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Submit ReviewNutlin-3 is a MDM2 antagonist; inhibits the MDM2-p53 interaction (IC50 = 0.09 μM) and activates p53. Antiproliferative agent; induces apoptosis in cancer cells.
Sold under license from F. Hoffmann-La Roche Ltd.
分子量 | 581.49 |
公式 | C30H30Cl2N4O4 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 548472-68-0 |
PubChem ID | 16755649 |
InChI Key | BDUHCSBCVGXTJM-IZLXSDGUSA-N |
Smiles | ClC1=CC=[C@@]([C@@H]3[C@@H](N(C(N5CC(NCC5)=O)=O)C(C4=CC=C(OC)C=C4OC(C)C)=N3)[C@]2=CC=C(Cl)C=C2)C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 58.15 | 100 | |
ethanol | 58.15 | 100 |
以下数据基于产品分子量 581.49。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.72 mL | 8.6 mL | 17.2 mL |
5 mM | 0.34 mL | 1.72 mL | 3.44 mL |
10 mM | 0.17 mL | 0.86 mL | 1.72 mL |
50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
参考文献是支持产品生物活性的出版物。
Vassilev et al (2004) In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science 303 844 PMID: 14704432
If you know of a relevant reference for Nutlin-3, please let us know.
关键词: Nutlin-3, Nutlin-3 supplier, Nutlin3, p53, activator, MDM2, antagonist, antagonists, p53-MDM2, Ubiquitin, E3, Ligases, 3984, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Nutlin-3 的部分引用包括:
Peter et al (2020) Loss of polycystins suppresses deciliation via the activation of the centrosomal integrity pathway. Life Sci Alliance 3 PMID: 32651191
Daniel P et al (2021) Replication stress promotes cell elimination by extrusion. Nature 593 591-596 PMID: 33953402
Yang et al (2016) A redox mechanism underlying nucleolar stress sensing by nucleophosmin. Nat Commun 7 13599 PMID: 27886181
Keeva et al (2018) Discovery and characterization of highly potent and selective allosteric USP7 inhibitors. Nat Chem Biol 14 118-125 PMID: 29200206
Alan R et al (2013) Small molecule induced reactivation of mutant p53 in cancer cells. Nucleic Acids Res 41 6034-44 PMID: 23630318
Gergely et al (2022) Comparison of Different Clinical Chemotherapeutical Agents' Toxicity and Cell Response on Mesenchymal Stem Cells and Cancer Cells. Cells 11 PMID: 36230904
Norlin et al (2018) The ATPase activity of Asna1/TRC40 is required for pancreatic progenitor cell survival. Development 145 PMID: 29180572
Bussey et al (2016) Targeting polo-like kinase 1, a regulator of p53, in the treatment of adrenocortical carcinoma. J Zhejiang Univ Sci B 5 1 PMID: 26754547
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It worked perfectly at 10microM concentration for 48 hours.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia