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InSolution I-BET-CAS 1260907-17-2-Calbiochem

品牌
Sigma-Aldrich
CAS
1260907-17-2
货号
5.06071
规格纯度
A 50 mM sterile-filtered solution of I-BET in DMSO.
价格
1538.21 *本价格含增值税费
促销
服务
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  • 增值税票
数量
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半岛bd体育手机客户端 名称:
1260907-17-2
InSolution I-BET-CAS 1260907-17-2-Calbiochem
( S)-2-(6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide
( S)-2-(6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

一般描述

A cell-permeable benzodiazepine compound that binds the tandem bromodomains of BET (bromodomain and extra terminal domain) family members BRD2 (1-473), BRD3 (1-434), and BRD4 (1-477) with high affinity (Kd= 61.3, 50.5, and 55.2 nM, respectively, by ITC) and effectively competes against tetra-acetylated H4 peptide (Millipore cat. no. 12-379) for BRD2/3/4 binding (IC50= 32.5, 42,4, and 36.1 nM, respectively, in competitive equilibrium binding assays), while exhibiting little affinity toward 5 other bromodomain-containing proteins (ATAD2, BAZ2B, CREBBP, PCAF, SP140) or a panel of 38 cellular enzymes, GPCRs, transporters, and ion channels. Shown to differentially modulate LPS-induced gene expression, notably suppressing LPS-induced upregulation of genes involved in inflammatory response, in murine BMDMs (bone marrow-derived macrophages)in vitro(30 min 1 ?M pretreatment) and effectively prevent LPS-, heat-killedSalmonella typhimurium-, and CLP- (caecal ligation and puncture) induced death in micein vivo(30 mg/kg i.v.). Cellular Brd2/3/4 knockdown using siRNA results in mostly the same effect as I-BET treatment in modulating LPS gene induction profile in murine BMDMs, but not without exceptions, indicating that not all BET-dependent transcription regulations are mediated via its binding to acetylated histones.

生化/生理作用

Cell permeable: yes
Primary Target
tandem bromodomains of BET
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

外形

A 50 mM (5 mg/236 ?L) sterile-filtered solution of I-BET (Cat. No. 401010) in DMSO.

重悬

Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C.

其他说明

Nicodeme, E., et al. 2010.Nature468,1119.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式 C22H22ClN5O2
分子量 423.90
MDL编号 MFCD22417091

半岛bd体育手机客户端 性质

质量水平 100
测定 ≥98% (HPLC)
形式 liquid
manufacturer/tradename Calbiochem?
储存条件 OK to freeze
avoid repeated freeze/thaw cycles
desiccated (hygroscopic)
protect from light
储存温度 ?70℃

安全信息

储存分类代码 10 - Combustible liquids
WGK WGK 2
闪点(F) 188.6 °F - (refers to pure substance)
闪点(C) 87 ℃ - (refers to pure substance)

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