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KY-05009 (KY05009) is a novel and potent ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor (Ki = 100 nM) with anti-cancer activity. KY-05009 inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. TNIK is involved in the interleukin-6-dependent proliferation of multiple myeloma cells and inhibition of Wnt signaling involving TNIK could be a therapeutic strategy for the treatment of interleukin-6-dependent multiple myeloma.
| ln Vitro |
RPMI8226 cells treated with KY-05009 (0.1–30 μM; 24 hours) exhibit quantitatively regulated inhibition of RPMI8226 cell growth [1]. TNIK, CTNNB1, and TCF7 activation of Wnt signaling-related genes was inhibited by KY-05009 (1-3 μM; 48-72 hours; RPMI8226 cells) treatment, whereas KY-05009 (3 μM; 1 hour; RPMI8226 cells) treatment was also inhibited. KY-05009 (3 μM; 9 hours; RPMI8226 cells) treatment prevents TCF4 phosphorylation and the IL-6-induced reaction between TCF4 and β-catenin [1]. [1]
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: RPMI8226 cell Tested Concentrations: 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited RPMI8226 cell proliferation. Apoptosis analysis [1] Cell Types: RPMI8226 Cell Tested Concentrations: 1 μM, 3 μM, 10 μM Incubation Duration: 48 hrs (hours), 72 hrs (hours) Experimental Results: Induction of fluorescent annexin V with 7-aminoactinomycin D (7- AAD) uptake binding. RT-PCR[1] Cell Types: RPMI8226 Cell Tested Concentrations: 3 μM Incubation Duration: 1 hour Experimental Results: Inhibits the transcriptional activity of Wnt signaling-related genes, including TNIK, CTNNB1, TCF7 and TCF4. Western Blot Analysis [1] Cell Types: RPMI8226 Cell Tested Concentrations: 3 μM Incubation Duration: 9 hrs (hours) Experimental Results: The interaction between TCF4 and β-catenin induced by IL-6 and the phosphorylation of TCF4 were inhibited. |
| References |
| Molecular Formula |
C18H16N4O2S
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|---|---|
| Molecular Weight |
352.41
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| Exact Mass |
352.099
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| CAS # |
1228280-29-2
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| PubChem CID |
46234348
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.728
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| LogP |
2.83
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
476
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WCEDGRTWDSHZHF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16N4O2S/c1-11-7-9-12(10-8-11)16(24)22-17-14(15(19)23)21-18(25-17)20-13-5-3-2-4-6-13/h2-10H,1H3,(H2,19,23)(H,20,21)(H,22,24)
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| Chemical Name |
2-anilino-5-[(4-methylbenzoyl)amino]-1,3-thiazole-4-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~236.46 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2838 mL | 1.4188 mL | 2.8376 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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