tcsc5664 MK-8745

MK-8745 is an aurora A kinase inhibitor with IC₅₀s of 0.6 nM.

IC50 & Target: IC50: 0.6 nM (Aurora A)^[1]

In Vitro: 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]. 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^[2].