A1874 - BRD4-degrading PROTAC - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEA1874Cat. No.: HY-114305CAS No.: 2064292-12-0分式: CHClFNOS分量: 1173.59作靶點: PROTAC; Epigenetic Reader Domain作通路: PROTAC; Epigenetics儲存式: 4C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored undernitrogen)溶解

2、性數據體外實驗 DMSO : 150 mg/mL (127.81 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.13 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (2.13 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 A1874種以

3、 nutlin 為基礎的、BRD4-降解的 PROTAC，DC50 值為 32 nM (誘導細胞內的 BRD4 降解)。有效抑制多種癌細胞增殖 1。IC50 & Target BRD4體外研究 Treatment of HCT116 cells of A1874 (0-10 M, 24 hours) induces a dose-dependent knockdown of BRD4levels, with near-maximum knockdown by 100 nmol/L and a maximum degradation (Dmax) of BRD4 of 98% ofthe lev

4、els in control (0.1% DMSO-treated) cells 1.Treatment of HCT116 cells of A1874 (0-10 M, 24 hours) increases p53 levels in the HCT116 cells andshowed dose-dependent p53 stabilization 1.Western Blot Analysis 1Cell Line: HCT116 cells.Concentration: 0-10 M.Incubation Time: 24 hours.Result: Induced a dose

5、dependent knockdown of BRD4 levels, with near-maximum knockdown by100 nM.Increased p53 levels and showed dose-dependent p53 stabilization.REFERENCES1. Hines J, et al. MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4and Stabilization of p53. Cancer Res. 2019 Jan 1;79(1):251-262.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 0