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You are here:Home-Inhibitors & Agonists-Wnt/Notch/Hedgehog-Porcupine

Request The Product List ofPorcupine Porcupine

Porcupine (Porc) protein may be involved in secretion or ER transport, as Wingless is retained in the ER in porcupine mutant Drosophila embryos. In C. elegans, the porcupine homolog mom-1 has a similar function in promoting secretion of the Wnt protein Mom-2. Porcupine has some homology to a family of o-acyl transferases and may be involved in lipid modification of Wnt proteins. A special form of monounsaturated palmitoylation has been detected on a serine residue in the Wnt protein and could be mediated by porc as well. The human Porcupine gene is implicated in a genetic disease, Focal dermal hypoplasia. Porcupine, encodes a multipass transmembrane ER protein, which is required for normal distribution of Wg in embryos. Porc stimulates the processing of Wg when expressed in Drosophila cells in vitro and is also necessary for the localization of Drosophila Wnt-3 on the axon tracts of the embryonic central nervous system.

Cat. No. Product Name CAS No. Information
H8283

WNT-974

 		1243244-14-5

A potent and specific small-molecule Porcupine (PORCN) inhibitor with IC50 of 1 nM in the PORCN radioligand binding assay; potently inhibits Wnt signaling with IC50 of 0.4 nM, with no major cytotoxicity; reduces Wnt-dependent LRP6 phosphorylation and the expression of Wnt target genes, such as AXIN2; is potent and efficacious in multiple tumor models at well-tolerated doses in vivo.
H8282

IWP-O1

 		2074607-48-8

IWP-O1 is a highly potent Porcupine (Porcn) inhibitor with EC50 of 80 pM in L-Wnt-STF cells, effectively suppresses the phosphorylation of Dvl2/3 and LRP6 in HeLa cells; suppresses Wnt signaling in L-Wnt-STF cells with an EC50 value of 80 pM, 2.5 times more active than LGK974; exhibits significantly improved metabolic stability, and suitable for model studies in mice.
H8281

GNF-6231

 		1243245-18-2

A potent, selective and orally bioavailable Porcupine (PORCN) inhibitor with IC50 of 0.8 nM; has no appreciable activities for more than 200 off-targets, and IC50 of >10 uM against all CYP isoforms; reduces Axin2 mRNA levels and inhibits Wnt secretion and pathway activation, induces robust antitumor efficacy in a mouse MMTV-WNT1 xenograft tumor model.

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