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KYA1797K Wnt/beta-catenin inhibitor

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

KYA1797K Wnt/beta-catenin inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 442.51

Purity & Quality Control

Batch: S832701 DMSO]29 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.59%
99.59

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Cell Culture and Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-N87 Function assay 5 or 25 μM 24 h reduces β-catenin, pan-Ras and p-ERK levels in a concentration-dependent manner 30965636
MKN74 cells Function assay 5 or 25 μM 24 h reduces β-catenin level at a concentration of 25 μM 30965636
NCI-H1650 Function assay 25 μmol/L  0, 3, 6, 9, 12 and 24 h KYA1797K treatment accelerated reduction of β-catenin and pan-Ras levels 30679620
NCI-H460 Function assay 25 μmol/L  0, 3, 6, 9, 12 and 24 h KYA1797K treatment accelerated reduction of β-catenin and pan-Ras levels 30679620
Click to View More Cell Line Experimental Data

Mechanism of Action

Targets
Wnt/β-catenin [1]
(in HEK293 cells)
0.75 μM

In vitro
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, this compound selectively regulates the Wnt/β-catenin and Ras/ERK pathways. It enhances the β-catenin binding affinity of endogenous axin, GSK3β and β-TrCP. Interaction between APC and β-catenin is not enhanced by this chemical. It promotes the formation of the β-catenin destruction complex. This compound degrades both β-catenin and Ras in these cells in a dose-dependent manner, cell proliferation is also suppressed by this treatment. It inhibits proliferation of CRC cells mainly via destabilization of β-catenin with additional Ras degradation. This chemical directly targeted axin and modulated conformation of the β-catenin destruction complex[1].
Cell Research 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, this compound, 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.

In Vivo
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. This compound 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 this chemical. It significantly reduces the subcellular localization of β-catenin in the nuclei and pan-Ras on the membrane of tumor cells. Thus, this compound has anti-tumor effect[1].
Animal Research Animal Models mice carrying xenografted tumors
Dosages 25 mg/kg
Administration i.p.

References
  • https://pubmed.ncbi.nlm.nih.gov/27294323/

Chemical Information

Molecular Weight 442.51 Formula

C17H11N2O6S2.K
CAS No. 1956356-56-1 SDF Download SDF
Synonyms N/A
Smiles C1=CC(=CC=C1C2=CC=C(O2)C=C3C(=O)N(C(=S)S3)CCC(=O)[O-])[N+](=O)[O-].[K+]

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 29 mg/mL ( (65.53 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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

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