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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.
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.
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.
M40753 Ritlecitinib tosylate Ritlecitinib tosylate is a first-in-class, orally active, dual covalent inhibitor of tyrosine kinases in the JAK3 and TEC families. The IC50 for JAK3 is 33.1 nM and there is no activity against JAK1, JAK2 and TYK2.
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.

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