ethacrynic acid

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.

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.

EA-B2L is an effective degrader of glutathione S-transferase (GSTP) with a DC50 of 48 μM. It is composed of Ethacrynic acid linked to Boc2Lys. EA-B2L plays a significant role in cancer research.

Ethacrynate Sodium, the sodium salt form of ethacrynic acid, could inhibit symport of chloride, potassium, and sodium primarily in the ascending limb of Henle, but also in the proximal and distal tubules.

CK1-IN-4 (Compound 59) is an inhibitor of casein kinase CK1δ with an IC50 of 2.74 μM. It exhibits neuroprotective activity in SH-SY5Y cells treated with Ethacrynic acid.