| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H12F3N3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
TA-01 is a potent inhibitor of CK1 and p38 MAPK, with IC50 values of 6.4 nM, 6.8 nM and 6.7 nM against CK1ε, CK1δ and p38 MAPK, respectively. It functions as a cardiogenic inhibitor. It is supplied as a white to off-white solid (C20H12F3N3, MW 351.32) at 99.29% purity.
Physical & Chemical Properties
| CAS Number | 1784751-18-3 |
|---|---|
| Molecular Formula | C20H12F3N3 |
| Molecular Weight | 351.32 g/mol |
| Purity | 99.29% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | FC(C=C1)=CC=C1C2=C(C3=CC=NC=C3)NC(C4=C(F)C=CC=C4F)=N2 |
| Target | CK1δ, p38 MAP kinase |
| Signaling Pathway | Cell Cycle/DNA Damage; Stem Cell/Wnt; MAPK/ERK Pathway; Autophagy |
| Solubility | In Vitro: DMSO: 50 mg/mL (142.32 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]
|
CK1δ 6.8 nM (IC50) |
p38 MAP kinase 6.7 nM (IC50) |
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 | 50 mg/mL (142.32 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 | ≥ 2.5 mg/mL (7.12 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 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. |
Protocol 2
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (7.12 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
TA-01 is a potent inhibitor of CK1 and p38 MAPK, with IC50 values of 6.4 nM for CK1ε, 6.8 nM for CK1δ and 6.7 nM for p38 MAPK. At 5 μM, TA-01 shows no cytotoxicity and completely inhibits cardiogenesis, whereas lower concentrations induce cardiogenesis[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Kinase Assay[1]
Dissolve the compounds (TA-01) in DMSO and test at 10 μM against a panel of 97 kinases related to stem cell differentiation and cell signaling pathways. Perform kinome profiling through a kinase profiling service[1].
Cell Assay[1]
Harvest HES-3, H7 and IPS cells and seed them as EBs at 1.1 × 106 cells/mL in ultra-low attachment 12-well plates containing bSFS medium (DMEM with 2 mM l-glutamine, 0.182 mM sodium pyruvate and 1% non-essential amino acids, along with 0.1 mM β-mercaptoethanol and 5.6 mg/L transferrin, plus Bovine Serum Albumin (0.25% w/vol), Hysoy (0.25% w/vol) and 20 μg/L sodium selenite). Incubate at 37°C and 5% CO2 to allow EB formation. Refresh the medium after 1 day, then every 2-3 days. From day 1 or day 4 until day 8, stimulate the cells with the respective compounds (TA-01), dissolved in DMSO at 1 μL DMSO/mL of media. Apply CHIR99021 for the first 24 h only[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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