jak3-in-14

JAK3-IN-14 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively.

JAK3 BTK-IN-7 (XL-12), characterized as a JAK3 BTK inhibitor, exhibits IC 50 values of 2 nM and 14 nM for JAK3 and BTK respectively. This compound demonstrates anti-inflammatory properties and is applicable in research related to rheumatoid arthritis [1].

JAK-IN-14 (compound 16) is a specific JAK1 inhibitor with IC50<5 μM. It prevents JAK1 phosphorylation by binding to the active site of JAK1, and is more than 8-fold selective for JAK1 over JAK2 JAK3, and can be used in immune, inflammation and cancer research.

JAK2-IN-7, a selective inhibitor targeting Janus Kinase 2 (JAK2), exhibits inhibitory concentrations (IC50) of 3 nM for JAK2, 11.7 nM for SET-2 cells, and 41 nM for Ba F3 V617F cells, indicative of its potency and selectivity. This compound demonstrates more than 14-fold selectivity against JAK1, JAK3, and FLT3, underlining its specificity. JAK2-IN-7 effectively induces cell cycle arrest at the G0 G1 phase and promotes apoptosis in tumor cells, manifesting significant antitumor activities [1].

JAK-IN-20 is a potent, orally active, broad-based JAK inhibitor, effective on JAK1 (IC50: 7 nM), JAK2 (IC50: 5 nM), and JAK3 (IC50: 14 nM), exhibiting excellent pharmacokinetic and anti-inflammatory activity in vivo.