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TG003 is a potent and ATP-competitive Cdc2-like kinase (Clk) inhibitor with IC50 of 20 nM, 200 nM, and 15 nM for Clk1, Clk2, and Clk4, respectively. No inhibitory effect on Clk3, SRPK1, SRPK2, or PKC.
| Cell Experiment | |
|---|---|
| Cell lines | HeLa cells and COS-7 cells |
| Preparation method | 2 × 105 HeLa cells or 1.5 × 105 COS-7 cells resuspended in 2 mL of medium are plated on 6-well dishes, and 2 μL of 10 mM TG003 dissolved in Me2SO (final concentration at 10 μM), or 2 μL of Me2SO, is added to some wells. Cells are trypsinized, and count the density every 24 h for 3 days. Then fixed the cells with 1 mL of ice-cold 70% ethanol, washed with PBS, incubated in 1 ml of PBS which is containing 1 μg/mL DNase-free RNase A and 50 μg/mL propidium iodide for 20 min at 37 °C, and proceeded to cell cycle analysis by FACSCalibur |
| Concentrations | ~10 μM |
| Incubation time | 3 days |
| Animal Experiment | |
|---|---|
| Animal models | Xenopus laevis embryos |
| Formulation | DMSO |
| Dosages | ~10 μM |
| Administration | |
| Molecular Weight | 249.33 |
| Formula | C13H15NO2S |
| CAS Number | 300801-52-9 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[4] Maki Sakuma, et al. Deciphering targeting rules of splicing modulator compounds: case of TG003
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