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 29uM in melanoma, breast, and ovarian tumor cells, respectively).
Molecular Formula:C₈H₁₈N₂O₃S
Solubility:H2O
Primary Target:gamma-glutamylcysteine synthetase
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
