SML1733
FINDY
≥98% (HPLC)
Sinónimos:
(5Z)-5-[[4-Methoxy-3-[2-(trimethylsilyl)ethynyl]phenyl]methylene]-2-thioxo-4-thiazolidinone, (Z)-5-(4-Methoxy-3-((trimethylsilyl)ethynyl)benzylidene)-2-thioxothiazolidin-4-one
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Fórmula empírica (notación de Hill):
C16H17NO2S2Si
Número CAS:
Peso molecular:
347.53
UNSPSC Code:
12352200
NACRES:
NA.77
Servicio técnico
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Permítanos ayudarleQuality Level
assay
≥98% (HPLC)
form
powder
color
light yellow to dark yellow
solubility
DMSO: 25 mg/mL, clear
storage temp.
2-8°C
SMILES string
C[Si](C)(C)C#CC1=C(OC)C=CC(/C=C2SC(NC\2=O)=S)=C1
InChI
1S/C16H17NO2S2Si/c1-19-13-6-5-11(9-12(13)7-8-22(2,3)4)10-14-15(18)17-16(20)21-14/h5-6,9-10H,1-4H3,(H,17,18,20)/b14-10-
InChI key
JHFDWHHUUUMRLK-UVTDQMKNSA-N
Biochem/physiol Actions
A thioxothiazolidinone that specifically targets newly synthesized cellular DYRK1A, but not DYRK1B or DYRK2, for proteasomal degradation.
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).
Clase de almacenamiento
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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