CR8, (R)-Isomer (CAS 294646-77-8)
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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.
CR8, (R)-Isomer (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
- Drug-related alopecia in patients treated with tricyclic antidepressants. | Warnock, JK., et al. 1991. J Nerv Ment Dis. 179: 441-2. PMID: 1869875
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
CR8, (R)-Isomer, 5 mg | sc-311306 | 5 mg | $174.00 |