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CAS No.: 2234897-35-7

Grp94 Inhibitor-1 Catalog No. CSN24783

Synonyms: Grp94 Inhibitor-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[1].

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

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].
参考文献

[1] Wu BX, Hong F, Zhang Y, Ansa-Addo E, Li Z. GRP94/gp96 in Cancer: Biology, Structure, Immunology, and Drug Development. Adv Cancer Res. 2016;129:165‐190.
[2] Jiang F, Guo AP, Xu JC, You QD, Xu XL. Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis. J Med Chem. 2018;61(21):9513‐9533.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8371 mL
- 14.1856 mL
- 28.3712 mL
- 5 mM
- 0.5674 mL
- 2.8371 mL
- 5.6742 mL
- 10 mM
- 0.2837 mL
- 1.4186 mL
- 2.8371 mL

技术信息

CAS号

2234897-35-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H28N2O2

运输

蓝冰

分子量

352.47

别名

Grp94 Inhibitor-1

溶解度

DMSO	115.0 mg/mL (326.3 mM)
Water	insoluble

动物实验配方

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