Grp94 Inhibitor-1
产品说明书
 |
同义名 : | - |
| CAS号 : | 2234897-35-7 | |
| 货号 : | A1176950 | |
| 分子式 : | C22H28N2O2 | |
| 纯度 : | 98%+ | |
| 分子量 : | 352.47 | |
| MDL号 : | MFCD32067891 | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Glucose-regulated protein 94 (GRP94), also known as gp96, is an endoplasmic reticulum (ER) paralog of heat-shock protein (HSP90). GRP94, induced by the accumulation of misfolded proteins, binds and hydrolyzes ATP and plays critical roles in general protein quality control in the ER[1]. Grp94 Inhibitor-1 is a potent, selective GRP94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α. Dextran sulfate sodium (DSS) induced mouse model of ulcerative colitis (UC) were treated with 10 mg/kg or 30 mg/kg of Grp94 Inhibitor-1, and the both dosages decreased the disease activity index (DAI) scores, significantly reduced the cytokine levels in a dose-dependent manner, which indicates Grp94 Inhibitor-1 is a potential UC treatment agent[2]. | ||
| 作用机制 | Grp94 Inhibitor-1 fits well into the Grp94 ATP-binding pocket[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.84mL 0.57mL 0.28mL |
14.19mL 2.84mL 1.42mL |
28.37mL 5.67mL 2.84mL |
| 参考文献 |
|---|