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)