Powder: -20°C for 3 years | In solvent: -80°C for 1 year
K-756 is a direct and selective inhibitor of tankyrase (TNKS), which inhibits the ADP-ribosylation activity of TNKS1 (IC50 = 31 nM) and TNKS2 (IC50 = 36 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 44.00 | |
5 mg | In stock | $ 97.00 | |
10 mg | In stock | $ 172.00 | |
25 mg | In stock | $ 333.00 | |
50 mg | In stock | $ 597.00 | |
100 mg | In stock | $ 852.00 | |
500 mg | In stock | $ 1,730.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 116.00 |
Description | K-756 is a direct and selective inhibitor of tankyrase (TNKS), which inhibits the ADP-ribosylation activity of TNKS1 (IC50 = 31 nM) and TNKS2 (IC50 = 36 nM). |
Targets&IC50 | TNKS1:31 nM, TNKS2:36 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]. |
Molecular Weight | 433.5 |
Formula | C24H27N5O3 |
CAS No. | 130017-40-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4.5 mg/mL (10.38 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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K-756 130017-40-2 Chromatin/Epigenetic Cytoskeletal Signaling DNA Damage/DNA Repair Stem Cells PARP Wnt/beta-catenin Inhibitor poly ADP ribose polymerase K756 K 756 inhibit inhibitor