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GSK3β-IN-3 is an ATP-competitive GSK-3β inhibitor (IC50= 0.90 μM) that demonstrates good blood-brain barrier permeability (Pe= 10.7 x 10^-6 cm/s). It effectively reduces tau protein phosphorylation in the BR5706 strain and decreases Aβ aggregate deposition in the CL2006 strain, indicating its potential as a candidate for Alzheimer's disease (AD) research.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | GSK3β-IN-3 is an ATP-competitive GSK-3β inhibitor (IC50= 0.90 μM) that demonstrates good blood-brain barrier permeability (Pe= 10.7 x 10^-6 cm/s). It effectively reduces tau protein phosphorylation in the BR5706 strain and decreases Aβ aggregate deposition in the CL2006 strain, indicating its potential as a candidate for Alzheimer's disease (AD) research. |
| Targets&IC50 | GSK-3β:0.90 μM |
| In vitro | GSK3β-IN-3 (compound 66) effectively inhibits GSK-3β with an IC50 of 0.90 μM at concentrations ranging from 0.01 to 100 μM. Additionally, GSK3β-IN-3 exhibits ATP-competitive inhibition of the GSK-3β enzyme at concentrations of 0-50 μM. |
| In vivo | GSK3β-IN-3 (compound 66), at a concentration of 10 μM, reduces p-Tau (Ser396) levels in the Caenorhabditis elegans BR5706 strain. It also increases the number of flagella and reduces Aβ deposition in the C. elegans CL2006 strain. Furthermore, GSK3β-IN-3 demonstrates good stability in human microsomes and shows potential for crossing the blood-brain barrier in PAMPA-BBB assays. It has a high plasma protein binding rate of 96.4%. |
| Molecular Weight | 310.80 |
| Formula | C14H15ClN2O2S |
| Cas No. | 301359-45-5 |
| Smiles | O=C(OCC)C1=C(NC(=S)NC1C=2C=CC=CC2Cl)C |
| 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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