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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Frizzled-Frizzled6 agonist SAG1.3
Frizzled6 agonist SAG1.3

Chemical Structure : Frizzled6 agonist SAG1.3

CAS No.: 364590-63-6

Frizzled6 agonist SAG1.3 (SAG1.3)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 490.062
分子式 C28H28ClN3OS
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-chloro-N-(4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide

参考文献

1. Paweł Kozielewicz, et al. Nat Commun. 2020 Jan 21;11(1):414.

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