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Description: Cdk inhibitor; potently inhibits cdk1 and cdk2; also inhibits CK1; acts as molecular glue
Chemical Name: (2R)-2-[[9-(Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-1-butanol trihydrochloride
Purity: ≥99% (HPLC)
Biological Activity for (R)-CR8
(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.
Compound Libraries for (R)-CR8
(R)-CR8 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 (R)-CR8
| M. Wt | 540.92 |
| Formula | C24H29N7O.3HCl |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1786438-30-9 |
| PubChem ID | 90488866 |
| InChI Key | ORYSYXHQFOWNDK-RGFWRHHQSA-N |
| Smiles | CC(C)N2C1=NC(N[C@H](CC)CO)=NC(NCC3=CC=C(C4=NC=CC=C4)C=C3)=C1N=C2.Cl.Cl.Cl |
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 (R)-CR8
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 54.09 | 100 | |
| DMSO | 54.09 | 100 |
Preparing Stock Solutions for (R)-CR8
The following data is based on the product molecular weight 540.92. 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 | 1.85 mL | 9.24 mL | 18.49 mL |
| 5 mM | 0.37 mL | 1.85 mL | 3.7 mL |
| 10 mM | 0.18 mL | 0.92 mL | 1.85 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.37 mL |
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Product Datasheets for (R)-CR8
References for (R)-CR8
References are publications that support the biological activity of the product.
Oumata et al (2008) Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1. J.Med.Chem. 51 5229 PMID: 18698753
Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987
Słabicki et al (2020) The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K. Nature 585 293 PMID: 32494016
If you know of a relevant reference for (R)-CR8, please let us know.
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Keywords: (R)-CR8, (R)-CR8 supplier, cdk1, cdk5, inhibitors, inhibits, CK1, cyclin-dependent, kinases, casein, kinase, 1, Cyclin-dependent, Kinase, Casein, Molecular, Glues, Non-selective, CDKs, 3605, Tocris Bioscience
7 Citations for (R)-CR8
Citations are publications that use Tocris products. Selected citations for (R)-CR8 include:
Malonia et al (2015) F-box protein FBXO31 directs degradation of MDM2 to facilitate p53-mediated growth arrest following genotoxic stress. Microvasc Res 112 8632 PMID: 26124108
Wu et al (2013) TrkB.T1 contributes to neuropathic pain after spinal cord injury through regulation of cell cycle pathways. J Neurosci 33 12447 PMID: 23884949
Wu et al (2013) Cell cycle activation contributes to increased neuronal activity in the posterior thalamic nucleus and associated chronic hyperesthesia after rat spinal cord contusion. Neurotherapeutics 10 520 PMID: 23775067
Wu et al (2012) Delayed expression of cell cycle proteins contributes to astroglial scar formation and chronic inflammation after rat spinal cord contusion. J Neuroinflammation 9 169 PMID: 22784881
Słabicki (2020) The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K Nature 585 293 PMID: 32494016
Goonesekere et al (2014) A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers. PLoS One 9 e93046 PMID: 24740004
Wu et al (2014) Spinal cord injury causes brain inflammation associated with cognitive and affective changes: role of cell cycle pathways. J Neurosci 34 10989 PMID: 25122899
Do you know of a great paper that uses (R)-CR8 from Tocris? Please let us know.
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