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
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
| Quality Level | 100 |
| assay | ≥95% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,desiccated |
| color | off-white |
| solubility | DMSO: 100 mg/mL,ethanol: 20 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | O=C1CCCC(=O)C1CC2C(=O)CCCC2=O |
| InChI | 1S/C13H16O4/c14-10-3-1-4-11(15)8(10)7-9-12(16)5-2-6-13(9)17/h8-9H,1-7H2 |
| InChI key | ILUMEPMGPCKGHH-UHFFFAOYSA-N |
