Ethacrynic acid | Glutathione transferase inhibitor

CAS:
 58-54-8
Catalog Number:
 10-2826
Ethacrynic acid chemical structure

Available Options

Size:PriceQuantity 
1 g$60.00
5 g$240.00
Request Quote / Bulk / Custom Size
Product Inquiry

Ethacrynic acid (58-54-8) was found to be an inhibitor of glutathione transferase P1-1 (GST P1-1) in a screen of FDA-approved drugs. It inhibits both GST P1-1 and A3-1, IC50s=4.9 and 0.4 µM respectively and apparently acts as an allosteric inhibitor.1 It forms conjugates with glutathione which also inhibit GST competitively.2 Ethacrynic acid is cytotoxic to a number of cancer cells3 and synergizes with anticancer agents like afatinib4. It is a clinically useful diuretic agent.5

References/Citations:

  1. Musdal et al. (2013), FDA-approved drugs and other compounds tested as inhibitors of human glutathione transferase P1-1; Chem. Biol. Interact. 205 53
  2. Awasthi et al. (1993), Interactions of glutathione S-transferase-pi with ethacrynic acid and its glutathione conjugate; Biochim. Biophys. Acta 1164 173
  3. Lu et al. (2009), Ethacrynic acid exhibits selective toxicity to chronic lymphocytic leukemia cells by inhibition of the Wnt/beta-catenin pathway; PLoS One 4 e8294
  4. Liu et al. (2016), Ethacrynic acid improves the antitumor effects of irreversible epidermal growth factor receptor tyrosine kinase inhibitors in breast cancer; Oncotarget 7 58038
  5. Ricci et al. (2015), Furosemide versus ethacrynic acid in pediatric patients undergoing cardiac surgery: a randomized controlled trial; Crit. Care 19 2
58-54-8, Ethacrynic acid, Ethacrynic acid supplier, Glutathione transferase inhibitor
CAS:
58-54-8
Catalog Number:
10-2826
Activity:
Glutathione transferase inhibitor
Chemical Names:
2,3-Dichloro-4-(2-methylenebutanoyl)phenoxyacetic acid
Alternate Name:
MK-595; NSC-85791
Molecular Weight:
303.14
Molecular Formula:

C13H12Cl2O4

Solubility:
Soluble in DMSO
Physical Properties:
White to off-white solid
Purity:

>99% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Download Product Data Sheet

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

Ethacrynic acid (58-54-8) was found to be an inhibitor of glutathione transferase P1-1 (GST P1-1) in a screen of FDA-approved drugs. It inhibits both GST P1-1 and A3-1, IC50s=4.9 and 0.4 µM respectively and apparently acts as an allosteric inhibitor.1 It forms conjugates with glutathione which also inhibit GST competitively.2 Ethacrynic acid is cytotoxic to a number of cancer cells3 and synergizes with anticancer agents like afatinib4. It is a clinically useful diuretic agent.5

References/Citations:

  1. Musdal et al. (2013), FDA-approved drugs and other compounds tested as inhibitors of human glutathione transferase P1-1; Chem. Biol. Interact. 205 53
  2. Awasthi et al. (1993), Interactions of glutathione S-transferase-pi with ethacrynic acid and its glutathione conjugate; Biochim. Biophys. Acta 1164 173
  3. Lu et al. (2009), Ethacrynic acid exhibits selective toxicity to chronic lymphocytic leukemia cells by inhibition of the Wnt/beta-catenin pathway; PLoS One 4 e8294
  4. Liu et al. (2016), Ethacrynic acid improves the antitumor effects of irreversible epidermal growth factor receptor tyrosine kinase inhibitors in breast cancer; Oncotarget 7 58038
  5. Ricci et al. (2015), Furosemide versus ethacrynic acid in pediatric patients undergoing cardiac surgery: a randomized controlled trial; Crit. Care 19 2

STEM CELL

BOGO