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Submit ReviewPHA 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.
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。
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 24.97 | 100 | |
DMSO | 24.97 | 100 |
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.
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 |
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
If you know of a relevant reference for PHA 767491 hydrochloride, please let us know.
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
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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