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Submit ReviewTG 003 is a potent, ATP-competitive inhibitor of Clk-family kinases (IC50 values are 15, 20 and 200 nM for mClk4, 1 and 2 respectively and >10 μM for mClk3). Also inhibits DYRK1A/B (IC50 values are 24 and 34 nM respectively). Suppresses serine/arginine-rich protein phosphorylation; affects the regulation of alternative splicing by phosphorylation of SR protein both in vitro and in vivo.
TG 003 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 249.33 |
Formula | C13H15NO2S |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 719277-26-6 |
PubChem ID | 647991 |
InChI Key | BGVLELSCIHASRV-UHFFFAOYSA-N |
Smiles | O=C(C)/C=C1SC2=CC=C(OC)C=C2N\1CC |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 24.93 | 100 | |
ethanol | 18.7 | 75 |
The following data is based on the product molecular weight 249.33. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 4.01 mL | 20.05 mL | 40.11 mL |
5 mM | 0.8 mL | 4.01 mL | 8.02 mL |
10 mM | 0.4 mL | 2.01 mL | 4.01 mL |
50 mM | 0.08 mL | 0.4 mL | 0.8 mL |
References are publications that support the biological activity of the product.
Muraki et al (2004) Manipulation of alternative splicing by a newly developed inhibitor of Clks. J.Biol.Chem. 279 24246 PMID: 15010457
Foucourt et al (2014) Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II. Molecules 19 15411 PMID: 25264830
If you know of a relevant reference for TG 003, please let us know.
Keywords: TG 003, TG 003 supplier, TG003, ATP-competitive, Cdc2-like, inhibitors, inhibits, Clk, Clk-family, kinases, DYRK1A, DYRK1B, DYRK1A/B, CLK, (Cdc2-like, kinases), DYRK, 4336, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for TG 003 include:
Lucas et al (2018) Kinase-controlled phase transition of membraneless organelles in mitosis. Nature 559 211-216 PMID: 29973724
Do you know of a great paper that uses TG 003 from Tocris? Please let us know.
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