Tideglusib(NP-031112)

    • 货号:MC0980
      • CasNo:
      • 865854-05-3
      • 分子式:
      • C19H14N2O2S
      • 纯度:
      • >98%
      • 靶点:
      • GSK-3
      • IC50:
      • IC50: 5 nM (GSK-3βWT), 60 nM (GSK-3βC199A)[1]
      • 体外研究:
      • Tideglusib (NP12) is a small heterocyclic thiadiazolidinone (TDZD) derivative, which is an ATP-non competitive inhibitor of GSK-3β with an IC50value in the micromolar range[2]. Incubation of both astrocyte and microglial cultures with Tideglusib (NP031112) completely abrogates the induction of TNF-α and COX-2 expression after glutamate treatment. These effects of NP031112 are not caused by a loss of cell viability, because the 24 h exposure of astrocyte and microglial cells to this TDZD does not modify cell viability[3].
      • 体内研究:
      • Tideglusib (NP12) treatment correlates with an increase of 46% as an average in the inhibitory phosphorylation of GSK-3β at Ser-9 in the brains of APPsw-tauvlw mice, and the levels of the inactive from of the enzyme in NP12 treated mice are comparable to those found in wild-type littermate controls (p=0.893) (n=6-8 for each treatment). NP12 treatment results in significantly decreased phosphorylation at the putative GSK-3β-directed sites Ser-202 (CP13) and Ser-396/404 (PHF-1) in 15-month-old mice by more than 60% (p=0.023 and p=0.024, respectively)[2]. Injection of Tideglusib (NP031112) (50 mg/kg) into the rat hippocampus dramatically reduces kainic acid-induced inflammation, as measured by edema formation using T2-weighted magnetic resonance imaging and glial activation and has a neuroprotective effect in the damaged areas of the hippocampus[3].
      • 简介:
      • Tideglusib(NP-031112) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM.
      • 特异性:
      • Target: GSK-3. Fields: Tideglusib(NP-031112) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM.
      • 稀释:
      • IC50: 5 nM (GSK-3βWT), 60 nM (GSK-3βC199A)[1]
      • 浓度:
      • >98%
      • 储存:
      • 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
      • 其他名称:
      • NP-12; NP031112; NP 031112; NP-031112
      • 分子量:
      • 334.39
      • 产品图片