| 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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Purity: ≥98%
TG003 (TG-003; TG 003) is a novel, potent, selective and ATP-competitive Cdc2-like kinase (Clk) inhibitor with potential anticancer activity. Its IC50 values for Clk1/2/4 inhibition are 20 nM, 200 nM, and 15 nM, respectively. TG003 exhibits no inhibitory action towards PKC, SRPK1, SRPK2, or Clk3.
| Targets |
CLK1 (IC50 = 20 nM); CLK2 (IC50 = 200 nM); CLK4 (IC50 = 15 nM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
In a reaction mixture containing 200 mM Tris-HCl (pH 7.5), 12.5 mM MgCl2, 8 mM dithiothreitol, 4 mM EGTA, 1–20 μM ATP, 1 μCi of [γ–32P]ATP, 1 μg of synthetic peptide of SF2/ASF RS domain, and 0.1–1 μg of purified kinases in a final volume of 40 μL are used to measure the kinase activity of Clks and SRPKs. Regardless of the concentration of the inhibitor, the final concentration of Me2SO is adjusted to 1%. Half of the reaction mixture is spotted on P81 phosphocellulose membrane after it is incubated for 10 minutes at 30 °C for mammalian recombinant proteins and 25 °C for Xenopus recombinant proteins. The incubation time and substrate and kinase concentrations are among the parameters of the kinase assay that are optimized to preserve linearity. For at least fifteen minutes, the membrane is cleaned with either a 5% phosphoric acid solution or a 5% trichloroacetic solution. A liquid scintillation counter is utilized to quantify the radioactivity [1].
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| Cell Assay |
Plate 2x105 HeLa or 1.5x105 COS-7 cells resuspended in 2 mL of medium on 6-well plates; in some wells, add 2 μL of 10 mM TG003 dissolved in Me2SO (final concentration at 10 mM) or 2 μL of Me2SO. Trypsinized cells are counted every 24 hours for three days, after which the density is determined. After fixing the cells in 1 mL of ice-cold 70% ethanol, they are next cleaned with PBS, incubated for 20 minutes at 37 °C in 1 mL of PBS containing 50 μg/mL propidium iodide and 1 μg/mL DNase-free RNase A, and then subjected to cell cycle analysis[1].
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| Animal Protocol |
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| References |
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| Molecular Formula |
C13H15NO2S
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| Molecular Weight |
249.33
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| Exact Mass |
249.08
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| Elemental Analysis |
C, 62.62; H, 6.06; N, 5.62; O, 12.83; S, 12.86
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| CAS # |
719277-26-6
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| Related CAS # |
300801-52-9;719277-26-6
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| Appearance |
white solid powder
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| SMILES |
CCN\1C2=C(C=CC(=C2)OC)S/C1=C\C(=O)C
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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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| Synonyms |
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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 |
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| 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) |
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| 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.
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