半岛bd体育手机客户端 说明
一般描述
A cell-permeable, non-toxic thienyl bis-isothiourea derived compound that acts as a pharmacological chaperone to increase neuronal retromer levels and improve the stability of trimeric Vps35-Vps29-Vps26 retromer complex. Shown to significantly increase the level of Vsp35 (EC50= 3.3 ?M) and Vsp29 in hippocampal neurons. Binds at the interface between Vps35 and Vps29 (Kd= 5 ?M) and interacts with side chains from both proteins. However, it does not affect the thermal unfolding of individual proteins and has no effect on mRNA levels of Vps35 and Vsp29. Shown to reduce the endogenous levels of both Aβ40 and Aβ42 and is also effective in reducing human Aβ40 and -42 levels in J20 transgenic murine model of AD36 (IC50~ 12 ?M). Also reduces the levels of both endogenous β-CTF and sAPPβ and increases the level of sAPPα in the medium. Displays a partial stabilizing effect on Vps35 even in the context of Vps29 knockdown.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
A cell-permeable, non-toxic thienyl bis-isothiourea derived compound that acts as a pharmacological chaperone to increase neuronal retromer levels and improve the stability of trimeric Vps35-Vps29-Vps26 retromer complex. Shown to significantly increase the level of Vsp35 (EC50= 3.3 ?M) and Vsp29 in hippocampal neurons. Binds at the interface between Vps35 and Vps29 (Kd= 5 ?M) and interacts with side chains from both proteins. However, it does not affect the thermal unfolding of individual proteins and has no effect on mRNA levels of Vps35 and Vsp29. Shown to reduce the endogenous levels of both Aβ40 and Aβ42 and is also effective in reducing human Aβ40 and -42 levels in J20 transgenic murine model of AD36 (IC50~ 12 ?M). Also reduces the levels of both endogenous β-CTF and sAPPβ and increases the level of sAPPα in the medium. Displays a partial stabilizing effect on Vps35 even in the context of Vps29 knockdown.
生化/生理作用
Cell permeable: yes
Primary Target
vacuolar protein sorting (Vps) proteins
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 3 months at -20°C.
其他说明
Mecozzi, V.J., et al. 2014.Nat. Chem. Biol.10,443.
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 | C8H12N4S3· xHCl |
| 分子量 | 260.40 (free base basis) |
半岛bd体育手机客户端 性质
| 测定 | ≥92% (HPLC) |
| 质量水平 | 100 |
| 形式 | powder |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze desiccated (hygroscopic) protect from light |
| 颜色 | off-white |
| 溶解性 | water: 50 mg/mL |
| 储存温度 | 2-8℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
