KYA1797K

Catalog No.S8327

KYA1797K Chemical Structure

Molecular Weight(MW): 442.51

KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 of 0.75 µM (TOPflash assay).

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1 Customer Review

  • A549 cells were treated with KYA1797K for 72 h, cells lysates were collected for western blotting, concentration gradient (1, 12.5 μM, 25 μM) was set for the analysis.

    Life Sciences, 2018, 197(15):91-100. KYA1797K purchased from Selleck.

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Choose Selective Wnt/beta-catenin Inhibitors

Biological Activity

Description KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 of 0.75 µM (TOPflash assay).
Targets
Wnt/β-catenin [1]
(in HEK293 cells)
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].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: CRC lines SW480, LoVo, DLD1 and HCT15.
  • Concentrations: 25 μM
  • Incubation Time: 72 h
  • Method:

    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)
Animal Research:

[1]

+ Expand
  • Animal Models: mice carrying xenografted tumors
  • Formulation: in a suspension of 90% PBS and 10% Tween 80
  • Dosages: 25 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 29 mg/mL (65.53 mM)
Water 29 mg/mL (65.53 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 442.51
Formula

C17H11N2O6S2.K

CAS No. 1956356-56-1
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID