Chemical Name: 4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Highly potent inhibitor of Porcupine (PORCN), a membrane-bound O-acyltransferase (MBOAT) (IC50 = 74 pM). Shown to inhibit Wnt signaling pathways. Blocks progression of mammary tumors in MMTV-WNT1 transgenic mice and downregulates Wnt/β-catenin target genes. Induces cardiomyocyte differentiation from human iPSCs following culture with CHIR 99021 (Cat. No. 4423). Cell permeable and orally bioavailable.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
7.59
20
ethanol
7.59
20
Preparing Stock Solutions
The following data is based on the product molecular weight 379.45. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.64 mL
13.18 mL
26.35 mL
5 mM
0.53 mL
2.64 mL
5.27 mL
10 mM
0.26 mL
1.32 mL
2.64 mL
50 mM
0.05 mL
0.26 mL
0.53 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Proffittet al (2013) Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer. Cancer Res. 73 502 PMID: 23188502
Wendet al (2013) WNT10B/β-catenin signalling induces HMGA2 and proliferation in metastatic triple-negative breast cancer. EMBO Mol.Med. 5 264 PMID: 23307470
Youssefet al (2012) Adult interfollicular tumour-initiating cells are reprogrammed into an embryonic hair follicle progenitor-like fate during basal cell carcinoma initiation. Nat. Cell Biol. 14 1282 PMID: 23178882
Burridgeet al (2014) Chemically defined generation of human cardiomyocytes. Nat.Methods 11 855 PMID: 24930130