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K-756

Catalog No. T15639 CAS 130017-40-2

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).

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K-756, CAS 130017-40-2

Pack Size	Availability	Price/USD
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

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Purity: 99.68%

Biological Description

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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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.5 mg/mL (10.38 mM), Sonication is recommended.

References and Literature

1. Okada-Iwasaki R, et al. The Discovery and Characterization of K-756, a Novel Wnt/β-Catenin Pathway Inhibitor Targeting Tankyrase. Mol Cancer Ther. 2016 Jul;15(7):1525-34.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Epigenetics Compound Library Anti-Prostate Cancer Compound Library Stem Cell Differentiation Compound Library DNA Damage & Repair Compound Library Anti-Cancer Metabolism Compound Library Bioactive Compounds Library Max Cytoskeletal Signaling Pathway Compound Library Anti-Colorectal Cancer Compound Library Bioactive Compound Library

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Related compounds with same targets

Niraparib tosylate monohyrate Polyporenic acid C PJ34 hydrochloride Senaparib Talazoparib PARP1-IN-15 BGP-15 PARP-1-IN-2

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Keywords

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

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