UNC 0646

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UNC 0646

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。

CAS NO:

1320288-17-2

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	询价
5mg	询价
10mg	询价
50mg	询价

UNC 0646 是一种有效的选择性组蛋白甲基转移酶 G9a 抑制剂，IC50 为 6 nM。 UNC 0646 也是一种有效的 GLP 抑制剂 (IC50 \u003c15 nM)，对 G9a/GLP 的选择性高于 SETD7、SUV39H2、SETD8 和 PRMT3。 UNC 0646 降低 MDA-MB-231 细胞中的 H3K9me2 水平，IC50 为 26 nM。

Cas No.	1320288-17-2
别名	N-(1-环己基-4-哌啶基)-2-[六氢-4-异丙基-1H-1,4-二氮杂卓-1-基]-6-甲氧基-7-[3-(1-哌啶基)丙氧基]-4-喹唑啉胺
化学名	N-(1-cyclohexylpiperidin-4-yl)-6-methoxy-7-(3-piperidin-1-ylpropoxy)-2-(4-propan-2-yl-1,4-diazepan-1-yl)quinazolin-4-amine
Canonical SMILES	CC(C)N1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)C5CCCCC5)OC)OCCCN6CCCCC6
分子式	C₃₆H₅₉N₇O₂
分子量	621.9
溶解度	≥ 24.1mg/mL in DMSO with gentle warming, ≥ 87 mg/mL in EtOH
储存条件	Store at 4℃
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	IC50: 6 nm (G9a IC50); 26 nm (Cellular IC50); 3.3 μM (Cell toxicity EC50) Histone-lysine N-methyltransferase, H3 lysine-9 specific 3, also known as euchromatic histone-lysine N-methyltransferase 2 (EHMT2) and G9a, is a histone methyltransferase that in humans is encoded by the EHMT2 gene. Protein lysinemethyltransferase G9a plays key roles in the transcriptional repression of a variety of genes via dimethylation of lysine 9 on histoneH3 (H3K9me2) of chromatin as well as dimethylation of nonhistone proteins including tumor suppressor p53. In vitro: UNC0646 is reported to be a potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50 values are 6 nM and 15 nM for G9a and GLP, respectively). UNC0646 also potently blocks G9a/GLP methyltransferase activity in cells (IC50 = 10 nM in MCF7 cells) and exhibits low cellular toxicity (EC50 = 4.7 μM in MCF7 cells). UNC0646 is selective for G9a/GLP over a range of other protein lysine methyltransferases and protein arginine methyltransferases [1]. In vivo: The authors previously discovered potent and selective G9a/GLP inhibitors including the cellular chemical probe UNC0638, which displays an excellent separation of functional potency and cell toxicity. However, this inhibitor is not suitable for animal studies due to its poor pharmacokinetic (PK) properties. In this study, the authors report the discovery of the first G9a and GLP in vivo chemical probe UNC0642, which not only maintains high in vitro and cellular potency, low cell toxicity, and excellent selectivity, but also displays improved in vivo PK properties, making it suitable for animal studies [2]. References: [1] Liu F, Barsyte-Lovejoy D, Allali-Hassani A, He Y, Herold JM, Chen X, Yates CM, Frye SV, Brown PJ, Huang J, Vedadi M, Arrowsmith CH, Jin J. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011;54(17):6139-50. [2] Liu F, Barsyte-Lovejoy D, Li F, Xiong Y, Korboukh V, Huang XP, Allali-Hassani A, Janzen WP, Roth BL, Frye SV, Arrowsmith CH, Brown PJ, Vedadi M, Jin J. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013;56(21):8931-42.