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化學性質:
規(guī)格 | 10mM (in 1mL DMSO) 5mg 25mg |
CAS | 1009816-48-1 |
別名 |
|
化學名 | 2-(ethylamino)-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol |
分子式 | C9H16N2O4S |
分子量 | 248.3 |
溶解度 | ≥ 12.4mg/mL in DMSO, ≥ 100mg/mL in H2O |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
Thiamet G is a potent and selective inhibitor of O-GlcNAcase with Ki value of 21 nM [1].
O-GlcNAcase is an enzyme that removes GlcNAc from proteins. O-GlcNAcylation refers to the posttranslational modification of O-linkage of N-acetyl-glucosamine moieties to threonine and serine residues on proteins [2].
Thiamet G is a potent and selective O-GlcNAcase inhibitor. In kinetic assays, thiamet G competitively inhibited human O-GlcNAcase with Ki value of 21 nM. Thiamet G was extremely stable in aqueous solution. In nerve growth factor (NGF)-differentiated PC-12 cells, thiamet G significantly increased cellular O-GlcNAc levels with EC50 value of 30 nM in a dose dependent way. Thiamet G significantly reduced phosphorylation levels at Ser396 and Thr231 of Tau by 2.1-fold and 2.7-fold, respectively. Also, thiamet G decreased the phosphorylation levels at Ser422 and Ser262 [1]. Thiamet G significantly sensitized human leukemia cell lines to paclitaxel, a microtubule-stabilizing agent [2].
In rats, thiamet G could readily cross the blood brain barrier and dose-dependently increased brain O-GlcNAc levels. Thiamet G reduced tau phosphorylation at Ser396, Thr231 and Ser422 by 2.7, 3.1 and 1.8-fold, respectively [1].
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原創(chuàng)作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業(yè)部
賬 號:2169 2341 6278