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merck millipore,默克密理博,401010,I-BET - CAS 1260907-17-2 - Calbiochem
产品名称：I-BET - CAS 1260907-17-2 - Calbiochem
产品型号：401010
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 affinit More>>
merck millipore,默克密理博,401010,I-BET - CAS 1260907-17-2 - Calbiochem
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重要规格表
经验配方 CAS号 C₂₂H₂₂ClN₅O₂ 1260907-17-2 描述 概述 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. Also available as a 50 mM solution in DMSO (Cat. No. 506071). 产品目录编号 401010 品牌系列 Calbiochem®
同义词 GSK525762A, (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, (2-[(4chlorophenyl)-1-methyl-8-(methyloxy)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide, BRD2 Inhibitor I, BRD3 Inhibitor I, BRD4 Inhibitor I 参考 参考 Nicodeme, E., et al. 2010. Nature 468, 1119. 产品信息 CAS号 1260907-17-2 形式 Yellowish white solid Hill配方 C₂₂H₂₂ClN₅O₂ 化学配方 C₂₂H₂₂ClN₅O₂ Molar Mass 423.9 结构配方图像 生物信息 纯度 ≥98% by Chiral HPLC 理化信息 溶解度 DMSO 储存和货运信息 货运代码 Shipped with Blue Ice or with Dry Ice
毒性 Regulatory Review
储存 -20°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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