MK-8745

"目录号: HY-13819

Cell Cycle/DNA DamageEpigenetics-

MK-8745是一个强的，有选择性的 Aurora A抑制剂，IC50是0.6 nM.

Aurora Kinase

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生物活性

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.target:  Aurora A, Aurora BIC50: 0.6 nM [1]MK-8745, a novel Aurora-A specifi c inhibitor, 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[2]. MK8745 induced apoptotic cell death in a p53-dependent manner. Exposure of p53 wild-type cells to MK8745 resulted in the induction of p53 phosphorylation (ser15) and an increase in p53 protein expression.[1] MK-8745 can aff ect downstream targets of Aurora-A and induce apoptotic cell death.[2]

References

[1].Jayasree S Nair et al. The induction of polyploidy or apoptosis by the Aurora A kinase inhibitor MK8745 is p53-dependent.

[2].Aparajita Chowdhury et al. A novel Aurora kinase A inhibitor MK-8745 predicts  TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines.  Leuk Lymphoma, 2012 Mar, 53(3):462-71.