IWP-L6

Research use only, not for human use.

IWP-L6 is an extremely effective Porcn inhibitor (EC50: 0.5 nM).

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.

IWP-L6 (Porcn?Inhibitor?III) 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 .

IWP-L6 (Porcn?Inhibitor?III) 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 | PORCN Inhibitor III

Others

Other Targets

Porcn

Cancer

——

1427782-89-5

472.58

C25H20N4O2S2

>98% (HPLC)

DMSO : 1.43 mg/mL 3.03 mM;

O=C(CSc1nc2c(SCC2)c(=O)n1c1ccccc1)Nc1ncc(cc1)c1ccccc1

N-(5-phenyl-2-pyridinyl)-2-[(3,4,6,7-tetrahydro-4-oxo-3-phenylthieno[3,2-d]pyrimidin-2-yl)thio]-acetamide

(-20℃)

With Ice Pack

≥ 2 years