Selective inhibitor of JNK2 and JNK3 10 mg
50 mg
135
595
3222 TCS JNK 6o Selective JNK inhibitor 10 mg
50 mg
179
759
p38 MAPK
Inhibitors 2186 CMPD-1 Non-ATP-competitive p38α inhibitor 10 mg
50 mg
155
619
2908 EO 1428 Selective inhibitor of p38α and p38b2 10 mg
50 mg
179
759
2657 JX 401 Potent, reversible p38α inhibitor 10 mg
50 mg
169
675
4586 ML 3403 p38 inhibitor 10 mg
50 mg
169
735
2999 RWJ 67657 Potent, selective p38α and p38b inhibitor 10 mg 179
1264 SB 202190 Potent, selective inhibitor of p38 MAPK 10 mg
50 mg
145
645
KINASES
www.tocris.com | 13
CMGC Group – continued
NN
NNH
H2NN
N
FR 180204 (3706)Selective ERK inhibitor
XMD 8-92 (4132)Selective ERK5/BMK1 inhibitor
N
N N
NO
HN
N
OH
EtO
N
HN
S
Me
O
N
F
SB 203580 (1202)Selective inhibitor of p38 MAPK
N
S
N
NH
O
TAK 715 (4254)Potent p38 MAPK inhibitor; anti-inflammatory
NN N
O
S
F
F
ClCl
VX 745 (3915)Potent and selective p38α inhibitor
Key MAPK Signaling Inhibitors
Category Cat. No. Product Name Description Unit Size USD
1202 SB 203580 Selective inhibitor of p38 MAPK 1 mg
10 mg
50 mg
95
179
819
1402 SB 203580 hydrochloride Selective inhibitor of p38 MAPK; water-soluble 10 mg 225
1962 SB 239063 Potent, selective p38 MAPK inhibitor; orally active 10 mg 235
3528 SCIO 469 Selective p38 MAPK inhibitor 10 mg
50 mg
199
845
2008 SKF 86002 p38 MAPK inhibitor; anti-inflammatory agent 10 mg
50 mg
169
675
3639 SX 011 p38 MAPK inhibitor 10 mg
50 mg
179
735
4254 TAK 715 Potent p38 MAPK inhibitor; anti-inflammatory 10 mg
50 mg
169
789
3916 VX 702 Orally active p38α and p38b inhibitor 10 mg 125
3915 VX 745 Potent and selective p38α inhibitor 10 mg
50 mg
179
819
Tocris Product Listing Series
14 |
PD 0325901 (4192)Selective inhibitor of MEK1/2
IPA 3 (3622)Group I p21-activated kinase inhibitor
NQDI 1 (4429)Inhibitor of ASK1
S
OH
S
HO
NH
O
O
EtO2C
HN
F
IF
F
HN
OHOO
OH
F
F
HN
NH
O
Cl I
O
PD 184352 (4237)Selective MEK inhibitor
STE GroupSTE (homologs of yeast sterile 7, sterile 11, sterile 20) kinases are so named because of their homology with yeast MAPKs. MEK, a STE7 kinase that phosphorylates MAPKs, is itself phosphorylated by members of the STE11 group (including ASK); the STE11 group may in turn be phosphorylated by STE20 kinases (e.g. PAK).
Key STE Kinase Inhibitors
Category Cat. No. Product Name Description Unit Size USD
ASK (Apoptosis Signal-regulating Kinase)
Inhibitors 4429 NQDI 1 Inhibitor of ASK1 10 mg
50 mg
179
819
MEK (Mitogen-activated Protein Kinase Kinase)
Inhibitors 1777 Arctigenin Potent MEK1 inhibitor. Also inhibits IkBα phosphorylation 10 mg
50 mg
79
325
4192 PD 0325901 Selective inhibitor of MEK1/2 10 mg
50 mg
219
909
4237 PD 184352 Selective MEK inhibitor 10 mg
50 mg
209
875
2605 PD 198306 Selective inhibitor of MEK1/2 10 mg 235
1213 PD 98059 MEK inhibitor 1 mg
10 mg
50 mg
59
125
525
1969 SL 327 Selective inhibitor of MEK1 and MEK2; brain penetrant 1 mg
10 mg
50 mg
95
179
819
1868 U0124 Inactive analog of U0126 (Cat. No. 1144) 10 mg 155
1144 U0126 Potent, selective inhibitor of MEK1 and 2 5 mg
25 mg
179
759
PAK (p21-activated Kinase)
Inhibitors 3622 IPA 3 Group I p21-activated kinase (PAK) inhibitor 10 mg
50 mg
99
389
4212 PIR 3.5 Negative control of IPA 3 (Cat. No. 3622) 10 mg
50 mg
105
389
KINASES
www.tocris.com | 15
TK GroupMembers of the TK (tyrosine kinase) group exclusively phosphorylate tyrosine residues. Receptor and non-receptor tyrosine kinases, including EGFR, FGFR, MET, PDGFR and Src kinases, are key members of this family. Receptor tyrosine kinases are particularly important therapeutic targets in cancer.
