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.
IC50&Target
GRP94
2 nM (IC50)
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.
分子式
C22H28N2O2
分子量
352.47
CAS号
2234897-35-7
运输条件
Room temperature in continental US; may vary elsewhere.