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NSC 668036

Names

[ CAS No. ]:
144678-63-7

[ Name ]:
NSC 668036

[Synonym ]:
nsc 668036 hydrate
NSC 668036

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> Wnt
Research Areas >> Inflammation/Immunology

[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H36N2O9

[ Molecular Weight ]:
460.51900

[ Exact Mass ]:
460.24200

[ PSA ]:
157.33000

[ LogP ]:
2.40630

Related Compounds