化合物Thiamet G T6056
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
25 mg | 1009816-48-1 | ¥1,770.00 | 询底价 |
5 mg | 1009816-48-1 | ¥497.00 | 询底价 |
2 mg | 1009816-48-1 | ¥286.00 | 询底价 |
500 mg | 1009816-48-1 | ¥9,820.00 | 询底价 |
10 mg | 1009816-48-1 | ¥828.00 | 询底价 |
50 mg | 1009816-48-1 | ¥3,210.00 | 询底价 |
100 mg | 1009816-48-1 | ¥4,680.00 | 询底价 |
1 mL | 1009816-48-1 | ¥516.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Thiamet G
描述: 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。
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.
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.
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]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 12.4 mg/mL (50 mM)
关键字: Thiamet G | Autophagy | Inhibitor | inhibit
相关产品: Indole-3-Glyoxylyl Chloride | Tanespimycin | Soyasapogenol B | Pogostone | Acacetin | Novobiocin Sodium | AG490 | Hydroxychloroquine sulfate | Oprozomib | GSK621
相关库: Anti-Aging Compound Library | Bioactive Lipid Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Highly Selective Inhibitor Library | Autophagy Compound Library | NO PAINS Compound Library | Bioactive Compound Library
化合物Thiamet G T6056信息由TargetMol中国为您提供,如您想了解更多关于化合物Thiamet G T6056报价、型号、参数等信息,欢迎来电或留言咨询。
注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途