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Description: Highly potent PORCN inhibitor
Chemical Name: 4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide
Purity: ≥99% (HPLC)
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.
Technical Data
| M. Wt | 379.45 |
| Formula | C25H21N3O |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1243243-89-1 |
| PubChem ID | 57519544 |
| InChI Key | KHZOJCQBHJUJFY-UHFFFAOYSA-N |
| Smiles | O=C(CC3=CC=C(C4=CC=NC(C)=C4)C=C3)NC1=CC=C(C2=CC=CN=C2)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 13.18 mL | 65.88 mL | 131.77 mL |
| 1 mM | 2.64 mL | 13.18 mL | 26.35 mL |
| 2 mM | 1.32 mL | 6.59 mL | 13.18 mL |
| 10 mM | 0.26 mL | 1.32 mL | 2.64 mL |
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References
References are publications that support the biological activity of the product.
Proffitt et al (2013) Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer. Cancer Res. 73 502 PMID: 23188502
Wend et al (2013) WNT10B/β-catenin signalling induces HMGA2 and proliferation in metastatic triple-negative breast cancer. EMBO Mol.Med. 5 264 PMID: 23307470
Youssef et 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
Burridge et al (2014) Chemically defined generation of human cardiomyocytes. Nat.Methods 11 855 PMID: 24930130
If you know of a relevant reference for Wnt-C59, please let us know.
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Keywords: Wnt-C59, Wnt-C59 supplier, Highly, potent, porcn, inhibitors, inhibits, membrane-bound, O-acyltransferase, MBOAT, Wnt, signaling, pathways, WntC59, PORCN, Cardiomyocyte, Stem, Cells, ESCs, and, iPSC, 5148, Tocris Bioscience
11 Citations for Wnt-C59
Citations are publications that use Tocris products. Selected citations for Wnt-C59 include:
Pfeiffer et al (2018) Cardiogenic programming of human pluripotent stem cells by dose-controlled activation of EOMES. Nat Commun 9 440 PMID: 29382828
Shafa et al (2018) Human-Induced Pluripotent Stem Cells Manufactured Using a Current Good Manufacturing Practice-Compliant Process Differentiate Into Clinically Relevant Cells From Three Germ Layers. Front Med (Lausanne) 5 69 PMID: 29600249
Hoes et al (2018) Iron deficiency impairs contractility of human cardiomyocytes through decreased mitochondrial function. Eur J Heart Fail 20 910 PMID: 29484788
Montefiori et al (2018) A promoter interaction map for cardiovascular disease genetics. Elife 7 PMID: 29988018
Pavlovic et al (2018) A Comparative Assessment of Human and Chimpanzee iPSC-derived Cardiomyocytes with Primary Heart Tissues. Sci Rep 8 15312 PMID: 30333510
Sharma et al (2018) Stage-specific Effects of Bioactive Lipids on Human iPSC Cardiac Differentiation and Cardiomyocyte Proliferation. Sci Rep 8 6618 PMID: 29700394
Jiang et al (2018) An Ultrasensitive Calcium Reporter System via CRISPR-Cas9-Mediated Genome Editing in Human Pluripotent Stem Cells. iScience 9 27 PMID: 30368079
Bernatik et al (2017) A Novel Role for the BMP Antagonist Noggin in Sensitizing Cells to Non-canonical Wnt-5a/Ror2/Disheveled Pathway Activation. Front Cell Dev Biol 5 47 PMID: 28523267
Marczenke et al (2017) Cardiac Subtype-Specific Modeling of Kv1.5 Ion Channel Deficiency Using Human Pluripotent Stem Cells. Front Physiol 8 469 PMID: 28729840
Nigmatullina et al (2017) Id2 controls specification of Lgr5+ intestinal stem cell progenitors during gut development. EMBO J 36 869 PMID: 28077488
Piccini et al (2017) Adrenergic Stress Protection of Human iPS Cell-Derived Cardiomyocytes by Fast Kv7.1 Recycling. Front Physiol 8 705 PMID: 28959214
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