2. MAPK/ERK Pathway Stem Cell/Wnt Apoptosis
  3. MAP4K Wnt Apoptosis
  4. KY-05009

KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki 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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KY-05009 Chemical Structure

KY-05009 Chemical Structure

CAS No. : 1228280-29-2

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

KY-05009 Related Antibodies

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MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

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Description

KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki 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[1].

IC50 & Target[1]

TNIK

100 nM (Ki)

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.

KY-05009 Related Antibodies

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.
Molecular Weight

352.41

Formula

C18H16N4O2S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8376 mL 14.1880 mL 28.3760 mL
5 mM 0.5675 mL 2.8376 mL 5.6752 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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KY-05009 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KY-050091228280-29-2KY05009KY 05009MAP4KWntApoptosisMAPK Kinase Kinase KinaseTNIKIL-6plasma-cellssmyelomaanti-proliferativecaspase-dependentapoptosisanti-canceraminothiazoleInhibitorinhibitorinhibit

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