4-Br-BnIm( —— )

Catalog No. M12525 CAS No. 1654775-71-9

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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Product Name

4-Br-BnIm
Note

Research use only, not for human use.
Brief Description

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

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.
In Vitro

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.
In Vivo

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.
Synonyms

——
Pathway

Cytoskeleton/Cell Adhesion Molecules
Target

HSP
Recptor

HSP
Research Area

——
Indication

——

CAS Number

1654775-71-9
Formula Weight

465.728
Molecular Formula

C20H18BrClN2O4
Purity

>98% (HPLC)
Solubility

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

——
Chemical Name

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

1. Stothert AR, et al. Sci Rep. 2017 Dec 20;7(1):17951. 2. Crowley VM, et al. J Med Chem. 2016 Apr 14;59(7):3471-88.

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