| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
TA-01 targets CK1δ, CK1ε, and p38 MAPK with high potency. It is a dual inhibitor that simultaneously inhibits these kinases, making it useful for studying their roles in various cellular processes.
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| ln Vitro |
TA-01 is a strong inhibitor of p38 MAPK and CK1, having IC50 values for CK1ε, CK1δ, and p38 MAPK of 6.4 nM, 6.8 nM, and 6.7 nM, respectively. Although it is neither cytotoxic and totally prevents cardiogenesis, TA-01 (5 μM) does cause cardiogenesis at lower doses [1].
In vitro, TA-01 acts as a potent inducer of cardiomyocyte differentiation from human embryonic stem cells following mesoderm induction. It inhibits TGF-β-induced epithelial-to-mesenchymal transition (EMT) in cancer cells. It also inhibits cardiac development when administered at 5 µM. |
| ln Vivo |
In vivo, TA-01 reduces fibrosis in animal models and has potential therapeutic applications in cancer and fibrotic diseases. Its ability to inhibit EMT makes it a promising anti-metastatic agent.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for TA-01 typically involve evaluating its inhibitory activity against purified CK1 or p38 MAPK kinases using radiometric or fluorescence-based assays. IC50 values are determined by measuring residual kinase activity after incubation with varying concentrations of the compound.
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| Cell Assay |
For in vitro cell-based assays, TA-01 is dissolved in DMSO and applied to cultured cells such as embryonic stem cells or cancer cells at concentrations ranging from 1 nM to 10 µM. Effects on differentiation, EMT, or cell viability are assessed after 24-72 hours of treatment.
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| Animal Protocol |
In vivo animal studies commonly use mouse models of fibrosis or cancer. TA-01 is administered orally or intraperitoneally at doses ranging from 1-50 mg/kg. Efficacy is evaluated by measuring fibrosis markers, tumor growth, and metastasis.
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| ADME/Pharmacokinetics |
TA-01 has a molecular weight of approximately 400-500 g/mol. It is soluble in DMSO and is typically stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
TA-01 has a favorable safety profile with no significant toxicity reported at research doses. Its selectivity for CK1 and p38 MAPK minimizes off-target effects.
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| References | |
| Additional Infomation |
TA-01 is a valuable tool compound for studying CK1 and p38 MAPK signaling in stem cell biology, cancer, and fibrosis. It is used to induce cardiomyocyte differentiation from human embryonic stem cells. Its potential therapeutic applications include cancer and fibrotic diseases.
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| Molecular Formula |
C20H12F3N3
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|---|---|
| Molecular Weight |
351.3246
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| Exact Mass |
351.098
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| CAS # |
1784751-18-3
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| Related CAS # |
TA-02;1784751-19-4
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| PubChem CID |
91691129
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
511.1±50.0 °C at 760 mmHg
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| Flash Point |
262.9±30.1 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.606
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| LogP |
4.66
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
442
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=C(C(=C1)F)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F)F
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| InChi Key |
TWPJJJZCYVFUOA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H12F3N3/c21-14-6-4-12(5-7-14)18-19(13-8-10-24-11-9-13)26-20(25-18)17-15(22)2-1-3-16(17)23/h1-11H,(H,25,26)
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| Chemical Name |
4-[2-(2,6-difluorophenyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]pyridine
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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 : ~50 mg/mL (~142.32 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8464 mL | 14.2320 mL | 28.4641 mL | |
| 5 mM | 0.5693 mL | 2.8464 mL | 5.6928 mL | |
| 10 mM | 0.2846 mL | 1.4232 mL | 2.8464 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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