Category Cat. No. Product Name Description Unit Size USD
Abl
Inhibitors 3716 Adaphostin p210bcr/abl kinase inhibitor 10 mg
50 mg
125
559
4274 AP 24534 Potent multi-kinase and pan-Bcr-abl inhibitor 10 mg
50 mg
219
909
4361 Bosutinib Dual Src-Abl inhibitor; antiproliferative 10 mg
50 mg
219
845
4399 GNF 2 Selective allosteric inhibitor of Bcr-abl tyrosine kinase activity 10 mg
50 mg
199
845
BTK (Bruton’s Tyrosine Kinase)
Inhibitors 1300 LFM-A13 Potent, selective BTK inhibitor 10 mg
50 mg
155
619
4710 PF 06465469 Potent inhibitor of BTK; also inhibits interleukin-2 inducible T cell kinase (ITK)
10 mg
50 mg
235
975
1405 (-)-Terreic acid Selective inhibitor of BTK 10 mg 155
EGFR (Epidermal Growth Factor Receptor)
Inhibitors 1276 AG 1478 Highly potent EGFR-kinase inhibitor 10 mg
50 mg
135
595
0414 AG 490 EGFR-kinase inhibitor. Also JAK2, JAK3 inhibitor 10 mg
50 mg
105
409
2617 AG 879 ErbB2 inhibitor; also inhibits TrkA and VEGFR-2 10 mg 155
2417 BIBU 1361 Selective inhibitor of EGFR-kinase 1 mg
10 mg
95
209
2416 BIBX 1382 Highly selective EGFR-kinase inhibitor 1 mg
10 mg
95
209
3360 CGP 52411 EGFR inhibitor. Also inhibits Ab42 fibril formation 10 mg
50 mg
125
559
1110 Genistein EGFR-kinase inhibitor. Also estrogen and PPARg ligand 10 mg
50 mg
49
155
2239 GW 583340 Potent dual EGFR/ErbB2 inhibitor; orally active 10 mg
50 mg
169
789
2646 HDS 029 Potent inhibitor of the ErbB receptor family 1 mg
10 mg
95
209
3000 Iressa Orally active, selective EGFR inhibitor 10 mg
50 mg
169
675
3352 JNJ 28871063 Potent ErbB receptor family inhibitor 10 mg
50 mg
179
735
1331 Lavendustin A EGFR, p60c-src inhibitor 1 mg 155
1037 PD 153035 EGFR-kinase inhibitor 10 mg
50 mg
125
525
2615 PD 158780 Potent ErbB receptor family inhibitor 10 mg
50 mg
169
675
2794 PP 3 EGFR-kinase inhibitor 10 mg 169
3599 TAK 165 Potent and selective ErbB2 inhibitor 10 mg
50 mg
179
759
3115 WHI-P 154 Potent EGFR inhibitor. Also inhibits JAK3 10 mg
50 mg
135
595
Tocris Product Listing Series
16 |
Bosutinib (4361)Dual Src-Abl inhibitor; antiproliferative
N
NH
O
ClCl
MeO
CNMeO
N
N
N
N
NH
HN OF3C
NH
SO2Me
PF 573228 (3239)Potent and selective FAK inhibitor
NNNC
ON
N NH
CP 690550 (4556)Potent JAK inhibitor
Ki 20227 (4481)c-Fms inhibitor; suppresses osteolysis
and osteoblast accumulation
NN
N
N
Cl
H2N
tBu
PP2 (1407)Potent, selective Src inhibitor
N
O
HN
HN
O
OMe
OMe
OMe
N
S
Key Receptor Tyrosine Kinase Inhibitors
Category Cat. No. Product Name Description Unit Size USD
FAK (Focal Adhesion Kinase)
Inhibitors 3414 FAK Inhibitor 14 Selective FAK inhibitor 10 mg
50 mg
99
389
4278 PF 431396 Dual FAK/PYK2 inhibitor 10 mg 219
3239 PF 573228 Potent and selective FAK inhibitor 10 mg
50 mg
169
789
4498 Y 11 Potent and selective FAK inhibitor 10 mg
50 mg
135
595
FGFR (Fibroblast Growth Factor Receptor)
Inhibitors 4002 FIIN 1 Potent, irreversible FGFR inhibitor 10 mg
50 mg
199
849
3724 PD 161570 Selective FGFR inhibitor 10 mg
50 mg
209
875
3785 PD 166285 FGFR, PDGFRb and Src inhibitor; also inhibits Wee1 1 mg
10 mg
89
209
3044 PD 173074 FGFR1 and -3 inhibitor 10 mg
50 mg
179
735
3300 SU 5402 Potent FGFR and VEGFR inhibitor 1 mg 199
FLT3 (FMS-like Receptor Tyrosine Kinase-3)
