| CAS NO: | 1084893-56-0 |
| 规格: | ≥98% |
Description: (S)-CR8, an analog of Roscovitine, is a novel, potent 2nd-generation cyclin-dependent kinase (CDK) inhibitor, also acting as a molecular glue degrader that depletes cyclin K. It acts by limiting microglial activation, astrocytosis, neuronal loss, and neurologic dysfunction after experimental traumatic brain injury. (S)-CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect. References: [1]. Bettayeb K, et al. CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases. Oncogene. 2008 Oct 2;27(44):5797-807. [2]. Kabadi SV, et al. CR8, a novel inhibitor of CDK, limits microglial activation, astrocytosis, neuronal loss, and neurologic dysfunction after experimental traumatic brain injury. J Cereb Blood Flow Metab. 2014 Mar;34(3):502-13. [3]. Slabicki M, et al. The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K [published online ahead of print, 2020 Jun 3]. Nature. 2020;10.1038/s41586-020-2374-x. [4]. Casein kinase 1ε and 1α as novel players in polycystic kidney disease and mechanistic targets for (R)-roscovitine and (S)-CR8. Am J Physiol Renal Physiol. 2018 Mar 14. Related CAS#: 1084893-56-0 (free base); 1786438-30-9 (triHCl)
纯度：≥98%
CAS：1084893-56-0
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