BET-IN-18 (Compound 3) is a pan- BET bromodomain small-molecule inhibitor, with K i values of 0.69 μM and 0.37 μM, and K d values of 1.6 μM and 8.4 μM against BrdT (1) and Brd4 (1) bromodomains, respectively. BET-IN-18 potently and competitively inhibits the binding of the known BET inhibitor (+)-JQ1 ( HY-13030 ) to Brd4 (1) and BrdT (1), with IC 50 values of 1.0 μM and 2.3 μM, respectively. BET-IN-18 also competitively inhibits the binding of acetylated histone substrates to Brd4 (1) ( IC 50 = 0.90 μM). BET-IN-18 can be used in the research of multiple myeloma.
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