產品描述: 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 |
靶點:
GRP94:2 nM (IC50);GPR;?HSP |
體外研究:
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. |
體內研究:
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. |
參考文獻:
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 |
保存條件:
-20°C |
配置溶液濃度參考:
|
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: |
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