Inhibitors 4033 5'-Fluoroindirubinoxime FLT3 inhibitor; displays antiproliferative activity 10 mg
50 mg
155
619
3395 Lestaurtinib FLT3, JAK2 and TrkA inhibitor 1 mg 245
2591 TCS 359 Potent FLT3 inhibitor 10 mg
50 mg
125
559
Insulin and Insulin-like Receptors (IRs and IGFRs)
Activators 1819 Demethylasterriquinone B1 Selective insulin RTK activator 5 mg 199
Inhibitors 2956 Picropodophyllotoxin Selective IGF1R inhibitor 10 mg 179
2768 PQ 401 IGF1R inhibitor 10 mg
50 mg
125
559
Ligands 3435 Insulin (human) recombinant, expressed in yeast
Endogenous IR peptide agonist 10 mg 59
KINASES
www.tocris.com | 17
TK Group – continued
N
N
HN
F
Cl
O
ON
O
Iressa (3000)Orally active, selective EGFR inhibitor
N
NHN N
N
OHN
O
Cl
Cl
OMe
OMe
N
FIIN 1 (4002)Potent, irreversible FGFR inhibitor
N
N N
OMe
OMe
NH
NH
NEt2
NHO
PD 173074 (3044)FGFR1 and -3 inhibitor
NH
NH
O
HO2C
SU 5402 (3300)Potent FGFR and VEGFR inhibitor
NH
Me
NH
O
NEt2HN
F
OMe
Sunitinib (3768)Potent VEGFR, PDGFRβ and KIT inhibitor
MeHN O
S
N
HN
N
Axitinib (4350)Potent VEGFR1, -2 and -3 inhibitor
Key Growth Factor Receptor Inhibitors
Category Cat. No. Product Name Description Unit Size USD
JAK
Inhibitors 4556 CP 690550 Potent JAK inhibitor 10 mg
50 mg
145
645
1571 Cucurbitacin I Selective inhibitor of STAT3/JAK2 signaling 1 mg 199
2291 1,2,3,4,5,6-Hexabromocyclohexane Inhibits JAK2 autophosphorylation 50 mg 99
4338 NSC 33994 JAK2 inhibitor 10 mg
50 mg
169
705
3035 SD 1008 JAK2/STAT3 signaling pathway inhibitor 10 mg
50 mg
135
595
3115 WHI-P 154 JAK3 kinase inhibitor. Also inhibits EGFR 10 mg
50 mg
135
595
1367 ZM 39923 Potent, selective JAK3 inhibitor 10 mg
50 mg
155
619
1366 ZM 449829 Potent, selective JAK3 inhibitor 10 mg
50 mg
125
559
MET Receptor
Inhibitors 4368 Crizotinib Potent c-MET/ALK inhibitor 10 mg
50 mg
219
909
4239 PF 04217903 Highly selective c-MET inhibitor 10 mg
50 mg
219
909
2693 PHA 665752 Potent and selective MET inhibitor 10 mg
50 mg
259
1089
4101 SU 11274 Selective inhibitor of MET kinase activity 10 mg
50 mg
219
909
PDGFR (Platelet-derived Growth Factor Receptor)
Inhibitors 1222 DMPQ Potent, selective inhibitor of PDGFRb 10 mg
50 mg
125
495
3304 SU 16f Potent and selective PDGFRb inhibitor 10 mg
50 mg
179
735
Tocris Product Listing Series
18 |
TK Group – continued
Category Cat. No. Product Name Description Unit Size USD
Src
Inhibitors 3914 A 419259 Inhibitor of Src family kinases 10 mg 245
3963 AZM 475271 Src tyrosine kinase inhibitor 10 mg
50 mg
209
875
4361 Bosutinib Dual Src-Abl inhibitor; antiproliferative 10 mg
50 mg
219
845
1331 Lavendustin A EGFR, p60c-src inhibitor 1 mg 155
2265 Lyn peptide inhibitor Inhibits Lyn-dependent activities of IL-5 receptor; cell permeable 1 mg 289
3063 1-Naphthyl PP1 Src family kinase inhibitor; also inhibits c-Abl 10 mg
50 mg
225
945
1554 Piceatannol p56lck and Syk kinase inhibitor 10 mg 155
1397 PP 1 Potent, selective Src inhibitor 10 mg 219
1407 PP 2 Potent, selective Src inhibitor 10 mg 219
2794 PP 3 Negative control for PP 2 (Cat. No. 1407). Inhibits EGFR-kinase 10 mg 169
3642 Src I1 Dual site Src kinase inhibitor 10 mg
50 mg
145
645
Syk
Inhibitors 2471 ER 27319 Selective Syk kinase inhibitor 10 mg
