GSTO1-IN-1 is a potent glutathione S-transferase omega 1 (GSTO1) inhibitor with an IC50 of 31 nM
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HazMat fee for 500 gram (Estimated)
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Glutathione S-transferases are a family of enzymes primarily involved in phase II metabolism. Glutathione S-transferase omega 1 (GSTO1) is an atypical GST isoform that catalyzes S-phenacyl glutathione reduction and monomethylarsonate (V) reduction. GSTO1-IN-1 is a potent GSTO1 inhibitor that inhibits the enzyme activity of GSTO1 with an IC50 value of 31nM. GSTO1-IN-1 potently competed with CMFDA for binding to endogenous and recombinant GSTO1 in HCT116 soluble proteome. Treatment with GSTO1-IN-1 at 0.12-10µM inhibited the colony formation of HCT116 cells. The incubation of HCT116 cells with 5µM GSTO1-IN-1 for 24 h led to a decrease in the G0/G1 population and a concomitant increase in the S-phase population. Administration of GSTO1-IN-1 at 20-45mg/kg/day for 5 weeks significantly inhibited tumor growth in nude mice bearing HCT116 xenografts as compared to the vehicle-treated group. In the KRAS-mutant CRM-13-180 PDX model, GSTO1-IN-1 treatment (50mg/kg) resulted in a modest inhibition of tumor growth with a percent treated/control (%T/C) of 67[1].
作用机制
GSTO1-IN-1 is a potent, covalent GSTO1 inhibitor that binds to GSTO1-IN-1 through both hydrophobic and hydrophilic interactions[1].
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