Apoptosis Inhibitor

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.

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

Packaged under inert gas

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Tsuda, T., et al. 2001. Eur. J. Pharmacol.433, 37.

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

Toxicity: Standard Handling (A)