382192
HMTase Inhibitor IV, UNC0638
The HMTase Inhibitor IV, UNC0638 controls the biological activity of HMTase. This small molecule/inhibitor is primarily used for Cancer applications.
别名:
HMTase Inhibitor IV, UNC0638, DNA Methyltransferase Inhibitor III, DNA MTase Inhibitor III, EHMT1/GLP Inhibitor II, EHMT2/G9a Inhibitor IV, 2-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine
质量水平
方案
≥98% (HPLC)
表单
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
off-white
溶解性
DMSO: 10 mg/mL
运输
ambient
储存温度
−20°C
SMILES字符串
CC(C)N(CC1)CCC1NC2=NC(C3CCCCC3)=NC4=C2C=C(C(OCCCN5CCCC5)=C4)OC
InChI
1S/C30H47N5O2/c1-22(2)35-17-12-24(13-18-35)31-30-25-20-27(36-3)28(37-19-9-16-34-14-7-8-15-34)21-26(25)32-29(33-30)23-10-5-4-6-11-23/h20-24H,4-19H2,1-3H3,(H,31,32,33)
InChI key
QOECJCJVIMVJGX-UHFFFAOYSA-N
一般描述
A cell-permeable quinazolinamine compound that acts as a potent and reversible inhibitor of G9a and GLP HMTases (histone methyltransferases) (IC50 = ≤ 15 and 19 nM for G9a and GLP, respectively) and displays ~15-fold greater selectivity over DNMT1 and minimally blocks the activities of JMJD2E (IC50 = 4.66 µM) and SETD7, SETD8, PRMT3 and SUV39H2 (IC50 >10 µM). Shown to lower H3K9Me2 levels in MDA-MB231 cells (IC50 = 81 nM; EC50 = 11.2 µM for cell toxicity) and 6-fold more potent than the HMTase Inhibitor, BIX-01294, (Cat. No. 382190). Also, affects the activities of adrenergic α1A, adrenergic α1B and muscarinic M2 by 90%, 69% and 64% and a panel of 26-receptors and ion-channels by ≤ 30% at 1 µM.
This probe is supplied in conjunction with the Structural Genomics Consortium (SGC). For further characterization details, please visit the UNC0638 probe summary on the SGC website.
This probe is supplied in conjunction with the Structural Genomics Consortium (SGC). For further characterization details, please visit the UNC0638 probe summary on the SGC website.
包装
Packaged under inert gas
其他说明
Vedadi, M., et al. 2011. Nat. Chem. Biol.7, 566.
Liu, F., et al. 2011. J. Med. Chem.54, 6139.
Liu, F., et al. 2011. J. Med. Chem.54, 6139.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Regulatory Review (Z)
储存分类代码
11 - Combustible Solids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系客户支持