半岛bd体育手机客户端 说明
一般描述
A cell-permeable carbazolohydroxamate that acts as a highly potent HDAC6-selective inhibitor (IC50= 15 nM) with much reduced or no activity against other known HDACs. Effectively prevents neuronal cell death (by ≥95% at 10 ?M) upon oxidative stress induction by HCA and selectively induces cellular α-tubulin, but not histone H4, hyperacetylation (2.5 to 5 ?M) in primary rat cortical neuron cultures.
A cell-permeable carbazolohydroxamate whose zinc-chelating hydroxamic acid moiety and catalytic channel rim-targeting aromatic cap structure render it a highly potent HDAC6-selective inhibitor (IC50= 15 nM against recombinant human HDAC6) with much reduced or no activity against HDAC8, HDAC1 (IC50= 0.854 and 16.4 ?M, respectively), and other known HDACs (HDAC2/3/4/5/7/9/10/11; IC50>30 ?M). Shown to selectively block HDAC6-, but not HDAC1-, dependent cellular deacetylation as evidenced by its selective induction (2.5 to 5 ?M) of α-tubulin, but not histone H4, hyperacetylation in cultured primary rat cortical neurons. Although failing to block cellular glutathione depletion by homocysteic acid (HCA), Tubastatin A nevertheless is reported to prevent neuronal cell death upon oxidative stress induction by HCA in a dose-dependent manner (≥95% protection at 10 ?M), presumably by preventing peroxiredoxins deacetylation.
包装
5 mg in Glass bottle
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Butler, K.V., et al. 2010.J. Am. Chem. Soc.132,10842.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C20H21N3O2 |
分子量 | 335.40 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem? |
储存条件 | OK to freeze desiccated (hygroscopic) protect from light |
颜色 | tan |
溶解性 | DMSO: 10 mg/mL ethanol: 250 μg/mL |
运输 | ambient |
储存温度 | ?20℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 2 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich