Home / PORCN Inhibitors / Wnt-C59

Wnt-C59

Catalog #: 5148
49 Citations 1 Review Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
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5148/50
Wnt-C59 | CAS No. 1243243-89-1 | PORCN Inhibitors
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Description: Highly potent PORCN inhibitor

Chemical Name: 4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide

Purity: ≥99%

Product Details
Citations (49)
Reviews (1)
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

Wnt-C59 is a highly potent inhibitor of the MBOAT (membrane-bound O-acyltranferase) family member, Porcupine (PORCN) (IC50 = 74 pM), that mediates WNT palmitoylation and secretion. Wnt-C59 potently inhibits the processing of both canonical (1, 2, 3a, 6, 7b, 8a, 9a, 9b, 10) and non-canonical (4, 5a, 11, 16) Wnt subtypes. Wnt-C59 blocks progression of mammary tumors in MMTV-WNT1 transgenic mice and downregulates Wnt/β-catenin target genes. Wnt-C59-treated tumors show a decrease in β-catenin, CyclinD1 and c-Myc. Wnt-C59 induces cardiomyocyte differentiation from human iPSCs following culture with CHIR 99021 (Cat. No. 4423). Wnt-C59 efficiently induces neural differentiation of CTIP2+/COUP-TF1- cells from PSCs in culture. When grafted into the cortex of adult mice, Wnt-C59-treated cells develop abundant axonal fiber extensions toward the spinal cord. The compound has also been used in protocols to generate β cells from human PSCs. Cell permeable and orally bioavailable.

Technical Data

M.Wt:
379.45
Formula:
C25H21N3O
Solubility:
Soluble to 20 mM in DMSO and to 20 mM in ethanol
Purity:
≥99%
Storage:
Store at -20°C
CAS No:
1243243-89-1

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.

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Citations for Wnt-C59

The citations listed below are publications that use Tocris products. Selected citations for Wnt-C59 include:

