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375680

Sigma-Aldrich

Hesperadin

Hesperadin primarily used in Inhibition.

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Synonym(s):
Hesperadin, Mammalian Ste20-like Kinase 4 Inhibitor, MST4 Inhibitor, Aurora Kinase Inhibitor X, AMPK Inhibitor II
Empirical Formula (Hill Notation):
C29H32N4O3S
CAS Number:
Molecular Weight:
516.65

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

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372040189410569397
Hesperadin Hesperadin primarily used in Inhibition.

375680

Hesperadin

Haspin Kinase Inhibitor, CHR-6494

372040

Haspin Kinase Inhibitor, CHR-6494

Staurosporine, Streptomyces sp. Staurosporine, CAS 62996-74-, is a cell-permeable, potent, reversible, ATP-competitive inhibitor of protein kinases (IC₅₀ = 7, 20, 1.3, 0.7, & 8.5 nM for PKA, CAMK, MLCK, PKC, & PKG, respectively).

569397

Staurosporine, Streptomyces sp.

assay

≥95% (HPLC)

assay

≥98% (HPLC)

assay

≥95% (HPLC)

assay

≥99% (HPLC)

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

−20°C

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

2-8°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

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).
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.

Packaging

Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

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.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


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