KYA1797K

Catalog No.S8327 Batch:S832701

Technical Data

Formula

C₁₇H₁₁N₂O₆S₂.K

Molecular Weight

442.51

CAS No.

1956356-56-1

Solubility (25°C)*

In vitro

DMSO

29 mg/mL (65.53 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	0.72mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 14.4 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.36mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 7.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	Animal Models mice carrying xenografted tumors Dosages 25 mg/kg Administration i.p.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

Animal Models
mice carrying xenografted tumors
Dosages
25 mg/kg
Administration
i.p.

References

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

Customer Product Validation

: Data from [Data independently produced by , , Life Sci, 2018, 197:91-100]

: Data from [Data independently produced by , , Life Sciences, 2018, 197(15):91-100]

Selleck's KYA1797K has been cited by 14 publications

YAP and β-catenin cooperate to drive H. pylori-induced gastric tumorigenesis [ Gut Microbes, 2023, 15(1):2192501]	PubMed: 36959122
TRIM28 suppresses cancer stem-like characteristics in gastric cancer cells through Wnt/β-catenin signaling pathways [ Exp Biol Med (Maywood), 2023, 248(23):2210-2218]	PubMed: 38058023
Sfrp2 regulates the WNT/β-catenin pathway to slow the development of aldosterone-producing adenoma [ Cardiovasc Diagn Ther, 2023, 13(3):523-533]	PubMed: 37405011
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7]	PubMed: 34997030
KYA1797K, a Novel Small Molecule Destabilizing β-Catenin, Is Superior to ICG-001 in Protecting against Kidney Aging [ Kidney Dis (Basel), 2022, 8(5):408-423]	PubMed: 36466073
Pygo1 Regulates the Behavior of Human Non-Small-Cell Lung Cancer via the Wnt/β-Catenin Pathway [ Dis Markers, 2022, 2022:6993994]	PubMed: 36398031
Heparanase-Induced Activation of AKT Stabilizes β-Catenin and Modulates Wnt/β-Catenin Signaling during Herpes Simplex Virus 1 Infection [ mBio, 2021, 12(6):e0279221]	PubMed: 34749529
c-Myc Upregulated by High Glucose Inhibits HaCaT Differentiation by S100A6 Transcriptional Activation [ Front Endocrinol (Lausanne), 2021, 12:676403]	PubMed: 34060533
Guanylate-binding protein-2 inhibits colorectal cancer cell growth and increases the sensitivity to paclitaxel of paclitaxel-resistant colorectal cancer cells by interfering Wnt signaling. [ J Cell Biochem, 2020, 121(2):1250-1259]	PubMed: 31489998
A positive feedback loop between EZH2 and NOX4 regulates nucleus pulposus cell senescence in age-related intervertebral disc degeneration. [ Cell Div, 2020, 1;15:2]	PubMed: 32025238

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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