Description
BC13 is a dual inhibitor of cyclin-dependent kinase 6 (Cdk6) and bromodomain-containing protein 4 (BRD4; IC50s = 36.03, 234.12, and 137.42 nM for Cdk6 and BRD4 bromodomain 1 (BD1) and BD2), respectively).1 It is selective for Cdk6 over Cdk1-Cdk5 at 500 nM and for BD1 and BD2 in BRD4 over those in BRD2 and BRD3 (IC50s = >1,000, >1,000, 863.41, and 967.5 nM, respectively). It inhibits the proliferation of MDA-MB-231 and BT-549 triple-negative breast cancer (TNBC) cells (IC50s = 2,250 and 980 nM, respectively) but not non-cancerous MCF-10A cells (IC50 = >16.1 µM). BC13 (2 µM) in combination with the ferroptosis inducer RSL3 (Item No. 19288) synergistically reduces colony formation of MDA-MB-231 cells. It also reduces tumor growth in an MDA-MB-231 mouse xenograft model when administered at a dose of 25 mg/kg every other day.WARNING This product is not for human or veterinary use.
