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Wnt-C59
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Product Name Wnt-C59
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Catalog No.: CN00463
CAS No.: 1243243-89-1
Molecular Formula: C25H21N3O
Molecular Weight: 379.45 g/mol
Purity: >=98%
Type of Compound: Alkaloids
Physical Desc.: Powder
Source:
Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
SMILES: O=C(Nc1ccc(cc1)c1cccnc1)Cc1ccc(cc1)c1ccnc(c1)C
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Description Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC50 of 74 pM.
Target IC50: 74 pM (PORCN)[1]
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[1].
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[1]. 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[2].
Cell Assay 1×104 HK1, CNE1, HNE1 and SUNE1 cells are seeded in 24-well plates, and Wnt-C59 (5 μM, 10 μM, and 20 μM) is added the next day. Cell confluence is determined by microscopy at 24, 48, 72, and 96 hours after seeding of cells. The IC50 is determined by MTT assay[2].
Animal Admin Mice[1] Female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors are treated with vehicle or Wnt-C59 10 mg/kg once daily for 17 days. Tumor volumes are measured on alternate days[1].
Density1.2±0.1 g/cm3
Boiling Point628.3±55.0 °C at 760 mmHg
Flash Point333.8±31.5 °C
Exact Mass379.168457
PSA54.88000
LogP4.19
Vapour Pressure0.0±1.8 mmHg at 25°C
Storage condition-20°C