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GSK-3β inhibitor 2

CAS No. : 1702428-31-6

MCE 国际站：GSK-3β inhibitor 2

产品活性：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。

研究领域：PI3K/Akt/mTOR | Stem Cell/Wnt

作用靶点：GSK-3

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.

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.

相关产品：Bioactive Compound Library Plus | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Wnt/Hedgehog/Notch Compound Library | CNS-Penetrant Compound Library | Anti-Aging Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Anti-Alzheimer’s Disease Compound Library | Anti-Pancreatic Cancer Compound Library | CHIR-99021 | SB 216763 | AR-A014418 | TDZD-8 | Kenpaullone | GSK 3 Inhibitor IX | Cromolyn sodium | R547 | SB 415286 | IM-12 | Indirubin-3'-monoxime | 1-Azakenpaullone | AZD2858 | BIO-acetoxime | CP21R7 | Bikinin | GNF4877 | GSK-3β inhibitor 1 | hSMG-1 inhibitor 11j | TCS 21311 | BIP-135 | 5-Iodo-indirubin-3'-monoxime | Alsterpaullone | GSK-3 inhibitor 1 | Manzamine A hydrochloride | 2B-(SP) | GSK3 Substrate, α, β subunit

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