General description
A cell-permeable inhibitor of apoptosis induction (IC50 = 67 µg/ml in FasL-stimulated WC8 cells, 130 µg/ml in etoposide-stimulated U937 cells). Effects attributable to the inhibition of caspase-3 activation but does not directly inhibit caspase-3 even at 1 mg/ml.
A cell-permeable, bis(cyclohexane-1,3-diketone) that is shown to inhibit apoptosis induction in FasL-stimulated WC8 cells (IC50 = 67 µg/ml) and etoposide-stimulated U937 cells (IC50 = 130 µg/ml). The anti-apoptotic effects have been shown to be attributable to inhibition of caspase-3 activation (IC50 = 334 nM), however it does not exhibit any direct inhibition of caspase-3 enzymatic activity. Shown to inhibit the elevation of the liver enzymes, alanine aminotransferase and aspartate aminotransferase, in a murine model of anti-Fas-induced hepatitis. Topical application has been shown to reduce chemotherapy-induced alopecia (hair loss) in newborn rats.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
apoptosis induction
Product does not compete with ATP.
Reversible: no
Target IC50: 67 µg/ml in FasL-stimulated WC8 cells, 130 µg/ml in etoposide-stimulated U937 cells
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Tsuda, T., et al. 2001. Eur. J. Pharmacol.433, 37.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51286505
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 178488-10MG