RX-37

A potent and specific BET bromodomain inhibitor with Ki of 3.2-24.7 nM for BD1 and BD2 domains of BRD2, BRD3, and BRD4; shows an excellent selectivity over other non-BET bromodomain-containing proteins with the exception of CREBBP (Kd=670 nM); potently and selectively inhibits cell growth in human acute leukemia cell lines harboring the rearranged MLL1 gene (IC50=20 nM for MV4;11 cells).

References 1. Ran X, et al. J Med Chem. 2015 Jun 25;58(12):4927-39. View Related Products by Target Bromodomain