50 mg
125
495
1554 Piceatannol Syk and p56lck kinase inhibitor 10 mg 155
Trk Receptors
Agonists 2837 BDNF (human) Activates TrkB and p75 receptors 10 µg 295
3826 7,8-Dihydroxyflavone TrkB agonist 10 mg
50 mg
135
595
4607 LM 22A4 Potent TrkB agonist 10 mg
50 mg
159
655
Inhibitors 2238 GW 441756 Potent, selective TrkA inhibitor 10 mg
50 mg
169
789
2272 Ro 08-2750 Inhibits NGF binding to p75NTR and TrkA 1 mg
10 mg
50 mg
69
169
675
VEGFR (Vascular Endothelial Growth Factor Receptor)
Inhibitors 4350 Axitinib Potent VEGFR-1, -2 and -3 inhibitor 10 mg
50 mg
219
845
4471 DMH4 Selective VEGFR-2 inhibitor 10 mg
50 mg
179
819
2542 Ki 8751 Potent, selective VEGFR-2 inhibitor 10 mg
50 mg
169
789
3768 Sunitinib Potent VEGFR, PDGFRb and KIT inhibitor 10 mg
50 mg
179
819
2499 ZM 306416 Inhibitor of VEGF receptor tyrosine kinase 1 mg
10 mg
79
179
2475 ZM 323881 Potent, selective inhibitor of VEGFR-2 1 mg
10 mg
95
219
Other RTKs
Inhibitors 4481 Ki 20227 c-Fms inhibitor; suppresses osteolysis and osteoclast accumulation
10 mg
50 mg
235
975
4405 NVP BHG 712 Potent EphB4 kinase inhibitor 1 mg 95
Multi-TK Inhibitors
Inhibitors 2086 GTP 14564 Class III receptor tyrosine kinase (RTK) inhibitor 10 mg 125
3037 SU 5416 Inhibitor of VEGFR, KIT, RET, MET and FLT3 10 mg
50 mg
125
559
3335 SU 6668 FGFR, VEGFR and PDGFR inhibitor 10 mg
50 mg
169
705
KINASES
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TKL GroupThe TKL (tyrosine kinase-like) kinases include BMP, Raf kinase and TGF-β receptor serine/threonine kinases. These enzymes exhibit sequence similarity to tyrosine kinases, but phosphorylate serine/threonine residues instead of tyrosine residues.
N
NCl
NH
NH
MeSO2NH OMe
N
O
CZC 54252 (4534)Potent LRRK2 inhibitor; neuroprotective
N F
O
HN
ON
GSK2578215A (4629)Potent, selective LRRK2 inhibitor; brain penetrant
N
N N
NO
HN
MeO
NO
N
N
LRRK2-IN-1 (4273)Potent and selective LRRK2 inhibitor
Key LRRK2 Inhibitors
Category Cat. No. Product Name Description Unit Size USD
BMP and Other Activin Receptors
Activators 4490 Alantolactone Antiproliferative; induces activin/SMAD3 signaling 10 mg
50 mg
169
675
Inhibitors 4126 DMH-1 BMP inhibitor; selectively inhibits ALK2 10 mg
50 mg
175
735
LRRK2 (Leucine-rich Repeat Kinase 2)
Inhibitors 4534 CZC 54252 Potent LRRK2 inhibitor; neuroprotective 10 mg
50 mg
189
819
4629 GSK2578215A Potent, selective LRRK2 inhibitor; brain penetrant 10 mg
50 mg
199
845
4273 LRRK2-IN-1 Potent and selective LRRK2 inhibitor 10 mg
50 mg
225
945
Raf
Inhibitors 4453 GDC 0879 Potent B-Raf inhibitor 10 mg
50 mg
199
845
1381 GW 5074 Potent, selective c-Raf1 kinase inhibitor 10 mg
50 mg
155
619
3185 L-779,450 Potent Raf kinase inhibitor 10 mg
50 mg
169
705
2650 SB 590885 Potent B-Raf inhibitor 10 mg
50 mg
209
875
1321 ZM 336372 Potent, selective c-Raf inhibitor 10 mg
50 mg
179
735
RIPK1 (Receptor-interacting Protein Kinase 1)
Inhibitors 2324 Necrostatin-1 RIPK1 inhibitor; inhibits necroptosis 10 mg
50 mg
105
409
TAK1 (TGFb-activated Kinase 1)
Inhibitors 3604 (5Z)-7-Oxozeaenol Potent and selective TAK1 MAPKKK inhibitor 1 mg 125
TGF-b Receptors (Transforming Growth Factor b Receptors)
