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Submit ReviewPurvalanol B is a cyclin-dependent kinase (cdk) inhibitor (reported IC50 values are 6 nM for cdk1 and cdk5, and 6 - 9 nM for cdk2, depending on binding partner). Purvalanol B is selective over a range of other protein kinases (IC50 >10,000 nM). Purvalanol B shows antiproliferative properties, mediated by ERK1 and ERK2. Purvalanol B induces autophagy in cellular models and induces apoptosis in cancer cells, the apoptotic effects can be increased by combining with Rapamycin (Cat. No. 1292).
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Purvalanol B is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 432.91 |
公式 | C20H25ClN6O3 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 212844-54-7 |
PubChem ID | 448991 |
InChI Key | ZKDXRFMOHZVXSG-HNNXBMFYSA-N |
Smiles | CC(C)[C@H](CO)NC1=NC(NC2=CC(Cl)=C(C=C2)C(O)=O)=C2N=CN(C(C)C)C2=N1 |
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 | |||
1eq. NaOH | 43.29 | 100 温和加热 | |
DMSO | 43.29 | 100 |
以下数据基于产品分子量 432.91。 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 | 2.31 mL | 11.55 mL | 23.1 mL |
5 mM | 0.46 mL | 2.31 mL | 4.62 mL |
10 mM | 0.23 mL | 1.15 mL | 2.31 mL |
50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
参考文献是支持产品生物活性的出版物。
Gray et al (1998) Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science 281 533 PMID: 9677190
Gray et al (1999) ATP-site directed inhibitors of cyclin-dependent kinases. Curr.Med.Chem. 6 859 PMID: 10495356
Knockaert et al (2002) p42/p44 MAPKs are intracellular targets of the CDK inhibitor purvalanol. Oncogene 21 6413 PMID: 12226745
Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987
Ozfiliz-Kilbas et al (2018) Cyclin-dependent kinase inhibitors, roscovitine and purvalanol, induce apoptosis and autophagy related to unfolded protein response in HeLa cervical cancer cells. Mol.Biol.Rep. 45 815 PMID: 29978381
If you know of a relevant reference for Purvalanol B, please let us know.
关键词: Purvalanol B, Purvalanol B supplier, Cyclin-dependent, protein, kinases, inhibitors, inhibits, Cdk, PurvalanolB, NG95, potent, cdk1, cdk2, cdk5, selective, antiproliferative, apoptosis, autophagy, NG, 95, Kinase, Non-selective, CDKs, 1581, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Purvalanol B 的部分引用包括:
Schreiber et al (2010) An integrated phosphoproteomics work flow reveals extensive network regulation in early lysophosphatidic acid signaling. Mol Cell Proteomics 9 1047 PMID: 20071362
Wissing et al (2007) Proteomics analysis of protein kinases by target class-selective prefractionation and tandem mass spectrometry. J Pharmacol Exp Ther 6 537 PMID: 17192257
Ma et al (2019) Characterization of the Src-regulated kinome identifies SGK1 as a key mediator of Src-induced transformation. Nat Commun 10 296 PMID: 30655532
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