1786438-30-9

1786438-30-9 structure

Name: (R)-CR8
Chemical Name: (R)-CR8 trihydrochloride
CAS Number: 1786438-30-9
Molecular Formula: C₂₄H₃₂Cl₃N₇O
Molecular Weight: 540.92
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2020-01-23 10:55:51
Modify Date: 2024-01-10 18:36:54
(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].

Name	(R)-CR8 trihydrochloride

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.

Molecular Formula	C₂₄H₃₂Cl₃N₇O
Molecular Weight	540.92

1786438-30-9	294646-77-8
1956437-40-3	73981-53-0
158749-75-8	1391515-37-9
122091-54-7	528566-21-4
1391519-06-4	1640848-93-6
2209843-08-1	2407920-81-2
1384972-90-0	1158522-08-7
940364-43-2	134104-43-1
131615-57-1	6906-52-1
930439-75-1	1018584-77-4