PHA 767491 hydrochloride

Cat. No. 3140

PHA 767491 hydrochloride C12H11N3O.HCl [942425-68-5]

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Chemical Name: 1,5,6,7-Tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-one hydrochloride

Biological Activity

Potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication. Inhibits cell proliferation in a variety of human cell lines (IC50 ~ 0.86 - 5.87 μM) and induces apoptosis in a p53-independent manner in vivo. Also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK2) (IC50 = 171 nM).

Technical Data

M.Wt:
249.7
Formula:
C12H11N3O.HCl
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
>99 %
Storage:
Desiccate at RT
CAS No:
942425-68-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

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.

Anderson et al (2007) Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J.Med.Chem. 50 2647. PMID: 17480064.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for PHA 767491 hydrochloride include:

FitzGerald et al (2014) A high through-put screen for small molecules modulating MCM2 phosphorylation identifies Ryuvidine as an inducer of the DNA damage response. PLoS One 9 e98891. PMID: 24902048.

Gardner et al (2011) Geminin overexpression prevents the completion of topoisomerase IIα chromosome decatenation, leading to aneuploidy in human mammary epithelial cells. Breast Cancer Res 13 R53. PMID: 21595939.

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Keywords: PHA 767491 hydrochloride, supplier, Dual, cdc7/cdk9, inhibits, inhibitors, MK-2, mitogen-activated, protein, kinase-activated, kinase-2, Cyclin-Dependent, Protein, kinases, Checkpoint, control, PHA767491, hydrochloride, Tocris Bioscience, MK2 Inhibitor products

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