TG 003

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Description: Potent inhibitor of Clk-family kinases; also inhibits DYRK1A/B
Chemical Name: (1Z)-1-(3-Ethyl-5-methoxy-2(3H)-benzothiazolylidene)-2-propanone
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews

Biological Activity for TG 003

TG 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.

Compound Libraries for TG 003

TG 003 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for TG 003

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.

Solubility Data for TG 003

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 24.93 100
ethanol 18.7 75

Preparing Stock Solutions for TG 003

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for TG 003

Certificate of Analysis / Product Datasheet
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References for TG 003

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.

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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

1 Citation for TG 003

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


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