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375680 Hesperadin - CAS 422513-13-1 - Calbiochem

375680
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₉H₃₂N₄O₃S

Products

Catalogue NumberPackaging Qty/Pack
375680-5MG Glass bottle 5 mg
Description
OverviewA 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).
Catalogue Number375680
Brand Family Calbiochem®
SynonymsMammalian Ste20-like Kinase 4 Inhibitor, MST4 Inhibitor, Aurora Kinase Inhibitor X, AMPK Inhibitor II
References
ReferencesXiong, 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. Science 311, 388.
Hirota, T., et al. 2005. Nature 438, 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.
Product Information
CAS number422513-13-1
FormYellow solid
Hill FormulaC₂₉H₃₂N₄O₃S
Chemical formulaC₂₉H₃₂N₄O₃S
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥95% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Regulatory Review
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot freeze at -(20°C). Stock solutions are stable for up to 6 months at -20°C..
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

Hesperadin - CAS 422513-13-1 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Hesperadin - CAS 422513-13-1 - Calbiochem Certificates of Analysis

TitleLot Number
375680

References

Reference overview
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. Science 311, 388.
Hirota, T., et al. 2005. Nature 438, 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.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision31-August-2011 RFH
SynonymsMammalian Ste20-like Kinase 4 Inhibitor, MST4 Inhibitor, Aurora Kinase Inhibitor X, AMPK Inhibitor II
DescriptionA 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.
FormYellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number422513-13-1
Chemical formulaC₂₉H₃₂N₄O₃S
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (50 mg/ml)
Storage -20°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot freeze at -(20°C). Stock solutions are stable for up to 6 months at -20°C..
Toxicity Regulatory Review
ReferencesXiong, 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. Science 311, 388.
Hirota, T., et al. 2005. Nature 438, 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.