MK-8745是极光激酶抑制剂 (aurora A)，IC₅₀ 值为0.6 nM。

MK-8745 is an aurora A kinase inhibitor with an IC 50 of 0.6 nM.

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Aurora A 0.6 nM (IC50)

MK-8745 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 MK-8745 results in the induction of p53 phosphorylation (ser15) and an increase in p53 protein expression. 1 μM of MK-8745 exposure for 24 h induces cell cycle arrest in all NHL cells, with variable degrees of G2/M arrest. Z138C cells are highly sensitive to MK-8745 (1 μ M) treatment and induces an approximate 5.5-fold increase in the G2/M phase cell population by 96 h. MK-8745 treatment inhibits phosphorylation of Aurora-A in Granta 519 and Z138C cells, while Akata and JVM2 has no effect. MK-8745 specifically inhibits Aurora-A specific function. MK-8745 treatment leads to apoptotic cell death. has not independently confirmed the accuracy of these methods. They

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[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.

In Vitro: DMSO : ≥ 100 mg/mL (231.53 mM)配制储备液