kinaseskomabiotech.co.kr/pdf/kinase_listing_us_2013.pdf · 2014-05-15 · kinases | 5 agc group –...

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


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


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


6 |

AGC Group – continued


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).


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


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


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:

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Contact UsTo discuss licensing opportunities, please contact our licensing team at [email protected]

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


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


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


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


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


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™.


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


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


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


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.


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


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


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


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


18 |

TK Group – continued


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

www.tocris.com | 19

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


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


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


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

www.tocris.com | 21

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


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


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


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

www.tocris.com | 23

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


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


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.


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

www.tocris.com | 25

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.


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


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

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Tumor- and Stromal Cell-Derived Pathways as Targets for Anti-Angiogenic TherapyN. Ferrara and Y. Crawford, Genentech

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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

© 2013 Tocris Cookson, Ltd.www.tocris.com

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kinaseskomabiotech.co.kr/pdf/kinase_listing_us_2013.pdf · 2014-05-15 · kinases | 5 agc group –...

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