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PROTACGSK-3β Degrader-1 (compound 1) is a degrader targeting GSK-3β with an IC50 of 833 nM. This compound consists of SB-216763 (a GSK-3β inhibitor), a PEG linker, and CRBN (E3 ligase ligand). It reduces neurotoxicity induced by Aβ25-35 peptide and CuSO4 and is applicable in Alzheimer's disease research.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | PROTACGSK-3β Degrader-1 (compound 1) is a degrader targeting GSK-3β with an IC50 of 833 nM. This compound consists of SB-216763 (a GSK-3β inhibitor), a PEG linker, and CRBN (E3 ligase ligand). It reduces neurotoxicity induced by Aβ25-35 peptide and CuSO4 and is applicable in Alzheimer's disease research. |
| Targets&IC50 | GSK-3β:833 nM |
| In vitro | PROTAC GSK-3β Degrader-1 exhibits low cytotoxicity in SH-SY5Y cells at low concentrations (1.25-40 μM, 24 h), but becomes cytotoxic above 20 μM. At 1 μM for 24 hours, it counteracts neurotoxicity induced by CuSO4 (150 μM) in SH-SY5Y cells. Additionally, at concentrations of 0.5-1 μM for 2 hours, it significantly reduces Aβ 25-35 peptide-induced neurotoxicity in a dose-dependent manner. PROTAC GSK-3β Degrader-1 also decreases GSK-3β protein levels in SH-SY5Y cells dose-dependently (0.5-10 μM, 48 h) with a DC50 of 6.22 μM, and at 10 μM for 24 hours, it degrades GSK-3β protein via the UPS pathway. |
| Formula | C43H42Cl2N6O9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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