RX-37 is a potent BET inhibitor. RX-37 binds to BET bromodomain proteins (BRD2, BRD3, and BRD4) with Ki values of 3.2-24.7 nM and demonstrates high selectivity over other non-BET bromodomain-containing proteins. RX-37 potently and selectively inhibits cell growth in human acute leukemia cell lines harboring the rearranged mixed lineage leukemia 1 gene. RX-37 represents a promising lead compound for the development of a new class of therapeutics for the treatment of human cancer and other conditions.
