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Nutlin-3

CAS No. : 548472-68-0

MCE 国际站：Nutlin-3

产品活性：Nutlin-3 是一种有效的 p53-MDM2 抑制剂，K_i 为 90 nM。

研究领域：Apoptosis | Metabolic Enzyme/Protease

作用靶点：MDM-2/p53 | E1/E2/E3 Enzyme

In Vitro: Nutlin-3 is an inhibitor of the MDM2-p53 interaction. In particular, co-treatment of p53-positive HCT116 cells with 1 µM of Inauhzin and 2 µM of Nutlin-3 more significantly activated p53 as measured by its protein level as well as the level of its target p21, PUMA or cleaved PARP as indication of apoptosis. Nutlin-3 is a small-molecule inhibitor that acts to inhibit MDM2 binding to p53 and subsequent p53-dependent DNA damage signaling. As a single agent, Nutlin-3 (2-10 µM) stabilizes p53 and p21^WAF levels and is toxic to WTp53-22RV1 cells (IC₅₀, 4.3 µM) but has minimal toxicity toward p53-deficient cells (IC₅₀, >10 µM). Nutlin-3 induces p53 and p21^WAF expression in a dose-dependent manner in 22RV1 cells. Short-term cell cycle assays show that, at a dose of 10 µM, Nutlin-3 increasea slightly the G₁-phase fraction and decreasea S-phase fraction of all three cell lines.

In Vivo: Nutlin-3 can suppress the growth of xenograft tumors derived from human osteosarcoma or leukemia cells, the anti-tumor activity of Nutlin-3 even at the dose of 200 mg/kg per oral administration is marginal in an HCT116-derived xenograft tumor model. Nutlin-3 may be a useful adjunct to improve the therapeutic ratio using precision radiotherapy targeted to hypoxic cells and warrants further study in vivo.

相关产品：Bioactive Compound Library Plus | Apoptosis Compound Library | Metabolism/Protease Compound Library | Anti-Cancer Compound Library | Autophagy Compound Library | Peptidomimetic Library | Anti-Aging Compound Library | Oxygen Sensing Compound Library | Ubiquitination Compound Library | Ferroptosis Compound Library | Pyroptosis Compound Library | Glutamine Metabolism Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Nutlin-3a | Pifithrin-α hydrobromide | Eprenetapopt | PYR-41 | BI8622 | Ginkgolic Acid | SZL P1-41 | 2-D08 | Amifostine | Pifithrin-µ | RITA | Indole-3-carbinol | NSC232003 | BI8626 | PRT4165 | MI⁻⁷73 | Pifithrin-α, p-Nitro, Cyclic | DKM 2-93 | NSC319726 | Amifostine thiol dihydrochloride | PYZD-4409 | PK11007 | SMIP004 | Solasodine | Inauhzin | SJ-172550 | TZ9 | GS143

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