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MST-312 is a telomerase inhibitor (IC50 = 0.67 μM in a TRAP assay).1 It is selective for telomerase over DNA polymerase when used at concentrations up to 3 μM. MST312 inhibits growth of U937 cells via telomere shortening (GI50 = 1.7 μM). It reduces cell number and expression of the proliferation marker MIB-1 as well as increases DNA damage in primary pediatric ependymoma tumor cells.2 MST-312 decreases survival of H460 and H1299 non-small cell lung cancer (NSCLC) cells in a dose-dependent manner with a greater effect on the aldehyde dehydrogenase positive (ALDH+) cancer stem cell population.3 In vivo, MST-312 (40 mg/kg) reduces tumor size by 70% in an H460 mouse xenograft model. MST-312 also inhibits replication of herpes simplex virus 2 (HSV-2) and a clinical isolate of HSV-1 and decreases accumulation of early and late viral proteins in HEp-2 cells infected with HSV-1.4
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1. Telomere shortening and growth inhibition of human cancer cells by novel synthetic telomerase inhibitors MST-
2. Telomerase inhibition as a novel therapy for pediatric ependymoma. Brain Pathol. 20(4), 780-786 (2010).
3. Inhibition of telomerase activity preferentially targets aldehyde dehydrogenase-
4. The telomerase inhibitor MST-