Wnt-C59 (C59) effectively suppresses PORCN activity at nanomolar levels in vitro, evidenced by its ability to inhibit Wnt palmitoylation, the interaction of Wnt with its transporter Wntless/WLS, the secretion of Wnt, and the activation of β-catenin reporter activity by Wnt. It prevents WNT3A-induced activation of a TCF-binding site multimer driving luciferase production with an IC50 of 74 pM[1].
体内研究
In mice, Wnt-C59 shows favorable bioavailability and halts the development of mammary tumors in MMTV-WNT1 transgenic mice by reducing the expression of Wnt/β-catenin target genes[1].
Wnt-C59 holds promise for eliminating cancer stem cells within human tumors, demonstrating a capacity to diminish the stemness of NPC cells in a dose-dependent manner through the inhibition of sphere formation in both HNE1 and SUNE1 cell lines[2].
体外研究
Wnt-C59 (C59) effectively suppresses PORCN activity at nanomolar levels in vitro, evidenced by its ability to inhibit Wnt palmitoylation, the interaction of Wnt with its transporter Wntless/WLS, the secretion of Wnt, and the activation of β-catenin reporter activity by Wnt. It prevents WNT3A-induced activation of a TCF-binding site multimer driving luciferase production with an IC50 of 74 pM[1].
作用机制
Serine acylation in Wnt protein is essential in Wnt secretion. PORCN is a key enzyme that resides in the endoplasmic reticulum, adding palmitate to a serine in Wnt protein. Wnt-C59 acts as a nanomolar inhibitor of the acyltransferase activity of PORCN.
Wnt-C59 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
human HT1080 cells
Function assay
Inhibition of porcupine activity (unknown origin) expressed in human HT1080 cells assessed as suppression of Wnt3A-mediated super top flash activity by STF luciferase assay, IC50=7.4e-05 μM.
Inhibition of porcupine activity (unknown origin) expressed in human HT1080 cells assessed as suppression of Wnt3A-mediated super top flash activity by STF luciferase assay, IC50=7.4e-05 μM.
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