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JAK Janus Kinase

Inhibitors

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.
M10377 Golidocitinib (AZD4205) Golidocitinib (AZD4205) is a novel potent and selective janus kinase 1 (JAK1) inhibitor, with IC50 value of 73 nM.
M9930 PF-06826647 PF-06826647, also known as Tyk2-IN-8, is a selective and orally administered tyrosine kinase 2 (TYK2) inhibitor, with IC50 of 17 nM.
M9853 Brepocitinib P-Tosylate PF-06700841 (Brepocitinib) tosylate is a dual inhibitor of JAK1 and TYK2, with IC50 values of 17 nM and 23 nM, respectively.
M9627 JAK3-IN-6 (Compound 2) JAK3-IN-6 (Compound 2) CAS#: 1443235-95-7 is a potent and highly selective JAK3 inhibitor, with an IC50 of 0.15 nM.
M9147 Peficitinib Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
M9142 FLLL32 FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM.
M9035 WHI-P97 WHI-P97 is a JAK3 inhibitor with an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 microM in EGFR kinase inhibition assays.
M8996 SAR-20347 SAR-20347 is a potent dual inhibitor of JAK1 and TYK2 with IC50 values of 23 and 0.6 nM, respectively.
M8876 Itacitinib Itacitinib (INCB039110) is a potent, selective JAK1 inhibitor with an IC50 value of 2 nM for human JAK1. It has oral bioactivity and potential anti-tumor activity.
M8090 PF-04965842 Abrocitinib is an orally active and selective JAK1 inhibitor with an IC50 value of 29 nM. Abrocitinib reversibly inhibits JAK1 kinase by blocking its ATP-binding site. Abrocitinib (PF-04965842) inhibited TYK2 activity (IC50, 1.253 μM) and phosphorylation of STAT1, STAT3, and STAT5 after stimulation. It can be used in the study of autoimmune diseases.
M7551 Solcitinib Solcitinib is an oral, competitive, potent, and selective JAK1 inhibitor with an IC50 value of 9.8 nM, which is 11,55, and 23 times more selective than JAK2, JAK3, and TYK2. Solcitinib can be used in studies of psoriasis.
M6308 Ritlecitinib (PF-06651600) Ritlecitinib (PF-06651600) is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2.
M6297 Upadacitinib Upadacitinib (ABT-494) 是一种高效的、具有口服活性的、选择性 Janus 激酶 1 (JAK1) 抑制剂 (IC50=43 nM)。Upadacitinib 对 JAK1 的选择性约为 JAK2 (200 nM)的 74 倍。Upadacitinib 可用于多种自身免疫性疾病的研究。
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.
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.



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