Cat. No. 5148
Chemical Name: 4-(2-Methyl-4-pyridinyl)-N-[4-(3-py
Biological ActivityHighly potent inhibitor of Porcupine (PORCN), a membrane-bound O-acyltransferase (MBOAT) (IC50 = 74 pM). Shown to inhibit Wnt signaling pathways. Blocks progression of mammary tumors in MMTV-WNT1 transgenic mice and downregulates Wnt/β-catenin target genes. Induces cardiomyocyte differentiation from human iPSCs following culture with CHIR 99021 (Cat. No. 4423). Cell permeable and orally bioavailable.
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All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
Burridge et al (2014) Chemically defined generation of human cardiomyocytes. Nat.Methods 11 855. PMID: 24930130.
Proffitt et al (2013) Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer. Cancer Res. 73 502. PMID: 23188502.
Wend et al (2013) WNT10B/β-catenin signalling induces HMGA2 and proliferation in metastatic triple-negative breast cancer. EMBO Mol.Med. 5 264. PMID: 23307470.
Youssef et al (2012) Adult interfollicular tumour-initiating cells are reprogrammed into an embryonic hair follicle progenitor-like fate during basal cell carcinoma initiation. Nat. Cell Biol. 14 1282. PMID: 23178882.
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Keywords: Wnt-C59, supplier, Highly, potent, porcn, inhibitors, inhibits, membrane-bound, O-acyltransferase, MBOAT, Wnt, signaling, pathways, WntC59, Tocris Bioscience, PORCN Inhibitor products
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