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 (t_1/2 = 10.1 min).

Cell permeable: yes

Primary Target
tankyrase 1 and 2

Reversible: yes

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Waaler, J., et al. 2012. Cancer Res.72, 2822.

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

Toxicity: Standard Handling (A)