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UNC 0631
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。
UNC 0631图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议
100mg电议

产品介绍
UNC 0631 是一种有效的组蛋白甲基转移酶 G9a 抑制剂,IC50 为 4 nM。 UNC 0631 有效降低 MDA-MB-231 细胞中的 H3K9me2 水平,IC50 为 25 nM。

Cell lines

MDA-MB-231 cells

Preparation method

The solubility of this compound in DMSO is >18.35mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

48 h

Applications

In MDA-MB-231 cells, UNC 0631 was highly potent in reducing H3K9me2 levels with IC50 value of 0.026 μM and had low cell toxicity with excellent tox/function ratios. UNC 0631 had high in vitro potency versus G9a and improved lipophilicity. UNC 0631 was valuable alternative tool compound that might be more suitable for investigating specific cellular systems.

产品描述

UNC 0631 is a potent inhibitor of Protein lysine methyltransferase G9a (also known as KMT1C or EHMT2) with the IC50 value of 4nM [1].

UNC 0631 has been revealed to inhibit the G9a in SAHH-coupled with the IC50 of 4nM. Besides, UNC 0631 has been found to be highly potent in reducing H3K9me2 levels in MDA-MB-231 cells with the ICW IC50 of 25nM. In addition, UNC 0631 has been shown the high in vitro potency against G9a and improved lipophilicity. Besides, UNC 0631 has also been reported to have low cell toxicity in MDA-MB-231 cells with the IC50 value of 2.8μM in MTT assay. In different cell lines, UNC 0631 has been demonstrated to potently reduce H3K9me2 levels with the ICW IC50 of 25nM, 18nM, 26nM, 24nM, 51nM, 72nM and 46nM in MDA-MB-231, MCF7, PC3, 22RV1, HCT116 wt, HCT 116 p53 and IMR90 cell lines, respectively [1].

References:
[1] Liu F1, 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 Sep 8;54( 17):6139-50.