jak/stat pathway products
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JAK/STAT Pathway Products
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JAK/STATPathway Products
InhibitorsJAK
STAT
EGFR
Pim
PI3K/AktPathwayMAPK
Pathway
JAK
STAT STAT
STAT
Bcl-XLp21
GrowthFactorsGGGGGGGGGGGGGGGGGGGGGGGGGGGGGGGrrrrrrrrrrrrrrrrrrrrrrrrrroooooooooooooooooooooooooooooowwwwwwwwwwwwwttttttFFactt
CytokinesCytokkkine
PIAS
CDK Pim
Tyk
Src PI3K
Akt
STAT
STAT
Table of ContentsJAK 1
EGFR 2
STAT 1
Pim 3
Janus Kinase
Signal Transducers and Activators of Transcription
Epidermal Growth Factor Receptor
Proto-oncogene Serine/threonine-protein Kinase
JAK/STAT pathway
The Janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway is a critical signaling cascade for mediating cytokine receptor-derived signals. JAK/STAT signaling contributes to the regulation of haematopoietic cell survival, proliferation and differentiation. Also, this signaling pathway is involved in the developmental process, growth regulation and maintenance of homeostasis in other cells and tissues. The JAK/STAT signaling pathway is made up of four JAKs (JAK1-3, and Tyk2) and seven STAT proteins (STAT1-4, 5A, 5B and 6).
Initiation of JAK/STAT signaling proceeds as a result of cytokine receptors activating a specific set of individual JAKs and STATs that is dependent on the characteristics of the intracellular domains of the receptor chains. The binding of cytokines to transmembrane receptors (i.e. interleukin-2 or interferon) results in cross-activation of receptor-associated JAKs by tyrosine phosphorylation due to receptor dimerization and reorganization events. Activated JAKs lead to the phosphorylation of tyrosine residues in the cytoplasmic domain that increases their catalytic activity for STAT proteins. JAKs mediate phosphorylation on the C-terminus. This in turn causes STAT proteins to dissociate from the receptor, dimerize (mediated by Src-homology-2 domains) and translocate to the cell nucleus where they induce gene transcription of intracellular regulators of cell proliferation (cyclins and Myc) and survival (Bcl family). Regulating the JAK/STAT signaling pathway are SOCS1, SOCS3 and PIAS3. Constitutive signaling of the JAK/STAT pathway, high levels of STAT3 proteins and/or deminished function of negative regulators can contribute to tumour initiation and progression events.
Growth Factors Cytokine
Src
STAT
Cyclin D1
p27KIP1
p21 CRP SERPINA3 Bcl-XLPim
TAP1
PIASERK
STAT STATRaf
JAK
PI3K
Akt SOCS2
P120GAPSTAT
STAT
MAPKPathway
Cell Cycle
Apoptosis Pathway
PI3K/AktPathway
Tyk
EGFR
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JAK/STAT
Terrific Validation, Tech Support & Prompt Delivery
JAK
S2686 NVP-BSK805
JAK Inhibitors
Cat.No. Product Name Target and IC50 ValueS5001 Tofacitinib citrate
(CP-690550)
S2162 AZD1480
S1134 AT9283
S1143 AG-490
S2219 Cyt387
S2214 AZ 960
S2179 LY2784544 A small molecule selective mutant JAK2 kinase inhibitor with an IC50 of 68 nM.
S2736 TG-101348
S2692 TG101209
A potent JAK kinase inhibitor of IL-2-mediated human T cell blast proliferation and IL-15-induced CD69 expression with IC50s of 11 and 48 nM, respectively.
A novel pyrazol pyrimidine ATP-competitive JAK1 and JAK2 inhibitor with IC50s of 1.3 and <0.4 nM, respectively.
A multi-targeted c-Abl, JAK2, Aurora A and B inhibitor. JAK2, IC50=1.2 nM; JAK3, IC50=1.1 nM; Bcr-Abl (T3151), IC50=4 nM; Aurora A and B, IC50 of approximate 3 nM.
A potent EGFR kinase autophosphorylation inhibitor. EGFR, IC50=100 nM; JAK, IC50=56.8 μM.
An ATP-competitive small molecule JAK1/JAK2 inhibitor. JAK1, IC50=11 nM; JAK2, IC50=18 nM.
A novel JAK2 kinase inhibitor. IC50=3 mM; Ki=0.45 nM.
