For research use only. Not for therapeutic Use.
NSC668036 is a Dishevelled (Dvl) PDZ domain inhibitor with a Kd of 237 µM. NSC668036 blocks Wnt signaling by interrupting the Frizzled-Dvl interaction[1].
In Xenopus, NSC668036 inhibiteds the signaling induced by Wnt3A[1].
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[2].
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[2].
| Catalog Number | I011309 |
| CAS Number | 144678-63-7 |
| Synonyms | 3-methyl-2-[2-[[3-methyl-2-[2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyloxy]butanoyl]amino]propanoyloxy]butanoic acid |
| Molecular Formula | C21H36N2O9 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H36N2O9/c1-10(2)14(30-19(28)13(6)23-20(29)32-21(7,8)9)16(24)22-12(5)18(27)31-15(11(3)4)17(25)26/h10-15H,1-9H3,(H,22,24)(H,23,29)(H,25,26) |
| InChIKey | IPICFSFUAKDZEI-UHFFFAOYSA-N |
| SMILES | CC(C)C(C(=O)NC(C)C(=O)OC(C(C)C)C(=O)O)OC(=O)C(C)NC(=O)OC(C)(C)C |
| Reference | [1]. Jufang Shan, et al. Identification of a specific inhibitor of the dishevelled PDZ domain. Biochemistry. 2005 Nov 29;44(47):15495-503. [2]. Cong Wang, et al. Targeted inhibition of disheveled PDZ domain via NSC668036 depresses fibrotic process. Exp Cell Res. 2015 Feb 1;331(1):115-122. |
