(R) -CR8 (trihydrochloride)

(R) -CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R) -CR8 trihydrochloride 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 trihydrochloride induces apoptosis and has neuroprotective effect[1][2]. (R) -CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K[3].

Product Specifications

CAS Number

[1786438-30-9]

Product Name Alternative

CR8, (R) -Isomer (trihydrochloride)

UNSPSC

12352005

Target

Apoptosis; CDK; Molecular Glues

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/r-cr8-trihydrochloride.html

Concentration

10mM

Purity

99.37

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

CC[C@@H](NC1=NC(NCC2=CC=C(C3=NC=CC=C3)C=C2)=C4N=CN(C(C)C)C4=N1)CO.[H]Cl.[H]Cl.[H]Cl

Molecular Formula

C24H32Cl3N7O

Molecular Weight

540.92

References & Citations

[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]Słabicki 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.