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(R)-CR8 trihydrochloride

CAS No. : 1786438-30-9

MCE 站：(R)-CR8 trihydrochloride

产品活性：(R)-CR8 (CR8) trihydrochloride 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 trihydrochloride 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 (1.1 μM)、CDK9/cyclin T (0.18 μM) 和 CK1δ/ε (0.4 μM)。(R)-CR8 trihydrochloride 诱导细胞凋亡并具有神经保护作用。(R)-CR8 trihydrochloride 作为一种分子胶降解剂来消耗细胞周期蛋白 K。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：CDK  |  Apoptosis

In Vitro: (R)-CR8 (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.
(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

In Vivo: (R)-CR8 trihydrochloride (5?mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment.

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