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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.

  • Wnt-C59
    T22421243243-89-1
    Wnt-C59 (C59)(C59) is a highly effective and specific Wnt signaling antagonis with PORCN enzymatic activity.
    • $33
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  • Porcn-IN-1
    T44382036044-77-4
    Porcn-IN-1 (Porcupine-IN-1) is an effective porcupine inhibitor (IC50: 0.5±0.2 nM).
    • $51
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  • IWP-O1
    T53422074607-48-8
    IWP-O1 is a highly potent Porcupine (Porcn) inhibitor (EC50: 80 pM), effectively suppresses the phosphorylation of Dvl2/3 and LRP6 in HeLa cells.
    • $37
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  • GNF-6231
    T114441243245-18-2
    GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling.
    • $53
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  • IWP L6
    T26831427782-89-5
    IWP L6 (Porcn Inhibitor III) is an extremely effective Porcn inhibitor (EC50: 0.5 nM).
    • $41
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  • LGK974
    T26181243244-14-5
    LGK974 (NVP-LGK974) is an effective and selective PORCN inhibitor and inhibits Wnt signaling (IC50: 0.4 nM) in TM3 cells. It has been used in trials studying the treatment of Metastatic Colorectal Cancer and Squamous Cell Carcinoma, Head And Neck.
    • $41
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  • IWP-2
    T2702686770-61-6
    IWP-2, an inhibitor of Wnt processing and secretion (IC50=27 nM) in a cell-free assay, selectively blocks Porcn-mediated Wnt palmitoylation.
    • $43
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  • ETC-159
    T40431638250-96-0
    ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
    • $43
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