Hesperadin

Catalog No.S1529

Hesperadin Chemical Structure

Molecular Weight(MW): 516.65

Hesperadin potently inhibits Aurora B with IC50 of 250 nM in a cell-free assay. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.

Size Price Stock Quantity  
In DMSO USD 350 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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5 Customer Reviews

  • HeLa cells treated with nocodazole containing DMSO or Hesperadin (100 nM) for 2 h and stained with the indicated antibodies.

    Nat Commun 2011 2, 316. Hesperadin purchased from Selleck.

    Time-lapse analysis of duration of mitotic arrest in U2OScells treated with Hec1 siRNA and indicated inhibitors in cells non-induced or induced to express LAP–Mis12-Mps1Δ200. Data indicate cumulative percentage of cells (from 50 cells per treatment) that exit mitosis (scored as cell flattening) at the indicated times after NEB, and are representative of three independent experiments.

    Nat Commun 2011 2, 316 . Hesperadin purchased from Selleck.

  • Hesperadin purchased from Selleck.

    Western blot analysis of p-histone and histone. 0-10μM Hesperadin was added.

     

     

    Dr. Zhang of Tianjin Medical University. Hesperadin purchased from Selleck.

  • Hesperadin purchased from Selleck.

Purity & Quality Control

Choose Selective Aurora Kinase Inhibitors

Biological Activity

Description Hesperadin potently inhibits Aurora B with IC50 of 250 nM in a cell-free assay. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.
Targets
TbAUK1 [2]
(Cell-free assay)
Aurora B (human) [1]
(Cell-free assay)
40 nM 250 nM
In vitro

Hesperadin inhibits the ability of immunoprecipitated Aurora B to phosphorylate histone H3 with IC50 of 250 nM and markedly reduces the activity of other kinases (AMPK, Lck, MKK1, MAPKAP-K1, CHK1, and PHK) at a concentration of 1 μM. In contrast, only 20-100 nM of Hesperadin is sufficient to induce the loss of mitotic histone H3-Ser10 phosphorylation in HeLa cells. Hesperadin treatment causes defects in mitosis and cytokinesis, leading to stoppage of proliferation of HeLa cells and polyploidization, which can be specifically ascribed to the inhibition of Aurora B function during the process of chromosome attachment. Hesperadin (100 nM) quickly overrides the mitotic arrest induced by taxol or monastrol but not by nocodazole. Hesperadin and nocodazole treatment in HeLa cells abolishes kinetochore localization of BubR1 and diminishes the intensity of Bub1 at kinetochores, suggesting that Aurora B function is required for efficient kinetochore recruitment of BubR1 and Bub1, which in turn might be necessary for prolonged checkpoint signaling. [1] Hesperadin prevents the phosphorylation of recombinant trypanosome histone H3 by the T. brucei Aurora kinase-1 (TbAUK1) from pathogenic Trypanosoma brucei with IC50 of 40 nM in vitro kinase assays. Hesperadin significantly inhibits cell growth of cultured infectious bloodstream forms (BF) with IC50 of 48 nM, and only weakly inhibits cell growth of insect stage procyclic forms (PF) with IC50 of 550 nM. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 cells NHXnNHVEgXSxdH;4bYNqfHliYYPzZZk> MUS0PEBp MmPqR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVxTzJiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhXEN3ME2wMlIh|ryP NH[3VVIzPDlzMEe2Oi=>

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:[1]
+ Expand

The Aurora B kinase assay:

For the Aurora B kinase assay, HeLa cells are lysed in a buffer containing 50 mM NaCl. The whole cell extract is spun at 13,000 rpm for 20 minutes at 4 °C using a table top centrifuge. The pellet obtained from 200 mg of whole cell extract is extracted again in 15 mL lysis buffer containing 250 mM NaCl in order to obtain active Aurora B kinase from mitotic chromatin. The low speed supernatant of the latter extract is used for immunoprecipitation. Monoclonal mouse anti–AIM-1, or mouse anti-HA, is coupled to GammaBind Plus Sepharose, and beads are rotated over-end in the extract for 90 minutes at 4 °C. Beads are washed, aliquoted, and washed in kinase buffer (20 mM Tris, pH 7.5, 150 mM NaCl, 10 mM MgCl2, 1 mM DTT, 10 mM NaF). The kinase assay is performed with 10 μL beads in 20 μL kinase buffer containing 5 μg histone H3, 10 μM ATP, 2.5 μCi [γ-32P]ATP, and different concentrations of Hesperadin for 20 minutes at 37 °C. SDS sample buffer is added, and samples are boiled and resolved by SDS-PAGE. The gel is dried, and the radioactive signal is detected by PhosphorImager analysis. The data is analyzed using ImageQuant software.
Cell Research:[1]
+ Expand
  • Cell lines: HeLa cells and PtK1 cells
  • Concentrations: Final concentration ~500 nM
  • Incubation Time: 24 and 48 hours
  • Method: Cells are exposed to different concentrations of Hesperadin for 24 and 48 hours. At indicated time points, methanol-fixed cell samples are washed with PBS and subsequently stained in PI buffer (50 μg/mL propidium iodide, 10 mM Tris, pH 7.5, 5 mM MgCl2, 200 μg/mL RNase A) for 20-40 minutes at 37 °C. The DNA content is determined by flow cytometry.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 103 mg/mL (199.36 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 516.65
Formula

C29H32N4O3S

CAS No. 422513-13-1
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID