gsto1

GSTO1-IN-1 is a potent glutathione S-transferase omega 1 inhibitor (GSTO1) with an IC50 of 31 nM.

GSTO1-IN-4 is a selective and potent inhibitor of GSTO1-1, exhibiting an IC50 of 0.04 μM and a KI of 0.16 μM. It has weaker inhibitory effects on GSTO2-2, GSTA1-1, and GSTP1-1. GSTO1-IN-4 alleviates inflammation in mice and significantly enhances the cytotoxicity of Cisplatin, making it useful for research in inflammation and breast cancer.

GSTO1-IN-5 is a potent and selective inhibitor of glutathione S-transferase ω1 (GSTO1), with an IC50 value of 0.22 nM. It is applicable in cancer and inflammation-related research, including studies on colon cancer.

GSTO1-IN-3 is a potent inhibitor of GSTO1-1, with an IC50 value of 0.11 μM, and exhibits selectivity towards GSTO2-2, GSTA1-1, and GSTP1-1 (IC50> 100 μM). It enhances the cytotoxic effects of Cisplatin on human breast cancer cells and inhibits IL-1β release in mouse bone marrow-derived macrophages (BMDM). Additionally, GSTO1-IN-3 reduces inflammation in mice and is applicable for research related to breast cancer and inflammation.

GSTO1-IN-6 is an allosteric covalent inhibitor of GSTO1 with an IC50 of 457 nM. It significantly reduces lipopolysaccharide (LPS)-induced secretion of IL-1β with an IC50 of 1.9 μM and IL-18 with an IC50 of 10 μM in human monocyte-derived macrophages. GSTO1-IN-6 covalently binds to GSTO1-Cys32, inducing conformational changes and protein instability. This compound is applicable in the study of inflammatory diseases.

GSTO1-IN-2 (Compound B-9) is a dual covalent inhibitor targeting GSTO1 and BTK with IC50 values of 441 nM and 6.2 nM, respectively.

ML175 is a specific inhibitor of glutathione transferase Omega 1-1 (GSTO1-1). Additionally, it significantly activates Akt and MEK1/2 kinases. ML175 can be utilized in research related to diseases such as Parkinson's.