Description
SAG (912545-86-9) is a smoothened agonist which binds directly to SMO and can block SMO inhibition by cyclopamine (Cat.# 10-1082). The conformation of SMO is altered by SAG binding which results in the accumulation of SMO in cilia and activated gene transcription. It should be noted that SAG inhibits hedgehog signaling at concentrations greater than 1 μM (EC50?for SMO activation is ~ 3 nM).1
Chemical Properties
Orange to Red Oil
Uses
Smoothened agonist (SAG) dihydrochloride has been used as a sonic hedgehog (SHH) pathway agonist:
- to study its effects on mouse hippocampal cells
- to determine its effects on the mitochondrial network in zebrafish embryo
- to study its effects on murine embryonic fibroblasts
Uses
A potent agonist of Hedgehog (Hh) signalling by activating the Smoothened (Smo) protein function. Studies identify novel properties of molecules displaying potential interest in the treatment of various cancers and brain diseases, and demonstrate that Smo is capable of signaling through G15.
Definition
ChEBI: 3-chloro-N-[trans-4-(methylamino)cyclohexyl]-N-[3-(pyridin-4-yl)benzyl]-1-benzothiophene-2-carboxamide is a member of the class of 1-benzothiophenes that is 3-chloro-1-benzothiophene-2-carboxamide in which the amide nitrogen is substituted by trans-4-(methylamino)cyclohexyl and 3-(pyridin-4-yl)benzyl groups. A smoothened (Smo) receptor agonist that antagonizes cyclopamine action at the Smo receptor. Activates the Hedgehog signaling pathway in a Patched independent manner. It has a role as a SMO receptor agonist. It is a member of 1-benzothiophenes, an organochlorine compound, a biaryl, a phenylpyridine, a tertiary carboxamide and a secondary amino compound.
Biochem/physiol Actions
SAG is a potent and cell-permeable smoothened (Smo) agonist that activates Hedgehog pathway and counteracts Cyclopamine inhibition of Smo.
References
References/Citations
1) Chen?et al. (2002), Small molecule modulation of Smoothened activity; Proc. Natl. Acad. Sci. USA,?99?1407
