Cat. No.: HY-124745

KY-05009

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a K_i of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.

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Pureté: 99.88%
CAS No.: 1228280-29-2
Formule: C₁₈H₁₆N₄O₂S
Masse moléculaire:352.41

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

KY-05009 Chemical Structure

CAS No.: 1228280-29-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

TNIK

100 nM (Ki)

Voir tous les produits spécifiques à Isoform MAP4K :

Voir tous les produits spécifiques à Isoform Wnt :

In Vitro

KY-05009 (0.1-30 μM; 24 hours; RPMI8226 cells) treatment inhibits the proliferation of RPMI8226 cells in a dose-dependent manner^[1].
KY-05009 (1-3 μM; 48-72 hours; RPMI8226 cells) treatment induces caspase-dependent apoptosis in RPMI8226 cells in a dose-dependent manner^[1].
KY-05009 (3 μM; 1 hour; RPMI8226 cells) treatment suppresses the transcriptional activity of Wnt signaling-related genes, including TNIK, CTNNB1, TCF7, and TCF4^[1].
. KY-05009 (3 μM; 9 hours; RPMI8226 cells) treatment inhibits the IL-6-induced interaction between TCF4 and β-catenin and the phosphorylation of TCF4^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

RPMI8226 cells
Concentration:

0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM
Incubation Time:

24 hours
Result:

Inhibited the proliferation of RPMI8226 cells.

Apoptosis Analysis^[1]

Cell Line:

RPMI8226 cells
Concentration:

1 μM, 3 μM, 10 μM
Incubation Time:

48 hours, 72 hours
Result:

Induced the binding of fluorescent Annexin V and 7-amino-actinomycin D (7-AAD) uptake.

RT-PCR^[1]

Cell Line:

RPMI8226 cells
Concentration:

3 μM
Incubation Time:

1 hour
Result:

Suppressed the transcriptional activity of Wnt signaling-related genes, including TNIK, CTNNB1, TCF7, and TCF4.

Western Blot Analysis^[1]

Cell Line:

RPMI8226 cells
Concentration:

3 μM
Incubation Time:

9 hours
Result:

The IL-6-induced interaction between TCF4 and β-catenin and the phosphorylation of TCF4 were inhibited.

Chemical Information

CAS No. 1228280-29-2
Appearance Solid
Masse moléculaire 352.41
Formule C₁₈H₁₆N₄O₂S
Color Light yellow to yellow
SMILES

O=C(C1=C(NC(C2=CC=C(C)C=C2)=O)SC(NC3=CC=CC=C3)=N1)N
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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bioRxiv

Human-chimpanzee tetraploid system defines mechanisms of species-specific neural gene regulation. [Abstract]

2025 Mar 31:2025.03.31.646367. PMID: 40236112

Solvant et solubilité

In Vitro:

DMSO : 83.33 mg/mL (236.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8376 mL

14.1880 mL

28.3760 mL

5 mM

0.5675 mL

2.8376 mL

5.6752 mL

10 mM

0.2838 mL

1.4188 mL

2.8376 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 12.5 mg/mL (35.47 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Lee Y, et al. Synergistic inhibition effect of TNIK inhibitor KY-05009 and receptor tyrosine kinase inhibitor dovitinib on IL-6-induced proliferation and Wnt signaling pathway in human multiple myeloma cells. Oncotarget. 2017 Jun 20;8(25):41091-41101. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8376 mL	14.1880 mL	28.3760 mL	70.9401 mL
	5 mM	0.5675 mL	2.8376 mL	5.6752 mL	14.1880 mL
	10 mM	0.2838 mL	1.4188 mL	2.8376 mL	7.0940 mL
	15 mM	0.1892 mL	0.9459 mL	1.8917 mL	4.7293 mL
	20 mM	0.1419 mL	0.7094 mL	1.4188 mL	3.5470 mL
	25 mM	0.1135 mL	0.5675 mL	1.1350 mL	2.8376 mL
	30 mM	0.0946 mL	0.4729 mL	0.9459 mL	2.3647 mL
	40 mM	0.0709 mL	0.3547 mL	0.7094 mL	1.7735 mL
	50 mM	0.0568 mL	0.2838 mL	0.5675 mL	1.4188 mL
	60 mM	0.0473 mL	0.2365 mL	0.4729 mL	1.1823 mL
	80 mM	0.0355 mL	0.1774 mL	0.3547 mL	0.8868 mL
	100 mM	0.0284 mL	0.1419 mL	0.2838 mL	0.7094 mL

Keywords

KY-05009

1 Cited Publications

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KY-05009

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Cytoskeleton Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Antihypertensive Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Extracellular Vesicles (EVs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) KY-05009

Voir tous les produits spécifiques à Isoform MAP4K

Voir tous les produits spécifiques à Isoform Wnt

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

KY-05009 Related Classifications

HY-124745 Related Classifications