Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DBEQ (JRF 12) 是一种选择性的,ATP 竞争性p97抑制剂,对 p97(wt) 和 p97(C522A) 的IC50值分别为 1.5 μM 和 1.6 μM,也可抑制Vps4,IC50值为 11.5 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 193 | 现货 | ||
5 mg | ¥ 417 | 现货 | ||
10 mg | ¥ 736 | 现货 | ||
25 mg | ¥ 1,480 | 现货 | ||
50 mg | ¥ 2,650 | 现货 | ||
100 mg | ¥ 3,880 | 现货 | ||
200 mg | ¥ 5,530 | 现货 | ||
500 mg | ¥ 8,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 417 | 现货 |
产品描述 | DBEQ (JRF 12) is a selective, potent, reversible, and ATP-competitive p97 inhibitor. |
靶点活性 | p97:1.5 μM |
体外活性 | 10 μM DBeQ完全抑制病毒和抗体的降解,但不抑制IgG Fc的降解。10 μM DBeQ快速促进HeLa细胞中caspases-3和-7激活。比激活外在caspase-8通路,DBeQ更有效激活内在caspase-9凋亡途径,而STS激活两种途径程度相似。10 μM DBeQ有效抑制HEK293细胞中TCRα-GFP降解。DBeQ作用于HEK293细胞,3小时内剂量依赖性诱导CHOP,但不增加p21水平。DBeQ作用于U20S细胞,降低基本的和营养刺激的MTOR靶点磷酸化,与雷帕霉素效果类似。15 μM DBeQ 作用于Hela细胞,诱导LC3-II 在在细胞核及浓缩膜和胞质级组分中大量积累。DBeQ作用于HeLa细胞,抑制UbG76V-GFP,ODD-Luc和Luc-ODC 降解,IC50分别为2.6 μM、56 μM 和45 μM。 |
激酶实验 | Manual ATPase Assay: Assay Buffer [20 μL of 2.5× concentration, where 1× = 50 mM Tris (pH 7.4), 20 mM MgCl2, 1 mM EDTA, and 0.5 mM tris(2-carboxyethyl)phosphine (TCEP)] is dispensed into each well of a 96-well plate. Puri?ed p97 (25 μL of 50 μM) is diluted in 975 μL of 1× Assay Buffer, and 10 μL is dispensed in each well. DBeQ (10 μL) or 5% DMSO (10 μL) is then added to each well, and the plate is incubated at room temperature for 10 min. The ATPase assay is carried out by adding to each well 10 μL of 500 μM ATP (pH 7.5), incubating at room temperature for 60 min, and then adding 50 μL Kinase Glo Plus reagent, followed by a ?nal 10-min incubation at room temperature in the dark. Luminescence is read on an Analyst AD. DBeQ is assayed at a range of concentrations (0, 0.048, 0.24, 1.2, 6, and 30 μM) in triplicate. |
细胞实验 | Cells are seeded on a 384-well solid white plate (5,000 cells/well). Cells are transfected with luciferase siRNA or p97 siRNA (10 nM) for 48 hours or treated with DBeQ for the indicated amount of time. Caspase-3/7 Glo, caspase-6 Glo, caspase-8 Glo, or caspase-9 Glo is added into each well and mixed by shaking at 500 rpm for 1 min. Luminescence signal is determined after incubation at room temperature for 1 hour. Cellular viability is determined with CellTiter-Glo reagen. To determine the IC50 of cellular viability, cells are treated with MG132 or DBeQ at seven concentrations (threefold serial dilutions starting at 33 μM) for 48 hours. IC50 values are calculated from ?tting the percentage of luminescence signal normalized to DMSO treated cells).(Only for Reference) |
别名 | JRF 12 |
分子量 | 340.42 |
分子式 | C22H20N4 |
CAS No. | 177355-84-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 34 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.9375 mL | 14.6877 mL | 29.3755 mL | 73.4387 mL |
5 mM | 0.5875 mL | 2.9375 mL | 5.8751 mL | 14.6877 mL | |
10 mM | 0.2938 mL | 1.4688 mL | 2.9375 mL | 7.3439 mL | |
20 mM | 0.1469 mL | 0.7344 mL | 1.4688 mL | 3.6719 mL | |
50 mM | 0.0588 mL | 0.2938 mL | 0.5875 mL | 1.4688 mL | |
100 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7344 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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