PHA 767491 hydrochloride

Name: PHA 767491 hydrochloride
Brand: Tocris Bioscience
SKU: 3140

Tocris Bioscience a Bio-Techne Brand

Catalog # 3140

Citations (5)

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Key Product Details

Description:	Cdk inhibitor; potently inhibits cdk9; also inhibits MK2
Chemical Name:	1,5,6,7-Tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-one hydrochloride
Purity:	≥99% (HPLC)
Molecular Weight:	249.7

View Full Technical Details for PHA 767491 hydrochloride

Biological Activity for PHA 767491 hydrochloride

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.

Compound Libraries for PHA 767491 hydrochloride

PHA 767491 hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for PHA 767491 hydrochloride

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 for PHA 767491 hydrochloride

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

Preparing Stock Solutions for PHA 767491 hydrochloride

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	4.00 mL	20.02 mL	40.05 mL
5 mM	0.80 mL	4.00 mL	8.01 mL
10 mM	0.40 mL	2.00 mL	4.00 mL
50 mM	0.08 mL	0.40 mL	0.80 mL

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References for PHA 767491 hydrochloride

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

Jorda How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 2018 PMID: 30234987
Jackson Stopping replication, at the beginning. Nature Chem.Biol. 2008 PMID: 18488006
Montagnoli A cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumour activity. Nature Chem.Biol. 2008 PMID: 18469809
Anderson Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J.Med.Chem. 2007 PMID: 17480064

Citations for PHA 767491 hydrochloride (5)

Showing 1 - 5 of 5 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for PHA 767491 hydrochloride include:

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
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
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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