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BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1 (IC50=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage[1]. | [References]
[1] Yu S et al. Discovery of (R)-4-(8-methoxy-2-methyl-1-(1-phenylethy)-1H-imidazo [4, 5-c] quinnolin-7-yl)-3, 5-dimethylisoxazole as a potent and selective BET inhibitor for treatment of acute myeloid leukemia (AML) guided by FEP calculation[J]. European Journal of Medicinal Chemistry, 2023: 115924. |
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