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KYA1797K Wnt/beta-catenin inhibitor

Name: KYA1797K
Brand: Selleck Chemicals
SKU: S8327
Availability: InStock
Rating: 5 (15 reviews)

Cat.No.S8327

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

Chemical Structure

Molecular Weight: 442.51

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

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, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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

Chemical Information, Storage & Stability

Molecular Weight	442.51	Formula	C₁₇H₁₁N₂O₆S₂.K	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1956356-56-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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+]

Solubility

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.720mg/ml (1.63mM)	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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.360mg/ml (0.81mM)	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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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, 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].
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].
References	https://pubmed.ncbi.nlm.nih.gov/27294323/

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