| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C18H16N4O2S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
KY-05009 competitively inhibits Traf2- and Nck-interacting kinase (TNIK) at the ATP-binding site, with a Ki of 100 nM. It pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells, reduces TNIK protein expression and the transcriptional activity of Wnt target genes, induces apoptosis in cancer cells, and exerts anti-cancer activity[1]. It is supplied as a light yellow to yellow solid (C18H16N4O2S, MW 352.41) at 99.88% purity.
Physical & Chemical Properties
| CAS Number | 1228280-29-2 |
|---|---|
| Molecular Formula | C18H16N4O2S |
| Molecular Weight | 352.41 g/mol |
| Purity | 99.88% |
| 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 |
| Target | TNIK |
| Signaling Pathway | MAPK/ERK Pathway; Stem Cell/Wnt; Apoptosis |
| Solubility | In Vitro: DMSO: 83.33 mg/mL (236.46 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
TNIK 100 nM (Ki) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 83.33 mg/mL (236.46 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (5.90 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 2
| Composition | 50% PEG300 + 50% saline |
|---|---|
| Result | 12.5 mg/mL (35.47 mM); suspension; requires sonication |
Data provided by the manufacturer.
In Vitro
KY-05009 (0.1-30 μM; 24 hours; RPMI8226 cells) treatment lowers proliferation of RPMI8226 cells dose-dependently[1]. KY-05009 (1-3 μM; 48-72 hours; RPMI8226 cells) treatment triggers caspase-dependent apoptosis in RPMI8226 cells, with dose dependence[1]. KY-05009 (3 μM; 1 hour; RPMI8226 cells) treatment reduces transcriptional activity of genes related to Wnt signaling, including TNIK, CTNNB1, TCF7, and TCF4[1]. KY-05009 (3 μM; 9 hours; RPMI8226 cells) treatment blocks TCF4 phosphorylation and the IL-6-induced interaction between TCF4 and β-catenin[1].
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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Need this compound in a format that drops straight into your assay? We can tailor formulation, chemistry, and documentation so your results stay consistent across runs and re-orders.
- Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
- Chemistry options: free base/acid vs salt forms, hydrate/solvate preference, stereoisomer control (single enantiomer or racemate), close analogs
- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
- QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
- Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity
To quote quickly, tell us: compound name + CAS/structure (SMILES or mol file), intended assay context, solvent preference, salt/stereochemistry requirements, purity/QC level, and the amount (mg–g).
Can’t find the compound you’re looking for?
Send the CAS or structure and your specs. We can help source it, suggest close equivalents, or discuss custom synthesis with the right QC documentation (RUO).
Human-chimpanzee tetraploid system defines mechanisms of species-specific neural gene regulation. bioRxiv 2025 Mar 31:2025.03.31.646367. PMID: 40236112
