375680

Hesperadin

Hesperadin primarily used in Inhibition.

• 別名: Hesperadin, Mammalian Ste20-like Kinase 4 Inhibitor, MST4 Inhibitor, Aurora Kinase Inhibitor X, AMPK Inhibitor II
• 実験式（ヒル表記法）: C₂₉H₃₂N₄O₃S
• CAS番号: 422513-13-1
• 分子量: 516.65
• UNSPSCコード: 51111800
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: yellow
• 溶解性: DMSO: 50 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C

詳細

詳細

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.

包装

Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

再構成

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

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 2
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable