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S80015

Thiamet G

源叶(MedMol) 99%
  • 英文名:
  • Thiamet G
  • 别名:
  • Thiamet G0nDiscontinued; Thiamet G; Thiamet G;
  • CAS号:
  • 1009816-48-1
  • 分子式:
  • C9H16N2O4S
  • 分子量:
  • 248.2993
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S80015-5mg 99% ¥346.80元 4 - - - EA 加入购物车
源叶(MedMol) S80015-10mg 99% ¥578.00元 5 - - - EA 加入购物车
源叶(MedMol) S80015-25mg 99% ¥1258.00元 2 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Thiamet G is a potent and selective inhibitor of O-GlcNAcase (OGA), which acts to remove O-GlcNAc from modified proteins, with Ki of 20 nM for human OGA
  • 靶点: Ki: 20 nM (Human OGA);Autophagy
  • 体外研究:
    Thiamet G (1 μM) induces a clear increase in the accumulation of O-GlcNAcylated proteins of ATDC5 cells. O-GlcNAc accumulation induced by Thiamet G also evokes a clear increase in the activity of these MMPs. Thiamet G (1 μM) induces the phosphorylation of JNK, ERK, and p38 but not phosphorylation of Akt. Thiamet G (0.1-10 μM) does not significantly affect the cell viability. Thiamet G decreases phosphorylation of tau and alters the microtubule dynamics
  • 体内研究:
    Thiamet G (500 mg/kg/d) increases global and tau O-GlcNAc and reduces neurodegeneration. Thiamet G-treated group has 1.4-fold more motor neurons and hinders tau-driven neurodegeneration within this transgenic model. Thiamet G treatment therefore has no detectable effect on mice lacking the P301L transgene, indicating that prevention of neurodegeneration and weight loss is mediated by Thiamet G treatment only in the context of the P301L transgene. In Thiamet G-treated mice, the O-GlcNAc increases in the brain and spinal cord tissues. Thiamet G (20 mg/kg, i.p.) increases O-GlcNAc levels in brain, liver, and knee of the C57BL/6 mice in a dose-dependent manner
  • 参考文献:
    1. Yuzwa SA, et al. Increasing O-GlcNAc slows neurodegeneration and stabilizes tau against aggregation. Nat Chem Biol. 2012 Feb 26;8(4):393-9.2. Andrés-Bergós J, et al. The increase in O-linked N-acetylglucosamine protein modification stimulates chondrogenic differentiation both in vitro and in vivo. J Biol Chem. 2012 Sep 28;287(40):33615-28. 3. Ding N, et al. Thiamet-G-mediated inhibition of O-GlcNAcase sensitizes human leukemia cells to microtubule-stabilizing agent NSC 125973. Biochem Biophys Res Commun. 2014 Oct 24;453(3):392-7.
  • 溶解性: Soluble  in  DMSO、H2O
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 4.027 ml 20.137 ml 40.274 ml
    5 mM 0.805 ml 4.027 ml 8.055 ml
    10 mM 0.403 ml 2.014 ml 4.027 ml
    50 mM 0.081 ml 0.403 ml 0.805 ml
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