Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Nutlin-3b ((+)-Nutlin-3) 是一种 p53/MDM2 拮抗剂或抑制剂,IC50为 13.6 μM。它与 MDM2 的结合活性比 Nutlin-3a 低 150 倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 462 | 现货 | ||
2 mg | ¥ 597 | 现货 | ||
5 mg | ¥ 828 | 现货 | ||
10 mg | ¥ 1,380 | 现货 | ||
25 mg | ¥ 2,770 | 现货 | ||
50 mg | ¥ 4,480 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,060 | 现货 |
产品描述 | Nutlin-3b ((+)-Nutlin-3) is a p53/MDM2 antagonist or inhibitor (IC50: 13.6 μM), 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a. |
靶点活性 | MDM2:13.6 μM |
体外活性 | Nutlin-3b is useful as a negative control s for non-MDM2-related cellular activities. Nutlin-3a induces the expression of MDM2 and p21 (but not p53) only in cells with wild-type p53. Nutlin-3b has no effect regardless of the p53 status of the cells. Only the active enantiomer Nutlin-3a shows a potent antiproliferative activity and clear separation of potency between the cells harboring wild-type p53 and those harboring mutant p53. The potency of Nutlin-3b is much lower in the wild-type p53 cells and nearly identical to the potency of Nutlin-3a against the mutant p53 cells. After 48 hours of exposure to the Nutlin-3a, 45% of the cell population became TUNEL positive, but cells treated with the Nutlin-3b are indistinguishable from the untreated controls. [1] |
激酶实验 | Biacore study: Competition assay is performed on a Biacore S51. A Series S Sensor chip CM5 is utilized for the immobilization of a PentaHis antibody for capture of the His-tagged p53. The level of capture is ~200 response units (1 response unit corresponds to 1 pg of protein per mm 2). The concentration of MDM2 protein is kept constant at 300 nM. Nutlin-3 is dissolved in DMSO at 10 mM and further diluted to make a concentration series of Nutlin-3 in each MDM2 test sample. The assay is run at 25°C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of Nutlin-3 is calculated as a percentage of binding in the absence of Nutlin-3 and IC50 is calculated |
细胞实验 | MTT assay(Only for Reference) |
别名 | (+)-Nutlin-3, 4-[[(4R,5S)-4,5-双(4-氯苯基)-4,5-二氢-2-[4-甲氧基-2-(1-甲基乙氧基)苯基]-1H-咪唑-1-基]羰基]-2-哌嗪酮 |
分子量 | 581.49 |
分子式 | C30H30Cl2N4O4 |
CAS No. | 675576-97-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (159.9 mM)
Ethanol: 93 mg/mL (159.9 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.7197 mL | 8.5986 mL | 17.1972 mL | 42.993 mL |
5 mM | 0.3439 mL | 1.7197 mL | 3.4394 mL | 8.5986 mL | |
10 mM | 0.172 mL | 0.8599 mL | 1.7197 mL | 4.2993 mL | |
20 mM | 0.086 mL | 0.4299 mL | 0.8599 mL | 2.1497 mL | |
50 mM | 0.0344 mL | 0.172 mL | 0.3439 mL | 0.8599 mL | |
100 mM | 0.0172 mL | 0.086 mL | 0.172 mL | 0.4299 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。
Nutlin-3b 675576-97-3 Apoptosis Ubiquitination Mdm2 E1/E2/E3 Enzyme Nutlin 3b Inhibitor MDM-2/p53 Ubiquitin activating enzyme Ubiquitin conjugating enzyme inhibit (+)-Nutlin-3 E1 activating enzyme 4-[[(4R,5S)-4,5-双(4-氯苯基)-4,5-二氢-2-[4-甲氧基-2-(1-甲基乙氧基)苯基]-1H-咪唑-1-基]羰基]-2-哌嗪酮 Ubiquitin ligase E3 ligating enzyme Nutlin-3 E2 conjugating enzyme Nutlin3b inhibitor