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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.
参考价格
1538.21 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

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 µM pretreatment) and effectively prevent LPS-, heat-killed Salmonella typhimurium-, and CLP- (caecal ligation and puncture) induced death in mice in 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 µL) 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

产品性质

质量水平100
测定≥98% (HPLC)
形式liquid
manufacturer/tradenameCalbiochem®
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
WGKWGK 2
闪点(F)188.6 °F - (refers to pure substance)
闪点(C)87 ℃ - (refers to pure substance)

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