375680
Hesperadin
≥95% (HPLC), MST4 kinase inhibitor, solid
Synonym(s):
Hesperadin, Mammalian Ste20-like Kinase 4 Inhibitor, MST4 Inhibitor, Aurora Kinase Inhibitor X, AMPK Inhibitor II
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About This Item
Empirical Formula (Hill Notation):
C29H32N4O3S
CAS Number:
Molecular Weight:
516.65
MDL number:
NACRES:
NA.77
UNSPSC Code:
51111800
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
Product Name
Hesperadin, Hesperadin primarily used in Inhibition.
Quality Level
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
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).
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot freeze at -(20°C). Stock solutions are stable for up to 6 months at -20°C..
Other Notes
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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Global Trade Item Number
| SKU | GTIN |
|---|---|
| 375680-5MG | 04055977212945 |