PHA 767491 hydrochloride

Pricing Availability   Qty
说明: Cdk inhibitor; potently inhibits cdk9; also inhibits MK2
化学名: 1,5,6,7-Tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-one hydrochloride
纯度: ≥99% (HPLC)
说明书
引用文献 (5)
评论

生物活性 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.

化合物库 for PHA 767491 hydrochloride

PHA 767491 hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。

技术数据 for PHA 767491 hydrochloride

分子量 249.7
公式 C12H11N3O.HCl
储存 Desiccate at RT
纯度 ≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for PHA 767491 hydrochloride

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
water 24.97 100
DMSO 24.97 100

制备储备液 for PHA 767491 hydrochloride

以下数据基于产品分子量 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 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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产品说明书 for PHA 767491 hydrochloride

分析证书/产品说明书
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参考文献 for PHA 767491 hydrochloride

参考文献是支持产品生物活性的出版物。

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 PMID: 18488006

Montagnoli et al (2008) A cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumour activity. Nature Chem.Biol. 4 357 PMID: 18469809

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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查看全部 Non-selective CDK Inhibitors

关键词: PHA 767491 hydrochloride, 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, MK2, Cyclin-dependent, Kinase, Non-selective, CDKs, 3140, Tocris Bioscience

5 篇 PHA 767491 hydrochloride 的引用文献

引用文献是使用了 Tocris 产品的出版物。 PHA 767491 hydrochloride 的部分引用包括:

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

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

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


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