| 产品描述： | 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 |
| 靶点： |
GRP94:2 nM (IC50);GPR; HSP |
| 体外研究： |
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. Western Blot Analysis Cell Line: Panc1 cells Concentration: 1 μM; 2.5 μM; 5 μM Incubation Time: 36 hours Result: Decreased integrin α2 and integrin αL protein expression. |
| 体内研究： |
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. Animal Model: C57BL/6 mice (male, 20-22 g) Dosage: 10 mg/kg or 30 mg/kg Administration: Intraperitoneal injection,qid.; coadminbistration 10 mg/kg or 30 mg/kg Result: Decreased disease activity index (DAI) scores in UC mices. |
| 参考文献： |
1. Jiang F, et al. Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis. J Med Chem. 2018 Nov 8;61(21):9513-9533. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20°C |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.837 ml |
14.186 ml |
28.371 ml |
| 5 mM |
0.567 ml |
2.837 ml |
5.674 ml |
| 10 mM |
0.284 ml |
1.419 ml |
2.837 ml |
| 50 mM |
0.057 ml |
0.284 ml |
0.567 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京