化合物 T10836 T10836

Product Introduction
Bioactivity


英文名: CLK1-IN-1

描述: CLK1-IN-1 is a potent and selective inhibitor of the Cdc2-like kinase 1 (CLK1; IC50: 2 nM).

体外活性: In addition to CLK1, only two kinases have an IC50 value less than 100 nM, namely CLK2 (IC50: 31 nM) and CLK4 (IC50: 8 nM), DYRK1A is the strongest off-target. The effects of CLK1-IN-1 on yellow LC3 puncta also displays obvious dose dependency, and a dose of 10 μM shows the best performance. In addition, in CLK1-IN-1-treated cells, the number of red LC3 puncta (mRFP signals only35) increases compared with that of DMSO-treated cells, indicating the formation of autolysosomes. Importantly, CLK1-IN-1 stimulates the degradation of SQSTM1/p62 and increases the ratio of red LC3 puncta to yellow LC3 puncta, both of which indicate induction of autophagic flux by CLK1-IN-1.

体内活性: APAP exposure results in severe liver injury and treatment with CLK1-IN-1 (i.p., 30 mg/kg) imparts a significant hepatoprotective effect. Treatment with CLK1-IN-1 decreases serum ALT and AST levels significantly such that both marker enzymes return to normal levels.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 25 mg/mL (61.06 mM)


关键字: CLK1IN1 | CLK1-IN-1 | CLK1 IN 1 | CLK-1-IN-1

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途