货号	规格	价格	上海	北京	武汉	南京
S80015-5mg	99%	￥346.80 S80015-5mg ￥346.80 现货	3 3	-	-	-
S80015-10mg	99%	￥578.00 S80015-10mg ￥578.00 现货	3 3	-	-	-
S80015-25mg	99%	￥1258.00 S80015-25mg ￥1258.00 现货	1 1	-	-	-

产品介绍

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

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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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Thiamet G