Roscovitine
Chemical Name: (2R)-2-[[9-(1-Methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-1-butanol
Purity: ≥98%
Biological Activity
Roscovitine is a cyclin-dependent kinase (cdk) inhibitor. Displays sub-micromolar inhibition of cdk1, cdk2, cdk5, cdk7 and cdk9 (reported IC50 values range from 0.16 - 0.28 μM for cdk5 to 0.8 μM for cdk7). Selective for cdks over a wide range of related kinases including ERK1 and ERK2. Arrests L1210 cells in G1 phase. Inhibits phosphorylation of vimentin in vivo. Antimitotic.Technical Data
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.
Background References
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How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
Jorda et al.
J.Med.Chem., 2018;61:9105 -
Inhibition of cyclin-dependent kinases by purine analogues.
De Azevedo et al.
Eur.J.Biochem., 1997;243:518 -
Chemical inhibitors of cyclin-dependent kinases.
Meijer
Trends Cell.Biol., 1996;6:393 -
Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5.
Meijer et al.
Eur.J.Biochem., 1997;243:527 -
Chronic Corticosterone Elevation Suppresses Adult Hippocampal Neurogenesis by Hyperphosphorylating Huntingtin
F Agasse, I Mendez-Dav, W Christalle, R Carpentier, BY Braz, DJ David, F Saudou, S Humbert
Cell Rep, 2020;32(1):107865.
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