CLK1-IN-3
Based on 1 Customer Validation
CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research.
For research use only. We do not sell to patients.
- Purity: 98.54%
- CAS No.: 2922550-28-3
- Formula: C24H23FN6O
- Molecular Weight:430.48
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
|
CLK1 5 nM (IC50) |
CLK2 42 nM (IC50) |
CLK4 108 nM (IC50) |
DYRK1A 1521 nM (IC50) |
CLK1-IN-3 (compound 10ad) shows potential in anti-tumor because of dual inhibition of Clk1 and Clk2[1].
CLK1-IN-3 (10 μM-1000 μM) can effectively bind to Clk1 protein and inhibit its degradation in a dose-dependent manner[1].
CLK1-IN-3 (0-10 μM, 24 h) induces autophagy in Hela, BNLCL.2 and HCT 116 cells[1].
CLK1-IN-3 stimulates the degradation of SQSTM1/p62 (a marker of autolysosomes)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hela cells, BNLCL.2 and HCT 116 cells
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Concentration:0.2, 1, 5, and 10 μM
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Incubation Time:24 h
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Result:Elevated the expression level of LC3II protein (a marker of autophagosomes) as well as the ratio of LC3II to LC3I (a sensitive index of autophagy) in a dose-dependent and time-dependent manner.
CLK1-IN-3 (10 mg/kg; IV, PO, IP, once) shows acceptable pharmacokinetic profile, has a relatively long T1/2 with 5.29 h and oral bioavailability of 19.5%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice(8 weeks, injected acetaminophen (HY-66005) (500 mg/kg, ip))[1]
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Dosage:10, 20, and 40 mg/kg
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Administration:IP, once
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Result:Decreased serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels significantly in dose-dependent.
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Animal Model:Male Balb/c mice (aged 8 weeks)[1]
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Dosage:10 mg/kg
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Administration:IV, PO, IP, once (Pharmacokinetic Analysis)
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Result:Pharmacokinetic Parameters of CLK1-IN-3 in male Balb/C mice[1].
IV (10 mg/kg) PO (10 mg/kg) IP (10 mg/kg) Cmax (ng/mL) 13166.5±875.9 1457.4±177.3 4654.3±435.3 T1/2 (h) 2.96±1.2 5.29±2.1 3.27 ±1.1 AUC0-t (ng/mL∗h) 9520.5±1011.3 1860.2±411.0 5010.4±987.2 CL (L/h/kg) 1.05±0.10 5.51±1.00 3.58±0.82 F (%) 19.5%
Chemical Information
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CAS No. 2922550-28-3
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Appearance Solid
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Molecular Weight 430.48
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Formula C24H23FN6O
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Color Off-white to light yellow
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SMILES
CN1CCN(CC1)C2=CC=C(C=C2)C(NC3=CN=C4NC=C(C4=C3)C5=CN=CC(F)=C5)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (232.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.81 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3230 mL | 11.6149 mL | 23.2299 mL | 58.0747 mL |
| 5 mM | 0.4646 mL | 2.3230 mL | 4.6460 mL | 11.6149 mL | |
| 10 mM | 0.2323 mL | 1.1615 mL | 2.3230 mL | 5.8075 mL | |
| 15 mM | 0.1549 mL | 0.7743 mL | 1.5487 mL | 3.8716 mL | |
| 20 mM | 0.1161 mL | 0.5807 mL | 1.1615 mL | 2.9037 mL | |
| 25 mM | 0.0929 mL | 0.4646 mL | 0.9292 mL | 2.3230 mL | |
| 30 mM | 0.0774 mL | 0.3872 mL | 0.7743 mL | 1.9358 mL | |
| 40 mM | 0.0581 mL | 0.2904 mL | 0.5807 mL | 1.4519 mL | |
| 50 mM | 0.0465 mL | 0.2323 mL | 0.4646 mL | 1.1615 mL | |
| 60 mM | 0.0387 mL | 0.1936 mL | 0.3872 mL | 0.9679 mL | |
| 80 mM | 0.0290 mL | 0.1452 mL | 0.2904 mL | 0.7259 mL | |
| 100 mM | 0.0232 mL | 0.1161 mL | 0.2323 mL | 0.5807 mL |
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