GSK-3β inhibitor 2 (Compound 3) 是一种有效，选择性和口服活性的 GSK-3β 抑制剂，IC₅₀ 为 1.1 nM。GSK-3β inhibitor 2 可以穿越血脑屏障。GSK-3β inhibitor 2 有用于阿尔茨海默氏病的潜力。

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 Alzheimers disease.

Solid

GSK-3β 1.1 nM (IC50)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 5 mg/mL (15.71 mM; Need ultrasonic)配制储备液