产品说明
一般描述
A cell-permeable, low molecular weight hydroxamate compound that acts as a potent histone deacetylase class IIb HDAC6-selective inhibitor (IC50 = 30 nM), while inhibiting class I HDAC1/2/3/8 only at higher concentrations (IC50 = 0.638, 1.79, 0.694, and 1.09 µM, respectively) and exhibiting much reduced potency against class IIa HDAC4/5/7/9 (IC50 >12.61 µM). Shown to selectively upregulate HDAC6 substrate α-tubulin acetylation in HeLa cells (10 & 30 µM; 24 h) without inducing histone H3 acetylation increase seen with another HDAC6-selective inhibitor Tubastatin A (Cat. No. 382187). Unlike other Zinc-binding group-containing HDAC inhibitors, BRD9757 does not contain an apparent selectivity-imparting capping structure linked to its hydroxamate.
A cell-permeable, low molecular weight hydroxamate compound that acts as a potent histone deacetylase class IIb HDAC6-selective inhibitor (IC50 = 30 nM), while inhibiting class I HDAC1/2/3/8 only at higher concentrations (IC50 = 0.638, 1.79, 0.694, and 1.09 µM, respectively) and exhibiting much reduced or little potency against class IIa HDAC4/5/7/9 (IC50 = 21.80, 18.32, 12.61, and >33.33 µM, respectively). Shown to selectively upregulate HDAC6 substrate α-tubulin acetylation level in HeLa cells (10 & 30 µM; 24 h) without inducing detectable histone H3 acetylation increase seen in cells treated with another HDAC6-selective inhibitor Tubastatin A (Cat. No. 382187) or the general HDAC inhibitor SAHA. BRD9757 does not contain an apparent selectivity-imparting capping structure linked to the zinc-binding hydroxamate as seen in other ZBG- (Zinc binding group) containing HDAC inhibitors.
生化/生理作用
Cell permeable: yes
Primary Target
HDAC6
Reversible: yes
包装
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
Wagner, F.F., et al. 2013. J. Med. Chem.56, 1772.
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 | C6H9NO2 |
| 分子量 | 127.14 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze protect from light |
| 颜色 | pale orange |
| 溶解性 | DMSO: 100 mg/mL |
| 储存温度 | 2-8℃ |
安全信息
| 象形图 |  |
| 警示用语： | Warning |
| 危险声明 | H319 - H412 |
| 预防措施声明 | P264 - P273 - P280 - P305 + P351 + P338 - P337 + P313 - P501 |
| 危险分类 | Aquatic Chronic 3 - Eye Irrit. 2 |
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
