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Wnt-C59

CAS No. : 1243243-89-1

MCE 国际站：Wnt-C59

产品活性：Wnt-C59 (C59)是高效可口服的 PORCN 抑制剂，IC₅₀ 为 74 pM。

研究领域：Stem Cell/Wnt

作用靶点：Porcupine  |  Wnt

In Vitro: Wnt-C59 (C59) inhibits PORCN activity in vitro at nanomolar concentrations, as assessed by inhibition of Wnt palmitoylation, Wnt interaction with the carrier protein Wntless/WLS, Wnt secretion, and Wnt activation of β-catenin reporter activity. Wnt-C59 inhibits WNT3A-mediated activation of a multimerized TCF-binding site driving luciferase with an IC₅₀ of 74 pM.

In Vivo: Wnt-C59 displays good bioavailability in mice. Wnt-C59 blocks progression of mammary tumors in MMTV-WNT1 transgenic mice while downregulating Wnt/β-catenin target genes. Wnt-C59 has the potential to eradicate cancer stem cells in human tumors. Wnt-C59 inhibits stemness properties of NPC cells in a dosage-dependent manner by arresting sphere formation in both HNE1 and SUNE1 cells.

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