glutathione transferases

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.

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.

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

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

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.

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

Ethacrynic acid, a diuretic, functions as an inhibitor of L-type voltage-dependent and store-operated calcium channels, facilitating the relaxation of airway smooth muscle (ASM) cells. It exhibits anti-inflammatory effects, notably reducing retinoid-induced ear edema in mice, and inhibits glutathione S-transferases (GSTs), making it a potent suppressor of the NF-kB signaling pathway. Additionally, ethacrynic acid modulates leukotriene formation. A variant, Ethacrynic acid D5, is distinguished by its deuterium labeling.

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.

DL-Goitrin is a potent antithyroid compound found naturally in crucifers. DL-Goitrin is responsible for the induction of glutathione S-transferases. DL-Goitrin is a moderate inhibitor of purified bovine adrenal dopamine beta-hydroxylase, leads to a depression of brain norepinephrine and to an elevation of heart and adrenal dopamine.

Trans-Methylisoeugenol is a compound with insecticidal activity isolated from Acorus calamus L. It is a natural food flavor. It is a natural food flavor with anxiolytic and antidepressant properties and moderately reversible inhibition of glutathione S-transferases (GSTs) (0.2 to 5.4 mmol for human GSTs and 0.4 to 4.9 mmol for rat GSTs).

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