Nutlin-3 NEW
| Price | $54 | $81 | $126 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-05 |
Product Details
| Product Name: Nutlin-3 | CAS No.: 548472-68-0 |
| Purity: 99.89% | Supply Ability: 10g |
| Release date: 2024/11/05 |
Product Introduction
Bioactivity
| 名稱 | Nutlin-3 |
| 描述 | Nutlin-3 is an MDM2 antagonist that inhibits MDM2-p53 interaction (Ki=90 nM) and activates p53. Nutlin-3 binds preferentially to the p53-binding pocket of MDM2, leading to stabilization of p53 and activation of the p53 pathway. Nutlin-3 has antitumor activity. |
| 細胞實驗 | Nutlin-3 (NUT) is dissolved with DMSO (100 mM) and diluted with appropriate media[2]. Human non-small-cell lung carcinoma wild type p53-containing H460 and A549, human non-small-cell lung carcinoma p53-null H1299, and human colon cancer HCT116 (p53+/+ and p53-/-) cells are used. Cells (1.5×105) are plated into 6-well plates, and incubated at 37°C overnight. After treatment of Inauhzin and Nutlin-3 at the indicated concentrations for 48 h, cells are harvested, fixed in 70% ice-cold ethanol overnight at -20°C, resuspended in propidium iodide-solution (50 μg/mL PI, 0.1 mg/mL RNase A, 0.05% Tritin X-100 in PBS) for 40 min at 37°C, then analyzed for DNA content using a flow cytometer and proprietary software[2]. |
| 激酶實驗 | 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 |
| 體外活性 | METHODS: 22RV1 (p53 WT), DU145 (p53 Mut) and PC-3 (p53 Null) cells were treated with Nutlin-3 (2-10 μM) for 48 h. Apoptosis was detected by Hoechst 33342 staining. RESULTS: Nutlin-3 induced a significant increase in apoptosis in 22RV1 cells, whereas apoptosis was not significantly increased in p53-deficient DU145 or PC-3 cells. Nutlin-3 preferentially increased apoptosis in cells expressing WT p53. [1] METHODS: H460 and HCT116 p53+/+ cells were treated with Nutlin-3 (0-100 μM) and Inauhzin (0-100 μM) for 72 h. Cell viability was measured by WST assay. RESULTS: Inauhzin and Nutlin-3 showed significant synergistic effects in inhibiting the growth of both tumor cell lines, as the CI values were significantly less than 1 in the effective dose range, especially when lower doses of Nutlin-3 were used. [2] |
| 體內(nèi)活性 | METHODS: To assay antitumor activity in vivo, Nutlin-3 (150 mg/kg, EtOH: Tween: 5% Glucose = 5:5:90; administered orally twice daily for four days and stopped for two days) and Inauhzin (15 mg/kg, intraperitoneally once daily) were administered to SCID mice bearing HCT116 p53+/+ xenografts for 21 days. RESULTS: Each compound alone reduced mean tumor volume by less than 20% after 21 days of treatment. However, when both treatments were combined at the same dose, the final average tumor volume was reduced by 60%. inauhzin and Nutlin-3 activated p53 and inhibited the growth of xenograft tumors in the animals. [2] |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 55 mg/mL (94.58 mM) |
| 關鍵字 | E3 ligating enzyme | E2 conjugating enzyme | E1/E2/E3 Enzyme | E1 activating enzyme | Ubiquitin conjugating enzyme | Nutlin-3 | inhibit | MDM-2/p53 | Nutlin 3 | Ubiquitin activating enzyme | Inhibitor | Ubiquitin ligase |
| 相關產(chǎn)品 | NSC697923 | WS-383 | PYZD-4409 | NAcM-OPT | RG7112 | PYR-41 | BC-1382 | NSC232003 | NAE-IN-M22 | Indole-3-carbinol | Idasanutlin | Navtemadlin |
| 相關庫 | 抗胰腺癌化合物庫 | 經(jīng)典已知活性庫 | 泛素化化合物庫 | HIF-1化合物庫 | 抑制劑庫 | 干細胞分化化合物庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 人代謝物化合物庫 | 抗癌活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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