375680

Hesperadin

Hesperadin primarily used in Inhibition.

• Sinonimo/i: Hesperadin, Mammalian Ste20-like Kinase 4 Inhibitor, MST4 Inhibitor, Aurora Kinase Inhibitor X, AMPK Inhibitor II
• Formula empirica (notazione di Hill): C₂₉H₃₂N₄O₃S
• Numero CAS: 422513-13-1
• Peso molecolare: 516.65
• Codice UNSPSC: 51111800
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: yellow
• Solubilità: DMSO: 50 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −20°C

Descrizione

Descrizione generale

A cell-permeable indolinone compound that interacts with both the ATP- and the adjacent hydrophobic binding pocket of Aurora B and acts as a rapid and reversible inhibitor of Aurora kinase B activity (IC₅₀ ~ 250 nM) with moderate selectivity over Cdk1/B, Cdk2/E and Cdk4/D1 (IC₅₀ = 1.2, >10 and >10 µM). Also, potently inhibits several kinases at 1 µM in a 25-kinase screening panel (100%, 100%, 96%, 88%, 87% and 84% against Lck, PHK, AMPK, MKK1, MAPKAP-K1 and Chk1, respectively). Reported to reduce histone H3-Ser¹⁰ phosphorylation, inhibit cytokinesis, promote chromosome biorientation, perturb mitosis and polyploidy in mammalian cells. Recently shown to potently inhibit MST4 kinase (IC₅₀ = 6.18 nM) in an ATP-competitive manner. Dose-dependently accelerates hypoxia-induced apoptosis and decreases survival (EC₅₀ = 10 nM in MST4 LβT2 gonadotrope cells).

A cell-permeable indolinone compound that interacts with both the ATP- and the adjacent hydrophobic binding pocket of Aurora B and acts as a rapid and reversible inhibitor of Aurora kinase B activity (IC₅₀ ~250 nM) with moderate selectivity over Cdk1/B, Cdk2/E and Cdk4/D1 (IC₅₀ = 1.2, >10 and >10 µM). Also, potently inhibits several kinases at 1 µM in a 25-kinase screening panel (100%, 100%, 96%, 88%, 87% and 84% against Lck, PHK, AMPK, MKK1, MAPKAP-K1 and Chk1, respectively). Reported to reduce histone H3-Ser¹⁰ phosphorylation, inhibit cytokinesis, promote chromosome biorientation, perturb mitosis and polyploidy in mammalian cells.

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Regulatory Review (Z)

Ricostituzione

Following reconstitution, aliquot freeze at -(20°C). Stock solutions are stable for up to 6 months at -20°C..

Altre note

Xiong, W., et al. 2016. Mol. Cancer Ther.15, In press.
Knowlton, A.L., et al. 2006. Curr. Biol.16, 1705.
Kapoor, T.M., et al. 2006. Science311, 388.
Hirota, T., et al. 2005. Nature438, 1176.
Sessa, F., et al. 2005. Mol. Cell.18, 379.
Lampson, M.A., et al. 2004. Nat. Cell Biol.6, 232.
Hauf, S., et al. 2003. J. Cell Biol.161, 281.

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 2
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable