| Bioactivity | 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]. |
| Invitro | 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 Vivo | 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]. |
| Name | NSC668036 |
| CAS | 144678-63-7 |
| Formula | C21H36N2O9 |
| Molar Mass | 460.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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. |