Products & ReviewLife Sciences
MK0457
Aurora kinase pathway inhibitor; Inhibits aurora kinase A
MK0457
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MK0457 is a pan-Aurora kinase inhibitor with a preference for Aurora A (Ki = 0.6 nM) over Aurora B (Ki = 18 nM) or Aurora C (Ki = 4.6 nM; Pollard & Mortimore; Harrington et al.). It is selective in a protein kinase screen (190 kinases tested) with the closest hit being Fms-related tyrosine kinase-3 (FLT-3; Ki = 30 nM; Pollard & Mortimore; Harrington et al.).
CANCER RESEARCH
- Inhibits proliferation of a wide variety of tumor cell lines in vitro (Harrington et al.; Li et al.; Arlot-Bonnemains et al.).
- Blocks the growth of tumors in xenograft models of cancer, inhibits histone H3 phosphorylation, and increases apoptosis (Harrington et al.; Li et al.; Lin et al.).
- Disrupts bipolar spindle formation during mitosis, arresting cell cycle progression at the G2/M phase (Li et al.).
