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AVANTI POLAR LIPIDS , CYGNUS , LARODAN , ADIPOGEN , MYBIOSOURCE , SERVA NORDMARK, BIOWORLD, EDGEBIO , PANREAC APPLICHEM
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Product description: Chemical. CAS: 1507367-37-4. Formula: C16H17NO2S2Si. MW: 347.5. Synthetic. 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 GSK3beta, 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.
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