1243243-89-1

Basic information

• Product Name: Wnt-C59
• Synonyms: Wnt-C59;2-(4-(2-Methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetaMide;C59;Wnt-C59 (C59);4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide;4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide Wnt-c59;Wnt-C59, >=98%;2-[4-(2-Methyl-4-pyridyl)phenyl]-N-[4-(3-pyridyl)phenyl]acetamide
• CAS NO: 1243243-89-1
• Molecular Formula: C25H21N3O
• Molecular Weight: 379.45374
• EINECS: -0
• Product Categories: Inhibitors
• Mol File: 1243243-89-1.mol
• Article Data: 0

Chemical Properties

• Boiling Point: 628.3±55.0 °C(Predicted)
• Appearance: /
• Density: 1.198±0.06 g/cm3(Predicted)
• Storage Temp.: +2C to +8C
• Solubility: Soluble in DMSO (up to 7 mg/ml) or in Ethanol (up to 6 mg/mL)
• PKA: 13.78±0.70(Predicted)
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
• CAS DataBase Reference: Wnt-C59(CAS DataBase Reference)
• NIST Chemistry Reference: Wnt-C59(1243243-89-1)
• EPA Substance Registry System: Wnt-C59(1243243-89-1)

Safety Data

• Hazardous Substances Data: 1243243-89-1(Hazardous Substances Data)

Usage

Description

Wnt-C59 is a potent inhibitor of Porcupine (PORCN), a Wnt-acyltransferase, with an IC50 of 74 pmol/L. It effectively blocks the secretion of all Wnt isoforms by inhibiting Wnt-acyltransferase. Wnt-C59 has demonstrated the ability to block the progression of mammary tumors in MMTV-WNT1 transgenic mice, inhibit the growth of intestinal neoplasia in RZ-mutant mice, efficiently differentiate pluripotent stem cells into cortical neurons, and attenuate kidney fibrosis by inhibiting collagen mRNA expression and inflammatory cytokines.

Uses

Used in Oncology:
Wnt-C59 is used as an inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase, playing a crucial role in the regulation of various cellular processes, including cell proliferation, migration, and differentiation. Its ability to block the progression of mammary tumors and inhibit the growth of intestinal neoplasia makes it a potential therapeutic agent for cancer treatment.
Used in Stem Cell Differentiation:
Wnt-C59 is used as a differentiation agent for pluripotent stem cells into cortical neurons (CTIP2+/COUP-TF1). This application can be beneficial in the field of regenerative medicine and neural tissue repair.
Used in Fibrosis Treatment:
Wnt-C59 is used as an anti-fibrotic agent, as it has been shown to dramatically attenuate kidney fibrosis by inhibiting collagen mRNA expression and expression of inflammatory cytokines. This makes it a potential therapeutic option for the treatment of fibrotic diseases.

References

1) Proffitt et al. (2013), Pharmacological Inhibition of the Wnt Acyltransferase PORCN Prevents Growth of Wnt-Driven Mammary Cancer; Cancer Res., 73 502 2) Koo et al. (2015), Porcupine inhibitor suppresses paracrine Wnt-driven growth of Rnf43;Znrf3-mutant neoplasia; Proc. Natl. Acad. Sci.USA, 112 7548 3) Motono et al. (2016), Wnt-C59, a Small-Molecule Wnt Inhibitor, Efficiently Induces Anterior Cortex That Includes Cortical Motor Neurons From Human Pluripotent Stem Cells; Stem Cells Transl.Med., 5 552 4) Madan et al. (2016), Experimental inhibition of porcupine-mediated Wnt O-acylation attenuates kidney fibrosis; Kidney Int., 89 1062