Wnt-C59 --- Wnt Antagonist
Overview | |
Catalog # | bs-60005c-2mg-solid |
Product Name | Wnt-C59 --- Wnt Antagonist |
Specifications | |
Storage Buffer | Powder |
Storage Condition | Store in dry, dark place at -20C for 1 year. |
Target | |
Product Information | Molecular Weight: 379.45 Formula: C25 H21 N3 O CAS Number: 1243243-89-1 InChi Key: KHZOJCQBHJUJFY-UHFFFAOYSA-N 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) Smiles: CC1C=C(C=CN=1)C1C=CC(CC(=O)NC2C=CC(=CC=2)C2C=NC=CC=2)=CC=1 Purity: 98.0 Solubility: DMSO up to 50 mM Appearance: Solid Power. Shelf Life: 1 year |
Description | Wnt-C59 is a very potent and highly selective Wnt signaling antagonist with an IC50 ~ 74 pM in the Wnt signaling reporter assay. It prevents palmitylation of Wnt proteins by Porcupine (a membrane-bound O-acyltransferase), thereby blocking Wnt protein secretion and activity. Wnt-C59 displayed good bioavailability as once daily oral administration and blocked progression of mammary tumors in MMTV-WNT1 transgenic mice model while downregulating Wnt/β-catenin target genes. Because Wnt-C59 exhibits much better potency and selectivity than the reported IWP series of Porcupine/Wnt inhibitors, it serves as the better Wnt pathway inhibitor for in vitro and in vivo studies. |