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- 详细信息
- 文献和实验
- 技术资料
- CAS号:
1374601-40-7
- 规格:
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg
| 规格: | 1mg | 产品价格: | ¥174.0 |
|---|---|---|---|
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥332.0 |
| 规格: | 5mg | 产品价格: | ¥356.0 |
| 规格: | 10mg | 产品价格: | ¥574.0 |
| 规格: | 25mg | 产品价格: | ¥1176.0 |
| 规格: | 50mg | 产品价格: | ¥1896.0 |
| 规格: | 100mg | 产品价格: | ¥2824.0 |
| 规格: | 200mg | 产品价格: | ¥3944.0 |
Product Introduction
Bioactivity
| 名称 | BRD4770 |
| 描述 | BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence. |
| 细胞实验 | PANC-1 cells are seeded and treated with BRD4770 in 6-well plates for 72 h. Cells are trypsinized and tested for soft agar colony formation using CytoSelect 96-Well Cell Transformation Assay, using the CyQuant GR dye to measure total cellular nucleic acid levels. Fluorescence is detected with an Analyst HT plate reader using a 485/520 nm filter set.(Only for Reference) |
| 激酶实验 | Biochemical activity of G9a: Dissociation Enhanced Lanthanide Fluoro-ImmunoAssays (DELFIA) are performed in white, opaque 384-well plates coated with Neutravidin. Test compounds are diluted to 12 μg/mL in 50 mM Tris-HCl pH 8.5 containing 4% DMSO and 10 μL is dispensed into the wells. Blank and control wells received only compound buffer. GST-G9a at 10 μg/mL and SAM at 40 μM are diluted in 50 mM Tris HCl pH 8.5/10 mM DTT and added in a volume of 20 μL. Blank wells receives Tris/DTT buffer only. The reactions are initiated by the addition of 800 nM H3(1-20)-cysbiotin substrate in 50 mM Tris pH 8.5 in a volume of 10 μl, and incubated at room temperature for 60 minutes. The plates are washed 3 times with 100 μl of Wash Buffer (50 mM Tris pH 7.4, 150 mM NaCl, 0.05% Tween 20, 0.2% BSA). Next, 50 μl of Fluoroimmunoassay (FI) Buffer (50 mM Tris HCl pH 7.8, 150 mM NaCl, 0.05% Tween 40, 25 μM DTPA, 0.2% BSA, 0.05% BGG) containing 5ng α-2X-di-meth H3-K9 and 5ng goat anti-rabbit Eu chelate is added to all wells of the plate, and the plate is incubated for an additional hour at room temperature. The plates are washed 3 times with 100 μL of Wash Buffer, and 50 μL of Enhancement Solution is added to each well. Time resolved fluorescence is measured after 45 minutes on a Viewlux Microplate Imager imaging for 15 seconds with a 354 μs window, 400 μs delay, excitation at 360 nm, and emission at 618 nm. |
| 体内活性 | BRD4770和棉酚联用可以增加LC3-II水平和自噬体数量,从而协同作用诱导PANC-1细胞死亡。BRD4770在胰腺癌细胞系PANC-1中,通过通过抑制G9a降低二 - 和三甲基化H3K9的细胞水平,诱导衰老,并抑制贴壁依赖性和非依赖性增殖。 |
| 存储条件 | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : < 1.52 mg/mL (3.68 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+90% (20% SBE-β-CD in Saline) : < 1.52 mg/mL (3.68 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+90% Corn oil : 1.52 mg/mL (3.68 mM), Solution. 10% DMSO+90% Saline : < 1.52 mg/mL (3.68 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. DMSO : 15.15 mg/mL (36.64 mM), Sonication is recommended. H2O : 10 mg/mL (24.19 mM), Sonication is recommended. 10% DMSO+90% Corn Oil : 0.5 mg/mL (1.21 mM), Sonication is recommended. |
| 关键字 | senescent | methylation | Inhibitor | inhibit | HistoneMethyltransferase | Histone Methyltransferase | H3K9 | G9a | EHMT2 | chromatin | cell-permeable | BRD-4770 | BRD4770 | BRD 4770 | ATR | ATM | anti-proliferation |
| 相关产品 | XY1 | MRTX-1719 | (Iso)-Flavokawain A | Tazemetostat | iso-Azalansta | SNDX-5613 | EPZ015666 | UNC 0631 | AMI-1 free acid | MS37452 | MAK-683 hydrochloride | Piribedil |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Bioactive Compounds Library Max | Chromatin Modification Compound Library | Anti-COVID-19 Compound Library | Epigenetics Compound Library | NO PAINS Compound Library | Stem Cell Differentiation Compound Library | Membrane Protein-targeted Compound Library | Methylation Compound Library | Target-Focused Phenotypic Screening Library | Reprogramming Compound Library |
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文献和实验网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广,其数量几乎占已知有机化合物的三分之一,用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等,都含有杂环化合物的结构。生物碱多是中草药的有效成分,绝大多数是含氮的杂环化合物。本章内容与医学关系密切,具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式(Ⅰ)和(Ⅱ)两种结构的高能化合物。其作用为贮藏能量(例如 ATP、肌酸磷酸)和作为产生 ATP源的中间代谢产物(例如磷酸烯醇丙酮酸)以及合成反应的中间物质(例如酰基辅酶 A),在蛋白质的结构( conformation)变化周期的第一阶段上(例如钠钾 ATP酶的羧基磷酸中间体)也具有重要作用。多数高等化合物具有磷酸基,但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质,不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开,而必须用化学方法才能分离。
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