PROTAC GSK-3β Degrader-1
Based on 1 Customer Validation
PROTAC GSK-3β Degrader-1 (compound 1) is a degrader targets GSK-3β PROTAC degrader with an IC50 value of 833 nM. PROTAC GSK-3β Degrader-1 contains SB-216763 (a GSK-3β inhibitor), a PEG linker and a CRBN (E3 ligase liand). PROTAC GSK-3β Degrader-1 reduces the neurotoxicity induced by Aβ25-35 peptide and CuSO4. PROTAC GSK-3β Degrader-1 can be used to research in Alzheimer's disease.
(Pink: GSK-3β ligand (HY-12012); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W068828)).
For research use only. We do not sell to patients.
- Purity: 99.05%
- CAS No.: 3093409-30-1
- Formula: C43H42Cl2N6O9
- Molecular Weight:857.73
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Storage: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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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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All PROTACs Isoforms
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Biological Activity
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GSK-3β 833 nM (IC50) |
PROTAC GSK-3β Degrader-1 (1.25-40 μM, 24 h) exhibits low cytotoxicity at low doses, exhibits cytotoxicity exceeds 20 μM in SH-SY5Y[1].
PROTAC GSK-3β Degrader-1 (1 μM, 24 h) counteracts the neurotoxicity induced by CuSO4 (150 μM) in SH-SY5Y[1].
PROTAC GSK-3β Degrader-1 (0.5-1 μM, 2 h) reduces the neurotoxicity induced by Aβ25-35 peptide, in a dose-dependent manner in SH-SY5Y[1].
PROTAC GSK-3β Degrader-1 (0.5-10 μM, 48 h) reduces GSK-3β protein levels in a dose-dependent manner in SH-SY5Y, with a DC50 value of 6.22 μM[1].
PROTAC GSK-3β Degrader-1 (10 μM, 24 h) degrades GSK-3β protein involves UPS in SH-SY5Y[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y
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Concentration:0.5 μM, 1 μM
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Incubation Time:2 h, 24 h
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Result:Counteracted the neurotoxicity induced by CuSO4 at 1 μM for 24 h.
Reduced the neurotoxicity induced by Aβ25-35 peptide in a dose-dependent manner for 2 h.
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Cell Line:SH-SY5Y
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Concentration:0.5 μM, 1 μM, 5 μM, 10 μM
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Incubation Time:48 h
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Result:Decreased GSK-3β protein levels in a dose-dependent manner, with a DC50 value of 6.22 μM.
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Cell Line:SH-SY5Y
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Concentration:10 μM
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Incubation Time:24 h
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Result:Had no effect on the total GSK-3β protein level in the presence of lactacystin at a concentration of 5 μM.
Chemical Information
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CAS No. 3093409-30-1
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Appearance Solid
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Molecular Weight 857.73
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Formula C43H42Cl2N6O9
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Color Yellow to orange
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SMILES
ClC1=CC(Cl)=CC=C1C(C(NC2=O)=O)=C2C3=CN(C4=CC=CC=C34)CC(NCCCOCCCCOCCCNC5=C(C6=CC=C5)C(N(C6=O)C7CCC(NC7=O)=O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (116.59 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)
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 (2.91 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.
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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. 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 | 1.1659 mL | 5.8293 mL | 11.6587 mL | 29.1467 mL |
| 5 mM | 0.2332 mL | 1.1659 mL | 2.3317 mL | 5.8293 mL | |
| 10 mM | 0.1166 mL | 0.5829 mL | 1.1659 mL | 2.9147 mL | |
| 15 mM | 0.0777 mL | 0.3886 mL | 0.7772 mL | 1.9431 mL | |
| 20 mM | 0.0583 mL | 0.2915 mL | 0.5829 mL | 1.4573 mL | |
| 25 mM | 0.0466 mL | 0.2332 mL | 0.4663 mL | 1.1659 mL | |
| 30 mM | 0.0389 mL | 0.1943 mL | 0.3886 mL | 0.9716 mL | |
| 40 mM | 0.0291 mL | 0.1457 mL | 0.2915 mL | 0.7287 mL | |
| 50 mM | 0.0233 mL | 0.1166 mL | 0.2332 mL | 0.5829 mL | |
| 60 mM | 0.0194 mL | 0.0972 mL | 0.1943 mL | 0.4858 mL | |
| 80 mM | 0.0146 mL | 0.0729 mL | 0.1457 mL | 0.3643 mL | |
| 100 mM | 0.0117 mL | 0.0583 mL | 0.1166 mL | 0.2915 mL |
PROTAC GSK-3β Degrader-1 Related Classifications
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