JAK Inhibitor

Pyridone 6 (JAK Inhibitor)(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.

JAK 3 inhibitor IV (ZM 39923 hydrochloride) is a 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.

Ruxolitinib (INCB018424) is a JAK1 2 inhibitor (IC50=3.3 2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.

Gusacitinib (ASN-002) (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).

Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable, allosteric TYK2 inhibitor for the treatment of autoimmune diseases. It blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain, inhibiting IL-12 23 and type I IFN pathways. It selectively binds to the TYK2 pseudokinase (JH2) domain with an IC50 of 1.0 nM.

Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.

Baricitinib (INCB028050) is a JAK1 and JAK2 inhibitor (IC50=5.9 5.7 nM) with selective and oral activity. Baricitinib has potential anti-inflammatory, immunomodulatory and anti-tumor activity.

Itacitinib (INCB039110) is an orally bioavailable Janus-associated kinase 1 (JAK1) inhibitor with potential antineoplastic activity.

Osunprotafib (ABBV-CLS-484) is a potent, orally bioavailable PTP1B PTPN2 inhibitor in clinical trials for solid tumors. [1] Osunprotafib (ABBV-CLS-484) stimulates the tumor microenvironment and promotes natural killer cell and CD8 T cell function and enhances T cell anti-tumor immunity by enhancing JAK-STAT signaling and reducing T cell dysfunction. [2]

Tofacitinib (Tasocitinib) is a Janus kinase inhibitor that inhibits JAK3 2 1 (IC50=1 20 112 nM) and is orally active. Tofacitinib is used for the treatment of moderate to severe rheumatoid arthritis.

Upadacitinib (ABT-494) (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43 nM.

Abrocitinib (PF-04965842) (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29 803 nM for JAK1 2).

CHZ868 is a type II JAK inhibitor with potential antitumor activity that reverses the persistence of type I JAK inhibitors and can be used to study leukemia.

JAK-IN-5 is a JAK inhibitor.

JAK-IN-5 hydrochloride is a JAK inhibitor [1].

JAK-IN-11 (R-348) is a potent and selective inhibitor of JAK, has the potential for the skin disorders treatment.

JAK-IN-10 is a JAK inhibitor that can be used for the research of dry eye disorders.

Izencitinib (JNJ-8398) is an orally active and gut-selective JAK inhibitor with potential anti-inflammatory activity for the study of ulcerative colitis and Crohn;s disease.

FLLL32 is an effective JAK2 STAT3 inhibitor (IC50 of <5 μM).

JAK-STAT-IN-1 is a specific JAK-STAT inhibitor indicated for the study of autoimmune diseases.

Tofacitinib Citrate (CP-690550 citrate) is a a potent, cell-permeable inhibitor of JAK1 2 3 (IC50s: 1 20 112 nM).

Ruxolitinib phosphate (INCB18424 phosphate) is a JAK1 2 inhibitor with IC50 of 3.3 nM 2.8 nM. Its selectivity for JAK1 2 is more than 130 times that of JAK3.

Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1 2) with IC50 of 11 nM 18 nM. JAK1 2 inhibitor CYT387 competes with JAK1 2 for ATP binding, which may result in inhibition of JAK1 2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1 2-expressing tumor cells.

Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 values of 10 nM for JAK1, 28 nM for JAK2, 810 nM for JAK3, and 116 nM for TYK2.