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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.

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 is a Wnt pathway inhibitor (IC50=27 nM) and an ATP-competitive CK1δ inhibitor (IC50=40 nM for M82FCK1δ). IWP-2 inhibits self-renewal of embryonic stem cells and has been used in stem cell and organoid research.
  • $43
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Wnt-C59
T22421243243-89-1
Wnt-C59 (C59) is a highly effective and specific Wnt signaling antagonis with PORCN enzymatic activity.
  • $33
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ETC-159
T40431638250-96-0
ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor that inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
  • $43
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IWP-O1
T53422074607-48-8
IWP-O1, a highly potent Porcupine (Porcn) inhibitor (EC50: 80 pM), effectively suppresses the phosphorylation of Dvl2 3 and LRP6 in HeLa cells.
  • $33
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GNF-6231
T114441243245-18-2
GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling.
  • $30
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IWP L6
T26831427782-89-5
IWP L6 (Porcn Inhibitor III) is a highly potent Porcn inhibitor with an EC50 of 0.5 nM.
  • $41
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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).
  • $48
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WHN-88
T898812490686-86-5
WHN-88, a Porcupine (PORCN) inhibitor, disrupts the palmitoylation of Wnt ligands, which inhibits their secretion and subsequent Wnt β-catenin signaling. This compound has shown efficacy in reducing cancer cell stemness and suppressing the progression and development of breast tumors in MMTV-Wnt1 transgenic mice.
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10-14 weeks
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