A potent, highly selective and ATP- competitive JAK2 inhibitor. JAK2, IC50=3 nM; Flt3, IC50=15 nM; RET, IC50=48 nM.
A potent small molecule JAK2-selective kinase inhibitor. JAK2, IC50=6 nM; Flt3, IC50=25 nM; RET, IC50=17 nM; JAK3, IC50=169 nM.
A selective quinoxaline JAK2 inhibitor. JAK2 JH1, IC50=0.48 nM; FL JAK V617F, IC50=0.56 nM; FL JAK2 wt, IC50=0.58 nM.
Inhibitor
Data from [Leukemia, 2012, 26(4), 708-715]AZD1480 purchased from SelleckMutations in the JAK2V617F kinase domain confer resistance to JAK2 tyrosine kinase inhibitors. Growth of BaF3.EpoR cells expressing JAK2V617F and the additional mutations was determined in response to AZD1480 at various concentrations, as indicated (n=4).
Data from [Int Immunol, 2011, 23(11), 701-712] Tofacitinib citrate (CP-690550) purchased from SelleckSTAT3 inhibition antagonizes arthritis effects in vivo. Whole-cell lysates were made from ankle joint tissues of CIA mice treated with or without CP690,550 for 2 weeks. Phosphorylated STAT3 was then analyzed by western blot (upper panel) and ELISA (lower panel).
S1378 INCB018424 (Ruxolitinib)
An orally bioavailable JAK inhibitor. JAK1, IC50=3 nM; JAK2, IC50=5 nM; JAK3, IC50=332 nM.
Janus Kinase
EGFR Inhibitors
EGFR
Cat.No. Product Name Target and IC50 Value Inhibitor
Data independently produced by Dr. Zhang of Tianjin Medical University WZ3146 purchased from SelleckT47D cells were pretreated with 100 ng/ml EGF for 20 min and then treated with the indicated concentrations of WZ3146 for 24 hours.
P-EGFR
EGFR
EGF(100ng/ml) + -
WZ3146(μM) 0 0.1 1 10 20 0
+ + + +
Data from [J Cell Sci, 2010, 123(Pt 18), 3102-3111]CI-1033 (Canertinib) purchased from SelleckEffect of pan-ErbB inhibitors on NRG-1 action on human melanocytes and MelanoDerms. (A) HEM-DP were treated for 9 days with 50 ng/ml ����������� �������������������������������������������������!���"�#$��%!����&������'!��%���the average of three independent experiments ± s.d. (B) Dark (from African-American skin) MelanoDerms were treated for 9 days with 50 ng/ml NRG-1 in the presence of ���������������������������������������!� (DMSO) alone. L values shown are the average of three spots measured in the center of each MelanoDerm.
Data from [Antiviral Res, 2011, 89(1), 64-70]PD153035 HCl purchased from SelleckInhibition of orthopoxvirus replication and spreading correlates with blocking of EGFR signaling by PD153035 (PD), Vandetanib (Van) and Gefitinib (Gef). Western blot of cell lysates obtained from VACV plaque reduction tests for analysis of EGFR-ERK1/2 signaling and VACV proteins. As an indicative band for VACV a 30KDa protein was depicted from detection of total VACV proteins by a polyclonal antibody in cell lysates of infected Hep2 cells.
S1019 CI-1033(Canertinib)
An orally bioavailable irreversible Pan-erbB tyrosine kinase inhibitor. EGFR, IC50=0.8 nM; HER2, IC50=19 nM; ErbB4, IC50=7 nM.
S1486 AEE788 (NVP-AEE788)
A novel multitargeted HER1/2 and VEGFR1/2 inhibitor. EGFR, IC50=2 nM; ErbB2, IC50=6 nM; KDR, IC50=77 nM; Flt1, IC50=59 nM.
S1143 AG-490 A potent EGFR kinase autophosphorylation inhibitor. EGFR, IC50=100 nM; JAK, IC50=56.8 μM.
BMS-599626(AC480)
S1056 A highly selective pan-HER kinase inhibitor. HER1, IC50=20 nM; HER2, IC50=30 nM.
S2192 AZD8931 A novel potent reversible small molecule inhibitor. EGFR, IC50=4 nM; ErbB2, IC50=3 nM; ErbB3, IC50=4 nM.
S1179 WZ8040 An irreversiblely EGFR T790M inhibitor with an IC50 of <10 nM.
S1011 BIBW2992(Afatinib)
An irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2.
