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BRD2 Inhibitor II, BIC1-Calbiochem
| 产品编号： | 4155433 |
| 规格： | The BRD2 Inhibitor II, BIC1 controls the biological activity of BRD2. |
| 包装规格： | 10 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
BRD2 Inhibitor II, BIC1-Calbiochem
1-(2-(1H-Benzimidazol-2-ylsulfanyl)ethyl)-3-methyl-1,3-dihydro-2H-benzimidazole-2-thione, 1-(2-(1H-Benzo[d]imidazol-2-ylthio)ethyl)-3-methyl-1H-benzo[d]imidazole-2(3H)-thione, BRD2 Bromodomain-Interactive Compound, BIC1
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C17H16N4S2 |
| Molecular weight | 340.47 |
| MDL number | MFCD03034582 |
| General description【一般描述】 | A cell-permeable benzimidazolyl-benzimidazolothione that targets the BD1 domain of the BET family member BRD2 (Kd = 28 µM), making it inaccessible for acetylated H4K12 (histone H4 Lys12) binding. Shown to effectively inhibit TSA- (Cat. No. 647925; 1 h 1 µM) induced BRD2 BD1-H4K12 association in COS7 cells (100% inhibition by 60 µM BIC1) and greatly suppress active Ras-induced SV40 promoter transcription activity in HeLa cells (70% inhibition by 5 µM BIC1), while being much less effective against BRDT BD1 binding to acetylated H4K5/K8. A cell-permeable benzimidazolyl-benzimidazolothione that targets BD1 (bromodomain 1) of the BET (bromodomain and extra terminal domain) family member BRD2 (Kd = 28 µM in equilibrium binding studies by SPR, using human BRD2 aa 74-194), making it inaccessible for acetylated H4K12 (histone H4 Lys12) binding. Shown to effectively inhibit TSA- (Cat. No. 647925; 1 h 1 µM) induced BRD2 BD1-H4K12 association in COS7 cells (59% and 100% inhibition, respectively, by 10 and 60 µM BIC1) and greatly suppress active Ras-induced SV40 promoter transcriptional activation in RasV12-transfected HeLa cells (70% inhibition by 5 µM BIC1), while being much less effective against BRDT BD1 and acetylated H4K5/K8 interaction in TSA-stimulated COS7 cells (Maximum inhibition = 47% by 60 µM BIC1). |
| Warning【警告】 | Toxicity: Regulatory Review (Z) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. |
| Other Notes【其他说明】 | Ito, T., et al. 2011. Chem. Biol.18, 495. |
| 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】 | ≥95% (HPLC) |
| form【形式】 | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | off-white |
| solubility【溶解性】 | DMSO: 50 mg/mL |
| shipped in【运输】 | ambient |
| storage temp.【储存温度】 | −20℃ |
| SMILES string | S=C(N(C)C1=C2C=CC=C1)N2CCSC3=NC4=C(N3)C=CC=C4 |
| packaging【包装】 | 10 mg in Glass bottle Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 2 |
