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KYA1797K

Catalog No. T6868 CAS 1956356-56-1

KYA1797K is a highly potent and selective inhibitor. Wnt/β-catenin IC50 is 0.75 μM through TOPflash assay.

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KYA1797K, CAS 1956356-56-1

Pack Size	Availability	Price/USD
2 mg	In stock	$ 41.00
5 mg	In stock	$ 67.00
10 mg	In stock	$ 117.00
25 mg	In stock	$ 257.00
50 mg	In stock	$ 437.00
100 mg	In stock	$ 648.00
1 mL * 10 mM (in DMSO)	In stock	$ 74.00

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Purity: 99.33%

Purity: 98%

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Description	KYA1797K is a highly potent and selective inhibitor. Wnt/β-catenin IC50 is 0.75 μM through TOPflash assay.
Targets&IC50	Wnt/β-catenin:0.75 μM
In vitro	KYA1797K significantly decreases reporter activities for the Wnt/β-catenin and MAPK/ERK pathways but does not affect the reporter activities of other cancer-related pathways, such as the Notch and TGFβ pathways, thus, KYA1797K selectively regulates the Wnt/β-catenin and Ras/ERK pathways. KYA1797K enhances the β-catenin binding affinity of endogenous axin, GSK3β and β-TrCP. Interaction between APC and β-catenin is not enhanced by KYA1797K. It promotes the formation of the β-catenin destruction complex. KYA1797K degrades both β-catenin and Ras in these cells(CRC lines SW480, LoVo, DLD1 and HCT15) in a dose-dependent manner, cell proliferation is also suppressed by KYA1797K treatment. KYA1797K inhibits proliferation of CRC cells mainly via destabilization of β-catenin with additional Ras degradation. KYA1797K directly targeted axin and modulated conformation of the β-catenin destruction complex[1].
In vivo	KYA1797K administration by intraperitoneally injection(i.p.) (25 mg/kg) reduces both weight and volume of the tumor by 70% in mice carrying xenografted tumors from the D-MT cell line that harbors both APC and KRAS mutations. KYA1797K treatment significantly reduces levels of β-catenin and Ras proteins as well as Wnt/β-catenin and Ras signaling target. No change in the weight and no abnormalities in liver tissues of mice treated with KYA1797K. KYA1797K significantly reduces the subcellular localization of β-catenin in the nuclei and pan-Ras on the membrane of tumor cells. Thus, KYA1797K has anti-tumor effect[1].
Cell Research	To assay cell proliferation, HCT15 or SW480 cells are plated at a density of 2 × 104 cells/well, and D-WT or D-MT cells were seeded at a density of 1×104 cells/well in a 24-well plate. The cells are then treated with 25 μM KYA1797K or with control (DMSO) for 72 h. In a 96-well plate, cells are seeded at a density of 3 × 103 cells/well. After 24 h, the cells are treated with KY1220, KYA1797K, IWR-1 or XAV939 for 4 d. Next, MTT reagent is added to each well at a concentration of 0.25 mg/ml. After incubation for 2 h at 37°C, insoluble purple formazan is obtained by removing the medium and incubating in 1 ml (24-well) or 200 μl (96-well) of DMSO for 1 h. The absorbance of the formazan product is determined at 590 nm every 24 h. (Only for Reference)

Molecular Weight	442.51
Formula	C17H11N2O6S2·K
CAS No.	1956356-56-1

Storage

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

Solubility Information

DMSO: 6 mg/mL (13.56 mM), Sonication is recommended.

References and Literature

1. Cha PH, et al. Nat Chem Biol. 2016, 12(8):593-600.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Neuronal Differentiation Compound Library Anti-Obesity Compound Library Anti-Prostate Cancer Compound Library Anti-Colorectal Cancer Compound Library Bioactive Compound Library Reprogramming Compound Library Anti-Aging Compound Library Osteogenesis Compound Library

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Keywords

KYA1797K 1956356-56-1 Cytoskeletal Signaling Stem Cells Wnt/beta-catenin Wnt Beta catenin β-catenin inhibit Inhibitor KYA-1797K inhibitor

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