GRP94

    
98%

GRP94

源叶(MedMol)
S87701 一键复制产品信息
2234897-35-7
C22H28N2O2
352.47
货号 产品规格 价格(RMB) 库存(上海) 北京 武汉 南京 购买数量
S87701-5mg 98% ¥280.00 >10 - - -
S87701-10mg 98% ¥450.00 >10 - - -
S87701-25mg 98% ¥800.00 >10 - - -
S87701-50mg 98% ¥1300.00 >10 - - -
S87701-100mg 98% ¥2300.00 10 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

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

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
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参考文献

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