OTS193320

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

OTS193320 (OTS-193320) 是蛋白质甲基转移酶 SUV39H2 的有效抑制剂，IC50 为 22.2 nM。

OTS193320 (OTS-193320) is a potent inhibitor of protein methyltransferase SUV39H2 with IC50 of 22.2 nM; significantly reduces global H3K9 tri-methylation (H3K9me3) in breast cancer cells in vitro and induces apoptotic cell death, attenuates γ-H2AX levels in combination with doxorubicin compared with the DOX treatment alone, and causes a significant reduction in breast cancer cell viability when compared to the treatment with a single agent; causes growth suppressive effect of SUV39H2-positive A549 lung cancer cells with IC50 of 0.38 uM.

Cell Viability Assay Cell Line:MCF-7, SK-BR-3, ZR-75-1, T-47D, MDA-MB-231, BT-20 breast cancer cell lines.Concentration:0-1 μM Incubation Time:72 hours Result:Had Growth inhibitory effect on MCF-7, SK-BR-3, ZR-75-1, T-47D, MDA-MB-231, and BT-20 breast cancer cell lines with IC50 values from 0.41 to 0.56 μM, respectively.Apoptosis AnalysisCell Line:MDA-MB-231 and BT-20 cells.Concentration:0.5 μM Incubation Time:48 hours Result:Showed an increase in the number of cells at early- and late-stage apoptosis.Western Blot Analysis Cell Line:MDA-MB-231 and BT-20 cells Concentration:0.125, 0.25, 0.5 μM Incubation Time:24 hours Result:Caused attenuation of H3K9me3 levels in a dose-dependent manner.

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OTS-193320 | OTS 193320

Chromatin/Epigenetic

HMTase

HMTase

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2093401-33-1

536.029

C28H30ClN5O4

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (116.60 mM)

COC1=CC(=C(C=C1C2=CN3C=CC(=CC3=N2)NC4CCC(CC4)NCC5=CC=C(C=C5)[N+](=O)[O-])Cl)OC

(1s,4s)-N1-(2-(5-chloro-2,4-dimethoxyphenyl)imidazo[1,2-a]pyridin-7-yl)-N4-(4-nitrobenzyl)cyclohexane-1,4-diamine

(-20℃)

With Ice Pack

≥ 2 years