product name IWP-L6
Description: IWP-L6 is a highly potent Porcn inhibitor with EC50 of 0.5 NM. It targets the Wnt signaling since Porcupine is the enzyme that catalyzes the palmitoylation of Wnt proteins. In HEK293 cells, IWP-L6 is found to inhibi the phosphorylation of dishevelled 2 (Dvl2) significantly. IWP-L6 has good stability in human plasma but weaker stability in rat and mouse plasma. In vivo assay shows that IWP-L6 is quite active in zebrafish. It blocks the regeneration of the tailfin effectively. It also shows inhibition of posterior axis formation at low micromolar concentrations. Additionally, in cultured mouse embryonic kidneys, 10nM IWP-L6 can significantly reduce branching morphogenesis while 50nM IWP-L6 completely blocks Wnt signaling.
References: J Med Chem. 2013 Mar 28;56(6):2700-4.
472.58
Formula
C25H20N4O2S2
CAS No.
1427782-89-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 25 mg/mL (52.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
Porcn Inhibitor III
other peoduct :
| In Vitro |
In vitro activity: IWP-L6 blocks the phosphorylation of the cytoplasmic Wnt pathway effector Dvl2 in HEK293 cells. In cultured embryonic kidneys, IWP-L6 also inhibits Wnt mediated branching morphogenesis by reversibly blocking Wnt signaling. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | IWP-L6 is stable in human plasma over 24 h, while rapidly metabolized in rat plasma (t1/2 = 190 min), murine plasma (t1/2 = 2 min), and the murine liver S9 fractions. In embryonic zebrafish, IWP-L6 effectively inhibits posterior axis formation, a Wnt/β-catenin dependent developmental process. |
| Animal model | |
| Formulation & Dosage | |
| References | J Med Chem. 2013 Mar 28;56(6):2700-4. |
