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MK-8745

Name: MK-8745
Brand: Selleck Chemicals
SKU: S7065
Rating: 5 (0 reviews)

Catalog No.S7065

For research use only.

MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6 nM, more than 450-fold selectivity for Aurora A over Aurora B.

CAS No. 885325-71-3

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Aurora Kinase Signaling Pathway Map

Biological Activity

Description

MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6 nM, more than 450-fold selectivity for Aurora A over Aurora B.

Targets

Aurora A ^[1]

0.6 nM

In vitro

MK-8745 leads to cell cycle arrest at the G2/M phase with accumulation of tetraploid nuclei followed by cell death in non-Hodgkin lymphoma (NHL) cell lines. Treatment with MK-8745 induces p21(waf1/cip1) and CycB1, indicating cell cycle arrest and an increase in the G2/M phase cell population. Following MK-8745 treatment, Aurora-A substrates (TACC3, Eg5 and TPX2) are rapidly degraded following the reduction of phospho-Aurora-A. ^[1] MK8745 induces apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages. Exposure of p53 wild-type cells to MK8745 results in the induction of p53 phosphorylation (ser15) and an increase in p53 protein expression. p53-dependent apoptosis by MK8745 is further confirmed in HCT 116 p53(-/-) cells transfected with wild-type p53. ^[2]

Protocol (from reference)

References

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	431.91
Formula	C₂₀ H₁₉ Cl F N₅ O S
CAS No.	885325-71-3
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1CN(CCN1CC2=NC(=CC=C2)NC3=NC=CS3)C(=O)C4=C(C(=CC=C4)Cl)F

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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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