General description
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 (t1/2 = 2 and 190 min, respectively, in murine or rat plasma).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Porcupine
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Wang, X., et al. 2013. J. Med. Chem.56, 2700.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5048190001