品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
light yellow to dark yellow
溶解度
DMSO: 25 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
C[Si](C)(C)C#CC1=C(OC)C=CC(/C=C2SC(NC\2=O)=S)=C1
生化／生理作用
FINDY is a 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. Unlike INDY and other ATP-competitive DYRK inhibitors, FINDY is ineffective against the kinase activity of DYRK1A, DYRK1B, DYRK2, or DYRK3 (IC50 >10 μM) and inhibits only five kinases (GSK3β, MARK4, PIM1, PIM3, PLK3) by over 75% at 10 μM among a panel of 271 other kinases. FINDY (2.5 μM) is shown to selectively rescue the developmental defect of Xenopus embryos induced by the overexpression of DYRK1A, but not DYRK1B, while INDY prodrug (2.5 μM) treatment indiscriminately prevents defect caused by both DYRK1A and DYRK1B expression.
FINDY is a structural analog of RD0392, a canonical ATP-competitive inhibitor of mature dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A).
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Koji Umezawa et al.
Molecules (Basel, Switzerland), 26(3) (2021-01-31)
Drug discovery using small molecule inhibitors is reaching a stalemate due to low selectivity, adverse off-target effects and inevitable failures in clinical trials. Conventional chemical screening methods may miss potent small molecules because of their use of simple but outdated
Isao Kii et al.
Nature communications, 7, 11391-11391 (2016-04-23)
Autophosphorylation of amino-acid residues is part of the folding process of various protein kinases. Conventional chemical screening of mature kinases has missed inhibitors that selectively interfere with the folding process. Here we report a cell-based assay that evaluates inhibition of
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