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(R)-CR8

Names

[ CAS No. ]:
1786438-30-9

[ Name ]:
(R)-CR8

Biological Activity

[Description]:

(R)-CR8 trihydrochloride (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].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> CDK
Research Areas >> Neurological Disease

[Target]

CDK1/cyclinB1:0.09 μM (IC50)

cdk2/cyclin A:0.072 μM (IC50)

CDK2/cyclinE:0.041 μM (IC50)

Cdk5/p25:0.11 μM (IC50)

CDK7/cyclin H:1.1 μM (IC50)

CDK9/Cyclin T:0.18 μM (IC50)

CK1δ/ε:0.4 μM (IC50)


[In Vitro]

(R)-CR8 trihydrochloride (CR8 trihydrochloride) (0.1-100 μM; 48 hours) is a potent inducer of apoptotic cell death with an IC50 of 0.49 μM for SH-SY5Y cell line[1]. (R)-CR8 trihydrochloride (0.25-10 μM) induces a dose-dependent induction of poly-(ADP-ribose)polymerase (PARP) cleavage[1]. Apoptosis Analysis[1] Cell Line: SH-SY5Y cell line Concentration: 0.1, 1, 10, 100 μM Incubation Time: 24 hours Result: Reduced cell survival in a dose-dependent manner.

[In Vivo]

(R)-CR8 trihydrochloride (5 mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment[2]. Animal Model: Adult (10 to 12 weeks old) male Sprague-Dawley rats (310 to 330 g)[2] Dosage: 5 mg/Kg Administration: i.p. Result: Resulted in a significant reduction in lesion size.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H32Cl3N7O

[ Molecular Weight ]:
540.92

Related Compounds