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Purvalanol B

Cat. No. 1581 3 Citations Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Selective cdk inhibitor; potently inhibits cdk1, cdk2 and cdk5
Alternative Names: NG 95
Chemical Name: (2R)-2-[[6-[(3-Chloro-4-carboxyphenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-1-butanol
Purity: ≥99% (HPLC)
Datasheet
Citations (3)
Reviews
Biological Activity Technical Data Solubility Calculators Datasheets References

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).

Licensing Information

Sold under license from the Regents of the University of California

Compound Libraries for Purvalanol B

Purvalanol B is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for Purvalanol B

M. Wt 432.91
Formula C20H25ClN6O3
Storage Store at +4°C
Purity ≥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

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
Solubility
1eq. NaOH 43.29 100 with gentle warming
DMSO 43.29 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for Purvalanol B

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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

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

Do you know of a great paper that uses Purvalanol B from Tocris? Please let us know.

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