DMU2139 _Cytochrome P450 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDMU2139Cat. No.: HY-101285CAS No.: 1821143-80-9分式: CHNO分量: 289.33作靶点: Cytochrome P450作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 77.5 mg/mL (267.86 mM; Nee

2、d ultrasonic)Ethanol : 5 mg/mL (17.28 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.58 mg/mL (8.92 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.58 mg/mL (8.92 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性

3、DMU2139有效的特异性细胞素 P4501B1 (CYP1B1) 的抑制剂，其对 CYP1B1 和 CYP1A1 的 IC50 值分别为9 nM，795 nM。IC50 & Target CYP1B1 CYP1A19 nM (IC50) 795 nM (IC50)体外研究 DMU2139 (6j) shows 88 and 133-fold selectivity for CYP1B1 over CYP1A1 and CYP1A2. In the presence ofDMU2139, the EC50 is reversed back to 8.3 M from 61 M (seen in

4、 CYP1B1-expressing cells without anyinhibitor). The EC50 value, in the presence of DMU2139, resembles the EC50 of cisplatin, 8.7M, in cellstransfected with the empty plasmid which has no CYP1B1 gene and therefore cannot express CYP1B1protein 1.REFERENCES1. Horley NJ, et al. Discovery and characteriz

5、ation of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatinresistance in CYP1B1-overexpressing lines. Eur J Med Chem. 2017 Mar 31;129:159-174.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 021-58955