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GSK-3β inhibitor 2 (5-Thiazolecarboxamide,2-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]-4-methoxy-) is a BBB-crossing and selective inhibitor of GSK-3β (IC50 = 1.1 nM). GSK-3β inhibitor 2 can be used in studies about Alzheimer's disease.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $50 | In Stock | |
10 mg | $67 | In Stock | |
25 mg | $107 | In Stock | |
50 mg | $197 | In Stock |
Description | GSK-3β inhibitor 2 (5-Thiazolecarboxamide,2-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]-4-methoxy-) is a BBB-crossing and selective inhibitor of GSK-3β (IC50 = 1.1 nM). GSK-3β inhibitor 2 can be used in studies about Alzheimer's disease. |
Targets&IC50 | GSK-3β:1.1 nM |
In vitro | The pyridine carboxamide of GSK-3β inhibitor 2 forms hydrogen bonds with the hinge V135 backbone amide, while the carbonyl oxygen of the thiazolyl primary amide establishes a critical hydrogen bond with K85. Single crystal X-ray diffraction confirms intramolecular hydrogen bonding between the methoxy -O- and the amide N-H in GSK-3β inhibitor 2 [1]. |
In vivo | In LaFerla 3xTg-C57BL6 mice with Alzheimer’s disease, GSK-3β inhibitor 2 (30 mg/kg; oral) significantly reduces hyperphosphorylated Tau396. GSK-3β inhibitor 2 shows only modest brain exposure (B/P = 0.26), determined as a single time point[1]. |
Alias | 5-Thiazolecarboxamide,2-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]-4-methoxy- |
Molecular Weight | 318.35 |
Formula | C14H14N4O3S |
Cas No. | 1702428-31-6 |
Smiles | COc1nc(sc1C(N)=O)-c1ccnc(NC(=O)C2CC2)c1 |
Relative Density. | 1.475 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 5 mg/mL (15.71 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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