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Wnt-C59

Development stage: Preclinical
Modality: Small Molecules
Administration: Oral (preclinical Studies)

Overview

Wnt-C59 (C59) is a highly potent and selective small molecule inhibitor of Porcupine (PORCN), a membrane-bound O-acyltransferase essential for the palmitoylation and secretion of Wnt proteins. By inhibiting PORCN, C59 blocks the activation of the canonical and non-canonical Wnt signaling pathways. This mechanism disrupts downstream β-catenin-mediated transcriptional activity, which is implicated in embryonic development, tissue regeneration, fibrosis, and various cancers. C59 has demonstrated nanomolar to picomolar potency in cellular assays (IC50 ~74 pM). It is primarily used as a research tool to study Wnt pathway biology and has not been approved for clinical use[3][4][5][6][7].

Other names: 2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide

Targets

PORCN (Porcupine protein)

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