1. Apoptosis Epigenetics Cell Cycle/DNA Damage
  2. Apoptosis Aurora Kinase
  3. Aurora A inhibitor 2

Aurora A inhibitor 2 (Compound 16h) is a potent Aurora A kinase inhibitor with an IC50 of 21.94 nM. Aurora A inhibitor 2 induces caspase-dependent apoptosis in MDA-MB-231 cells.

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Aurora A inhibitor 2 Chemical Structure

Aurora A inhibitor 2 Chemical Structure

CAS No. : 2412144-74-0

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Description

Aurora A inhibitor 2 (Compound 16h) is a potent Aurora A kinase inhibitor with an IC50 of 21.94 nM. Aurora A inhibitor 2 induces caspase-dependent apoptosis in MDA-MB-231 cells[1].

IC50 & Target

Aurora A

21.94 nM (IC50)

Aurora B

273.18 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 IC50
0.38 μM
Compound: 16h
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 32058239]
PC-3 IC50
1.09 μM
Compound: 16h
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 32058239]
SH-SY5Y IC50
0.77 μM
Compound: 16h
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 32058239]
In Vitro

Aurora A inhibitor 2 (Compound 16h) (0-20 µM, 48 h) shows potent antiproliferative activity against various human cancer cells, and inhibits colony formation[1].
Aurora A inhibitor 2 (0-4 µM, 24 h) inhibits the expression of phosphorylation of Aurora A and Histone H3 in a dose-dependent manner, and induces G2/M cell cycle arrest [1].
Aurora A inhibitor 2 (0-4 µM, 48 h) induces obvious apoptosis in MDA-MB-231 cells in a concentration-dependent manner[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: Breast cancer MDA-MB231, prostate cancer PC3, and neuroblastoma SH-SY5Y cells
Concentration: 0-20 µM
Incubation Time: 48 h
Result: Displayed potent antiproliferative activity with IC50 values of 0.38 ± 0.08, 1.09 ± 0.24, and 0.77 ± 0.12 µM against MDA-MB-231, PC3, and SH-SY5Y cells.

Western Blot Analysis[1]

Cell Line: MDAMB-231
Concentration: 1, 2, and 4 µM
Incubation Time: 24 h
Result: A dose-dependent and significant reduction in the phosphorylation of Aurora A and Histone H3 was observed. Significantly increased the levels of cleaved caspase 3/9 and cleaved-PARP.

Cell Cycle Analysis[1]

Cell Line: MDAMB-231
Concentration: 1, 2, and 4 µM
Incubation Time: 24 h
Result: Dose-dependently increased the and population of cells in the G2/M phase.

Apoptosis Analysis[1]

Cell Line: MDAMB-231
Concentration: 1, 2, and 4 µM
Incubation Time: 48 h
Result: Induced obvious apoptosis in a concentration-dependent manner.
Molecular Weight

446.50

Formula

C24H26N6O3

CAS No.
SMILES

CCC(NC1=NC2=CC=C(C3=CC4=C(N=CN(CCN5CCOCC5)C4=O)C=C3)C=C2N1)=O

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
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Aurora A inhibitor 2
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HY-146037
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