(R)-CR8

(R)-CR8用途

(R)-CR8 (CR8) 是 Roscovitine 的第二代类似物,是一种有效的 CDK1/2/5/7/9 抑制剂。(R)-CR8 (CR8) 抑制 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 (1.1μM)、CDK9/cyclin T (0.18μM) 和 CK1δ/ε (0.4 μM)。(R)-CR8 (CR8) 诱导细胞凋亡并具有神经保护作用。

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(R)-CR8名称

[ CAS 号 ]:
294646-77-8

[ 中文名 ]:
(R)-2-((9-异丙基-6-((4-(吡啶-2-基)苄基)氨基)-9H-嘌呤-2-基)氨基)丁醇

[ 英文名 ]:
(R)-CR8

[英文别名 ]:

3ddp
CR-8
HMS3229B13

(R)-CR8生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> CDK

[ 靶点 ]

Cdk1/cyclin B: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)

[参考文献]

[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.

(R)-CR8物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
671.4±65.0 °C at 760 mmHg

[ 分子式 ]:
C₂₄H₂₉N₇O

[ 分子量 ]:
431.533

[ 闪点 ]:
359.8±34.3 °C

[ 精确质量 ]:
431.243347

[ PSA ]:
100.78000

[ LogP ]:
2.10

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.664

[ 储存条件 ]:
2-8°C，密闭，干燥

(R)-CR8安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

(R)-CR8合成路线

详细合成路线

(R)-CR8上下游产品

(R)-CR8上游产品

(R)-CR8下游产品

(R)-CR8文献

Natural product extracts of the Canadian prairie plant, Thermopsis rhombifolia, have anti-cancer activity in phenotypic cell-based assays.

Nat. Prod. Res. 29 , 1026-34, (2015)

Many plant species within the terrestrial ecological zones of Canada have not yet been investigated for anti-cancer activity. We examined the scientific literature describing the endemic flora from th...

Substitutions in the Escherichia coli RNA polymerase inhibitor T7 Gp2 that allow inhibition of transcription when the primary interaction interface between Gp2 and RNA polymerase becomes compromised.

Microbiology 158 , 2753-64, (2012)

The Escherichia coli-infecting bacteriophage T7 encodes a 7 kDa protein, called Gp2, which is a potent inhibitor of the host RNA polymerase (RNAp). Gp2 is essential for T7 phage development. The inter...

Delayed expression of cell cycle proteins contributes to astroglial scar formation and chronic inflammation after rat spinal cord contusion.

J. Neuroinflammation 9 , 169, (2012)

Traumatic spinal cord injury (SCI) induces secondary tissue damage that is associated with astrogliosis and inflammation. We previously reported that acute upregulation of a cluster of cell-cycle-rela...

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(R)-CR8

(R)-CR8用途

(R)-CR8名称

(R)-CR8生物活性

(R)-CR8物理化学性质

(R)-CR8安全信息

(R)-CR8合成路线

详细合成路线

(R)-CR8上下游产品

(R)-CR8上游产品

(R)-CR8下游产品

(R)-CR8文献

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(R)​-​CR8用途

(R)​-​CR8名称

(R)​-​CR8生物活性

(R)​-​CR8物理化学性质

(R)​-​CR8安全信息

(R)​-​CR8合成路线

详细合成路线

(R)​-​CR8上下游产品

(R)​-​CR8上游产品

(R)​-​CR8下游产品

(R)​-​CR8文献

推荐生产厂家/供应商：

相关化合物

(R)-CR8

(R)-CR8用途

(R)-CR8名称

(R)-CR8生物活性

(R)-CR8物理化学性质

(R)-CR8安全信息

(R)-CR8合成路线

(R)-CR8上下游产品

(R)-CR8上游产品

(R)-CR8下游产品

(R)-CR8文献