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CAS No. : 2123491-32-5
MCE 国际站: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.
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Anti-Aging Compound Library | Chemical Probe Library | Anti-Breast Cancer Compound Library | Anti-Blood Cancer Compound Library | Targeted Diversity Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | SY-5609 | CLK1/2-IN-1 | MFH290 | SB-218078 | Toyocamycin | (S)-LY3177833 hydrate | Dinaciclib | EGFR/HER2/CDK9-IN-2 | CDK8-IN-11 | SNS-032 | M2N12 | Palbociclib-d8 | EGFR/CDK2-IN-1 | BSJ-04-132 | (E/Z)-Zotiraciclib | CCT-251921 | BS-181 | Ribociclib-d8 | CDK9-IN-9 | Flavopiridol | SRI-29329 | dCeMM4 | GSK 3 Inhibitor IX | CDK9-IN-7 | PROTAC CDK9 degrader-8 | BSJ-03-204 | Amantadine-d6 | K00546 | Abemaciclib metabolite M18 hydrochloride | Ribociclib-d6
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