| Name | K-756 |
| Description | K-756 is a direct and selective inhibitor of tankyrase (TNKS), inhibiting the ADP-ribosylation activity of TNKS1 [IC50 = 31 nM] and TNKS2 [IC50 = 36 nM]. |
| In vitro | K-756 inhibits the cell growth of APC-mutant colorectal cancer COLO 320DM and SW403 cells by inhibiting the Wnt/β-catenin pathway. K-756 is a novel and selective Wnt/β-catenin pathway inhibitor targeting tankyrase (TNKS). TNKS is one of the members of the PARP family. K-756 binds to the induced pocket of TNKS and inhibits its enzyme activity. K-756 inhibits TNKS1 and TNKS2 by 97% and 100%, respectively. The inhibitory activity of K-756 against PARP1, PARP2, PARP3, PARP6, PARP7, and PARP11 is less than 13%. K-756 strongly inhibits the reporter activity in DLD-1/TCF-Luc cells (IC50: 110 nM) but does not inhibit DLD-1/mtTCF-Luc cells, even at 1,000 nM. APC-mutant colorectal cancer cell line COLO 320DM and SW403 cells are treated with K-756 and after 144 hours, cell growth inhibition is measured by an XTT assay. The application of K-756 inhibits the cell growth of COLO 320DM with a GI50 of 780 nM. K-756 also inhibits SW403 with a GI50 of 270 nM[1]. |
| In vivo | Vehicle (0.5% MC400) or K-756 is given orally once daily for three consecutive days at doses of 100, 200, and 400 mg/kg. The inhibition of the Wnt/β-catenin pathway in tumors is assessed by measuring the levels of FGF20 and LGR5, as well as luciferase activity. Inhibition of the Wnt/β-catenin pathway is evident at a 400 mg/kg dose after just one day of administration. After three days of treatment, significant reductions in FGF20 expression and reporter activity are observed at doses of 100 mg/kg and higher, while LGR5 expression significantly decreases at doses of 200 mg/kg and higher. The greatest inhibitory effect is achieved with a three-day administration of K-756 at 400 mg/kg [1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 4.5 mg/mL (10.38 mM), Sonication is recommended.
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| Keywords | PARP | Inhibitor | poly ADP ribose polymerase | K756 | K 756 | K-756 | inhibit |
| Inhibitors Related | Urea | 4'-Methoxychalcone | Wnt pathway activator 1 | CHIR-99021 | 3-Aminobenzamide | XAV-939 | Niraparib | Olaparib | Benzamide | Nefopam hydrochloride | OUL35 | Bisdemethoxycurcumin |
| Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Anti-Ovarian Cancer Compound Library | Neuroprotective Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Neuronal Differentiation Compound Library |
United States
