MRT-83 is a potent Smoothened antagonist that blocks Hedgehog (Hh) signaling in various assays with IC50 of 10 nM.
MRT-83 inhibits Bodipy-cyclopamine binding to human and mouse Smo but does not modify Wnt signaling, blocks BC binding to HEK-hSmo cells with IC50 of 4.6 nM.
MRT-83 abrogates the agonist-induced trafficking of endogenous mouse or human Smo, efficiently antagonizes Hh signaling in vivo.
