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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[4] Maki Sakuma, et al. Deciphering targeting rules of splicing modulator compounds: case of TG003
Related CDK Products |
---|
PF-07224826
PF-07224826 is a CDK2/4/6 inhibitor. |
INCB123667
INCB123667 is a CDK2 inhibitor. |
Senexin B
Senexin B is a potent, orally active CDK8/19 inhibitor with Kd values of 140 nM and 80 nM for CDK8 and CDK19, respectively. |
Q901
Q901 is a CDK7 inhibitor for tumor-related studies. |
NUV-422
NUV-422 is a CDK2/4/6 inhibitor that can be used in studies related to malignant gliomas. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.