Inhibitors 2939 A 83-01 Selective inhibitor of TGF-bRI, ALK4 and ALK7 10 mg
50 mg
179
735
2902 D 4476 TGF-bRI inhibitor. Also inhibits CK1 10 mg
50 mg
179
759
3264 GW 788388 Selective inhibitor of TGF-bRI 10 mg
50 mg
199
845
Tocris Product Listing Series
20 |
TKL Group – continued
A 83-01 (2939)Selective inhibitor of TGF-βRI, ALK4 and ALK7
N
N N
S
HN
N
N
N
NHN
N
SB 525334 (3211)Selective inhibitor of TGF-βRI
HN
NO
NHON
N
SB 590885 (2650)Potent B-Raf inhibitor
Key TKL Kinase Inhibitors
Category Cat. No. Product Name Description Unit Size USD
2718 LY 364947 Selective inhibitor of TGF-bRI 1 mg
10 mg
79
179
3742 RepSox Selective inhibitor of TGF-bRI; enhances cellular reprogramming efficiency
10 mg
50 mg
145
645
1614 SB 431542 Potent, selective inhibitor of TGF-bRI, ALK4 and ALK7 1 mg
10 mg
105
235
3263 SB 505124 Selective inhibitor of TGF-bRI, ALK4 and ALK7 10 mg
50 mg
199
845
3211 SB 525334 Selective inhibitor of TGF-bRI 10 mg
50 mg
169
789
3269 SD 208 Potent ATP-competitive TGF-bRI inhibitor 10 mg
50 mg
145
645
KINASES
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Other Protein Kinases The Other Protein Kinases group contains protein kinases that do not readily fit into existing kinome categorization. Members include the Aurora kinases A, B and C; CAM kinase kinase (CAMKK); Polo-like kinase (PLK); and IkB kinase (IKK).
HN
O
NHS
O
O
HN
N
Hesperadin (3988)Potent Aurora B kinase inhibitor
N
N
O
CO2H
STO-609 (1551)Selective CaM kinase kinase inhibitor
TPCA-1 (2559)Potent, selective inhibitor of IKK-2
N
N N
NO
NH
OMe
O
N
AZ 3146 (3994)Potent and selective Mps1 kinase inhibitor
S NH
F
NH2
O
H2NO
Other Protein Kinase Inhibitors
Category Cat. No. Product Name Description Unit Size USD
Aurora Kinase
Inhibitors 4291 CCT 137690 Potent pan-Aurora kinase inhibitor 10 mg
50 mg
219
909
3988 Hesperadin Potent Aurora kinase B inhibitor 10 mg
50 mg
235
975
4066 TC-A 2317 Potent, selective Aurora kinase A inhibitor 10 mg
50 mg
199
845
2458 ZM 447439 Inhibits Aurora kinase B 10 mg 219
CaMKK (CaM Kinase Kinase)
Inhibitors 1551 STO-609 Selective CaM kinase kinase inhibitor 1 mg
10 mg
50 mg
95
199
845
IKK (IkB Kinase)
Inhibitors 2539 IKK 16 Selective inhibitor of IKK 10 mg
50 mg
199
845
2611 IMD 0354 Inhibitor of IKK-2 10 mg
50 mg
135
595
4238 PF 184 Potent and selective IKK-2 inhibitor 10 mg 245
3318 SC 514 IKK-2 inhibitor; attenuates NF-kB-induced gene expression 10 mg
50 mg
115
439
2559 TPCA-1 Potent, selective inhibitor of IKK-2 10 mg 199
Mps1 (Monopolar Spindle Kinase 1)
Inhibitors 3994 AZ 3146 Potent and selective monopolar spindle 1 (Mps1) kinase inhibitor 10 mg
50 mg
199
845
PLK (Polo-like Kinase)
Inhibitors 3116 Cyclapolin 9 Selective, ATP-competitive PLK1 inhibitor 10 mg
50 mg
125
495
2977 GW 843682X Selective inhibitor of PLK1 and PLK3 10 mg
50 mg
179
759
4292 SBE 13 Potent and selective PLK1 inhibitor 10 mg
50 mg
99
389
Tocris Product Listing Series
22 |
Atypical KinasesAtypical kinases are kinases that do not exhibit sequence similarity with conventional protein kinases, but are reported to have protein kinase activity. These include ATM and ATR kinases, mTOR, DNA-dependent protein kinase (DNA-PK) and eEF2 kinase (eEF-2 K).