49 Citations: Showing 1 - 10

  1. Engineered cardiac tissue model of restrictive cardiomyopathy for drug discovery.
    Authors: Yulia V Et al.
    Cell Rep Med  2023;4:100976
  2. Optimized synthesis and pharmacological evaluation of HCN channel inhibitor EC18.
    Authors: Guiscard Et al.
    Arch Pharm (Weinheim)  2023;356:e2200665
  3. A pesticide and iPSC dopaminergic neuron screen identifies and classifies Parkinson-relevant pesticides.
    Authors: Tim Et al.
    Nat Commun  2023;14:2803
  4. IGF-1 boosts mitochondrial function by a Ca2+ uptake-dependent mechanism in cultured human and rat cardiomyocytes.
    Authors: Sergio Et al.
    Front Physiol  2023;14:1106662
  5. Reengineering Ponatinib to Minimize Cardiovascular Toxicity.
    Authors: Wenqi Et al.
    Cancer Res  2022;82:2777-2791
  6. Virus-induced inhibition of cardiac pacemaker channel HCN4 triggers bradycardia in human-induced stem cell system.
    Authors: Nathalie Et al.
    Cell Mol Life Sci  2022;79:440
  7. SOX transcription factors direct TCF-independent WNT/β-catenin responsive transcription to govern cell fate in human pluripotent stem cells.
    Authors: Aaron M Et al.
    Cell Rep  2022;40:111247
  8. STK25 inhibits PKA signaling by phosphorylating PRKAR1A.
    Authors: Gordana Et al.
    Cell Rep  2022;40:111203
  9. Functional microvascularization of human myocardium in vitro.
    Authors: Anna M Et al.
    Cell Rep Methods  2022;2:100280
  10. Single-cell sequencing reveals lineage-specific dynamic genetic regulation of gene expression during human cardiomyocyte differentiation.
    Authors: Guanghao Et al.
    PLoS Genet  2022;18:e1009666
  11. Time-regulated transcripts with the potential to modulate human pluripotent stem cell-derived cardiomyocyte differentiation.
    Authors: Jose E Et al.
    Stem Cell Res Ther  2022;13:437
  12. Contribution of Trp63CreERT2-labeled cells to alveolar regeneration is independent of tuft cells.
    Authors: Timothy C Et al.
    Elife  2022;11
  13. Paraxial mesoderm organoids model development of human somites.
    Authors: Olivier Et al.
    Elife  2022;11
  14. Selective Surface and Intraluminal Localization of Wnt Ligands on Small Extracellular Vesicles Released by HT-22 Hippocampal Neurons.
    Authors: Nibaldo C Et al.
    Front Cell Dev Biol  2021;9:735888
  15. A Comparative Assessment of Marker Expression Between Cardiomyocyte Differentiation of Human Induced Pluripotent Stem Cells and the Developing Pig Heart.
    Authors: Yong Et al.
    Stem Cells Dev  2021;30:374-385
  16. Isolation of human ESC-derived cardiac derivatives and embryonic heart cells for population and single-cell RNA-seq analysis.
    Authors: Kenneth R Et al.
    STAR Protoc  2021;2:100339
  17. Massive expansion and cryopreservation of functional human induced pluripotent stem cell-derived cardiomyocytes.
    Authors: Joseph C Et al.
    STAR Protoc  2021;2:100334
  18. Oxygen Is an Ambivalent Factor for the Differentiation of Human Pluripotent Stem Cells in Cardiac 2D Monolayer and 3D Cardiac Spheroids.
    Authors: Alain Et al.
    Int J Mol Sci  2021;22
  19. Selenoprotein DIO2 Is a Regulator of Mitochondrial Function, Morphology and UPRmt in Human Cardiomyocytes.
    Authors: Rudolf A Et al.
    Int J Mol Sci  2021;22
  20. The thrombin receptor links brain derived neurotrophic factor to neuron cholesterol production, resiliency and repair after spinal cord injury.
    Authors: Ha Neui Et al.
    Neurobiol Dis  2021;152:105294
  21. Dynamic effects of genetic variation on gene expression revealed following hypoxic stress in cardiomyocytes.
    Authors: Matthew Et al.
    Elife  2021;10
  22. Functional dynamic genetic effects on gene regulation are specific to particular cell types and environmental conditions.
    Authors: David E Et al.
    Elife  2021;10
  23. 16p11.2 microdeletion imparts transcriptional alterations in human iPSC-derived models of early neural development.
    Authors: Hui Et al.
    Elife  2020;9
  24. Modeling polymorphic ventricular tachycardia at rest using patient-specific induced pluripotent stem cell-derived cardiomyocytes.
    Authors: Andrew R Et al.
    EBioMedicine  2020;60:103024
  25. 4,4'-Diisothiocyanato-2,2'-Stilbenedisulfonic Acid (DIDS) Modulates the Activity of KCNQ1/KCNE1 Channels by an Interaction with the Central Pore Region.
    Authors: Nathalie Et al.
    Cell Physiol Biochem  2020;54:321-332
