4-Br-BnIm

Research use only, not for human use.

A potent, subtype-selective Grp94 inhibitor with Kd of 0.96 uM.

A potent, subtype-selective Grp94 inhibitor with Kd of 0.96 uM, 13-fold selectivity over Hsp90α; facilitates mutant myocilin degradation and rescues phenotypes in a transgenic mouse model of hereditary primary open-angle glaucoma.

Cell Viability Assay Cell Line:Primary human HTM cells.Concentration:30 μM.Incubation Time:24 h.Result:Significantly reduced the level of Y437H mutant myocilin without affecting WT myocilin and the RFP vector in HEK cells.Western Blot Analysis Cell Line:HEK cells.Concentration:0, 1, 3, 10, 30 and 100 μM.Incubation Time:24 h.Result:Significantly decreased 1477N mutant myocilin in HEK cells expression without causing the degradation of other Hsp90-dependent clients Akt and Ras.

Animal Model:Tg-MYOCY437Hmice.Dosage:300 μM.Administration:Eye drops; once daily for 12 weeks.Result:Inhibited mutant myocilin expression and restored the PhNR deficits.

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Cytoskeleton/Cell Adhesion Molecules

HSP

HSP

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1654775-71-9

465.728

C20H18BrClN2O4

>98% (HPLC)

In Vitro:?DMSO : 33.33 mg/mL (71.57 mM)

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methyl 2-(2-(1-(4-bromobenzyl)-1H-imidazol-2-yl)ethyl)-3-chloro-4,6-dihydroxybenzoate

(-20℃)

With Ice Pack

≥ 2 years