GSTO1-IN-1 是一种有效的谷胱甘肽 S-转移酶 omega 1 (GSTO1) 抑制剂，IC₅₀ 为 31 nM。

GSTO1-IN-1 is a potent glutathione S-transferase omega 1 (GSTO1) inhibitor with an IC 50 of 31 nM.

Solid

IC50: 31 nM (GSTO1)

GSTO1-IN-1 (C1-27) potently inhibits GSTO1 enzyme activity with an IC50 value of 31 nM. GSTO1-IN-1 also potently competes with 5-chloromethylfluorescein diacetate (CMFDA) for binding to 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 inhibits the clonogenic survival of HCT116 cells at sub-micromolar concentrations. has not independently confirmed the accuracy of these methods. They are for reference only.

To test whether GSTO1-IN-1 had in vivo efficacy, its effects are evaluated in a human colon cancer cell line xenograft model. 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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Ramkumar K, et al. Mechanistic evaluation and transcriptional signature of a glutathione S-transferase omega 1 inhibitor. Nat Commun. 2016 Oct 5;7:13084.

In Vitro: DMSO : ≥ 300 mg/mL (964.07 mM)配制储备液