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- 文献和实验
- 技术资料
- CAS号:
72882-78-1
- 规格:
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg/200mg
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥1032.0 |
|---|---|---|---|
| 规格: | 1mg | 产品价格: | ¥378.0 |
| 规格: | 5mg | 产品价格: | ¥936.0 |
| 规格: | 10mg | 产品价格: | ¥1256.0 |
| 规格: | 25mg | 产品价格: | ¥2024.0 |
| 规格: | 50mg | 产品价格: | ¥3032.0 |
| 规格: | 100mg | 产品价格: | ¥4312.0 |
| 规格: | 200mg | 产品价格: | ¥6040.0 |
Product Introduction
Bioactivity
| 名称 | PF-9366 |
| 描述 | PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor (IC50: 420 nM; Kd: 170 nM). |
| 细胞实验 | Huh-7 cells are seeded at a concentration of 15,000 cells per well for 6-h incubation with compound (PF-9366) and 4,000 cells per well for 72-h incubation with the compound in 96-well plates in 200 μL of growth medium. NCI-H520 MAT2B knockdown cells are seeded at a concentration of 20,000 cells per well for 6 h incubation or 10,000 cells per well for 72 h incubation with the compound in 96 well plates in 200 μL of growth medium. Cells are allowed to attach overnight at 37°C with 5% CO2. A 5× solution of cycloleucine is prepared fresh from powder stock in the growth medium. Other compounds (PF-9366) are diluted in 100% DMSO using a three-fold dilution scheme and further diluted in growth medium to give 0.5% DMSO final. Consistency of cellular confluence for each cell line is monitored with the IncuCyte Zoom live cell imager. Proliferation is measured using CellTiterGlo reagent. Growth media is removed from the cell plates following compound treatment and 80 μL/well CellTiter Glo diluted 1:1 in PBS added. |
| 激酶实验 | The Mat2A and Mat2B proteins are extensively dialyzed into a buffer containing 150 mM KCl, 25 mM HEPES, pH 7.4, 5 mM MgCl2, 5% (v/v) glycerol, 2 mM TCEP. Concentrations are determined spectrophotometrically using an ?280 of 44,350 /M.cm for Mat2A and an ?280 of 36,440 /M.cm for Mat2B. PF-9366 are diluted from 100% DMSO stocks into a buffer without DMSO. In a typical experiment, nineteen 15 μL injections of 200 μM compound or 30-35 μM Mat2B are made into 10 μM Mat2A on a VP ITC or nineteen 2 μL injections of 200 μM compound into 10 μM Mat2A on an Auto iTC200. |
| 体外活性 | H520肺癌细胞经PF-9366处理6小时后,PF-9366抑制了细胞内SAM的产生,其半抑制浓度(IC50)为1.2 μM。在经Mat2B基因敲减的H520细胞中,PF-9366的IC50略微降低至0.86 mM。相比H520细胞系,Huh-7细胞对该化合物的敏感性更高。PF-9366处理6小时后,针对SAM合成抑制的IC50为225 nM。 |
| 存储条件 | 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+90% Saline : < 1.32 mg/mL (3.76 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. DMSO : 13.18 mg/mL (37.57 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1.32 mg/mL (3.76 mM), Solution. |
| 关键字 | PF-9366 | PF9366 | PF 9366 | MethionineAdenosyltransferase(MAT) | MethionineAdenosyltransferase | Methionine Adenosyltransferase (MAT) | Methionine Adenosyltransferase | Mat2A | MAT | Inhibitor | inhibit |
| 相关产品 | MAT2A inhibitor 5 | MAT2A inhibitor 2 | MAT2A inhibitor 4 | AGI-25696 | AG-270 | FIDAS-3 | FIDAS-5 | MAT2A-IN-20 | 3-TYP | AGI-24512 | MAT2A-IN-9 | AGI-43192 |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | NO PAINS Compound Library | Epigenetics 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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