gutathione s-transferase

Ethacrynic acid (Edecrin) is a nonsulfonamide loop diuretic that inhibits the activity of the Na+/K+/2Cl- cotransporter NKCC2 in the thick ascending limb of the loop of Henle. It also inhibits glutathione S-transferase and Wnt signalling, producing cytotoxicity in chronic lymphocytic leukaemia cells and other tumour cells.

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

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.

Coniferyl ferulate is a strong inhibitor of glutathione S-transferase (GST) isolated from Radix Angelicae sinensis. It shows strong inhibition of human placental GST (IC50: 0.3 μM). It also reverses multidrug resistance and downregulates P-glycoprotein.

Curzerene, a sesquiterpene compound derived from the rhizome of Curculigo orchioides Gaertn, possesses potent anti-cancer properties. It is known to induce apoptosis in cells[1] and also suppress the expression of glutathione S-transferase A1 (GSTA1) mRNA and protein.

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

α-Angelica lactone has cardiotonic activity, may exert their effects by providing an increased contraction-dependent calcium pool to be released upon systolic depolarization.

Seneciphylline, one of the hepatotoxic pyrolizidine alkaloids, has mutagenic activity in Drosophila and their transfer into rat milk.Seneciphylline can significantly increased the activities of epoxide hydrase and glutathione-S-transferase but cause reduc

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].