405273

INDY

• Sinonimo/i: INDY, (1Z)-1-(3-ethyl-5-hydroxy-2(3H)-benzothiazoylidene)-2-propanone, Dyrk/Clk Dual Inhibitor
• Formula empirica (notazione di Hill): C₁₂H₁₃NO₂S
• Numero CAS: 1169755-45-6
• Peso molecolare: 235.30
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Saggio: ≥98% (HPLC)
• Livello qualitativo: 100
• Forma fisica: powder
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: off-white
• Solubilità: DMSO: 50 mg/mL
• Condizioni di spedizione: wet ice
• Temperatura di conservazione: −20°C

Descrizione

Descrizione generale

A benzothiazole compound that acts as an ATP competitive Dyrk inhibitor (IC₅₀ = 0.24 µM and 0.23 µM for Dyrk1A and Dyrk1B, respectively), and displays >90% inhibition on DYRK2, DYRK3, CLK1, CLK4, casein kinase 1 (CSNK1D), and PIM1 among a panel of 66 kinases, in an in vitro screening assay. Unlike harmine, another potent Dyrk inhibitor, this compound does not affect MAOA activity. It is shown to decrease substrate phosphorylation of tau-protein at Thr212 in COS7 cells, dose-dependently, from 3 µM to 30 µM and ameliorates the inhibitory effect of Dyrk1A on NFAT response element mediated calcineurin/NFAT signaling in HEK293 cells. In addition, its prodrug, proINDY is shown to effectively reverse developmental defects associated with Dyrk1A overexpression in a Xenopus embryo model at 2.5 µM in vivo, without apparent toxicity.

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Altre note

Ogawa, Y., et al. 2010. Nat Commun1, 1.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable