NSC 668036

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NSC 668036 是 Disheveled (Dvl) PDZ 结构域的特异性抑制剂，与 GRIP 的 PSD-95、PSD95 和 PDZ7 结构域的结合极弱。

NSC 668036 is a specific inhibitor of the Dishevelled (Dvl) PDZ domain, extremely weakly binds to PSD-95, PSD95, and PDZ7 domain of GRIP; inhibits the signaling induced by Wnt3A and blocks Wnt signaling by interrupting the Fz-Dvl interaction; suppresses β-catenin-driven gene transcription and abolishes TGF-β1-induced migration, expression of collagen I and α-α-SMA in fibroblasts; depresses fibrotic process in vivo.

In Xenopus, NSC668036 inhibiteds the signaling induced by Wnt3A. NSC668036 (10 μM) suppresses β-catenin-driven gene transcription and abolished TGF-β1-induced migration, expression of collagen I and α-smooth muscle actin (α-SMA) in fibroblasts.

In Bleomycin-induced pulmonary fibrosis murine model, NSC668036 (5 mg/kg) significantly suppresses accumulation of collagen I, α-SMA, and TGF-β1 but increased the expression of CK19, Occludin and E-cadherin that can inhibit pulmonary fibrogenesis.

NSC668036

Wnt/Notch/Hedgehog

Dishevelled

Dishevelled

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144678-63-7

460.52

C21H36N2O9

>98% (HPLC)

——

C[C@@H](C(O[C@H](C(O)=O)C(C)C)=O)N(C([C@H](C)NC(OC(C)(C)C)=O)=O)C(C(O)C(C)C)=O

N-[(1,1-dimethylethoxy)carbonyl]-L-alanyl-(2S)-2-hydroxy-3-methylbutanoyl-L-alanine-(1S)-1-carboxy-2-methylpropyl ester

(-20℃)

With Ice Pack

≥ 2 years