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Merck

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:
422513-13-1
Molecular Weight:
516.65
MDL number:
MFCD08064332
NACRES:
NA.77
UNSPSC Code:
51111800
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, protect from light

Key Documents

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Product Name

Hesperadin, Hesperadin primarily used in Inhibition.

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

Quality Level

100

Related Categories

Disclaimer

Toxicity: Regulatory Review (Z)

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).

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.

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..

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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