Wnt-C59

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Cat.No. 5148 - Wnt-C59 | C25H21N3O | CAS No. 1243243-89-1
Description: Highly potent PORCN inhibitor
Chemical Name: 4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide
Purity: ≥99% (HPLC)
Datasheet
Citations (4)
Reviews
Literature

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.

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
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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Product Datasheets

Certificate of Analysis / Product Datasheet
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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


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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

4 Citations for Wnt-C59

Citations are publications that use Tocris products. Selected citations for Wnt-C59 include:

Piccini et al (2017) Adrenergic Stress Protection of Human iPS Cell-Derived Cardiomyocytes by Fast Kv7.1 Recycling. Front Physiol 8 705 PMID: 28959214

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


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