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Biological Activity for Purvalanol B
Purvalanol 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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Compound Libraries for Purvalanol B
Technical Data for Purvalanol B
|Storage||Store at +4°C|
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 for Purvalanol B
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|1eq. NaOH||43.29||100 with gentle warming|
Preparing Stock Solutions for Purvalanol B
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References for Purvalanol B
References are publications that support the biological activity of the product.
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.
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3 Citations for Purvalanol B
Citations are publications that use Tocris products. Selected citations for Purvalanol B include:
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
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
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
Do you know of a great paper that uses Purvalanol B from Tocris? Please let us know.
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