Biochem/physiol Actions

Reversible: yes

Primary TargetSmo

Cell permeable: yes

General description

A cell-permeable 2,5-dichlorobenzamido compound that acts as a potent and competitive inhibitor of Smo activity. Occupies the SAG binding pocket in the hepta-helical domain to block Smoothened (Smo) agonist (SAG) access (IC₅₀ = 19 nM) and blocks SAG-induced Hedgehog pathway (IC₅₀ = 3.1 nM). Basal wild-type Smo activity is also shown to be equally sensitive to its action (IC₅₀ = 14 nM). Blocks Gli2 accumulation at the ciliary tip in response to SAG treatment and reduces Smo-mediated Gli processing and Sufu/Gli interaction in NIH3T3 cells. Also shown to promote a loss of Smo-dependent Gli activity in cells with W535L and L412F oncogenic Smo mutations.

Legal Information

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

Other Notes

Fan, C. W., et al. 2014. Chem. Biol.21, 1680.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Warning

Toxicity: Standard Handling (A)