Wnt-C59

Wnt-C59 Property

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

HS Code 

2933399990

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Wnt-C59 Chemical Properties,Usage,Production

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