UNC 0631 |
| カタログ番号GC12548 |
UNC 0631 は、4 nM の IC50 を持つ強力なヒストンメチルトランスフェラーゼ G9a 阻害剤です。 UNC 0631 は、MDA-MB-231 細胞の H3K9me2 レベルを 25 nM の IC50 で強力に低下させます。
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Cas No.: 1320288-19-4
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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