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Chemical Structure
Chemical Structure
Chemical Structure

TG003 [300801-52-9]

Research Use Only
AG-CR1-3656
AdipoGen Life Sciences
CAS Number300801-52-9
Product group Chemicals
Estimated Purity>98%
Molecular Weight249.3
Price on request
Packing Size
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    TG003 [300801-52-9]
  • Delivery Days Customer
    10
  • CAS Number
    300801-52-9
  • Certification
    Research Use Only
  • Estimated Purity
    >98%
  • Hazard Information
    Non-hazardous,Warning
  • Molecular Formula
    C13H15NO2S
  • Molecular Weight
    249.3
  • Scientific Description
    Chemical. CAS: 300801-52-9. Formula: C13H15NO2S. MW: 249.3. Synthetic. Potent, specific, reversible and ATP-competitive cell permeable inhibitor of Cdc2-like kinase (Clk) (IC50=15nM, 20nM, 200nM and >10microM for mClk4, mClk1, mClk2 and mClk3, respectively). Cdc2-like kinase (Clk), among a number of other kinases, phosphorylates serine/arginine-rich proteins which play a role in alternative splicing of pre-mRNA. DYRK1A and DYRK1B inhibitor. Splicing modulator compound. Regulates alternative splicing and reduces the phosphorylation of SF2/ASF1. Suppresses serine/arginine-rich protein phosphorylation and affects the regulation of alternative splicing by phosphorylation of SR protein both in vitro and in vivo. Potential drug for Duchenne muscular dystrophy. The reduction of Clk2 expression in the hypothalamus by chronic pharmacological inhibition abolished the anorexigenic effect of insulin and leptin, to increase body weight, fat mass, food intake and to decrease energy expenditure in mice. - Potent, specific, reversible and ATP-competitive cell permeable inhibitor of Cdc2-like kinase (Clk) (IC50=15nM, 20nM, 200nM and >10microM for mClk4, mClk1, mClk2 and mClk3, respectively). Cdc2-like kinase (Clk), among a number of other kinases, phosphorylates serine/arginine-rich proteins which play a role in alternative splicing of pre-mRNA. DYRK1A and DYRK1B inhibitor. Splicing modulator compound. Regulates alternative splicing and reduces the phosphorylation of SF2/ASF1. Suppresses serine/arginine-rich protein phosphorylation and affects the regulation of alternative splicing by phosphorylation of SR protein both in vitro and in vivo. Potential drug for Duchenne muscular dystrophy. The reduction of Clk2 expression in the hypothalamus by chronic pharmacological inhibition abolished the anorexigenic effect of insulin and leptin, to increase body weight, fat mass, food intake and to decrease energy expenditure in mice.
  • SMILES
    CC(/C=C1SC2=CC=C(OC)C=C2N\1CC)=O
  • Storage Instruction
    2°C to 8°C,-20°C
  • UNSPSC
    12352200

References

  • Manipulation of alternative splicing by a newly developed inhibitor of Clks: M. Muraki, et al.; J. Biol. Chem. 279, 24246 (2004)
  • Alternative splicing: a new drug target of the post-genome era: M. Hagiwara; Biochim. Biophys. Acta 1754, 324 (2005) (Review)
  • Chemical treatment enhances skipping of a mutated exon in the dystrophin gene: A. Nishida, et al.; Nat. Commun. 2, 308 (2001)
  • Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk): B.T. Mott, et al.; Bioorg. Med. Chem. Lett. 19, 6700 (2009)
  • Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A: Y. Ogawa, et al.; Nat. Commun. 1, 86 (2010)
  • Stress-responsive maturation of Clk1/4 pre-mRNAs promotes phosphorylation of SR splicing factor: K. Ninomiya, et al.; J. Cell Biol. 195, 27 (2011)
  • Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II: A. Foucourt, et al.; Molecules 19, 15411 (2014)
  • Deciphering targeting rules of splicing modulator compounds: case of TG003: M. Sakuma, et al.; BMC Mol. Biol. 16, 16 (2015)
  • Cdc2-like kinase 2 in the hypothalamus is necessary to maintain energy homeostasis: P.G. Quaresma, et al.; Int. J. Obes. 41, 268 (2017)