PHA 767491 hydrochloride

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Cat.No. 3140 - PHA 767491 hydrochloride | C12H11N3O.HCl | CAS No. 942425-68-5
Description: MK2 inhibitor; also cdk inhibitor; potently inhibits cdk9
Chemical Name: 1,5,6,7-Tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-one hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (5)
Reviews
Literature

Biological Activity

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.

Compound Libraries

PHA 767491 hydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 249.7
Formula C12H11N3O.HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 942425-68-5
PubChem ID 11715766
InChI Key IMVNFURYBZMFDZ-UHFFFAOYSA-N
Smiles O=C1NCCC2=C1C=C(C3=CC=NC=C3)N2.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 24.97 100
DMSO 24.97 100

Preparing Stock Solutions

The following data is based on the product molecular weight 249.7. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4 mL 20.02 mL 40.05 mL
5 mM 0.8 mL 4 mL 8.01 mL
10 mM 0.4 mL 2 mL 4 mL
50 mM 0.08 mL 0.4 mL 0.8 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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

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

Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987


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View Related Products by Product Action

View all MK2 Inhibitors

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5 Citations for PHA 767491 hydrochloride

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

Wu et al (2016) DDK dependent regulation of TOP2A at centromeres revealed by a chemical genetics approach. Nucleic Acids Res 44 8786 PMID: 27407105

Bartley et al (2016) Mammalian FMRP S499 Is Phosphorylated by CK2 and Promotes Secondary Phosphorylation of FMRP. Eneuro 3 PMID: 27957526

Liachko et al (2013) CDC7 inhibition blocks pathological TDP-43 phosphorylation and neurodegeneration. Ann Neurol 74 39 PMID: 23424178

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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