Grp94 Inhibitor-1

Research use only, not for human use.

Grp94 Inhibitor-1 is a potent selective Grp94 inhibitor (IC50 : 2 nM).

Grp94 Inhibitor-1 is a potent selective Grp94 inhibitor (IC50 : 2 nM).

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.

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.

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Cell Cycle/DNA Damage

GPR

Grp94

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2234897-35-7

352.47

C22H28N2O2

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (709.28 mM)

CC(C)c1ccc(cc1)-c1ccc(N[C@H]2CC[C@H](O)CC2)c(c1)C(N)=O

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(-20℃)

With Ice Pack

≥ 2 years