Wnt-C59 Chemical Properties

Melting point:

>159°C (dec.)

Boiling point:

628.3±55.0 °C(Predicted)

Density 

1.198±0.06 g/cm3(Predicted)

storage temp. 

+2C to +8C

solubility 

Soluble in DMSO (up to 7 mg/ml) or in Ethanol (up to 6 mg/mL)

form 

Off-white powder

pka

13.78±0.70(Predicted)

color 

Tan

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.

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)

InChIKey

KHZOJCQBHJUJFY-UHFFFAOYSA-N

SMILES

C1(CC(NC2=CC=C(C3=CC=CN=C3)C=C2)=O)=CC=C(C2C=CN=C(C)C=2)C=C1

Safety Information

HS Code 

2933399990

Wnt-C59 Usage And Synthesis

Description

Wnt-C59 (1243243-89-1) is a potent (IC50 = 74 pmol/L) inhibitor of Porcupine (PORCN), a Wnt-acyltransferase.1 Blockage of Wnt-acyltransferase prevents secretion of all Wnt isoforms.? It was able to block progression of mammary tumors in MMTV-WNT1 transgenic mice.1? Wnt-C59 strongly inhibited the growth of intestinal neoplasia in RZ-mutant mice.2? Wnt-C59 was able to efficiently differentiate pluripotent stem cells into cortical neurons (CTIP2+/COUP-TF1).3? Wnt-C59 was also able to dramatically attenuate kidney fibrosis via inhibition of collagen mRNA expression and expression of inflammatory cytokines.4

Uses

Wnt-C59 is a porcupine homolog – Drosophila (PORCN) inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase.

in vivo

storage

-20°C

References

[1] KYLE DAVID PROFFITT. Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer.[J]. Cancer research, 2013, 73 2: 502-507. DOI:10.1158/0008-5472.can-12-2258
[2] BON-KYOUNG KOO. Porcupine inhibitor suppresses paracrine Wnt-driven growth of Rnf43;Znrf3-mutant neoplasia.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2015, 112 24: 7548-7550. DOI:10.1073/pnas.1508113112
[3] M. MOTONO. WNT‐C59, a Small‐Molecule WNT Inhibitor, Efficiently Induces Anterior Cortex That Includes Cortical Motor Neurons From Human Pluripotent Stem Cells[J]. Stem Cells Translational Medicine, 2016, 5 1. DOI:10.5966/sctm.2015-0261
[4] BABITA MADAN . Experimental inhibition of porcupine-mediated Wnt O-acylation attenuates kidney fibrosis[J]. Kidney international, 2016, 89 5: Pages 1062-1074. DOI:10.1016/j.kint.2016.01.017

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