The Tankyrase1/2 Inhibitor IV, JW55 controls the biological activity of Tankyrase1/2. This small molecule/inhibitor is primarily used for Biochemicals applications.
Synonym(s):
Tankyrase1/2 Inhibitor IV, JW55, TNKS1/2 Inhibitor IV, Wnt Pathway Inhibitor XVII, N-(4-((4-(4-Methoxyphenyl)tetrahydro-2H-pyran-4-yl)methylcarbamoyl)phenyl)furan-2-carboxamide
A cell-permeable phenylcarbamoylfuran-carboxamide compound that acts as a potent, selective, and reversible inhibitor of poly(ADP-ribosyl)ation activity of tankyrase 1 and 2 (IC50 = 1.9 and 0.83 µM, respectively). Exhibits high selectivity over PARP1 (IC50 = 20 µM). Stabilizes and increases AXIN2 levels, thereby enhancing phosphorylation and degradation of β-catenin resulting in reduced canonical Wnt signaling (IC50 = 470 nM in Wnt 3a-induced HEK293 cells transfected with ST-Luc). Shown to induce cell cycle arrest and diminish the proliferation of SW480 colorectal cancer cells (~ 5 µM). Suppresses tumor growth in tamoxifen-induced polyposis in Apc knock-out murine model (100 mg/kg, i.p.). Displays adequate human liver microsomal stability (t1/2 = 10.1 min).
Biochem/physiol Actions
Cell permeable: yes
Primary Target tankyrase 1 and 2
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 6 months at -20°C.
Other Notes
Waaler, J., et al. 2012. Cancer Res.72, 2822.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
Certificates of Analysis (COA)
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