PI 103 (2930)Inhibitor of mTOR, PI 3-kinase and DNA-PK
Torin 2 (4248)Potent and selective mTOR inhibitor
Torin 1 (4247)Potent and selective mTOR inhibitor
N
NN
ON
N
O
CF3
N O
N
N
N
O
OH
N
N
O
NNH2
CF3
N
N
N N
N
HN
O
N
N
MeO
O
WYE 687 (4282)Potent and selective mTOR inhibitor
Key mTOR Inhibitors
Category Cat. No. Product Name Description Unit Size USD
ATM and ATR Kinase
Inhibitors 3544 KU 55933 Potent and selective ATM kinase inhibitor 10 mg 179
4176 KU 60019 Potent ATM kinase inhibitor 10 mg
50 mg
225
945
3190 Mirin MRN-ATM pathway inhibitor 10 mg
50 mg
125
559
DNA-PK (DNA-dependent Protein Kinase)
Inhibitors 3271 Compound 401 Selective DNA-PK and mTOR inhibitor 10 mg
50 mg
169
675
2828 NU 7026 Selective DNA-PK inhibitor 10 mg
50 mg
145
645
3712 NU 7441 Potent and selective DNA-PK inhibitor 10 mg
50 mg
169
789
eEF-2 (Eukaryotic Elongation Factor-2) Kinase
Inhibitors 4483 A 484954 CaM kinase III (eEF-2 kinase) inhibitor 10 mg
50 mg
169
675
3439 NH 125 CaM kinase III (eEF-2 kinase) inhibitor 10 mg
50 mg
145
645
mTOR (Mammalian Target of Rapamycin)
Inhibitors 3725 KU 0063794 Selective mTOR inhibitor 10 mg 219
4079 Niclosamide STAT3 inhibitor; also inhibits mTORC1 signaling 50 mg 79
2930 PI 103 Inhibitor of mTOR, PI 3-kinase and DNA-PK 1 mg
10 mg
50 mg
79
179
735
4257 PP 242 Dual mTORC1/mTORC2 inhibitor 10 mg
50 mg
199
845
1292 Rapamycin mTOR inhibitor; immunosuppressant 1 mg 229
4247 Torin 1 Potent and selective mTOR inhibitor 10 mg
50 mg
219
909
4248 Torin 2 Potent and selective mTOR inhibitor 10 mg
50 mg
199
845
4282 WYE 687 Potent and selective mTOR inhibitor 10 mg
50 mg
225
945
KINASES
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Lipid KinasesLipid kinases have lipid molecules as their substrate, rather than proteins. These enzymes are particularly important for signal transduction. PI 3-kinase is a well-characterized member of this group; other members include diacylglycerol kinase and sphingosine kinase.
LY 294002 (1130)Selective PI 3-kinase inhibitor
GSK 1059615 (4026)Potent PI 3-kinase inhibitor
CZC 24832 (4674)Selective inhibitor of PI 3-kinase γ
NN N
NNH2
F
SNH
O
O
O
O
N
O
N
N
SHN
O
O
Key PI 3-Kinase Inhibitors
Category Cat. No. Product Name Description Unit Size USD
CerK (Ceramide Kinase)
Inhibitors 3960 NVP 231 Potent, selective and reversible CerK inhibitor 10 mg
50 mg
145
645
DGK (Diacylglycerol Kinase)
Inhibitors 0484 Dioctanoylglycol Diacylglycerol kinase inhibitor 50 mg 125
2194 R 59-022 Diacylglycerol kinase inhibitor; increases PKC activity 10 mg
50 mg
125
559
PI 3-K (PI 3-Kinase)
Activators 1983 740 Y-P Cell-permeable PI 3-kinase activator 1 mg 239
Inhibitors 3671 AS 252424 Selective inhibitor of PI 3-kinase g 10 mg 199
3578 AS 605240 Potent and selective PI 3-kinase g inhibitor 10 mg
50 mg
135
595
4674 CZC 24832 Selective PI 3-kinase g inhibitor 10 mg
50 mg
225
945
4026 GSK 1059615 Potent PI 3-kinase inhibitor 10 mg
50 mg
179
819
1130 LY 294002 Selective PI 3-kinase inhibitor 5 mg
25 mg
115
469
2418 LY 303511 Negative control of LY 294002 (Cat. No. 1130) 5 mg 115
3977 3-Methyladenine Class III PI 3-kinase inhibitor; also inhibits autophagy 50 mg 89
2814 PI 828 PI 3-kinase inhibitor 1 mg
10 mg
50 mg
79
179
735
3894 PP 121 Dual kinase inhibitor; inhibits PI 3-K family kinases 10 mg
50 mg
145
645
1125 Quercetin Non-selective PI 3-kinase inhibitor 100 mg 55
4264 TG 100713 PI 3-kinase inhibitor 10 mg
50 mg
199
845
1232 Wortmannin Potent, irreversible inhibitor of PI 3-kinase. Also inhibitor of PLK1 1 mg
5 mg
79
295
SphK (Sphingosine Kinase)
Inhibitors 4640 N,N-Dimethylsphingosine Sphingosine kinase inhibitor 10 mg 119
3711 SK1-I Sphingosine kinase 1 inhibitor; antiproliferative 10 mg 245
2097 SKI II Selective non-lipid inhibitor of sphingosine kinase 10 mg
50 mg
125
559
Tocris Product Listing Series
24 |
Broad Spectrum Kinase Inhibitors Broad spectrum kinase inhibitors have found use in a wide range of applications, particularly in high-throughput screening assays designed to discover selective inhibitors, where a standard inhibitor curve is required. Broad spectrum inhibitors are often both highly potent and cell permeable, offering a high degree of versatility.
