Apoptosis Inhibitor

Biochem/physiol Actions

Target IC₅₀: 67 µg/ml in FasL-stimulated WC8 cells, 130 µg/ml in etoposide-stimulated U937 cells

Reversible: no

Product does not compete with ATP.

Primary Targetapoptosis induction

Cell permeable: yes

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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

10 mg in Plastic ampoule

Reconstitution

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

Warning

Toxicity: Standard Handling (A)