Taladegib is a Smoothened ( SMO ) antagonist. Taladegib hydrochloride inhibits the Hedgehog signaling pathway, with an IC 50 of 5.5 nM for suppressing GLI1 mRNA expression in DAOY cells and an IC 50 of 7.6 nM in CGNP cell proliferation assays. Taladegib binds to the extracellular loop region (site 1) of the transmembrane domain of the SMO receptor, competes with cyclopamine for SMO binding, and thereby inhibits Gli -dependent transcription. Taladegib can be used in studies of Hedgehog pathway-related cancers.
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