IWP-2

Short Summary : Wnt production inhibitor,PORCN inhibitor

Category : Stem Cell|Wnt/β-catenin

Purity : 0.98

CAS Number : 686770-61-6

Formula : C22H18N4O2S3

Molecular Weight : 466.6

SMILE : CC1=CC2=C(C=C1)N=C(S2)NC(=O)CSC3=NC4=C(C(=O)N3C5=CC=CC=C5)SCC4

Solubility : >23.35mg/mL in DMF with gentle warming

Storage : Store at -20°C

Description : IC50: 27 nM for Wnt pathway activityThe Wnt signaling pathway is important in embryonic development as well as the initiation and progression of a number of types of human cancer. Porcn, a member of the membrane-bound O-acyltransferase (MBOAT) family, adds a palmitoyl group to Wnt proteins that is essential to their signaling ability and is required for Wnt secretion. IWP-2 is a small-molecule antagonist of the Wnt/b-catenin pathway.In vitro: Expression of Porcn but not Evi alleviated the effects of IWP-2 on pathway activity and Wnt secretion, which suggests that in general IWP-2 may act on Porcn [1]. In vivo: In order to test the in vivo activity of IWP-2, the authors turned to a simple and rapid assay of Wnt/b-catenin pathway activity: regeneration of the zebrafish caudal fin following resection. The addition of IWP-2 to the aquarium water of zebrafish failed to suppress fin regeneration after mechanical resection, which suggests either that IWP-2 have poor bioavailability or that the determinants in the gene product that they target are not conserved in zebrafish [1]. Clinical trial: Up to now, IWP-2 is still in the preclinical development stage.Reference:[1] Chen B, Dodge ME, Tang W, Lu J, Ma Z, Fan CW, Wei S, Hao W, Kilgore J, Williams NS, Roth MG, Amatruda JF, Chen C, Lum L. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7.

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