OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with
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Product Description
OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (DOX; HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX
In Vitro
OTS193320 (0.125-0.5 μM; 24 hours) has growth inhibitory effect on breast cancer cell lines. OTS193320 exhibits a high inhibitory effect against SUV39H2 enzymatic activity (IC 50 =22.2 nM) and a growth suppressive effect of SUV39H2-positive A549 lung cancer cells (IC 50 =0.38 μM). OTS193320 (0.5 μM; 48 hours) induces apoptosis in breast cancer cells. OTS193320 (0.125-0.5 μM; 24 hours) causes attenuation of H3K9me3 levels in a dose-dependent manner. OTS193320 sensitizes breast cancer cells to doxorubicin via attenuation of γ-H2AX. Combination of OTS193320 and doxorubicin (DOX) significantly attenuates cancer cell viability in vitro, compared to single agent treatment of either drug. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 IC 50 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 AnalysisCell 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.
