Wnt-C59 (C59) - ≥98%, high purity , CAS No.1243243-89-1, Inhibitor of porcupine O-acyltransferase

Item Number
W125232
Grouped product items
SKUSizeAvailabilityPrice Qty
W125232-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$59.90
W125232-25mg
25mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$171.90
W125232-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$477.90

Potent, cell-permeable Wnt signaling pathway inhibitor

Basic Description

SynonymsWnt-C59 | 1243243-89-1 | 2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide | C25H21N3O | 2-[4-(2-Methyl-pyridin-4-yl)-phenyl]-N-(4-pyridin-3-yl-phenyl)-acetamide | Wnt-C59 (C59) | CHEMBL2139947 | 2-[4-(2-methylpyridin-4-yl)phenyl]-N-(4-pyridin-3-yl
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological Mechanisms C59 inhibits PORCN activity in vitro at nanomolar concentrations, as assessed by inhibition of Wnt palmitoylation, Wnt interaction with the carrier protein Wntless/WLS, Wnt secretion, and Wnt activation of β-catenin reporter activity . Wnt-C59 was used
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of porcupine O-acyltransferase
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM in HEK293 cells.
A porcupine homolog - Drosophila (PORCN) inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase

Associated Targets(Human)

PORCN Tchem Protein-serine O-palmitoleoyltransferase porcupine (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
YES1 Tclin Tyrosine-protein kinase YES (2781 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PORCN Tchem Probable protein-cysteine N-palmitoyltransferase porcupine (135 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK-293T (167025 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Names and Identifiers

IUPAC Name 2-[4-(2-methylpyridin-4-yl)phenyl]-N-(4-pyridin-3-ylphenyl)acetamide
INCHI InChI=1S/C25H21N3O/c1-18-15-22(12-14-27-18)20-6-4-19(5-7-20)16-25(29)28-24-10-8-21(9-11-24)23-3-2-13-26-17-23/h2-15,17H,16H2,1H3,(H,28,29)
InChi Key KHZOJCQBHJUJFY-UHFFFAOYSA-N
Canonical SMILES CC1=NC=CC(=C1)C2=CC=C(C=C2)CC(=O)NC3=CC=C(C=C3)C4=CN=CC=C4
Isomeric SMILES CC1=NC=CC(=C1)C2=CC=C(C=C2)CC(=O)NC3=CC=C(C=C3)C4=CN=CC=C4
PubChem CID 57519544
Molecular Weight 379.45

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Certificate of Analysis(COA)

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Lot NumberCertificate TypeDateItem
E1712139Certificate of AnalysisJan 16, 2023 W125232

Chemical and Physical Properties

SolubilityDMSO 76 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

Related Documents

References

1. Ho SY, Keller TH.  (2015)  The use of porcupine inhibitors to target Wnt-driven cancers..  Bioorg Med Chem Lett,  25  (23): (5472-6).  [PMID:26522946]
2. Kozielewicz P, Shekhani R, Moser S, Bowin CF, Wesslowski J, Davidson G, Schulte G.  (2021)  Quantitative Profiling of WNT-3A Binding to All Human Frizzled Paralogues in HEK293 Cells by NanoBiT/BRET Assessments..  ACS Pharmacol Transl Sci,  (3): (1235-1245).  [PMID:34151213]
3. Arthofer E, Hot B, Petersen J, Strakova K, Jäger S, Grundmann M, Kostenis E, Gutkind JS, Schulte G.  (2016)  WNT Stimulation Dissociates a Frizzled 4 Inactive-State Complex with Gα12/13..  Mol Pharmacol,  90  (4): (447-59).  [PMID:27458145]
4. Lin HK et al..  (2018)  Caveolin-1 down-regulation is required for Wnt5a-Frizzled 2 signalling in Ha-RasV12 -induced cell transformation..  J Cell Mol Med,      [PMID:29502342]
5. Willems L et al..  (2020)  Differentiation of Human Cardiac Atrial Appendage Stem Cells into Adult Cardiomyocytes: A Role for the Wnt Pathway?.  Int J Mol Sci,  21  (11):   [PMID:32486259]
6. Lu W et al..  (2016)  CXCL12/CXCR4 Axis Regulates Aggrecanase Activation and Cartilage Degradation in a Post-Traumatic Osteoarthritis Rat Model..  Int J Mol Sci,  17  (10):   [PMID:27690009]
7. Valnohova J et al..  (2018)  Functional dissection of the N-terminal extracellular domains of Frizzled 6 reveals their roles for receptor localization and Dishevelled recruitment..  J Biol Chem,  293  (46): (17875-17887).  [PMID:30237173]
8. Takakura N et al..  (2019)  Generation and characterization of Suncus murinus intestinal organoid: a useful tool for studying motilin secretion..  Cell Biol Int,      [PMID:31293061]
9. Xian L et al..  (2017)  HMGA1 amplifies Wnt signalling and expands the intestinal stem cell compartment and Paneth cell niche..  Nat Commun,  (15008).  [PMID:28452345]
10. Marruecos L et al..  (2020)  I?Ba deficiency imposes a fetal phenotype to intestinal stem cells..  EMBO Rep,  21  (6): (e49708).  [PMID:32270911]
11. Zhou W et al..  (2020)  miR-6838-5p Affects Cell Growth, Migration, and Invasion by Targeting GPRIN3 via the Wnt/ß-Catenin Signaling Pathway in Gastric Cancer..  Pathobiology,  87  (6): (327-337).  [PMID:33254176]
12. Jobe NP et al..  (2021)  Reduced WNT5A signaling in melanoma cells favors an amoeboid mode of invasion..  Mol Oncol,  15  (7): (1835-1848).  [PMID:33969605]
13. Radaszkiewicz T et al..  (2021)  RNF43 inhibits WNT5A-driven signaling and suppresses melanoma invasion and resistance to the targeted therapy..  Elife,  10    [PMID:34702444]
14. Shinkawa T et al..  (2022)  Subtypes in pancreatic ductal adenocarcinoma based on niche factor dependency show distinct drug treatment responses..  J Exp Clin Cancer Res,  41  (89).  [PMID:35272688]

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