Frizzled6 agonist SAG1.3

Published date: 2022-06-22 21:57:40

Frizzled6 agonist SAG1.3 Structure
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Name Smoothened Agonist, HCl CAS# 364590-63-6
Price $Inquiry/100mg $Inquiry/250mg $Inquiry/1g Purity 98.0%
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Frizzled6 agonist SAG1.3 is a small molecule SMO agonist that targets Frizzled6 (FZD6) as a partial agonist with limited subtype selectivity;
Frizzled6 agonist SAG1.3 binds FZD6 and evokes a conformational change reminiscent of that seen in other agonist-bound GPCRs.
In competition experiments, increasing concentrations of unlabeled SAG1.3 decreased BODIPY-cyclopamine (300 nM) binding to Nluc-FZD6 in a concentration-dependent manner (pKi=5.6).
SAG1.3 mediates recruitment of mGsi proteins to FZD6 and induces conformational changes in FZD6, induces FZD6-dependent dissociation of heterotrimeric Gi and phosphorylation of ERK1/2, and modifies the interactions between FZD6 and DVL2.

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