2. Cell Cycle/DNA Damage Epigenetics
  3. Aurora Kinase
  4. AurkA allosteric-IN-1

AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor (IC50: 6.50 μM) that inhibits the catalytic activity and non-catalytic functions of Aurora A. Aurora A regulates the assembly of the bipolar mitotic spindle and the fidelity of chromosome segregation during mitosis and has non-catalytic functions. AurkA allosteric-IN-1 blocks the interaction of AurkA with the activator TPX2 by binding to the Y pocket of AurkA.

For research use only. We do not sell to patients.

AurkA allosteric-IN-1 Chemical Structure

AurkA allosteric-IN-1 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

AurkA allosteric-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All Aurora Kinase Isoform Specific Products:

View All Isoforms
Aurora Kinase Aurora A Aurora B Aurora C

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor (IC50: 6.50 μM) that inhibits the catalytic activity and non-catalytic functions of Aurora A. Aurora A regulates the assembly of the bipolar mitotic spindle and the fidelity of chromosome segregation during mitosis and has non-catalytic functions. AurkA allosteric-IN-1 blocks the interaction of AurkA with the activator TPX2 by binding to the Y pocket of AurkA[1].

IC50 & Target

Aurora A

6.5 μM (IC50, [1])

In Vitro

AurkA allosteric-IN-1 (100 μM; 48 h) differentially induces cell cycle arrest in different cell types, including lung cancer cell lines and rectal cancer cell lines[1].
AurkA allosteric-IN- 1 (20 μM; 48 h) can downregulate the levels of phospho-histone H3 in cancer cells[1].
AurkA allosteric-IN-1 (25-400 μM; 48 h) exhibits significant anti-cell proliferation on HeLa cells activity, and has a synergistic effect with PHA-767491 (HY-13461), further amplifying its anti-proliferative activity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AurkA allosteric-IN-1 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: HeLa and Panc-1 cells, Lung cancer cell lines (A549 and H358), and colon cancer cell lines (HT29 and HCT116)
Concentration: 20 μM
Incubation Time: 12, 24, and 48 h
Result: Arrested cell cycle at G1/S transition in lung cancer cell lines (A549 and H358), and arrested cell cycle at G2/M in colon cancer cell lines (HT29 and HCT116).
Almostly unaffected HeLa and Panc-1 cells.

Western Blot Analysis[1]

Cell Line: HT29 and HCT116 cells
Concentration: 20 μM
Incubation Time: 48 h
Result: Sharply downregulated the level of phospho-histone H3 (Ser10).

Cell Cytotoxicity Assay[1]

Cell Line: HeLa cells
Concentration: 25 μM, 50 μM, 100 μM, 200 μM, and 400 μM
Incubation Time: 12, 24, and 48 h; with or without PHA-767491
Result: With PHA-767491 sensitized HeLa cells, significantly augmented anti-proliferative activity GI50: 71.7 μM to GI50: 14.0 μM by co-treatment of 1.5 μM PHA-76749.
Molecular Weight

332.35

Formula

C20H16N2O3
SMILES

O=C(C1=CC=CC(C2=CC=NC=C2)=C1)NCC3=CC4=C(OCO4)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

AurkA allosteric-IN-1 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AurkA allosteric-IN-1Aurora KinaseAllosteric inhibitorAurkAAurora kinaseTPX2Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
AurkA allosteric-IN-1
Cat. No.:
HY-158038
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (0 KB) Français - FR (0 KB) Deutsch - DE (0 KB) Norwegian - NO (0 KB) Español - ES (0 KB) Swedish - SV (0 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.