A1874,2064292-12-0

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抑制剂描述：

产品名称：A1874

产品别名：见爱必信官网

英文别名：A1874

靶点：Bromodomain BET/PROTAC

CAS：2064292-12-0

纯度：98%

外观：见爱必信官网

保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

描述：A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.

溶解性：DMSO : 150 mg/mL (127.81 mM; Need ultrasonic)

体外研究：

Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) induces a dose-dependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nmol/L and a maximum degradation (Dmax) of BRD4 of 98% of the levels in control (0.1% DMSO-treated) cells.Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) increases p53 levels in the HCT116 cells and showed dose-dependent p53 stabilization.Western Blot AnalysisCell Line:HCT116 cells.Concentration:0-10 μM.Incubation Time:24 hours.Result:Induced a dosedependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nM.Increased p53 levels and showed dose-dependent p53 stabilization.

体内研究：

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