(R)-CR8 (CAS 294646-77-8)
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(R)-CR8, also known as CR8, (R)-Isomer, is a cell-permeable (R)-DRF053 (sc-221408) analog that acts as an ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor (IC50 = 0.09, 0.072, 0.041, 0.11, 1.10, 0.18, and 0.40 muM against CDK1/B (cyclin dependent kinase 1/B), CDK2/A (cyclin dependent kinase 2/A), CDK2/E (cyclin dependent kinase 2/E), CDK5/p25 (cyclin dependent kinase 5/p25), CDK7/H (cyclin dependent kinase 7/H), CDK9/T (cyclin dependent kinase 9/T), and CK1delta/epsilon, respectively). (R)-CR8 inhibits CDK/CK1 more effectively than (R)-Roscovitine, while maintaining similar selectivity profile over other types of kinases (IC50 = 3.6, 3.6, and 12.0 muM against Dyrk1A, Erk2, and GSK-3alpha/beta (glycogen synthase kinase-3alpha/beta), respectively). Both (R)-CR8 and (S)-enantiomers are much more effective than (R)-Roscovitine in apoptosis induction in cell cultures.
(R)-CR8 (CAS 294646-77-8) References
- CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases. | Bettayeb, K., et al. 2008. Oncogene. 27: 5797-807. PMID: 18574471
- CDK5-induced p-PPARγ(Ser 112) downregulates GFAP via PPREs in developing rat brain: effect of metal mixture and troglitazone in astrocytes. | Rai, A., et al. 2014. Cell Death Dis. 5: e1033. PMID: 24481447
- Antitumoral effects of cyclin-dependent kinases inhibitors CR8 and MR4 on chronic myeloid leukemia cell lines. | Troadec, S., et al. 2015. J Biomed Sci. 22: 57. PMID: 26184865
- Visualization of global RNA synthesis in a human (mini-) organ in situ by click chemistry. | Purba, TS., et al. 2018. Biotechniques. 65: 97-100. PMID: 30091388
- Dietary Polyphenols: A Multifactorial Strategy to Target Alzheimer's Disease. | Dhakal, S., et al. 2019. Int J Mol Sci. 20: PMID: 31615073
- The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K. | Słabicki, M., et al. 2020. Nature. 585: 293-297. PMID: 32494016
- Inhibitors of Cyclin-Dependent Kinases: Types and Their Mechanism of Action. | Łukasik, P., et al. 2021. Int J Mol Sci. 22: PMID: 33802080
- Protein degradation technology: a strategic paradigm shift in drug discovery. | Li, H., et al. 2021. J Hematol Oncol. 14: 138. PMID: 34488823
- Labeling and measuring stressed mitochondria using a PINK1-based ratiometric fluorescent sensor. | Uesugi, R., et al. 2021. J Biol Chem. 297: 101279. PMID: 34624312
- Inhibitors, PROTACs and Molecular Glues as Diverse Therapeutic Modalities to Target Cyclin-Dependent Kinase. | Rana, S., et al. 2021. Cancers (Basel). 13: PMID: 34771669
- Molecular Glues: Capable Protein-Binding Small Molecules That Can Change Protein-Protein Interactions and Interactomes for the Potential Treatment of Human Cancer and Neurodegenerative Diseases. | Li, F., et al. 2022. Int J Mol Sci. 23: PMID: 35682885
- Key Considerations in Targeted Protein Degradation Drug Discovery and Development. | Qin, L., et al. 2022. Front Chem. 10: 934337. PMID: 35978859
- Novel 2,6,9-Trisubstituted Purines as Potent CDK Inhibitors Alleviating Trastuzumab-Resistance of HER2-Positive Breast Cancers. | Kuchukulla, RR., et al. 2022. Pharmaceuticals (Basel). 15: PMID: 36145262
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
(R)-CR8, 10 mg | sc-361306 | 10 mg | $240.00 | |||
(R)-CR8, 50 mg | sc-361306A | 50 mg | $989.00 |