Aurora A Inhibitor I

Catalog No.S1451

Aurora A Inhibitor I Chemical Structure

Molecular Weight(MW): 588.07

Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B.

Size Price Stock Quantity  
In DMSO USD 280 In stock
USD 120 In stock
USD 210 In stock
USD 670 In stock
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3 Customer Reviews

  • Inhibition of CDK5 by roscovitine resulted in defective neuronal migration, which was rescued by expression of GFP-Ndel1 (S251E). a, Granular neurons were treated with roscovitine. Western blotting was performed 24 h after start of culture. Aurora-A and NDEL1 displayed similar expression levels with untreated neurons, whereas the levels of phosphorylated Aurora-A and NDEL1 proteins were decreased after treatment with roscovitine. Relative intensities of the bands of Western blotting are shown at the bottom.

    J Neurosci 2012 32, 11050-11066. Aurora A Inhibitor I purchased from Selleck.

     

    Aurora-A inhibitors severely impair neuronal migration. Migration of granular neurons after treatment of Aurora-A inhibitors was examined. a, Western blotting analysis of proteins or phosphorylated proteins. Aurora-A and NDEL1 displayed similar expression levels, whereas phosphorylated Aurora-A and NDEL1 proteins were decreased during treatment with Aurora-A inhibitors. Relative intensities of the bands of Western blotting are displayed at the bottom.

    J Neurosci 2012 32, 11050-11066. Aurora A Inhibitor I purchased from Selleck.

  • Western blot analysis of Histone and p-Histone. 0-10μM Aurora inhibitor I was added.

     

     

    Dr. Zhang of Tianjin Medical University. Aurora A Inhibitor I purchased from Selleck.

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Biological Activity

Description Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B.
Features Aurora A Inhibitor I is a novel, potent, and selective inhibitor to Aurora A.
Targets
Aurora A [1]
(Cell-free assay)
3.4 nM
In vitro

Aurora A Inhibitor I is a 2,4-dianilinopyrimidine that selectively and potently inhibits Aurora A. Aurora A Inhibitor I effectively inhibits the proliferation of HCT116 and HT29 cells, with IC50 of 190 nM and 2.9 μM, respectively. The Aurora A selectivity of Aurora A Inhibitor I against Aurora B depends on a single amino acid (Thr217) of Aurora A. [1] In KCL-22 cells, Aurora A Inhibitor I (1-5 μM) increases G2/M cell fraction, induces histone H3 serine 10 phosphorylation, and suppresses mitotic Aurora A autophosphorylation on Thr288. Aurora A Inhibitor I (0.5-5 μM) also suppresses cell proliferation in KCL-22 cells, as well as BCR-ABL-negative leukemia cell lines KG-1 and HL-60. Aurora A Inhibitor I effectively induces apoptosis in KCL-22 cells at 5 μM. [2] In a recent study, Aurora A Inhibitor I is also found to inhibit cell growth of HCT116, HT29, and HeLa cells, with IC50 of 377.6 nM, 5.6 μM, and 416 nM. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 cells MlzrVJJwdGmoZYLheIlwdiCjc4PhfS=> MknkOEBl[Xm| NGe3UYtCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC0JIRigXNiYomgZ4VtdHSrdHXyJIF{e2G7LDDJR|UxRTBwMUmg{txO MYCxPVQxOjZ|Mx?=
HT-29 cells NELIOG1Rem:uaX\ldoF1cW:wIHHzd4F6 MmnzOEBl[Xm| M{XFXmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGStNlkh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IHPlcIx1cXSncjDhd5NigSxiSVO1NF0zNjlizszN MWixPVQxOjZ|Mx?=

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:[1]
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Auroras A and B Inhibition Assays:

Both Auroras A and B are assayed in ELISA format using a GST fusion (pGEX-4T) of the N-terminus of Histone H3 (aa 1−18) as substrate. Plates are coated with 2 μg/mL substrate in PBS then blocked with 1 mg/mL I-block in PBS. Kinase reactions are run for 40 min with 5 ng/mL (0.16 nM) Aurora A or 45 ng/mL (1.1 nM) Aurora B at 30 μM ATP (~ Km) in kinase buffer. Final DMSO concentration is 4%. Product is detected by incubation with antiphosphohistone H3 (Ser10) 6G3 mouse monoclonal antibody and sheep-anti-mouse HRP conjugate, followed by washing and addition of TMB substrate. After quenching with 1 M phosphoric acid, plates are read at 450 nM.
Cell Research:[1]
+ Expand
  • Cell lines: HCT116 and HT29 cells
  • Concentrations: 0.1 nM - 10 μM, dissolved in medium lacking serum and glutamine (dissolved in DMSO as stock solution)
  • Incubation Time: 72 hours
  • Method: Cells are seeded in 384-well plates on day 0 in 50 μL of complete medium and incubated overnight in a 5% CO2 atmosphere at 37 °C. On day 1, 10 μL of Aurora A Inhibitor I is added. On day 4, plates are allowed to reach room temperature, and 30 μL Cell Titer-Glo reagent is added to each well to measure total ATP levels. Plates are read after shaking 15 min at room temperature.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 118 mg/mL (200.65 mM)
Water Insoluble
Ethanol Insoluble

* 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 588.07
Formula

C31H31ClFN7O2

CAS No. 1158838-45-9
Storage powder
Synonyms N/A

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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