Description:

GDC-0449 (Vismodegib) is potent antagonist of SMO (smoothened). This
small molecule compound is a hedgehog pathway inhibitor by directly
binding to SMO. This molecule has been developed by Genentech for
clinical application against hedgehog-dependent cancers.

Ref: Robarge KD, et al. Bioorg Med Chem Lett. Oct 1 2009 19: 5576-81; van
Hoff DD, et al. N Engl J Med. Sep 17, 2009 361: 1164-72; Rudin CM et al. N Engl
J Med. 2009 Sep 17; 361(12):1173-8.

Biological Activity:

In a cell-based assay measuring the activation of the Gli-1 reporter gene,
this compound gives IC50 of 5-20 nM.