General description
A highly potent inducer of phenobarbital-like class of cytochrome P450 (CYP) enzymes. A tumor promoter that induces hepatocyte proliferation, independent of the presence of cytokines or transcription factors. Activates orphan nuclear receptors mCAR (mouse constitutive androstane receptor) and hPXR (human pregane X receptor), but has little or no effect on hCAR and mPXR. Also suppresses the expression of multi-drug resistance genes mdr2 and mdr3 in mouse liver.
The most potent known member of the phenobarbital-like class of cytochrome P450 (CYP)-inducing agents. Acts as a tumor promoter of murine hepatocarcinogenesis; activates orphan nuclear receptors mCAR (mouse Constitutive Androstane Receptor) and hPXR (human Pregnane X Receptor), but has little or no activity on hCAR and mPXR. Also suppresses the multidrug resistance gene expression in the mouse liver.
Biochem/physiol Actions
Cell permeable: no
Primary Target
Cytochrome P450 (CYP)-inducing agents
Product does not compete with ATP.
Reversible: no
Packaging
Packaged under inert gas
Warning
Toxicity: Carcinogenic / Teratogenic (D)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Ledda-Columbano, G.M., et al. 2000. Am. J. Pathol.156, 91.
Moore, L.B., et al. 2000. J. Biol. Chem.275, 15122.
Tzameli, I., et al. 2000. Mol. Cell. Biol.20, 2951.
Forman, B.M., et al. 1998. Nature395, 612.
Honkakoski, P., et al. 1998. Mol. Pharmacol.53, 597.
Russell, A.L., et al. 1994. Int. J. Cancer58, 550.
Smith, G., et al. 1993. Biochem. J.289, 807.
Dargani, T.A., et al. 1990. Carcinogenesis11, 1153.
Poland, A., et al. 1980. Mol. Pharmacol.18, 571.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 41181513
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 580563-25MG