OTS186935hydrochloride是一种有效的蛋白甲基转移酶SUV39H2抑制剂，IC50值为6.49nM。OTS186935hydrochloride对小鼠异种移植模型的肿瘤生长有明显的抑制作用，且无明显毒性。OTS193320hydrochloride调节癌细胞中γ-H2AX的产生。
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells[1].
OTS186935 hydrochloride inhibits A549 cell growth with an IC50 of 0.67 μM[1].
OTS186935 hydrochloride (10 mg/kg or 25 mg/kg; intravenously; once daily for 14 days) exhibits growth suppressive effects in human cancer cell line derived xenograft models[1]. Animal Model: Female NOD.CB17-Prkdcscid/J mice (bearing MDA-MB-231 cells )[1]
[1]. Vougiouklakis T, et al. Development of novel SUV39H2 inhibitors that exhibit growth suppressive effects in mouse xenograft models and regulate the phosphorylation of H2AX. Oncotarget. 2018 Aug 7;9(61):31820-31831.
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