IWP-L6

SKU: orb1223308

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.

Key Properties

• CAS Number: 1427782-89-5
• MW: 472.58
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₀N₄O₂S₂
• SMILES: O=C(CSc1nc2c(SCC2)c(=O)n1c1ccccc1)Nc1ncc(cc1)c1ccccc1
• Target: Porcn
• Solubility: DMSO : 1.43 mg/mL 3.03 mM

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

IWP-L6 | PORCN Inhibitor III

Quick Database Links

Gene Symbol

Porcn