PHA 767491 is a potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication. PHA 767491 hydrochloride induces apoptosis in a p53-independent manner, and inhibits cell proliferation in a variety of human cell lines (IC50 ~ 0.86 - 5.87 μM). The compound also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK-2) (IC50 = 171 nM).
Anderson et al (2007) Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2) J.Med.Chem. 50 2647. Jackson (2008) Stopping replication, at the beginning. Nature Chem.Biol. 4 331. Montagnoli et al (2008) A cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumour activity. Nature Chem.Biol. 4 357.
See how others have used PHA 767491 hydrochloride. Click on the entry to view the PubMed entry .
PMID: # 28630312 2017. Proc. Natl. Acad. Sci. U.S.A. 114: E5352-E5361.
PMID: # 27587400 Xu, X. et al. 2016. J. Biol. Chem. 291: 22544-22558.
PMID: # 25737283 Sansam, CG. et al. 2015. Genes Dev. 29: 555-66.
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