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GSK-3β inhibitor 2

CAS No. : 1702428-31-6

MCE 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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