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Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM[1]. Antitumor activity[1].

Y06036 (0.001-100 nM, 96 hours for LNCaP, C4-2B, and 22Rv1 cells; 144 hours for VCaP cells) exhibits low micromolar or nanomolar potencies (IC50: 0.29-2.6 μμ) in the four androgen receptor (AR)-positive prostate cancer cell lines LNCaP, C4-2B, 22Rv1, and VCaP. Treatment of 22Rv1 cells with Y06036 (1, 2, 4, 8, and 16 μM, 48 hours) results in significant down-regulation of both full-length (AR-fl) and AR variants levels[1].|| Cell Viability Assay[1]||Cell Line:|LNCaP, C4-2B, 22Rv1, and VCaP prostate cancer cells |Concentration:|0.001-100 μM|Incubation Time:|96 hours for LNCaP, C4-2B, and 22Rv1; 144 hours for VCaP|Result:|Inhibited LNCaP, C4-2B, 22Rv1, and VCaP cells with IC50s of 1.06, 2.62, 1.50, 0.63 μM, respectively.|| Western Blot Analysis[1]||Cell Line:|22Rv1 cells|Concentration:|1,2,4,8, and 16 μM|Incubation Time:|48 hours|Result:|Resulted in significant down-regulation of both AR-fl and AR variants levels

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