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Hesperadin

Name: Hesperadin
Brand: MM

≥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

Storage condition:

OK to freeze, protect from light

Pricing and availability is not currently available.

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Properties

Product Name

Hesperadin, Hesperadin primarily used in Inhibition.

Quality Segment

100

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

Description

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.

Legal Information

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

Disclaimer

Toxicity: Regulatory Review (Z)

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This Item	372040	189410	569397
Sigma-Aldrich 375680 Hesperadin	Sigma-Aldrich 372040 Haspin Kinase Inhibitor, CHR-6494	Sigma-Aldrich 189410 Aurora Kinase Inhibitor VI, ZM447439	Sigma-Aldrich 569397 Staurosporine, Streptomyces sp.
description Hesperadin primarily used in Inhibition.	description -	description The Aurora Kinase Inhibitor VI, ZM447439, also referenced under CAS 331771-20-1, controls the biological activity of Aurora Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.	description 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).
form solid	form solid	form solid	form solid
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
solubility DMSO: 50 mg/mL	solubility DMSO: 25 mg/mL	solubility DMSO: 50 mg/mL	solubility DMSO: 5 mg/mL

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

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