PHA 767491 hydrochloride
Chemical Name: 1,5,6,7-Tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-one hydrochloride
Purity: ≥99%
Biological Activity
PHA 767491 hydrochloride is an ATP-competitive cyclin-dependent kinase (cdk) inhibitor (reported IC50 values are 0.034 - 0.75, 0.24 - 1.2, 0.25 - 1.1 and 0.46 - 1 μM for cdk9, cdk2, cdk1 and cdk5, respectively). Also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK2; IC50 = 171 nM). Prevents initiation of DNA replication. Inhibits cell proliferation in a variety of human cell lines and induces apoptosis in a p53-independent manner in vivo.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).
Anderson et al.
J.Med.Chem., 2007;50:2647 -
How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
Jorda et al.
J.Med.Chem., 2018;61:9105
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Citations for PHA 767491 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for PHA 767491 hydrochloride include:
5 Citations: Showing 1 - 5
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DDK dependent regulation of TOP2A at centromeres revealed by a chemical genetics approach.
Authors: Wu Et al.
Nucleic Acids Res 2016;44:8786
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Mammalian FMRP S499 Is Phosphorylated by CK2 and Promotes Secondary Phosphorylation of FMRP.
Authors: Bartley Et al.
Eneuro 2016;3
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A high through-put screen for small molecules modulating MCM2 phosphorylation identifies Ryuvidine as an inducer of the DNA damage response.
Authors: FitzGerald Et al.
PLoS One 2014;9:e98891
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CDC7 inhibition blocks pathological TDP-43 phosphorylation and neurodegeneration.
Authors: Liachko Et al.
Ann Neurol 2013;74:39
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Geminin overexpression prevents the completion of topoisomerase IIα chromosome decatenation, leading to aneuploidy in human mammary epithelial cells.
Authors: Gardner Et al.
Breast Cancer Res 2011;13:R53
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