(R)-CR8

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

(R)-CR8 是一种有效的选择性 CDK 抑制剂。CR8 是一种有效的第二代细胞周期蛋白依赖性激酶 (CDK) 抑制剂，LFP 后 3 小时延迟全身给药。

(R)-CR8 is a potent and selective CDK inhibitor.A delayed systemic post-LFP administration at 3 hours of CR8--a potent second-generation cyclin-dependent kinase (CDK) inhibitor--reduced CCA;?cortical, hippocampal, and thalamic neuronal loss;?and cortical microglial and astrocyte activation.?Furthermore, CR8 treatment attenuated sensorimotor and cognitive deficits, alleviated depressive-like symptoms, and decreased lesion volume.

(R)-CR8 (CR8) (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.(R)-CR8 (0.25-10 μM) induces a dose-dependent induction of poly-(ADP-ribose)polymerase (PARP) cleavage.The CDK-bound form of (R)-CR8 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 AnalysisCell 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 (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:i.p. Administration:5?mg/Kg Result:Resulted in a significant reduction in lesion size.

CR8 ,(R)-Isomer

Angiogenesis

CDK

CDK

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294646-77-8

431.53

C24H29N7O

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (115.87 mM)

CC[C@H](CO)Nc1nc(NCc2ccc(cc2)-c2ccccn2)c2ncn(C(C)C)c2n1

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(-20℃)

With Ice Pack

≥ 2 years