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Submit ReviewPurvalanol A is a cyclin-dependent kinase (cdk) inhibitor (reported IC50 values are 4, 4 - 70, 75 - 240 and 100 nM for cdk1, cdk2, cdk5 and cdk 7, respectively). Reversibly arrests synchronised cells in G1 and G2, and inhibits cell proliferation and cell death.
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Purvalanol A is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 388.9 |
Formula | C19H25ClN6O |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 212844-53-6 |
PubChem ID | 456214 |
InChI Key | PMXCMJLOPOFPBT-HNNXBMFYSA-N |
Smiles | ClC1=CC=CC(NC2=C3C(N(C(C)C)C=N3)=NC(N[C@H]([C@@H](C)C)CO)=N2)=C1 |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
ethanol | 19.45 | 50 | |
DMSO | 38.89 | 100 |
The following data is based on the product molecular weight 388.9. 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 | 2.57 mL | 12.86 mL | 25.71 mL |
5 mM | 0.51 mL | 2.57 mL | 5.14 mL |
10 mM | 0.26 mL | 1.29 mL | 2.57 mL |
50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
References are publications that support the biological activity of the product.
Bain et al (2003) The specificities of protein kinase inhibitors: an update. Biochem.J. 371 199 PMID: 12534346
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
Villerbu et al (2002) Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities. Int.J.Cancer 97 761 PMID: 11857351
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 Purvalanol A, please let us know.
Keywords: Purvalanol A, Purvalanol A supplier, Cyclin-dependent, protein, kinases, inhibitors, inhibits, Cdk, PurvalanolA, NG60, NG, 60, Kinase, Non-selective, CDKs, 1580, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Purvalanol A include:
Gayek and Ohi (2016) CDK-1 Inhibition in G2 Stabilizes Kinetochore-Microtubules in the following Mitosis. PLoS One 11 e0157491 PMID: 27281342
Seldin et al (2013) NuMA localization, stability, and function in spindle orientation involve 4.1 and Cdk1 interactions. Mol Biol Cell 24 3651 PMID: 24109598
Origanti et al (2013) Synthetic lethality of Chk1 inhibition combined with p53 and/or p21 loss during a DNA damage response in normal and tumor cells. Oncogene 32 577 PMID: 22430210
Ozlü et al (2010) Binding partner switching on microtubules and aurora-B in the mitosis to cytokinesis transition. Mol Cell Proteomics 9 336 PMID: 19786723
Rowe et al (2010) Compounds that target host cell proteins prevent varicella-zoster virus replication in culture, ex vivo, and in SCID-Hu mice. Antiviral Res 86 276 PMID: 20307580
Pennati et al (2005) Potentiation of PacT.-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation. Mol Cancer Ther 4 1328 PMID: 16170024
Karayel et al (2018) Comparative phosphoproteomic analysis reveals signaling networks regulating monopolar and bipolar cytokinesis. Sci Rep 8 2269 PMID: 29396449
Fabritius et al (2011) Initial diameter of the polar body contractile ring is minimized by the centralspindlin complex. Dev Biol 359 137 PMID: 21889938
Do you know of a great paper that uses Purvalanol A from Tocris? Please let us know.
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