gstp1-1

GSTP1-1 inhibitor 2 (Compound 5g) is an inhibitor of hGSTP1-1 (glutathione S-transferase P1-1), exhibiting an IC50 of 12.2 μM. It demonstrates substantial cytotoxicity against the cell lines DU-145, PC3, and MCF-7, with CC50 values of 36.6, 11.9, and 17.4 μM respectively, making it relevant for research in cancer therapeutics.

GSTP1-1 Inhibitor 1 (compound 6b) is an irreversible, long-acting inhibitor of glutathione S-transferase with a specific focus on GSTP 1-1, exhibiting an IC 50 of 21 μM. As GSTP 1-1 plays a crucial role in tumor suppression, this compound shows promising potential for anticancer activity [1].

GSTO-IN-2 is a glutathione S-transferase inhibitor with IC50 values of 1.4 μM for GSTP1-1, 16.3 μM for GSTM1, and 3.6 μM for GSTA2.

NBDHEX is a potent inhibitor of glutathione S-transferase P1-1 (GSTP1-1) .

Ezatiostat (TER199(free base)) is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity.

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-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.

Ezatiostat hydrochloride (TLK199 HCl) is an effective inhibitor of glutathione S-transferase. Ezatiostat hydrochloride is a novel glutathione analog and the potential treatment of cytopenias. In addition, Ezatiostat hydrochloride has been revealed to selectively bind to and thus inhibit GSTP1-1.

Cyclopropenone probe 1 can specifically and efficiently modify a triple-negative breast cancer driver, glutathione S-transferase pi-1 (GSTP1) , by covalently binding at the catalytic active site.

BRD2889, an analog of the alkaloid piperlongumine, serves as a potent modulator of the GSTP1-ISCU axis in pulmonary hypertension (PH) [1].