JAK

Ifidancitinib (ATI-50002) is a potent and selective inhibitor of JAK kinases 1/3.

Lorpucitinib is a Gut-Restricted JAK Inhibitor for the research of Inflammatory Bowel Disease.

Povorcitinib is a potent and selective inhibitor of JAK1.

JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC50s of 4 and 2 nM for JAK2 and HDAC, respectively.

Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα.

JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells.

JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively.

NDI-034858 is a TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM.

Butyzamide is an orally effective Mpl activator, where Mpl is a receptor for thrombopoietin (TPO) involved in platelet production. Butyzamide increases the phosphorylation levels of JAK2, STAT3, STAT5 and MAPK. In mouse xenograft experiments, Butyzamide increases human platelet levels.

GS-829845 is the main active metabolite of Filgotinib. It is a JAK1 inhibitor, but its potency is about 10 times lower than that of the parent compound and it has a longer half-life.

JAK2/FLT3-IN-1 is an orally effective dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3 respectively. It has anti-cancer activity.

JAK-IN-25 (compound 19) is an effective JAK inhibitor with IC50 values of 6 nM, 21 nM, 8 nM, and 1051 nM for TYK2, JAK1, JAK2, and JAK3 respectively. It inhibits human whole blood IL-12 (HEB IL-12) with an IC50 value of 28 nM. JAK-IN-25 has potential for use in cancer research.

Pumecitinib is a JAK inhibitor with anti-inflammatory activity.

Ritlecitinib tosylate is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM.

JAK3i is a highly selective JAK3 inhibitor (IC50: 0.43 nM).

Fosifidancitinib is a potent and selective inhibitor of JAK kinases 1/3.

Nimucitinib is a Janus kinase (JAK) inhibitor.

PROTAC TYK2 degradation agent1 is a potent and subtype-selective TYK2 degrader.

JAK-IN-24 is a JAK inhibitor, with IC50s of 0.534 and 24 nM at the presence of 4 μM or 1mM ATP, respectively.

Lepzacitinib is a Janus kinase inhibitor targeting to JAK 1/3.