IWP-L6 (1427782-89-5) Description
IWP-L6, also known as PORCN Inhibitor III and Wnt Pathway Inhibitor XIX, is a potent inhibitor of PORCN (EC50 = 0.5 nM). Porcupine is a member of the membrane-bound O-acyltransferase family of proteins. It catalyzes the palmitoylation of Wnt proteins, a process required for their secretion and activity.
Target: Porcupine in vitro: IWP-L6 effectively suppressed the phosphorylation of dishevelled 2 (Dvl2) in HEK293 cells, a biochemical event associated with many Wnt-dependent cellular responses. IWP-L6 inhibits Wnt mediated branching morphogenesis in cultured embryonic kidneys. in vivo: IWP-L6 is stable in human plasma over 24 h, it was rapidly metabolized in rat plasma (t1/2 = 190 min), murine plasma (t1/2 = 2 min), and the murine liver S9 fractions (t1/2 = 26 min). The major metabolites are the amide cleavage products. Similar species-dependent metabolitic profiles due to the involvement of carboxylesterase (CES) have been reported with other drug candidates. Despite its modest metabolic stability in mouse-derived plasma, IWP-L6 was highly active in zebrafish. IWP-L6 exhibited more potent activity.
IWP-L6 (1427782-89-5) Specifications
|Synonyms||IWP-L6; IWP L6; IWPL6; PORCN Inhibitor III; Wnt Pathway Inhibitor XIX.|
|Purity||>98% (or refer to the Certificate of Analysis)|
|Monoisotopic Mass||472.103 g/mol|
|Solubility||Soluble in DMSO, not in water|
|Storage Temp.||Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).|
|Shelf life||>2 years if stored properly|
|Handling||Protect from air and light|
|Application||Potent PORCN inhibitor|