Description
An inhibitor of BRD bromodomains; inhibits BD1 and BD2 in BRDT, BRD2, BRD3, and BRD4 (IC50s = 52-217 nM in a time-resolved FRET assay); reduces the levels of c-Myc, as well as induces cell cycle arrest at the G1 phase and apoptosis, in MM.1S cells at 500 nM; decreases the proliferation of RPMI-8226, MM.1S, KMS-20, L-363, and AMO1 cells when co-cultured with HS-5 cells at 1 µM; decreases tumor burden and increases survival in an MM.1S orthotopic mouse model at 50 mg/kg per day; reduces testis weight, sperm count, sperm motility, testis tubule area, and the number of pups per litter without reducing the levels of testosterone, luteinizing hormone, or FSH in mice at 50 mg/kg per day