65 CHF CHF 65.00
AG-CR1-3662-M0011 mgCHF 65.00
AG-CR1-3662-M0055 mgCHF 260.00
|Purity Chemicals||≥98% (HPLC)|
|Appearance||Light to dark yellow solid.|
|Solubility||Soluble in DMSO (25mg/ml).|
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
Keep cool and dry.
Protect from light and moisture.
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
- Suppressor of DYKR1A intramolecular Ser97 autophosphorylation. Cell permeable thioxothiazolidinone derivative that specifically targets newly synthesized cellular DYRK1A, but not DYRK1B or DYRK2, for proteasomal degradation by suppressing DYKR1A intramolecular Ser97 autophosphorylation, a necessary event for folding/maturation of newly translated DYRK1A.
- Highly selective inhibitor for DYKR1A over other DYRK family members. Unlike INDY and other ATP-competitive DYRK inhibitors, ineffective against the kinase activity of DYRK1A, DYRK1B, DYRK2 or DYRK3 (IC50>10μM). Inhibits only GSK3β, MARK4, PIM1, PIM3, PLK3 by over 75% at 10μM among a panel of 271 kinases.
- Selectively rescues the developmental defect of Xenopus embryos induced by the overexpression of DYRK1A, but not DYRK1B.
- Selective inhibition of the kinase DYRK1A by targeting its folding process: I. Kii, et al.; Nat. Commun. 7, 11391 (2016)
- 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)