Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Thiamet G 是一种有效选择性O-GlcNAcase 抑制剂,抑制人 OGA 的Ki 值为 20 nM。O-GlcNAcase 的作用是从修饰的蛋白质中去除 O-GlcNAc。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 286 | 现货 | ||
5 mg | ¥ 497 | 现货 | ||
10 mg | ¥ 828 | 现货 | ||
25 mg | ¥ 1,770 | 现货 | ||
50 mg | ¥ 3,210 | 现货 | ||
100 mg | ¥ 4,680 | 现货 | ||
500 mg | ¥ 9,820 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 516 | 现货 |
产品描述 | Thiamet G is a potent, selective O-GlcNAcase inhibitor with Kiof 21 nM, while exhibiting 37, 000-fold selectivity over human lysosomal –hexosaminidase. |
靶点活性 | O-GlcNAcase (OGA):21 nM(Ki) |
体外活性 | In NGF-differentiated PC-12 cells, inhibition of O-GlcNAcase by Thiamet G increases the cellular levels of O-GlcNAc with EC50 of approximately 30 nM. Thiamet G (100 mM) reduces tau phosphorylation by approximately 2.1-fold, 2.7-fold, 1.2-fold and 1.3-fold for Ser396, Thr231, Ser422 and Ser262, respectively. [1] Thiamet G (12.5 nM and 25 nM) significantly enhances p38 phosphorylation by increasing O-GlcNAcylation in mesangial cells. [2] In O-GlcNAc transferase or O-GlcNAcase gain of function cells, thiamet-G restores the assembly of the spindle and partially rescues histone phosphorylation. [3] |
体内活性 | In rats, thiamet G (50 mg/kg) administrated by i.v. crosses the blood brain barrier and then results in increase in brain O-GlcNAc levels in a dose- and time-dependent manner, and reduction of tau phosphorylation in rat brain. Thiamet G is also orally bioavailable. [1] O-GlcNAc accumulation induced by thiamet G stimulates chondrogenic differentiation in C57/bl mice by increasing the gene expression of differentiation markers, as well as the activity of MMP-2 and -9. [4] |
激酶实验 | All enzymatic assays are performed in triplicate at 37°C using 4-methylumbelliferyl N-acetyl-β-d-glucosaminide dehydrate as substrate. 1 nM of purified OGA is incubated with the compounds for 5 min, and then 0.2 mM of the substrate is added. The liberation of 4-methylumbellifery is monitored by kinetic reading at excitation/emission 355/460 nm using a Tecan M200 plate in a mode of 60 s/cycle and 15 cycles in total. |
细胞实验 | Jurkat cells are seeded at 6000 cells/well in a 96-well plate, and 12 h later, cells are treated with compounds for the indicated time. Cell viability is determined by XTT assay. |
别名 | TMG |
分子量 | 248.3 |
分子式 | C9H16N2O4S |
CAS No. | 1009816-48-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12.4 mg/mL (50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.0274 mL | 20.1369 mL | 40.2739 mL | 100.6847 mL |
5 mM | 0.8055 mL | 4.0274 mL | 8.0548 mL | 20.1369 mL | |
10 mM | 0.4027 mL | 2.0137 mL | 4.0274 mL | 10.0685 mL | |
20 mM | 0.2014 mL | 1.0068 mL | 2.0137 mL | 5.0342 mL | |
50 mM | 0.0805 mL | 0.4027 mL | 0.8055 mL | 2.0137 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Thiamet G 1009816-48-1 Autophagy Others Inhibitor TMG inhibit inhibitor