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JAK Janus Kinase

Cat.No.  Name Information
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.
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.
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.
M2346 Filgotinib Filgotinib (GLPG0634) is the first selective inhibitor of JAK1 and JAK2 with IC50 of 10nM and 28nM respectively.
M2125 WP1066 WP1066 is a potent, novel inhibitor of JAK2 and STAT3 with IC50 of 2.3 μM and 2.43 μM in HEL cells.
M2044 AZD1480 AZD1480 is a novel small-molecule inhibitor of JAK1/2 with IC50 of 1.3 nM and 0.26 nM, respectively.
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.
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.
M1733 TG101348 TG101348 is a selective small-molecule Janus kinase 2 (JAK2) inhibitor with IC50 of 3 nM.
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).
M49615 Oclacitinib Oclacitinib is a novel JAK inhibitor.
M43806 Londamocitinib Londamocitinib is a potent and selective JAK1 inhibitor with anti-inflammatory activity.
M31205 G5-7  G5-7 is an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.
M30102 Coumermycin A1  Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria. Coumermycin A1 shows anti-orthopoxvirus activity.
M28457 Ivarmacitinib Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects.
M28279 Fedratinib hydrochloride hydrate Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively.
M25460 Zasocitinib Zasocitinib (NDI-034858) is a highly selective, orally active TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM.
M13853 Itacitinib adipate Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.




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