CR8 3HCl (R)
CDK inhibitor / Second generation analog of roscovitine which inhibits cyclin-dependent kinases with increased potency, Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk5, p25, and Cdk9/cyclin T, IC50s=0.09, 0.072, 0.041, 0.11 and 0.18 uM respectively.1,2 Acts as a molecular glue degrader that depletes cyclin K.3 CR8 displays neuroprotective effects in various models including traumatic brain injury.4
Biochemicals & reagents
294646-77-8
1) Bettayeb et al. (2008), C8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases; Oncogene, 27 5797 2) Bettayeb et al. (2010), CDK Inhibitors Roscovitine and CR8 Trigger Mcl-1 Down-Regulation and Apoptotic Cell Death in Neuroblastoma Cells; Genes Cancer, 1 369 3) Slabiki et al. (2020), The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K; Nature, 585 293 4) Aubrecht et al. (2018), Comparing effects of CDK inhibitor and E2F1/2 ablation on neuronal cell death pathways in vitro and after traumatic brain injury; Cell Death Dis., 9 1121
-20°C
TARGET: Kinase; Molecular glue -- PATHWAY: Cell cycle; Apoptosis inducer; NFkappaB; Myc; Bcl -- RESEARCH AREA: Neuroscience; Cell death; Ubiquitin/Proteasome -- DISEASE AREA: Cancer; NeurodegenerationLiver disease; Kidney disease