4-Br-BnIm ( —— )

产品货号. M12525 CAS No. 1654775-71-9

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

4-Br-BnIm
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

一种有效的亚型选择性 Grp94 抑制剂，Kd 为 0.96 uM。
产品描述

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.
体外实验

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.
体内实验

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.
同义词

——
通路

Cytoskeleton/Cell Adhesion Molecules
靶点

HSP
受体

HSP
研究领域

——
适应症

——

CAS Number

1654775-71-9
分子量

465.728
分子式

C20H18BrClN2O4
纯度

>98% (HPLC)
溶解度

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

——
化学全称

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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