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.
Cat.No
DC70418
Name
Frizzled6 agonist SAG1.3
Chemical Properties
CAS
364590-63-6
Formula
C28H28CLN3OS
MW
490.062
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
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