1786438-30-9
1786438-30-9 结构式
基本信息
(R)-CR8 3HCL
(2R)-2-[[9-(甲基乙基)-6-[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇三盐酸盐
CR8, (R)-Isomer trihydrochloride
常见问题列表
|
CDK1/cyclinB1 0.09 μM (IC 50 ) |
cdk2/cyclin A 0.072 μM (IC 50 ) |
CDK2/cyclinE 0.041 μM (IC 50 ) |
Cdk5/p25 0.11 μM (IC 50 ) |
CDK7/cyclin H 1.1 μM (IC 50 ) |
CDK9/Cyclin T 0.18 μM (IC 50 ) |
CK1δ/ε 0.4 μM (IC 50 ) |
(R)-CR8 (CR8) trihydrochloride (0.1-100 μM; 48 hours) is a potent inducer of apoptotic cell death with an IC
50
of 0.49 μM for SH-SY5Y cell line.
(R)-CR8 trihydrochloride (0.25-10 μM) induces a dose-dependent induction of poly-(ADP-ribose)polymerase (PARP) cleavage.
The CDK-bound form of (R)-CR8 trihydrochloride has a solvent-exposed pyridyl moiety that induces the formation of a complex between CDK12-cyclin K and the CUL4 adaptor protein DDB1, bypassing the requirement for a substrate receptor and presenting cyclin K for ubiquitination and degradation
Apoptosis Analysis
| 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. |
(R)-CR8 trihydrochloride (5 mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment.
| Animal Model: | Adult (10 to 12 weeks old) male Sprague-Dawley rats (310 to 330 g) |
| Dosage: | 5 mg/Kg |
| Administration: | i.p. |
| Result: | Resulted in a significant reduction in lesion size. |