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JAK Janus Kinase

Cat.No.  Name Information
M3030 S-Ruxolitinib S-Ruxolitinib is the chirality of INCB018424, which is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.
M1820 Tofacitinib Tofacitinib (formerly tasocitinib, CP-690550) is a novel Janus Kinase 3 (JAK-3) kinase inhibitor with an IC50 value estimated at 0.2 μM.
M1660 AZ 960 AZ 960 is a novel and specific inhibitor of the JAK2 kinase with a Ki of 0.45nM in vitro.
M1646 AG490 AG490 (Tyrphostin AG490) is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively).
M1733 TG101348 TG101348 is a selective small-molecule Janus kinase 2 (JAK2) inhibitor with IC50 of 3 nM.
M1787 INCB18424 Ruxolitinib (INCB018424) is a first-in-class, potent, selective JAK1/2 inhibitor with an IC50 of 3.3 nM/2.8 nM. It is more than 130-fold more selective for JAK1, JAK2, and JAK3 than JAK3. It can be used in studies related to pemphigus, myelofibrosis and vitiligo.
M5944 Ruxolitinib phosphate Ruxolitinib phosphate(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.
M3616 Tofacitinib citrate Tofacitinib (CP-690550) Citrate is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.
M2346 Filgotinib Filgotinib (GLPG0634) is the first selective inhibitor of JAK1 and JAK2 with IC50 of 10nM and 28nM respectively.
M2044 AZD1480 AZD1480 is a novel small-molecule inhibitor of JAK1/2 with IC50 of 1.3 nM and 0.26 nM, respectively.
M6315 1,2,3,4,5,6-Hexabromocyclohexane 1,2,3,4,5,6-Hexabromocyclohexane is a inhibits JAK2 autophosphorylation.
M6297 Upadacitinib Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research.
M5827 Oclacitinib maleate Oclacitinib is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, which did not inhibit a panel of 38 non-JAK kinases.
M5315 Baricitinib phosphate Baricitinib phosphate(INCB 028050; LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.
M5028 JANEX-1 Janex-1 is a cell-permeable, reversible, potent, ATP-competitive, and specific inhibitor of JAK3 (IC50 = 78 μM); has no effect on JAK1, JAK2, or Zap/Syk or SRC tyrosine kinases.
M4980 Decernotinib Decernotinib is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.
M4912 GLPG0634 analogue GLPG0634 analogue is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
M4870 Cerdulatinib Cerdulatinib (PRT-062070, PRT2070) is an orally active multi-target tyrosine kinase inhibitor with IC50s of JAK1/JAK2/JAK3/TYK2 and Syk 12 nM/6 nM/8 nM/0.5 nM and 32 nM, respectively. It was also able to inhibit the other 19 kinases tested, all with IC50 below 200 nM.
M4670 Curculigoside Curculigoside is the main saponin in C. orchioide, which has significant antioxidant, anti-osteoporosis, anti-depression and neuroprotective effects. By regulating the JAK/STAT/NF-κB signaling pathway, it showed significant anti-arthritis effects in vivo and in vitro.
M4572 Limonin Limonin, a triterpenoid rich in citrus fruits, has antiviral and anti-tumor activities.
M4138 Deucravacitinib (BMS-986165) Deucravacitinib (BMS-986165) is a first-in-class, selective, orally bioavailable inhibitor of TYK2 transitions.Deucravacitinib selectively binds the TYK2 pseudokinase (JH2) structural domain with an IC50 of 1.0 nM and a Ki value of 0.02 nM. Deucravacitinib (BMS-986165) blocks receptor-mediated Tyk2 activation by stably regulating the JH2 structural domain. deucravacitinib also inhibits the IL-12/23 and type I IFN pathways. deucravacitinib may be used in psoriasis research.
M3801 TCS 21311 TCS 21311 is a potent JAK3 inhibitor with IC50 of 8 nM.
M3737 Pyridone 6 Pyridone 6 is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK1 (IC50 = 15 nM for murine JAK1), JAK2 (IC50 = 1 nM), JAK3 (Ki = 5 nM), and Tyk 2 (IC50 = 1 nM) (Janus protein tyrosine kinases).
M3735 JAK2 Inhibitor V JAK2 Inhibitor V, Z3 is a novel specific inhibitor of Jak2 which inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
M3535 LY2784544 (Gandotinib) LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3.
M3141 ZM 39923 hydrochloride ZM 39923 is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase.
M3130 WHI-P154 WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation.
M2912 Pacritinib Pacritinib (SB1518) is an effective mutant inhibitor of wild-type JAK2 and JAK2V617F with IC50 of 23 nM and 19 nM, respectively. Pacritinib also inhibited FLT3 and its mutant FLT3D835Y with IC50 of 22 nM and 6 nM, respectively.
M2566 XL019 XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2.
M2466 BMS-911543 BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.

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