Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC50 of 74 pM.
IC50&Target
IC50: 74 pM (PORCN)
体外研究
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.
体内研究
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.
分子式
C25H21N3O
分子量
379.45
CAS号
1243243-89-1
运输条件
Room temperature in continental US; may vary elsewhere.