| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
(E/Z)-TG003 targets Cdc2-like kinases (Clk), particularly Clk1 and Clk4. Clk kinases are involved in the regulation of alternative splicing and other cellular processes. By inhibiting Clk1 and Clk4, the compound modulates splicing and other Clk-dependent pathways. (Z)-TG003 is a potent and ATP-competitive Clk inhibitor. It inhibits Clk1 with an IC50 of 20 nM and Clk4 with an IC50 of 15 nM.
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| ln Vitro |
In cell-free biochemical assays, (Z)-TG003 potently inhibits Clk1 and Clk4 with IC50 values of 20 nM and 15 nM, respectively. This activity demonstrates the compound's direct inhibition of Clk kinase activity. The compound is a specific and ATP-competitive inhibitor of Clk family members. It has no inhibitory effect on Clk3. The compound's selectivity can be assessed using kinase profiling assays.
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| ln Vivo |
In cell-based assays, (E/Z)-TG003 inhibits Clk1 and Clk4 activity, leading to modulation of alternative splicing and other Clk-dependent cellular processes. The compound's effects are evaluated in various cell lines. By inhibiting Clk kinases, the compound can alter the expression of splice variants and affect cell function. The compound is a benzothiazole agent.
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| Enzyme Assay |
The cell-free assay for Clk inhibition involves measuring the kinase activity of purified Clk enzymes in the presence of the compound. The assay uses a peptide substrate and ATP, and the phosphorylation of the substrate is measured using radioactivity, fluorescence, or luminescence. The IC50 values of 20 nM for Clk1 and 15 nM for Clk4 are determined from dose-response curves.
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| Cell Assay |
Cell-based assays for (E/Z)-TG003 involve culturing relevant cell lines and treating them with the compound at concentrations ranging from 0.001 to 10 μM. The compound's effects on Clk activity are assessed by measuring the phosphorylation of downstream substrates or by monitoring alternative splicing events using RT-PCR or RNA-seq. The compound's effects on cell proliferation, viability, and function are also assessed.
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| Animal Protocol |
There is no established animal experimental protocol for (E/Z)-TG003 specifically. As a Clk inhibitor, the compound could potentially be evaluated in animal models of diseases where Clk kinases play a role, such as cancer or neurological disorders. Typical studies involve administration of the compound to mice via intraperitoneal or oral routes. Pharmacodynamic endpoints include assessment of Clk inhibition and splicing modulation in tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of (E/Z)-TG003 have not been extensively reported. As a small molecule with a molecular weight of 249.33 g/mol, the compound would be expected to have moderate oral bioavailability and tissue penetration. The compound is soluble in DMSO. It is a light-sensitive solid. Further pharmacokinetic studies would be required to determine plasma half-life, clearance, and metabolic pathways.
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| Toxicity/Toxicokinetics |
(E/Z)-TG003 is intended for research use only and lacks established toxicity profiles for therapeutic applications. Standard laboratory safety precautions should be observed when handling this chemical reagent. As a Clk inhibitor, the compound may have effects on normal cellular processes. Standard toxicity studies in rodents would be required to determine the safety profile if therapeutic development is pursued.
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| References | |
| Additional Infomation |
(E/Z)-TG003 is a research-grade compound supplied for Clk kinase research. It is not an approved pharmaceutical and has no clinical trial history. The compound is a racemic mixture of (Z)-TG003 and (E)-TG003. (Z)-TG003 is a potent Clk1 and Clk4 inhibitor with IC50 values of 20 nM and 15 nM, respectively. This product is intended for research use only.
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| Molecular Formula |
C13H15NO2S
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|---|---|
| Molecular Weight |
249.33
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| Exact Mass |
237.082
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| CAS # |
300801-52-9
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| PubChem CID |
1893668
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
353.6±42.0 °C at 760 mmHg
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| Melting Point |
132-132.5ºC
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| Flash Point |
167.6±27.9 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.635
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| LogP |
1.82
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
17
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| Complexity |
329
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1/C(=C(/[H])\C(C([H])([H])[H])=O)/N(C([H])([H])C([H])([H])[H])C2C([H])=C(C([H])=C([H])C1=2)OC([H])([H])[H]
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| InChi Key |
BGVLELSCIHASRV-QPEQYQDCSA-N
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| InChi Code |
InChI=1S/C13H15NO2S/c1-4-14-11-8-10(16-3)5-6-12(11)17-13(14)7-9(2)15/h5-8H,4H2,1-3H3/b13-7-
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| Chemical Name |
(1Z)-1-(3-ethyl-5-methoxy-1,3-benzothiazol-2-ylidene)propan-2-one
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0107 mL | 20.0537 mL | 40.1075 mL | |
| 5 mM | 0.8021 mL | 4.0107 mL | 8.0215 mL | |
| 10 mM | 0.4011 mL | 2.0054 mL | 4.0107 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.
Products are for research use only; We do not sell to patients
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