包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
25mg | 电议 |
Thiamet G, a potent inhibitor of O-GlcNAcase (Ki =21 nM) was used to increase O-GlcNAcylation levels .
Cell lines | A549, HT29 and H1299 cell lines |
Preparation Method | Cells were treated with 5 μM Thiamet-G for 24 h or the indicated time period. |
Reaction Conditions | 5μM for 24 hours |
Applications | Thiamet G could markedly elevate the O-GlcNAcylation of A549, H1299 and HT29 cells. Thiamet-G treatment did not significantly affect the proliferation of A549, H1299 and HT29. Thiamet-G treatment significantly increased colony formation ability of A549, H1299 and HT29 cells. |
Animal models | Six-week-old male Sprague-Dawley rats |
Preparation Method | For tau western blot study, rats were treated orally with thiamet-G, by inclusion of inhibitor in the drinking water at a dose of 200 mg kg-1 d-1. Animals were euthanized after one day of treatment. For the thiamet-G dose and time dependency study, six-week-old male Sprague-Dawley rats received single intravenous tail vein injections of either 2, 10 or 50 mg kg-1 and were euthanized at indicated times. |
Dosage form | 200 mg kg-1 d-1, oralGBP>>2, 10 or 50 mg kg-1 d-1, intravenous injection. |
Applications | Thiamet-G is orally bioavailable, thiamet-G can cross the blood brain barrier and inhibit O-GlcNAcase in vivo to cause increased O-GlcNAc levels in brain. |
产品描述 | Thiamet G, a potent inhibitor of O-GlcNAcase (Ki =21 nM) was used to increase O-GlcNAcylation levels[1]. Thiamet G is a stable compound whose fused thiazoline ring system geometrically mimics a transition state of the substrate-assisted enzymatic hydrolysis of protein-O-GlcNAc units and, in this way, effectively inhibits O-GlcNAcase function[2]. Thiamet-G is orally bioavailable, and thiamet-G can cross the blood brain barrier[1]. Thiamet G (5 μM, 24h) could markedly elevate the O-GlcNAcylation of human lung epithelial carcinoma A549, non-small cell lung carcinoma H1299 and colon tumor HT29 cells[3]. Thiamet G (25 μM, 24 h) treated PC-12 cells showed a gradual time-dependent increase in cellular O-GlcNAc levels that reached a maximum after approximately 12 h of exposure[1]. Thiamet G (2.5 μl of 35 μg/μl) dissolved in 0.9% NaCl was injected bilaterally into the lateral ventricles of the brains at a dose of 175 μg/mouse, RL2 positive bands showed a 5-fold increase in global O-GlcNAcylation 4.5 h after thiamet G injection and a 10-fold increase 24 h after injection[4]. Thiamet G (500 mg/kg/day p.o.) treatment was able to decrease the number of neurons showing tau pathology, decrease behavioral defects and reduce mice mortality in the Tau.P301L mouse model[5]. Thiamet-G treated Tau.P301L mice for 3 days in the drinking water (2.5 mg/ml) in the home-cage, improved their breathing deficit in normocapnia and in hypercapnia[6]. References: |