95 CHF CHF 95.00
AG-CR1-3665-M0055 mgCHF 95.00
|Purity Chemicals||≥98% (HPLC)|
|Appearance||White to off-white solid.|
|Solubility||Soluble in DMSO (10mg/ml).|
|Identity||Determined by 1H-NMR.|
|Shipping and Handling|
|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.|
|Product Specification Sheet|
- 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.
- Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A: Y. Ogawa, et al.; Nat. Commun. 1, 86 (2010)
- Inhibition of DYRK1A destabilizes EGFR and reduces EGFR-dependent glioblastoma growth: N. Pozo, et al.; J. Clin. Invest. 123, 2475 (2013)
- 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)
- Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases: M.F. Lindberg, et al.; J. Med. Chem. ahead of print (2023)