Biochem/physiol Actions

Primary Targetgamma-glutamylcysteine synthetase

General description

A cell-permeable, sulfoximine based compound that acts a potent, fast acting, irreversible inhibitor of g-glutamylcysteine synthetase and depletes cellular glutathione levels. Closely resembles the structure of g-glutamylphosphate cysteine adduct. The inhibition follows the first order kinetics with t_1/2 = ~ 11 sec at saturating inhibitor concentration. Does not affect the activity of glutamine synthetase. Shown to improve the outcome of chemotherapy by lowering the levels of glutathione in cancer cells (IC₅₀ = 1.9, 8.6, and 29 µM in melanoma, breast, and ovarian tumor cells, respectively).

A cell-permeable, sulfoximine based compound that acts a potent, fast acting, irreversible inhibitor of g-glutamylcysteine synthetase and depletes cellular glutathione levels. Closely resembles the structure of g-glutamylphosphate cysteine adduct. The inhibition follows the first order kinetics with t1/2 = ~ 11 sec at saturating inhibitor concentration. Does not affect the activity of glutamine synthetase. Shown to improve the outcome of chemotherapy by lowering the levels of glutathione in cancer cells (IC₅₀ = 1.9, 8.6, and 29 µM in melanoma, breast, and ovarian tumor cells, respectively).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Fruehauf, J.P., et al. 1997. Pigment Cell Res.10, 236.O'Dwyer, P.J., et al. 1996. J. Clin. Oncol.14, 249.Griffith, O. W., 1982. J. Biol. Chem.257, 13704.r>Griffith, O. W., et al. 1979. J. Biol. Chem.254, 7558.

Packaging

100 mg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)