1702428-31-6
1702428-31-6 structure
- Name: GSK-3β inhibitor 2
- Chemical Name: GSK-3β inhibitor 2
- CAS Number: 1702428-31-6
- Molecular Formula: C14H14N4O3S
- Molecular Weight: 318.35
- Catalog: Signaling Pathways PI3K/Akt/mTOR GSK-3
- Create Date: 2020-04-20 00:24:05
- Modify Date: 2024-01-23 17:45:10
-
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].
| Name | GSK-3β inhibitor 2 |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
GSK-3β:1.1 nM (IC50) |
| In Vitro | The pyridine carboxamide of GSK-3β inhibitor 2 (Compound 3) makes hydrogen bonds with the hinge V135 backbone amide, and the carbonyl oxygen of the thiazolyl primary amide formed a critical hydrogen bond with K85. The quality of the electron density for the methyl group of the methoxy moiety in GSK-3β inhibitor 2 does not allow its unambiguous placement in the model, but a small molecule crystal structure of GSK-3β inhibitor 2 determined by single crystal X-ray diffraction method confirmed the intramolecular hydrogen bonding between the methoxy -O- and the amide N-H in GSK-3β inhibitor 2[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]. |
| References |
| Molecular Formula | C14H14N4O3S |
|---|---|
| Molecular Weight | 318.35 |