SGC-CDKL2/AAK1/BMP2K-1
Based on 1 Customer Validation
SGC-CDKL2/AAK1/BMP2K-1 (Compound 9) is a potent and selective CDKL2 (Cyclin-dependent kinase-like 2) inhibitor with an IC50 value of 460 nM. CDKL2 is involved in various biological processes such as tumorigenesis, development, and viral infections. SGC-CDKL2/AAK1/BMP2K-1 serves as a powerful tool for studying the biological functions of CDKL2 and holds promise for research in fields related to cancer, infections, and other diseases.
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- Pureté : 98.55%
- CAS No.: 2471972-15-1
- Formule: C22H26N4O3S
- Masse moléculaire:426.53
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
IC50: 460 nM (Cyclin-dependent kinase-like 2 (CDKL2))[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10000 nM
Compound: 36
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Inhibition of tracer K5 binding to N-terminal nano luciferase-fused STK16 (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay
Inhibition of tracer K5 binding to N-terminal nano luciferase-fused STK16 (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay
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[PMID: 32184967] |
| HEK293 | IC50 |
1530 nM
Compound: 36
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Inhibition of tracer K5 binding to N-terminal nano luciferase-fused AAK1 (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay
Inhibition of tracer K5 binding to N-terminal nano luciferase-fused AAK1 (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay
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[PMID: 32184967] |
| HEK293 | IC50 |
6550 nM
Compound: 36
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Inhibition of tracer K5 binding to N-terminal nano luciferase-fused BMP2K (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay
Inhibition of tracer K5 binding to N-terminal nano luciferase-fused BMP2K (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay
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[PMID: 32184967] |
| HEK293 | IC50 |
>10000 nM
Compound: 36
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Inhibition of tracer K5 binding to N-terminal nano luciferase-fused GAK (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay
Inhibition of tracer K5 binding to N-terminal nano luciferase-fused GAK (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay
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[PMID: 32184967] |
In Vitro
SGC-CDKL2/AAK1/BMP2K-1 (0-4 μM, 1 h) disrupts CDKL2-mediated downstream signaling in rat primary neurons by inhibiting CDKL2, and has an inhibitory effect on CDKL2 activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Rat primary neurons
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Concentration:0-4 μM
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Incubation Time:1 h
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Result:Completely suppressed the CDKL2-mediated EB2 (microtubule end binding protein 2) phosphorylation in a dose-dependent manner.
Chemical Information
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CAS No. 2471972-15-1
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Appearance Solid
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Masse moléculaire 426.53
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Formule C22H26N4O3S
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Color White to off-white
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SMILES
O=S(NCC1=CC(C2=CC(NN=C3NC(C4CC4)=O)=C3C=C2)=CC=C1)(CC(C)C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (234.45 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. 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. 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)
In Vivo:
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 (5.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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.
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.
Pureté et documentation
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Fiche technique (271 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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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. 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 | 2.3445 mL | 11.7225 mL | 23.4450 mL | 58.6125 mL |
| 5 mM | 0.4689 mL | 2.3445 mL | 4.6890 mL | 11.7225 mL | |
| 10 mM | 0.2345 mL | 1.1723 mL | 2.3445 mL | 5.8613 mL | |
| 15 mM | 0.1563 mL | 0.7815 mL | 1.5630 mL | 3.9075 mL | |
| 20 mM | 0.1172 mL | 0.5861 mL | 1.1723 mL | 2.9306 mL | |
| 25 mM | 0.0938 mL | 0.4689 mL | 0.9378 mL | 2.3445 mL | |
| 30 mM | 0.0782 mL | 0.3908 mL | 0.7815 mL | 1.9538 mL | |
| 40 mM | 0.0586 mL | 0.2931 mL | 0.5861 mL | 1.4653 mL | |
| 50 mM | 0.0469 mL | 0.2345 mL | 0.4689 mL | 1.1723 mL | |
| 60 mM | 0.0391 mL | 0.1954 mL | 0.3908 mL | 0.9769 mL | |
| 80 mM | 0.0293 mL | 0.1465 mL | 0.2931 mL | 0.7327 mL | |
| 100 mM | 0.0234 mL | 0.1172 mL | 0.2345 mL | 0.5861 mL |
SGC-CDKL2/AAK1/BMP2K-1 Related Classifications
HY-162653 Related Classifications
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