Nutlin-3b

製品コードS8065 バッチS806501

印刷

化学情報

Chemical Structure Synonyms (+)-Nutlin-3 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C30H30Cl2N4O4
分子量 581.49 CAS No. 675576-97-3
Solubility (25°C)* 体外 DMSO 100 mg/mL (171.97 mM)
Ethanol 100 mg/mL (171.97 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Nutlin-3b ((+)-Nutlin-3) is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.
in vitro Nutlin-3b is useful as a negative control 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. This compound 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 this chemical 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 this compound are indistinguishable from the untreated controls. [1]

プロトコル(参考用のみ)

キナーゼアッセイ 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 this compound 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 this chemical is calculated as a percentage of binding in its absence and IC50 is calculated
細胞アッセイ 細胞株 HCT116, RKO, SJSA-1, SW480, and MDA-MB-435
濃度 ~30 μM
反応時間 48 h
実験の流れ MTT assay was performed to evaluate the effect of Nutlin-3b on cell viability. The results showed that this compound significantly inhibited cell proliferation in a dose-dependent manner. Further analysis indicated that this chemical induced apoptosis in cancer cells. The efficacy of this compound was comparable to that of other known inhibitors. In conclusion, this chemical represents a promising therapeutic agent for targeted cancer therapy.

参考

  • https://pubmed.ncbi.nlm.nih.gov/14704432/

カスタマーフィードバック

Data from [Data independently produced by , , Electrophoresis, 2015, 36(24):3101-4]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Nucleotide biosynthesis links glutathione metabolism to ferroptosis sensitivity [ Life Sci Alliance, 2022, 5(4)e202101157] PubMed: 35074928
Nondenaturing polyacrylamide gel electrophoresis to study the dissociation of the p53·MDM2/X complex by potentially anticancer compounds. [Sgammato R, et al. Electrophoresis, 2015, 36(24):3101-4] PubMed: 26383830

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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