Porcupine Inhibitor

IWP-2 is an inhibitor of Wnt processing and secretion with an IC₅₀ of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC₅₀ of 40 nM for the gatekeeper mutant ^M82FCK1δ.

Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC₅₀ of 74 pM.

LGK974 (WNT974) is an orally bioavailable and specific Porcupine (PORCN) inhibitor with an IC₅₀ of 0.1 nM.

ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. ETC-159 inhibits β-catenin reporter activity with an IC₅₀ of 2.9 nM.

Zamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. Zamaporvint targete membrane-bound o-acyltransferase Porcupine and inhibited Wnt ligand palmitoylation, secretion, and pathway activation. Zamaporvint displays a favorable pharmacokinetic profile and shows potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines. Zamaporvint possesses multiple antitumor mechanisms and can be used in cancer research.

IWP L6 (Porcn Inhibitor III) is a Porcupine (Porcn) inhibitor with an EC₅₀ of 0.5 nM. IWP L6 disrupts well-established Wnt-dependent developmental processes of embryonic and juvenile zebrafish.

GNF-6231 is a porcupine (IC₅₀= 0.8 nM), Pron, and endoplasmic reticulum protein inhibitor with oral activity. GNF-6231 has anticancer activity. GNF-6231 can prevent the activation of the Wnt pathway by blocking the secretion of all Wnt ligands. GNF-6231 can be used in the study of myocardial infarction.

IWP-3 is a Wnt production inhibitor with an IC₅₀ of 40 nM. IWP-3 also acts as a CK1δ inhibitor, with an IC₅₀ of 1.89 μM against rat full-length CK1δ. IWP-3 inhibits the function of Porcupine (Porcn), thereby blocking the palmitoylation of Wnt proteins, suppressing the canonical Wnt signaling pathway, reducing the proliferative capacity of cancer cells, promoting the differentiation of mesoderm into cardiomyocytes and increasing cardiomyocyte yield. IWP-3 reduces embryonic cell division, alters the cell movement along the anterior-posterior axis of embryos, and causes embryonic shortening. IWP-3 can be used in studies related to cancers such as pancreatic cancer.

IWP-O1 is a highly potent Porcupine (Porcn) inhibitor, with an EC₅₀ of 80 pM in L-Wnt-STF cells. IWP-O1 prevents the secretion of Wnt proteins. IWP-O1 suppresses the phosphorylation of Dvl2/3 and LRP6 in HeLa cells.

Porcn-IN-1 is potent porcupine inhibitor with an IC₅₀ of 0.5±0.2 nM.

Wnt-C59 (C59) GMP is a GMP grade Wnt-C59 (HY-15659). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC₅₀ of 74 pM.

Wnt-C59 (Standard) is the analytical standard of Wnt-C59. This product is intended for research and analytical applications. Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC50 of 74 pM.

GNF-1331 (compound 19) is a potent, selective and orally bioavailable porcupine inhibitor (IC₅₀=12 nM). GNF-1331 blocks Wnt ligand secretion and subsequent Wnt signaling activity, and induces significant antitumor effects in the mouse MMTV-WNT1 xenograft tumor model.

IWP L6 (GMP) (Porcn Inhibitor III (GMP)) is IWP L6 (HY-15825) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. IWP L6 (Porcn Inhibitor III) is a Porcupine (Porcn) inhibitor with an EC₅₀ of 0.5 nM. IWP L6 disrupts well-established Wnt-dependent developmental processes of embryonic and juvenile zebrafish.

Y-99 is a PORCN inhibitor with an IC₅₀ of 155.4 nM against the Wnt/β-catenin signaling pathway. Y-99 inhibits the expression of p-LRP6, β-catenin, and c-Myc.

GNF-6231 (Standard) is the analytical standard of GNF-6231 (HY-100408). This product is intended for research and analytical applications. GNF-6231 is a porcupine (IC50= 0.8 nM), Pron, and endoplasmic reticulum protein inhibitor with oral activity. GNF-6231 has anticancer activity. GNF-6231 can prevent the activation of the Wnt pathway by blocking the secretion of all Wnt ligands. GNF-6231 can be used in the study of myocardial infarction.

WHN-88 is a Porcupine (PORCN) inhibitor. WHN-88 can eliminate the palmitoylation of Wnt ligands, preventing their secretion and subsequent Wnt/β-catenin signaling. WHN-88 can inhibit cancer cell stemness and suppress the occurrence and development of breast tumors in MMTV-Wnt1 transgenic mice.