CLK1-IN-1
目录号 : GC30245
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2nM。
Cas No.:2123491-32-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | BNL CL.2 (mouse embryonic liver cell line) is selected, and three concentrations (20 nM, 100 nM, and 10 μM) of CLK1-IN-1 are used[1]. |
Animal experiment: | Mice[1]Drug-induced liver injury (DILI) is a major public health concern and accounts for more than 50% of acute liver failure cases. APAP is a widely used antipyretic analgesic drug. Herein, the APAP-induced hepatotoxicity mouse model is used to examine the therapeutic effect of CLK1-IN-1 in vivo. Male C57BL/6 mice are given either saline (n=3, ip) or APAP (500 mg/kg) (n=15, ip). To examine the hepatoprotective effect, mice are injected (ip) with CLK1-IN-1 (25) (30 mg/kg), 30 (30 mg/kg, positive control), rapamycin (30 mg/kg, positive control), or solvent (12.5% ethanol and 12.5% castor oil, 10 mL/kg), immediately followed by APAP (500 mg/kg) injection (ip). All mice are sacrificed 6 h later. Liver sections are examined by H&E staining, and the serum from the blood samples is used for ALT and AST activity tests[1]. |
References: [1]. Sun QZ, et al. Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers. J Med Chem. 2017 Jul 27;60(14):6337-6352. | |
CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 (CLK1) inhibitor, with an IC50 of 2 nM.
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[1].
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[1].
[1]. Sun QZ, et al. Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers. J Med Chem. 2017 Jul 27;60(14):6337-6352.
| Cas No. | 2123491-32-5 | SDF | |
| Canonical SMILES | C[C@@H](C1=CC=C(F)C=C1)N2N=NC3=C2C4=CC(C5=CC=C6C(N=CO6)=C5)=CC=C4N=C3 | ||
| 分子式 | C24H16FN5O | 分子量 | 409.42 |
| 溶解度 | DMSO : ≥ 50 mg/mL (122.12 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4425 mL | 12.2124 mL | 24.4248 mL |
| 5 mM | 0.4885 mL | 2.4425 mL | 4.885 mL |
| 10 mM | 0.2442 mL | 1.2212 mL | 2.4425 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。