PeptideDB

CLK8

CAS No.: 898920-65-5

CLK8 is a selective CLOCK inhibitor that binds to and interferes with CLOCK activity, disrupts the interaction between C
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Description CLK8 is a selective CLOCK inhibitor that binds to and interferes with CLOCK activity, disrupts the interaction between CLOCK and BMAL1, and modulates circadian rhythm amplitude.CLK8 can be used to study circadian rhythm-related disorders.
In vitro CLK8 最高浓度为 40 μM,对 U2OS 细胞无毒性,细胞活力>80%。同样 CLK8 以剂量依赖性方式增强了 U2OS 和 NIH 3T3 细胞中 Bmal1-d Luc 信号的振幅,并且在两种细胞系中均未观察到周期变化[1].
In vivo CLK8 以 25mg/kg 的浓度腹膜内施用到小鼠中。结果表明 CLK8 能使小鼠肝脏的全细胞裂解物中的 CLOCK 水平降低,而 BMAL1 和 CRY1 的水平没有改变[1]。
molecular weight 498.53
Molecular formula C29H26N2O6
CAS 898920-65-5
Storage keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility DMSO: 30 mg/mL (60.12 mM)
References 1. Doruk YU, et al. A CLOCK-binding small molecule disrupts the interaction between CLOCK and BMAL1 and enhances circadian rhythm amplitude. J Biol Chem. 2020 Mar 13;295(11):3518-3531.