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CM-579 trihydrochloride
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。
CM-579 trihydrochloride图片

CM-579 trihydrochloride 是一线的、可逆的,G9a 和DNA 甲基转移酶 (DNMT) 的双抑制剂,其IC50 值分别为 16 nM 和32 nM。在多种癌细胞中发挥有效活性作用。
Canonical SMILESCN1CCC(CNC2=CC(C3=CC=C(C)O3)=NC4=CC(OCCCN5CCCC5)=C(OC)C=C24)CC1.Cl.Cl.Cl
分子式C29H43Cl3N4O3
分子量602.04
溶解度DMSO: 125 mg/mL (207.63 mM); Methanol: 75 mg/mL (124.58 mM); Water: 37.5 mg/mL (62.29 mM)
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

CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells[1]. DNA Methyltransferase|32 nM (IC50)|DNMT1|1.5 nM (Kd)|DNMT3A|92 nM (IC50)|DNMT3B|1000 nM (IC50)|G9a|16 nM (IC50)

The Kd of CM-579 for DNMT1 is 1.5 nM, CM-579 also inhibits DNMT3A and DNMT3B, with IC50s of 92 nM and 1000 nM, respectively[1].

[1]. San JosÉ-EnÉriz E, et al. Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies. Nat Commun. 2017 May 26;8:15424.

 
 
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