General description

A cell-permeable imidazopyridine compound that acts as downstream Hedgehog (Hh) pathway blocker by directly targeting the enzymatic activity of Adh7 (IC₅₀ = 210 nM), the class IV alcohol dehydrogenase. Inhibits Hg-Ag-induced Gli-transcription activity (IC₅₀ = 30 nM) as well as Gli1 and Ptc1 mRNA expression in a dose-dependent manner in H3H10T1/2 cells. Shown to exhibit ≥100-fold greater cytotoxicity towards five Hh activated tumor cells (GI₅₀ ≤21 nM vs. 1.6 µM for the non-Hh activated H3H10T1/2 cells) in vitro and inhibit the growth of two xenografted tumors in mice (30-50% inhibition, 0.2 mg/mouse/day by p.o.) in vivo. Also acts as a microtubule-depolymerizing agent.

Legal Information

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

Other Notes

Cupido, T., et al. 2009. Angew Chem.48, in press.Lee, J., et al. 2007. ChemBioChem.8, 1916.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution aliquot and freeze (-70°C). Stock solutions are stable for up to 2 weeks at -70°C.

Warning

Toxicity: Standard Handling (A)