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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).
Catalogue Number
508228
Brand Family
Calbiochem®
References
References
Fruehauf, J.P., et al. 1997. Pigment Cell Res.10, 236. OʹDwyer, P.J., et al. 1996. J. Clin. Oncol.14, 249. Griffith, O. W., 1982. J. Biol. Chem.257, 13704. Griffith, O. W., et al. 1979. J. Biol. Chem.254, 7558.
Fruehauf, J.P., et al. 1997. Pigment Cell Res.10, 236. OʹDwyer, P.J., et al. 1996. J. Clin. Oncol.14, 249. Griffith, O. W., 1982. J. Biol. Chem.257, 13704. Griffith, O. W., et al. 1979. J. Biol. Chem.254, 7558.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
31-October-2013 JSW
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 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).
Form
White powder
Intert gas (Yes/No)
Packaged under inert gas
CAS number
83730-53-4
Chemical formula
C₈H₁₈N₂O₃S
Structure formula
Purity
≥97% by TLC
Solubility
H₂O (50 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Fruehauf, J.P., et al. 1997. Pigment Cell Res.10, 236. OʹDwyer, P.J., et al. 1996. J. Clin. Oncol.14, 249. Griffith, O. W., 1982. J. Biol. Chem.257, 13704. Griffith, O. W., et al. 1979. J. Biol. Chem.254, 7558.
