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InSolution I-BET-CAS 1260907-17-2-Calbiochem
| 产品编号： | 4083678 |
| 规格： | A 50 mM sterile-filtered solution of I-BET in DMSO. |
| CAS NO： | 1260907-17-2 |
| 包装规格： | 5 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品价格查看更多规格...
| 产品编号 | 包装单位 | 单价(元) | 国内现货 | 国外库存 | 询价单 |
| 4083678 | 5 MG | 1690 |
产品别名
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
基本信息
| Empirical Formula【经验(实验)分子式】 | C22H22ClN5O2 |
| Molecular weight | 423.90 |
| MDL number | MFCD22417091 |
| General description【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. |
| Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Primary Target tandem bromodomains of BET Reversible: yes |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Physical form【外形】 | A 50 mM (5 mg/236 µL) sterile-filtered solution of I-BET (Cat. No. 401010) in DMSO. |
| Reconstitution【重悬】 | Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C. |
| Other Notes【其他说明】 | Nicodeme, E., et al. 2010. Nature468, 1119. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | liquid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze avoid repeated freeze/thaw cycles desiccated (hygroscopic) protect from light |
| storage temp.【储存温度】 | −70℃ |
| packaging【包装】 | Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 10 - Combustible liquids |
| WGK | WGK 2 |
| Flash Point(F)【闪点(F)】 | 188.6 °F - (refers to pure substance) |
| Flash Point(C)【闪点(C)】 | 87 ℃ - (refers to pure substance) |
