GSK-3β inhibitor 2 (C09-1135-497)

GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC 50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's diseaseIn VitroThe 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoThe 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:GSK-3β 1.1 nM (IC 50 ). Specifications and Purity: 96%. Molecular Formula: C14H14N4O3S. Molecular Weight: 318.35. PubChem CID: 73333976. Isomeric SMILES: COC1=C(SC(=N1)C2=CC(=NC=C2)NC(=O)C3CC3)C(=O)N.