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CLK1-IN-1

CAS No. : 2123491-32-5

MCE 站：CLK1-IN-1

产品活性：CLK1-IN-1 是一个有效的、Cdc2-like 激酶 (CLK1) 的选择性抑制剂，其 IC₅₀ 值为 2 nM。

研究领域：Cell Cycle/DNA Damage

作用靶点：CDK

In Vitro: CLK1 is the most potently inhibited kinase (IC₅₀: 2 nM). 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 ability of CLK1-IN-1 to induce autophagy in BNL CL.2 and SKOV-3 (human ovarian cancer cell line) cells is also examined. 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 stimulats the degradation of SQSTM1/p62 and increases the ratio of red LC3 puncta to yellow LC3 puncta, both of which indicate an induction of autophagic flux by CLK1-IN-1.

In Vivo: APAP exposure results in severe liver injury, and treatment with CLK1-IN-1 (ip, 30 mg/kg) imparts a significant hepatoprotective effect. The results show that treatment with CLK1-IN-1 decreases serum ALT and AST levels significantly such that both marker enzymes return to normal levels.

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