Y06036

Research use only, not for human use.

Y06036 a potent and selective BET inhibitor can bind to the BRD4(1) bromodomain (Kd: 82 nM).

Y06036 a potent and selective BET inhibitor can bind to the BRD4(1) bromodomain (Kd: 82 nM).

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. Cell Viability Assay 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 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

Y06036 (50 mg/kg, i.p. injection, 5 times per week, 25 days) demonstrates therapeutic effects in a C4-2B CRPC xenograft tumor model in mice. Y06036 is well tolerated in the treated mice, based on the weight of the animal body and their general behavior. Animal Model:Four-week-old male mice (strain: C.B-17/IcrHsd-Prkdcscid for C4-2B) with C4-2B mouse xenograft model Dosage:50 mg/kg, 100 μL Administration:Intraperitoneal (i.p.) injection, 5 times per week, 25 days Result:Exhibited strong antitumor activities during the 25-day treatment period, with a tumor growth inhibition (TGI) of 70%.

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Chromatin/Epigenetic

Epigenetic Reader Domain

BRD4

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1832671-96-1

427.27

C16H15BrN2O5S

>98% (HPLC)

DMSO: 100 mg/mL (234 mM)

COc1ccc(Br)cc1S(=O)(=O)Nc1cc2c(C)noc2cc1OC

5-Bromo-2-methoxy-N-(6-methoxy-3-methylbenzo[d]-isoxazol-5-yl)benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years