Wnt-C59 | Porcupine Inhibitor

CAS:
1243243-89-1
Catalog Number:
10-4605
Activity:
Porcupine Inhibitor
Chemical Name:
4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide
Molecular Weight:
379.46
Molecular Formula:
C25H21N3O
Solubility:
Soluble in DMSO (up to 7 mg/ml) or in Ethanol (up to 6 mg/mL)
Physical Properties:
Tan solid
Purity:
>98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$50.00
25 mg$150.00

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

References/Citations:

1) Proffitt et al. (2013), Pharmacological Inhibition of the Wnt Acyltransferase PORCN Prevents Growth of Wnt-Driven Mammary Cancer; Cancer Res., 73 502
2) Koo et al. (2015), Porcupine inhibitor suppresses paracrine Wnt-driven growth of Rnf43;Znrf3-mutant neoplasia; Proc. Natl. Acad. Sci.USA, 112 7548
3) Motono et al. (2016), Wnt-C59, a Small-Molecule Wnt Inhibitor, Efficiently Induces Anterior Cortex That Includes Cortical Motor Neurons From Human Pluripotent Stem Cells; Stem Cells Transl.Med., 5 552
4) Madan et al. (2016), Experimental inhibition of porcupine-mediated Wnt O-acylation attenuates kidney fibrosis; Kidney Int., 89 1062

CAS:
1243243-89-1
Catalog Number:
10-4605
Activity:
Porcupine Inhibitor
Chemical Name:
4-(2-Methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]benzeneacetamide
Molecular Weight:
379.46
Molecular Formula:
C25H21N3O
Solubility:
Soluble in DMSO (up to 7 mg/ml) or in Ethanol (up to 6 mg/mL)
Physical Properties:
Tan solid
Purity:
>98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee