BSK805

BSK805 (also referred to as NVP-BSK805) is a potent and selective ATP-competitive small molecule inhibitor of Janus kinase 2 (JAK2)[1][4][6]. JAK2 is a member of the Janus kinase family, involved in the signaling of type II cytokine receptor family, GM-CSF receptor family, gp130 receptor family, and single-chain receptors[1][4]. BSK805 exhibits high selectivity for JAK2 over other JAK family members (>20-fold) and over a panel of unrelated kinases, and strongly blocks STAT phosphorylation and downstream cytokine signaling related to oncogenesis and immunoregulation[1][4][6]. BSK805 displays potent antiproliferative and proapoptotic effects in vitro in various JAK2-dependent cell lines and animal models, particularly those with the JAK2V617F mutation seen in myeloproliferative neoplasms, and it sensitizes cells to radiotherapy[4][5][6][8]. The compound is orally bioavailable in preclinical models and shows a favorable pharmacokinetic profile but is not clinically developed due to photoinstability issues[4][6]. Developed mainly as a research tool, BSK805 was originally made available by Novartis[6].

Other names

NVP-BSK805NVP-BSK-805NVP-BSK 805NVP-BSK805 dihydrochlorideNVP-BSK-805 dihydrochlorideNVP-BSK 805 dihydrochloride