(R)-CR8 (CR8)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
(R)-CR8是(R)-roscovitin的第二代类似物,也是有效的细胞周期蛋白依赖性激酶(CDK)抑制剂。Potency/IC50: Cdk1/cyclin B = 0.09 μM, cdk2/cyclin A = 0.072 μM, CDK2/cyclinE = 0.041 μM, Cdk5/p25 = 0.11 μM, CDK7/cyclin H = 1.1 μM, CDK9/Cyclin T = 0.18 μM, CK1δ/ε= 0.4 μM.
CR8疗法能降低CCA;皮质、海马和丘脑神经元丢失;皮质小胶质细胞和星形胶质细胞的激活。此外,它还减轻了感觉运动和认知缺陷,减轻了抑郁样症状,并减少了病变体积。
在体内,与载体处理的LFP组相比,CR8处理的LFP组大鼠在所有时间点均显著改善DG神经元的恢复,并且在复合neuroscore试验中显著改善感官运动的结果。在抑郁样症状中,使用强迫游泳任务,LFP损伤大鼠表现出典型的抑郁症状,而CR8疗法可显著缓解这些症状。
此外,CR8还可作为分子胶降解剂。溶剂接触的CR8的吡啶基,以其cdk结合的形式,诱导CDK12-cyclin K与CUL4 adaptor蛋白DDB1形成CDK12-cyclin K复合物,无需底物受体,并呈递cyclin K (cycK)进行泛素化和降解。
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.
Storage | Store at -20°C |
M.Wt | 431.53 |
Cas No. | 294646-77-8 |
Formula | C24H29N7O |
Synonyms | CR8,(R)-Isomer |
Solubility | ≥45.4 mg/mL in DMSO |
Chemical Name | (R)-2-((9-isopropyl-6-((4-(pyridin-2-yl)benzyl)amino)-9H-purin-2-yl)amino)butan-1-ol |
SDF | Download SDF |
Canonical SMILES | OC[C@@H](CC)NC1=NC(NCC2=CC=C(C3=NC=CC=C3)C=C2)=C(N=CN4C(C)C)C4=N1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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