Brief Description

Wnt-C59(C59) is a very potent and highly selective Wnt signaling antagonist with an IC50 ~ 74 pM in the Wnt signaling reporter assay.
IC50 Value: 74 pM
Wnt-C59 prevents palmitylation of Wnt proteins by Porcupine (a membrane-bound Oacyltransferase), thereby blocking Wnt protein secretion and activity.
in vitro: 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 at 0.1-0.2 ?M to completely block Wnt protein secretion. When used at 0.5 ?M, it can be used functionally replace the Dkk protein in many assay conditions.
in vivo: In mice, 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. Surprisingly, mice exhibit no apparent toxicity, such that at a therapeutically effective dose there were no pathologic changes in the gut or other tissues. Wnt-C59 was used to dose mice orally at 5-10 mg/kg once per day or 5 mg/kg twice per day.

Solubility

DMSO up to 50 mM

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

Yellow to khaki solid