  26. Accelerated differentiation of human pluripotent stem cells into neural lineages via an early intermediate ectoderm population.
    Authors: Walter C Et al.
    Stem Cells  2020;38:1400-1408
  27. Metabolic Maturation Media Improve Physiological Function of Human iPSC-Derived Cardiomyocytes.
    Authors: Hui Et al.
    Cell Rep  2020;32:107925
  28. Reengineering an Antiarrhythmic Drug Using Patient hiPSC Cardiomyocytes to Improve Therapeutic Potential and Reduce Toxicity.
    Authors: Mark Et al.
    Cell Stem Cell  2020;27:813-821.e6
  29. The role of cathepsin D in the pathophysiology of heart failure and its potentially beneficial properties: a translational approach.
    Authors: Nilesh J Et al.
    Eur J Heart Fail  2020;22:2102-2111
  30. Wnt regulates amino acid transporter Slc7a5 and so constrains the integrated stress response in mouse embryos.
    Authors: Melanie Et al.
    EMBO Rep  2020;21:e48469
  31. Systematic Comparison of High-throughput Single-Cell and Single-Nucleus Transcriptomes during Cardiomyocyte Differentiation.
    Authors: Yoav Et al.
    Sci Rep  2020;10:1535
  32. A generally conserved response to hypoxia in iPSC-derived cardiomyocytes from humans and chimpanzees.
    Authors: Ward and Gilad
    Elife  2019;8
  33. Canonical Wnt signaling promotes pacemaker cell specification of cardiac mesodermal cells derived from mouse and human embryonic stem cells.
    Authors: Liang Et al.
    Stem Cells  2019;38:352
  34. Wnt family member 4 (WNT4) and WNT3A activate cell-autonomous Wnt signaling independent of porcupine O-acyltransferase or Wnt secretion.
    Authors: Rebecca L Et al.
    J Biol Chem  2019;294:19950-19966
  35. Long-Term Stability and Differentiation Potential of Cryopreserved cGMP-Compliant Human Induced Pluripotent Stem Cells.
    Authors: Fan Et al.
    Int J Mol Sci  2019;21
  36. Engineering of human cardiac muscle electromechanically matured to an adult-like phenotype.
    Authors: Kumi Et al.
    Nat Protoc  2019;14:2781-2817
  37. Capacitation of human na�ve pluripotent stem cells for multi-lineage differentiation.
    Authors: Rostovskaya Et al.
    Development  2019;146
  38. Cardiogenic programming of human pluripotent stem cells by dose-controlled activation of EOMES.
    Authors: Pfeiffer Et al.
    Nat Commun  2018;9:440
  39. An Ultrasensitive Calcium Reporter System via CRISPR-Cas9-Mediated Genome Editing in Human Pluripotent Stem Cells.
    Authors: Jiang Et al.
    iScience  2018;9:27
  40. Stage-specific Effects of Bioactive Lipids on Human iPSC Cardiac Differentiation and Cardiomyocyte Proliferation.
    Authors: Sharma Et al.
    Sci Rep  2018;8:6618
  41. A Comparative Assessment of Human and Chimpanzee iPSC-derived Cardiomyocytes with Primary Heart Tissues.
    Authors: Pavlovic Et al.
    Sci Rep  2018;8:15312
  42. A promoter interaction map for cardiovascular disease genetics.
    Authors: Montefiori Et al.
    Elife  2018;7
  43. Human-Induced Pluripotent Stem Cells Manufactured Using a Current Good Manufacturing Practice-Compliant Process Differentiate Into Clinically Relevant Cells From Three Germ Layers.
    Authors: Shafa Et al.
    Front Med (Lausanne)  2018;5:69
  44. Iron deficiency impairs contractility of human cardiomyocytes through decreased mitochondrial function.
    Authors: Hoes Et al.
    Eur J Heart Fail  2018;20:910
  45. Adrenergic Stress Protection of Human iPS Cell-Derived Cardiomyocytes by Fast Kv7.1 Recycling.
    Authors: Piccini Et al.
    Front Physiol  2017;8:705
  46. Cardiac Subtype-Specific Modeling of Kv1.5 Ion Channel Deficiency Using Human Pluripotent Stem Cells.
    Authors: Marczenke Et al.
    Front Physiol  2017;8:469
  47. A Novel Role for the BMP Antagonist Noggin in Sensitizing Cells to Non-canonical Wnt-5a/Ror2/Disheveled Pathway Activation.
    Authors: Bernatik Et al.
    Front Cell Dev Biol  2017;5:47
  48. Id2 controls specification of Lgr5+ intestinal stem cell progenitors during gut development.
    Authors: Nigmatullina Et al.
    EMBO J  2017;36:869
  49. Universal cardiac induction of human pluripotent stem cells in two and three-dimensional formats: implications for in vitro maturation.
    Authors: Guiscard Et al.
    Stem Cells  2015;33:1456-69

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iPSC differentiation
By Anonymous on 10/28/2021
Species: Human

Used to differentiate human iPSC into cardiac cells. dose of 2uM was used

iPSC differentiation 5148
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