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- 文献和实验
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
2234897-35-7
- 规格:
10 mM * 1 mL/5 mg/10 mg/50 mg/100 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥550.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥500.0 |
| 规格: | 10 mg | 产品价格: | ¥800.0 |
| 规格: | 50 mg | 产品价格: | ¥2400.0 |
| 规格: | 100 mg | 产品价格: | ¥4100.0 |
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Grp94 Inhibitor-1
CAS No. : 2234897-35-7
MCE 国际站:Grp94 Inhibitor-1
产品活性:Grp94 Inhibitor-1 是一种有效的、选择性的 Grp94 抑制剂,IC50 值为 2 nM,对 Grp94 的抑制作用是 Hsp90α 的 1000 倍。
研究领域:Cell Cycle/DNA Damage | Metabolic Enzyme/Protease
作用靶点:HSP
In Vitro: Grp94-specific clients include a subset of integrin subunits such as integrin α2 and integrin αL. Their maturation and trafficking to the cell surface are dependent on the Grp94 chaperone function but have no association with cytoplasmic Hsp90α.
Grp94 Inhibitor-1 (1-5 μM; 36 hours) significantly downregulated the cell surface expression levels of integrin α2 and integrin αL in a dose-dependent manner in panc1 cells.
In Vivo: Grp94 Inhibitor-1 (intraperitoneal injection,qid.; coadminbistration 10 mg/kg or 30 mg/kg; 8 days) does not attenuate the colon shortening, but decreases disease activity index (DAI) scores. It also TNFα and IL-6 levels in the serum and colonic tissues and significantly reduces the p65 expression in colonic tissues, especially those in the 30 mg/kg dose group.
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Cellular stress proteins like the classical heat-shock proteins (HSPs) hsp70 (1 –3 ), hsp90 (3 ) and hsp110 (4 ); the glucose-regulated proteins gp96/GRP94 (3 ,5 ) and grp170 (4 ); as well as the endoplasmic chaperone calreticulin
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