NVP-BSK805 trihydrochloride

NVP-BSK805 trihydrochloride (BSK 805) is a JAK2 inhibitor, with IC₅₀s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively. NVP-BSK805 trihydrochloride inhibits the full-length wild-type JAK2 (FL JAK2 wt) and FL JAK2 V617F activity, with IC₅₀s of 0.58 ± 0.03 and 0.56 ± 0.04 nM. NVP-BSK805 trihydrochloride is ATP-competitive, with aclculated K_i of 0.43 ± 0.02 nM. NVP-BSK805 trihydrochloride suppresses the growth of JAK2^V617F-bearing acute myeloid leukemia cell lines with GI₅₀ of <100 nM. NVP-BSK805 trihydrochloride blocks the STAT5 phosphorylation at ≥100 nM concentrations, and shows a bias for JAK2 over JAK1 and JAK3 inhibition in the JAK2^V617F-mutant cell lines^[1].
NVP-BSK805 trihydrochloride (5 μM) improves P-gp inhibitory activity. NVP-BSK805 trihydrochloride increases sensitization of drug-resistant KBV20C cancer cells to VIC treatment at 10 μM, and such an effect is more effective than a 5 μM dose^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.