购物车
- 全部删除
- 您的购物车当前为空
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。
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 | 库存 | 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 x 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 作为非MDM2相关细胞活动的负控制物质有其应用价值。Nutlin-3a 仅在带有野生型p53的细胞中诱导MDM2和p21的表达(但不是p53)。而Nutlin-3b 不论细胞的p53状态如何都无效果。仅有活性异构体Nutlin-3a 显示出强大的抗增殖活性,并在带有野生型p53的细胞与带有突变型p53的细胞之间明确分离出效力差异。Nutlin-3b 在野生型p53细胞中的效力显著低于对突变型p53细胞的Nutlin-3a 的效力。经过48小时暴露于Nutlin-3a 之后,45%的细胞群体变为TUNEL阳性,但用Nutlin-3b 处理的细胞与未处理的对照组无异。[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 | 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, (+)-Nutlin-3 |
分子量 | 581.49 |
分子式 | C30H30Cl2N4O4 |
CAS No. | 675576-97-3 |
Smiles | COc1ccc(C2=N[C@@H]([C@@H](N2C(=O)N2CCNC(=O)C2)c2ccc(Cl)cc2)c2ccc(Cl)cc2)c(OC(C)C)c1 |
密度 | 1.36 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 93 mg/mL (159.9 mM) Ethanol: 93 mg/mL (159.9 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.
评论内容