(R)-CR8
Chemical Name: (2R)-2-[[9-(Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-1-butanol trihydrochloride
Purity: ≥99%
Biological Activity
(R)-CR8 is a cyclin dependent kinase (cdk) inhibitor (reported IC50 values are 0.036 - 0.07, 0.09 - 0.8, 0.13 - 0.68, 0.18 - 1 and >1 μM for cdk2, cdk1, cdk5, cdk9 and cdk7, respectively). Also inhibits casein kinase 1 (CK1; IC50 = 0.6 μM). Acts as molecular glue; forms a complex between CDK12-cyclin K and the CUL4 adapter protein DDB1 resulting in ubiquination and degradation of cyclin K.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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Inhibition of E2F1/CDK1 pathway attenuates neuronal apoptosis in vitro and confers neuroprotection after spinal cord injury in vivo.
Wu J, Kharebava G, Piao C, Stoica B, Dinizo M, Sabirzhanov B, Hanscom M, Guanciale K, Faden A
PLoS ONE, 2012;7(7):e42129. -
Delayed expression of cell cycle proteins contributes to astroglial scar formation and chronic inflammation after rat spinal cord contusion.
Wu J, Pajoohesh-Ganji A, Stoica BA, Dinizo M, Guanciale K, Faden AI
J Neuroinflammation, 2012;9(1):169. -
Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1.
Oumata et al.
J.Med.Chem., 2008;51:5229 -
How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
Jorda et al.
J.Med.Chem., 2018;61:9105 -
The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K.
Słabicki et al.
Nature, 2020;
Product Datasheets
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Citations for (R)-CR8
The citations listed below are publications that use Tocris products. Selected citations for (R)-CR8 include:
7 Citations: Showing 1 - 7
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The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K
Authors: Słabicki
Nature 2020;585:293
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F-box protein FBXO31 directs degradation of MDM2 to facilitate p53-mediated growth arrest following genotoxic stress.
Authors: Malonia Et al.
Microvasc Res 2015;112:8632
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A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers.
Authors: Goonesekere Et al.
PLoS One 2014;9:e93046
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Spinal cord injury causes brain inflammation associated with cognitive and affective changes: role of cell cycle pathways.
Authors: Wu Et al.
J Neurosci 2014;34:10989
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TrkB.T1 contributes to neuropathic pain after spinal cord injury through regulation of cell cycle pathways.
Authors: Wu Et al.
J Neurosci 2013;33:12447
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Cell cycle activation contributes to increased neuronal activity in the posterior thalamic nucleus and associated chronic hyperesthesia after rat spinal cord contusion.
Authors: Wu Et al.
Neurotherapeutics 2013;10:520
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Delayed expression of cell cycle proteins contributes to astroglial scar formation and chronic inflammation after rat spinal cord contusion.
Authors: Wu Et al.
J Neuroinflammation 2012;9:169
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