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) |
Sigma-Aldrich