Category Cat. No. Product Name Description Unit Size USD
Broad Spectrum Protein Kinase Inhibitors
Inhibitors 1227 Apigenin Protein kinase inhibitor 10 mg
50 mg
49
155
0542 H-7 dihydrochloride Protein kinase inhibitor 10 mg
50 mg
115
439
1520 Hypericin Inhibits tyrosine kinases 1 mg 85
1813 Indirubin-3'-oxime Protein kinase inhibitor 10 mg
50 mg
145
645
1745 5-Iodotubercidin Broad spectrum kinase inhibitor 1 mg 115
1683 K 252a Protein kinase inhibitor 200 µg 225
2992 PKC 412 Broad spectrum protein kinase inhibitor 1 mg 155
2002 Ro 31-8220 Protein kinase inhibitor 10 mg 209
1285 Staurosporine Non-selective protein kinase inhibitor 100 µg 119
KINASES
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PhosphatasesPhosphatases mediate the activity of kinases by catalyzing the removal of phosphate groups. This family of enzymes can be further subdivided along lines of substrate specificity: Cdc25 phosphatases exhibit dual specificity, whilst protein ser/thr phosphatases and tyrosine phosphatases selectively remove phosphate groups from specific residues.
Category Cat. No. Product Name Description Unit Size USD
Cdc25 Phosphatase
Inhibitors 1867 NSC 663284 Potent, selective Cdc25 phosphatase inhibitor 10 mg 199
1547 NSC 95397 Selective Cdc25 dual specificity phosphatase inhibitor 10 mg
50 mg
169
675
Inositol Phosphatase
Inhibitors 3718 AS 1949490 SH2 domain-containing inositol 5'-phosphatase 2 (SHIP2) inhibitor
10 mg
50 mg
135
595
1420 D-myo-Inositol-1,3,4,5-tetrakisphosphate
Potent inhibitor of Ins(1,4,5)P3 5-phosphatase 100 µg 179
0681 L-690,330 Inositol monophosphatase inhibitor 10 mg
50 mg
135
595
0682 L-690,488 Cell permeable prodrug of L-690,330 (Cat. No. 0681) 5 mg 225
Protein Ser/Thr Phosphatase
Activators 0744 Ceramide Ser/Thr protein phosphatase activator 10 mg
50 mg
125
525
Inhibitors 1336 Calyculin A Protein phosphatase 1 and 2A inhibitor 100 µg 415
1548 Cantharidin Protein phosphatase 1 and 2A inhibitor 50 mg 115
1101 Cyclosporin A Calcineurin inhibitor 100 mg 99
0125 DL-AP3 Phosphoserine phosphatase inhibitor 100 mg 99
3631 FK 506 Potent calcineurin inhibitor; immunosuppressant 10 mg 125
1840 Fostriecin Potent PP2A and PP4 inhibitor 50 µg 235
3103 Fumonisin B1 Inhibitor of Ser/Thr phosphatase. Also inhibits sphingosine N-acyltransferase
1 mg 89
2162 INCA-6 Inhibitor of calcineurin-substrate association 10 mg
50 mg
115
439
3930 NFAT Inhibitor Inhibitor of calcineurin-mediated NFAT activation 1 mg 179
1136 Okadaic acid Protein phosphatase 1 and 2A inhibitor 25 µg 99
3657 Sal 003 Cell permeable inhibitor of eIF2α dephosphorylation 10 mg
50 mg
145
645
2347 Salubrinal Selective inhibitor of eIF2α dephosphorylation 10 mg 169
2302 Sanguinarine Inhibitor of protein phosphatase 2C (PP2C) 10 mg
50 mg
125
559
2305 Tautomycetin Selective PP1 inhibitor 50 µg 235
Protein Tyrosine Phosphatase
Inhibitors 3979 Alexidine Selective inhibitor of PTPMT1 50 mg 89
2613 NSC 87877 Potent inhibitor of shp2 and shp1 PTP 50 mg 119
2754 TCS 401 Selective inhibitor of PTP1B 10 mg 179
Prices are correct at the time of publication. For the latest information please visit www.tocris.com
Tocris Product Listing Series
26 |
Tocriscreen® collections are small molecule libraries for high-throughput screening (HTS), cell-based high-content screening (HCS) and chemical biology applications. Each set comprises biologically active molecules selected from the Tocris catalog, creating a unique collection with excellent structural diversity and wide coverage of pharmacological space. Available pre-dissolved in DMSO, the libraries include compounds active at GPCRs, kinases, ion channels, nuclear receptors and transporters. Many of the molecules are unavailable elsewhere, and the collections are periodically updated with products from the very latest research. For full details and up to date listings of our unique and diverse compound collections, please visit www.tocris.com/tocriscreen.
