(R) ​-​CR8

CAT: 0804-HY-18340-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-18340-01Size:5 mg
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Description
(R) -CR8, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R) -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[1][2]. (R) -CR8 acts as a molecular glue degrader that depletes cyclin K[3].
CAS Number
[294646-77-8]
Product Name Alternative
CR8, (R) -Isomer
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
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.html
Purity
99.61
Solubility
DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
CC[C@@H](NC1=NC(NCC2=CC=C(C3=NC=CC=C3)C=C2)=C4N=CN(C(C)C)C4=N1)CO
Molecular Formula
C24H29N7O
Molecular Weight
431.53
Precautions
H302, H315, H319, H335
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
CDK1; CDK2; CDK5; CDK7; CDK9

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