Non disponible en dehors du Royaume-Uni et de l'Irlande
Biochem/physiol Actions
Reversible: no
Target IC50: 30 nM in blocking TCDD-induced AhR transcription activity in HepG2 cells in vitro
Product does not compete with ATP.
Primary TargetAhR (aryl hydrocarbon receptor)
Cell permeable: yes
General description
A cell-permeable pyrazolo-amide compound that potently blocks the binding of TCDD (2,3,7,8-tetrachlorodibenzo-p-dioxin) to AhR (aryl hydrocarbon receptor) in a dose-dependent manner. Shown to Inhibit TCDD-induced AhR transcription activity in HepG2 cells in vitro (IC50 = 30 nM) and prevent TCDD-elicited liver toxicity and wasting syndrome in mice in vivo. Unlike the commonly used AhR antagonist flavone, this inhibitor has no effect on estrogen receptor transcription activity, nor does it exhibit TCDD-like agonist activity even at concentrations as high as 10 µM.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Kim, S.H., et al. 2006. Mol. Pharmacol.69, 1871.
Packaging
Packaged under inert gas
10 mg in Plastic ampoule
Warning
Toxicity: Irritant (B)
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