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Wnt&Beta catenin

Wnt-c59 (1243243-89-1)

Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM.

Not Intended for Therapeutic Use. For research use only.

CAS: 1243243-89-1 Category

Wnt-c59 (1243243-89-1) Description

Wnt-C59 is a potent porcupine (PORCN) inhibitor. Wnt-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. In mice, Wnt-C59 displayed good bioavailability, as once daily oral administration was sufficient to maintain blood concentrations well above the IC(50). C59 blocked progression of mammary tumors in MMTV-WNT1 transgenic mice while downregulating Wnt/β-catenin target genes. Porcupine (PORCN) is a membrane bound O-acyltransferase that is required for Wnt palmitoylation, secretion, and biologic activity.

 

Wnt-c59 (1243243-89-1) Specifications

Product Name Wnt-C59
Synonyms WntC59; Wnt-C 59; Wnt-C59
Chemical Names 2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 1243243-89-1
Molecular Formula C25H21N3O
Molecular Weight 379.45
Monoisotopic Mass 379.168 g/mol
MDL number MFCD22201167
InChIKey KHZOJCQBHJUJFY-UHFFFAOYSA-N
InChi Code 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)
SMILES O=C(NC1=CC=C(C2=CC=CN=C2)C=C1)CC3=CC=C(C4=CC(C)=NC=C4)C=C3
Form Powder
Color White to off-white
Solubility  Soluble in DMSO, not in water
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and light
Application A porcupine homolog – Drosophila (PORCN) inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase

 


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RIDADR NONH for all modes of transport

References:

  • 1: Wang B, Zou Q, Sun M, Chen J, Wang T, Bai Y, Chen Z, Chen B, Zhou M. Reversion of trichostatin A resistance via inhibition of the Wnt signaling pathway in human pancreatic cancer cells. Oncol Rep. 2014 Nov;32(5):2015-22. doi: 10.3892/or.2014.3476. Epub 2014 Sep 10. PubMed PMID: 25224651.
  • 2: Bengoa-Vergniory N, Gorroño-Etxebarria I, González-Salazar I, Kypta RM. A switch from canonical to noncanonical wnt signaling mediates early differentiation of human neural stem cells. Stem Cells. 2014 Dec;32(12):3196-208. doi: 10.1002/stem.1807. PubMed PMID: 25100239.
  • 3: Proffitt KD, Madan B, Ke Z, Pendharkar V, Ding L, Lee MA, Hannoush RN, Virshup DM. Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer. Cancer Res. 2013 Jan 15;73(2):502-7. doi: 10.1158/0008-5472.CAN-12-2258. Epub 2012 Nov 27. PubMed PMID: 23188502.
  • D. Proffitt et al. Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer. Cancer Res. 2013, 73, 502-507.
  • Cheng Y, et al. Wnt-C59 arrests stemness and suppresses growth of nasopharyngeal carcinoma in mice by inhibiting the Wnt pathway in the tumor microenvironment. Oncotarget. 2015 Jun 10;6(16):14428-39.