References
Tocriscreen collections have been successfully used in numerous cell-based assays and chemical genomic screens. For further information, please refer to the following citations:Beacham et al (2010) Cell-based potassium ion channel screening using the FluxORTM assay. J.Biomol.Screen. 15 44.Hattori et al (2010) Small-molecule screen identifies reactive oxygen species as key regulators of neutrophil chemotaxis. Proc.Natl.Acad.Sci. USA 107 3546.Hermanson et al (2012) Screening for novel LRRK2 inhibitors using a high-throughput TR-FRET cellular assay for LRRK2 Ser935 phosphorylation. PLoS One. 7 e43580.Jester et al (2010) A coiled-coil enabled split-luciferase three-hybrid system: applied toward profiling inhibitors of protein kinases. J.Am.Chem.Soc. 132 11727.Li et al (2011) Generation of iPSCs from mouse fibroblasts with a single gene, Oct4, and small molecules. Cell Research 21 196.
Key Format and Product Details
• All compounds are biologically active, with chemical and biological data available for each compound
• Many compounds are exclusive to Tocris
• Excellent coverage of pharmacological space
• Includes marketed drugs, well-characterized standards, and novel research compounds
• Exceptional purity in ready to screen formats
• 96-well racks with TrackMate tubes and SepraSeal® caps
www.tocris.com/tocriscreen
Product Description Size USD
Tocriscreen Total (2884)1120 biologically active compounds pre-dissolved in DMSO (250 mL, 10 mM solutions)
1 set 19,199
Tocriscreen Mini (2890)1120 biologically active compounds pre-dissolved in DMSO (50 mL, 10 mM solutions)
1 set 6,239
Tocriscreen Kinase Inhibitor Toolbox (3514)80 kinase inhibitors pre-dissolved in DMSO (250 mL, 10 mM solutions)
1 set 2,515
KINASES
www.tocris.com | 27
Related literature from Tocris that you may be interested in:
Cancer Research Product GuideOver 350 Products for Cancer Research
Our updated guide contains products with supporting information and figures to illustrate the relevance of each target within the areas of: • Receptor Signaling • Cell Cycle and DNA Damage Repair • Cell Death and Drug Resistance • Angiogenesis • Invasion and Metastasis
Tumor- and Stromal Cell-Derived Pathways as Targets for Anti-Angiogenic TherapyN. Ferrara and Y. Crawford, Genentech
Angiogenesis is an integral process that occurs during tumorigenesis to supply nutrients to tumor cells. This poster summarizes antiangiogenic therapies targeting the VEGF pathway and the mechanisms of therapy resistance.
MAPK Signaling E. Zaganjor and M. Cobb, University of Texas Southwestern Medical Center
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer research. This review discusses the regulation of the MAPK pathway and properties of MAPK cascades.
Checkpoint Kinases and the DNA Damage ResponseM. Garrett and I. Collins, Institute of Cancer Research
Checkpoint kinases are a group of enzymes which regulate the progression of a cell through the cell cycle. This poster summarizes the response of the checkpoint kinase signaling network to DNA damage. It also highlights the different types of DNA damage that can occur and some of the treatment methods that are utilized in cancer therapy.
To download or request copies, please visit www.tocris.com/requestliterature
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