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AG-CR1-3662-M001 1 mg INQ
AG-CR1-3662-M005 5 mg INQ
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Additional Information

Product Data
Synonyms (Z)-5-(4-Methoxy-3-((trimethylsilyl)ethynyl)benzylidene)-2-thioxothiazolidin-4-one
Properties
Formula C16H17NO2S2Si
MW 347.5
CAS 1507367-37-4
Purity ≥98% (HPLC)
Appearance Light to dark yellow solid.
Solubility Soluble in DMSO (25mg/ml).
InChi Key JHFDWHHUUUMRLK-UVTDQMKNSA-N
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry. Protect from light and moisture.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
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Product Description

  • 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.

Product References

  1. Selective inhibition of the kinase DYRK1A by targeting its folding process: I. Kii, et al.; Nat. Commun. 7, 11391 (2016)
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