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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.

RX-37 is a selective BET inhibitor. RX-37 binds to BET bromodomain proteins (BRD2, BRD3, and BRD4) with Ki values of 3.2-24.7 nM. RX-37 can be used for research of cancers[1].

[1] Ran X, et al. Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. J Med Chem. 2015 Jun 25;58(12):4927-39. DOI:10.1021/acs.jmedchem.5b00613