BI-2536

BI-2536 is a small molecule inhibitor of Polo-like kinase 1 (PLK1), a serine/threonine-protein kinase that plays a critical role in mitosis and cell division. By binding to and inhibiting PLK1, BI-2536 induces mitotic arrest, disrupts cytokinesis, and triggers apoptosis in susceptible tumor cells. It has demonstrated potent antineoplastic activity in preclinical models and was investigated for the treatment of various cancers including non-small cell lung cancer, acute myeloid leukemia, pancreatic cancer, prostate cancer, small cell lung cancer, solid tumors, and non-Hodgkin's lymphoma. The drug was developed by Boehringer Ingelheim but its clinical development for these indications has been discontinued[1][3][5]. Additionally, it exhibits high selectivity for PLK1 (IC50 = 0.83 nM) with some activity against other polo-like kinases (PLK2/PLK3) at higher concentrations[4][8]. Recent research also suggests potential effects on BRD4 inhibition and possible utility outside oncology such as diabetic kidney disease[8].

Other names

755038-02-94LJG22T9C6