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[1].
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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]. |
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 2234897-35-7 |
分子式 | C22H28N2O2 |
分子量 | 352.47 |
SMILES Code | O[C@@H](CC1)CC[C@H]1NC2=C(C(N)=O)C=C(C3=CC=C(C(C)C)C=C3)C=C2 |
MDL No. | MFCD32067891 |
别名 | |
运输 | 蓝冰 |
InChI Key | JMGDXIHGWTVBMX-UHFFFAOYSA-N |
Pubchem ID | 137321151 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, inert atmosphere, room temperature |
溶解方案 |
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