5.04819

Porcn Inhibitor III, IWP-L6

• Synonym(e): Porcn Inhibitor III, IWP-L6, IWPL6, Wnt Pathway Inhibitor XIX
• Empirische Formel (Hill-System): C₂₅H₂₀N₄O₂S₂
• CAS-Nummer: 1427782-89-5
• Molekulargewicht: 472.58
• UNSPSC-Code: 12352200

Eigenschaften

• Assay: ≥99% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: off-white
• Löslichkeit: DMSO: 10 mg/mL
• Lagertemp.: 2-8°C
• InChI: 1S/C25H20N4O2S2/c30-22(28-21-12-11-18(15-26-21)17-7-3-1-4-8-17)16-33-25-27-20-13-14-32-23(20)24(31)29(25)19-9-5-2-6-10-19/h1-12,15H,13-14,16H2,(H,26,28,30)
• InChIKey: QESQGTFWEQMCMH-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

A cell-permeable pyridinyl-phenylacetamide that is reported to be 60-times more potent than IWP-2 (Cat. No. 681671) in suppressing autonomous Wnt signaling in murine L-Wnt-STF fibroblasts (IC₅₀ = 0.5 nM) and 100-times more potent in blocking branching morphogenesis in cultured murine embryonic kidney (complete blockage at 50 nM). Also shown to be at least twice as potent as TNKS inhibitor IWR-1 (Cat. No. 681669) in preventing the regeneration of severed zebrafish tailfin and in inhibiting zebrafish embryo prosterior axis formation (Effective conc = 5 µM). Its susceptibility to metabolization by serum carboxylesterase limits its in vivo use in rats and mice.

A cell-permeable, benzothiazole-to-5-phenylpyridin substituted IWP-2 (Cat. No. 681671) derivative that is reported to be 60-times more potent than IWP-2 in suppressing autonomous Wnt signaling in murine L-Wnt-STF fibroblasts (IC₅₀ = 0.5 vs. 30 nM) and 100-times more potent in blocking Wnt signaling-mediated branching morphogenesis in cultured murine embryonic kidneys (complete blockage with 50 nM IWP-L6 or 5 µM IWP-2). Also shown to be at least twice as potent as TNKS inhibitor IWR-1 (Cat. No. 681669) in preventing the regeneration of severed zebrafish tailfin and in inhibiting zebrafish embryo prosterior axis formation (Effective conc = 5 µM). Its susceptibility to metabolization by serum carboxylesterase limits its in vivo use in rats and mice (t_1/2 = 2 and 190 min, respectively, in murine or rat plasma).

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
Porcupine

Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sonstige Hinweise

Wang, X., et al. 2013. J. Med. Chem.56, 2700.

Rechtliche Hinweise

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 2
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable