TG003

CHF 30.00
In stock
AG-CR1-3656-M0011 mgCHF 30.00
AG-CR1-3656-M0055 mgCHF 120.00
AG-CR1-3656-M02525 mgCHF 360.00
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Product Details
Synonyms (Z)-1-(3-Ethyl-5-methoxy-2,3-dihydrobenzothiazol-2-ylidene)propan-2-one
Product Type Chemical
Properties
Formula

C13H15NO2S

MW 249.3
CAS 300801-52-9
Purity Chemicals ≥98%
Appearance Solid.
Solubility Soluble in DMSO (20mg/ml), ethanol (15mg/ml) or DMF (15mg/ml).
Identity Determined by 1H-NMR.
InChi Key BGVLELSCIHASRV-QPEQYQDCSA-N
Smiles CC(/C=C1SC2=CC=C(OC)C=C2N\1CC)=O
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Keep under inert gas.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
  • Potent, specific, reversible and ATP-competitive cell permeable inhibitor of Cdc2-like kinase (Clk) (IC50=15nM, 20nM, 200nM and >10µM 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.
Product References
  1. Manipulation of alternative splicing by a newly developed inhibitor of Clks: M. Muraki, et al.; J. Biol. Chem. 279, 24246 (2004)
  2. Alternative splicing: a new drug target of the post-genome era: M. Hagiwara; Biochim. Biophys. Acta 1754, 324 (2005) (Review)
  3. Chemical treatment enhances skipping of a mutated exon in the dystrophin gene: A. Nishida, et al.; Nat. Commun. 2, 308 (2001)
  4. 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)
  5. Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A: Y. Ogawa, et al.; Nat. Commun. 1, 86 (2010)
  6. Stress-responsive maturation of Clk1/4 pre-mRNAs promotes phosphorylation of SR splicing factor: K. Ninomiya, et al.; J. Cell Biol. 195, 27 (2011)
  7. Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II: A. Foucourt, et al.; Molecules 19, 15411 (2014)
  8. Deciphering targeting rules of splicing modulator compounds: case of TG003: M. Sakuma, et al.; BMC Mol. Biol. 16, 16 (2015)
  9. Cdc2-like kinase 2 in the hypothalamus is necessary to maintain energy homeostasis: P.G. Quaresma, et al.; Int. J. Obes. 41, 268 (2017)
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