OTS186935 trihydrochloride

OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

IC50: 6.49 nM (SUV39H2)[1]

OTS186935 trihydrochloride inhibits A549 cell growth with IC50 of 0.67 μM[1].

OTS186935 trihydrochloride (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] Dosage: 10 mg/kg Administration: Intravenously; once daily for 14 days Result: Tumor growth inhibition of 42.6% on day 14. Animal Model: Female BALB/cAJcl-nu/nu mice (bearing A549 cells)[1] Dosage: 25 mg/kg Administration: Intravenously; once daily for 14 days Result: Yielded a tumor growth inhibition of 60.8% without significant body weight loss or toxicity.

[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.