S1173 WZ4002 An EGFR T790M inhibitor with an IC50 of <20 nM.
S1194 CUDC-101 A potent multitargeted inhibitor. EGFR, IC50=2.4 nM; HDAC, IC50=4.4 nM; HER2, IC50=15.7 nM.
S1392 Pelitinib(EKB-569)
A 3-cyanoquinoline EGFR and pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity.
S1079 PD153035 HCl An inhibitor of EGFR, competitive with ATP. EGFR, IC50=25 pM, Ki=6 pM.
S1170 WZ3146 An irreversiblely inhibitor against EGFR T790M.
S1023 Erlotinib HCl An HER1/EGFR with an IC50 of 2 nM.
S2406 Chrysophanic acid(Chrysophanol)
An EGFR/mTOR pathway inhibitor.
Mubritinib(TAK 165)
S2216 A potent EGFR and p34cdc2 inhibitor with IC50s of 6 nM %*�������>���� �����!?�
S1083 XL647 An EGFR and ErbB2 inhibitor with IC50s of 0.3 nM and 16 nM, respectively.
S2727 PF299804 A potent, orally available, irreversible tyrosine kinase HER1 (EGFR), HER2 and HER4 inhibitor. EGFR, IC50=6 nM; ErbB2, IC50=45.7 nM; ErbB4, IC50=73.7 nM.
S2733 AV-412 A second-generation, orally bioavailable dual EGFR/HER2 tyrosine kinase inhibitor.
S2728 AG-1478(Tyrphostin AG-1478)
A highly potent and specific EGFR tyrosine kinase inhibitor with an IC50 of 3 nM.
Epidermal Growth Factor Receptor
STAT STAT Inhibitors
Cat.No. Product Name Target and IC50 Value
S1155 NSC 74859 (S3I-201)
S2285 Cryptotanshinone
A selective inhibitor of STAT3 with an IC50����QY����
A small-molecule STAT3 inhibitor with an IC50����\�Y�����
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We give free samples and rewards to people who would like to provide us useful scientific data (western blot, etc.)
Signal Transducers and Activators of Transcription
EGFR/Pim
Terrific Validation, Tech Support & Prompt Delivery
PimPim Inhibitor
Cat.No. Product Name Target and IC50 Value
S2198 SGI-1776 free base A selective Pim family kinase inhibitor. Pim-1, IC50=7 ± 1.8 nM; Pim-2, IC50=363 ± 27.6 nM; Pim-3, IC50=69 ± 9.2 nM.
Data from [Sci Signal, 2011, 4(191), rs9]SGI-1776 free base purchased from SelleckMean IL-8 concentrations determined by ELISA of the supernatants of HeLa cells infected with wild-type Salmonella. Kinase inhibitors are indicated on the x axis, and the target families of the inhibitors are indicated above each column. CEC, chelerythrine; Pim Inh, Pim-1 inhibitor 2. Inhibitors that significantly affected IL-8 production relative to the control (P < 0.05, Bonferroni post hoc test from one-way ANOVA) are indicated with an asterisk. Relative cell viability is also shown, as determined by reduction of XTT by viable cells. A450, absorbance at 450 nm.
Proto-oncogene Serine/threonine-protein Kinase
S1028 Lapatinib ditosylate (Tykerb)
An EGFR and HER2 autophosphorylation inhibitor, with IC50 values against purified EGFR and HER2 of 10.2 nM and 9.8 nM, respectively.
Vandetanib (Zactima)
S1046 A VEGFR and EGFR antagonist and a tyrosine kinase inhibitor with IC50s of 60 nM, 90 nM, 40 nM for HUVEC proliferation, PC-9 cells and tyrosine kinase activity, respectively.
S2755 ARRY334543
S2205 OSI-420 (Desmethyl Erlotinib, CP-473420)
An orally active EGFR tyrosin kinase inhibitor with IC50s of 2 nM and 20 nM for the inhibition of human EGFR and EGFR autophosphorylation in tumor cells.
A selective and potent kinase ErbB1 and ErbB2 inhibitor with IC50s of 7 nM and 2 nM, respectively.
S1025 Gefitinib (Iressa) A novel potent EGFR tyrosine kinase and Akt phosphorylations inhibitor with IC50s of 37 nM, 26 nM and 57 nM for Tyr1173, Tyr1173 and Tyr992, respectively, the low and high EGFR expressing cell lines.
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