A loop diuretic with anticancer activity; inhibits the NKCC cotransporter in duck erythrocytes (IC50 = 0.18 mM); inhibits ATP-dependent chloride uptake in rat renal plasma membrane vesicles at 0.3 mM; inhibits GSTP1-1 and GSTA3-3 (IC50s = 4.9 and ~0.4 μM

Ethacrynic Acid – 1 g

Brand:
Cayman
CAS:
58-54-8
Storage:
-20
UN-No:
Non-Hazardous - /

Ethacrynic acid is a loop diuretic with anticancer activity.{53194},{33064,33063} It inhibits the Na-K-2Cl (NKCC) cotransporter in duck erythrocytes (IC50 = 0.18 mM) and ATP-dependent chloride uptake in rat renal plasma membrane vesicles when used at a concentration of 0.3 mM.{53194},{33062} Ethacrynic acid also inhibits glutathione S-transferase P1-1 (GSTP1-1) and GSTA3-3 (IC50s = 4.9 and ~0.4 μM, respectively), and inhibits Wnt/β-catenin signaling in a cell-based reporter assay.{41510,33064} It is cytotoxic to primary chronic lymphocytic leukemia cells (IC50 = 8.56 μM), as well as MCF-7, MDA-MB-231, and 4T1 cancer cells (IC50s = 45.53, 39.64, and 25.23 μM, respectively).{33064,33063} Ethacrynic acid (250 μg per day) increases tumor growth reduction induced by the EGFR family inhibitors afatinib (Item Nos. 11492 | 21567) or neratinib (Item No. 18404) in a 4T1 murine breast cancer model.{33063} Formulations containing ethacrynic acid have been used in the treatment of edema.  

 

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Description

A loop diuretic with anticancer activity; inhibits the NKCC cotransporter in duck erythrocytes (IC50 = 0.18 mM); inhibits ATP-dependent chloride uptake in rat renal plasma membrane vesicles at 0.3 mM; inhibits GSTP1-1 and GSTA3-3 (IC50s = 4.9 and ~0.4 μM, respectively); inhibits Wnt/β-catenin signaling in a cell-based reporter assay; cytotoxic to primary chronic lymphocytic leukemia cells (IC50 = 8.56 μM), as well as MCF-7, MDA-MB-231, and 4T1 cancer cells (IC50s = 45.53, 39.64, and 25.23 μM, respectively); increases tumor growth reduction induced by afatinib or neratinib in a 4T1 murine breast cancer model at 250 μg per day

Formal name: 2-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxy]-acetic acid

Synonyms:  MK-595|NSC 624008|NSC 85791

Molecular weight: 303.1

CAS: 58-54-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cancer|Cell Death||Research Area|Cardiovascular System|Blood|Erythrocytes & Hemoglobin||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Cell Biology|Cell Signaling|Wnt Signaling||Research Area|Immunology & Inflammation

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