GSTO1-IN-1 是谷胱甘肽 S-转移酶 omega 1 抑制剂，IC50=31 nM。

GSTO1-IN-1 is a potent glutathione S-transferase omega 1 inhibitor (GSTO1; IC50: 31 nM).

GSTO1-IN-1 inhibits the clonogenic survival of HCT116 cells at sub-micromolar concentrations. GSTO1-IN-1 also potently competes with 5-chloromethylfluorescein diacetate (CMFDA) for binding to the recombinant protein, as well as endogenous GSTO1 in the milieu of a soluble proteome.?HCT116 cells treated with GSTO1-IN-1 also show a decrease in cell viability in a dose-dependent manner.

GSTO1-IN-1 (20-45 mg/kg) is administered as a single agent to nude mice bearing HCT116 xenografts. After 5 weeks of treatment, tumor growth is significantly inhibited in GSTO1-IN-1-treated mice compared with the vehicle-treated group (P<0.05). GSTO1-IN-1 treatment is generally well tolerated by mice up to 45 mg/kg, with no overt signs of toxicity and no significant variations in average body weights throughout the duration of the study.

568544-03-6

C10H12Cl2N2O3S

311.19

DMSO:300 mg/mL (964.07 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years