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DMU2139
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
DMU2139图片
CAS NO:1821143-80-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
DMU2139 是一种有效且特异性的 CYP1B1 抑制剂,对 CYP1B1 和 CYP1A1 的 IC50 分别为 9 nM 和 795 nM。
Cas No.1821143-80-9
Canonical SMILESO=C(C1=CC=C2C=C(OC)C=CC2=C1)/C=C/C3=CC=CN=C3
分子式C19H15NO2
分子量289.33
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.

DMU2139 (6j) shows 88 and 133-fold selectivity for CYP1B1 over CYP1A1 and CYP1A2. In the presence of DMU2139, the EC50 is reversed back to 8.3 μM from 61 μM (seen in CYP1B1-expressing cells without any inhibitor). The EC50 value, in the presence of DMU2139, resembles the EC50 of cisplatin, 8.7μM, in cells transfected with the empty plasmid which has no CYP1B1 gene and therefore cannot express CYP1B1 protein[1].

[1]. Horley NJ, et al. Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines. Eur J Med Chem. 2017 Mar 31;129:159-174.