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Chemical Structure : Frizzled6 agonist SAG1.3
CAS No.: 364590-63-6
Catalog No.: PC-38140Not For Human Use, Lab Use Only.
Frizzled6 agonist SAG1.3 is a small molecule SMO agonist that targets Frizzled6 (FZD6) as a partial agonist with limited subtype selectivity.
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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.
| M.Wt | 490.062 | |
| Formula | C28H28ClN3OS | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
3-chloro-N-(4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide |
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1. Paweł Kozielewicz, et al. Nat Commun. 2020 Jan 21;11(1):414.
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