| Identification | Back Directory | [Name]
GSK-3 β inhibitor 2 | [CAS]
1702428-31-6 | [Synonyms]
GSK-3β inhibitor 2
GSK-3 β inhibitor 2 | [Molecular Formula]
C14H14N4O3S | [MDL Number]
MFCD32708518 | [MOL File]
1702428-31-6.mol | [Molecular Weight]
318.35 |
| Chemical Properties | Back Directory | [density ]
1.475±0.06 g/cm3(Predicted) | [solubility ]
DMSO: Sparingly soluble: 1-10 mg/ml | [form ]
Solid | [pka]
13.08±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease[1]. | [in vivo]
The elevation of hyperphosphorylated Tau (pTau) is mimicked in LaFerla 3xTg-C57BL6 mice, and accordingly, these mice are used as an in vivo model of Alzheimer’s disease. GSK-3β inhibitor 2 (Compound 3) shows a significant reduction in pTau396 when administered orally at 30 mg/kg as a nanosuspension to LaFerla 3xTg-C57BL6 male mice. GSK-3β inhibitor 2 shows only modest brain exposure (B/P = 0.26) as determined as a single time point[1]. | [IC 50]
GSK-3β: 1.1 nM (IC50) | [References]
[1] Sivaprakasam P, et al. Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core. Bioorg Med Chem Lett. 2015 May 1;25(9):1856-63. DOI:10.1016/j.bmcl.2015.03.046 |
|
|