INDY

CHF 90.00
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AG-CR1-3665-M0055 mgCHF 90.00
AG-CR1-3665-M02525 mgCHF 360.00
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Product Details
Synonyms (1Z)-1-(3-Ethyl-5-hydroxy-2(3H)-benzothiazolylidene)-2-propanone
Product Type Chemical
Properties
Formula

C12H13NO2S

MW 235.3
CAS 1169755-45-6
Purity Chemicals ≥98% (HPLC)
Appearance White to off-white solid.
Solubility Soluble in DMSO (10mg/ml).
Identity Determined by 1H-NMR.
InChi Key GCSZJMUFYOAHFY-SDQBBNPISA-N
Smiles OC1=CC=C(S/C(N2CC)=C\C(C)=O)C2=C1
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
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 and selective ATP-competitive DYRK1A and DYRK1B inhibitor (IC50=240nM and 230nM respectively). Binds at the ATP-binding cleft of the enzyme.
  • Inhibits also DYRK2, DYRK3, CLK1, CLK4, casein kinase 1 (CSNK1D) and PIM1 (>90% inhibition at the same concentration).
  • Reverses aberrant tau-phosphorylation and rescues repressed calcineurin/NFAT signaling.
  • Impairs the self-renewal capacity of neural stem cells and glioblastoma tumor-initiating cells.
  • Shown to induce regeneration and expansion of rat and adult human β-cells in vivo or ex vivo.
Product References
  1. Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A: Y. Ogawa, et al.; Nat. Commun. 1, 86 (2010)
  2. Inhibition of DYRK1A destabilizes EGFR and reduces EGFR-dependent glioblastoma growth: N. Pozo, et al.; J. Clin. Invest. 123, 2475 (2013)
  3. A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication: P. Wang, et al.; Nat. Med. 21, 383 (2015)
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