product name IWP-2
Description: IWP-2 is an potent inhibitor of Wnt processing and secretion with IC50 of 27 nM in a cell-free assay, it showed selective blockage of Porcn-mediated Wnt palmitoylation, and does not affect Wnt/β-catenin in general; also it displays no effect against Wnt-stimulated cellular responses. IWP-2 can decrease MKN28 cell proliferation, migration and invasion, and elevate caspase 3/7 activity. IWP-2 can also downregulate the transcriptional activity of the Wnt/β-catenin signaling pathway and downregulate the expression levels of downstream Wnt/β-catenin target genes in MKN28 cells. IWP-2 may be a potential therapeutic option for gastric cancer.
References: Nat Chem Biol. 2009 Feb;5(2):100-7.
466.6
Formula
C22H18N4O2S3
CAS No.
686770-61-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 4 mg/mL (8.6 mM)
Water: <1 mg/mL
Ethanol:
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: IWP-2 is useful in both regenerative medicine and anticancer efforts. IWP-2 inactivates Porcn, a membrane-bound O-acyltransferase (MBOAT), and selectively inhibits palmitoylation of Wnt. IWP-2 blocks Wnt-dependent phosphorylation of Lrp6 receptor and Dvl2, and β-catenin accumulation. Kinase Assay: Cell Assay: Expression of Porcn but not Evi alleviated the effects of IWP-2 on pathway activity and Wnt secretion, which suggests that in general IWP-2 may act on Porcn. |
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| In Vivo | In order to test the in vivo activity of IWP-2, the authors turned to a simple and rapid assay of Wnt/b-catenin pathway activity: regeneration of the zebrafish caudal fin following resection. The addition of IWP-2 to the aquarium water of zebrafish failed to suppress fin regeneration after mechanical resection, which suggests either that IWP-2 have poor bioavailability or that the determinants in the gene product that they target are not conserved in zebrafish. |
| Animal model | |
| Formulation & Dosage | |
| References | Nat Chem Biol. 2009 Feb;5(2):100-7. |
