Grp94 Inhibitor-1 |
| رقم الكتالوجGC64988 |
Grp94 Inhibitor-1 هو مثبط فعال ، انتقائي Grp94 بقيمة IC50 تبلغ 2 نانومتر ، وانتقائية تزيد عن 1000 ضعف لـ Grp94 مقابل Hsp90α
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2234897-35-7
Sample solution is provided at 25 µL, 10mM.
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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].
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[1].
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[1].
[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.
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