Highly 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.
Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer.
Proffitt et al.
Cancer Res., 2013;73:502
WNT10B/β-catenin signalling induces HMGA2 and proliferation in metastatic triple-negative breast cancer.
Wend et al.
EMBO Mol.Med., 2013;5:264
Adult interfollicular tumour-initiating cells are reprogrammed into an embryonic hair follicle progenitor-like fate during basal cell carcinoma initiation.
Youssef et al.
Nat. Cell Biol., 2012;14:1282
Chemically defined generation of human cardiomyocytes.
Burridge et al.