產品屬性：
產品名稱 | CM-579 trihydrochloride |
規格 | 10mM*1mL in DMSO、5mg、10mg、50mg、100mg、200mg、500mg |
貨號 | EY-01Y13162 |
Cas No.: N/A
別名: N/A
化學名: N/A
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); H2O: 37.5 mg/mL (62.29 mM)
儲存條件: 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
產品描述：
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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