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Nutlin 3

Nutlin 3 is a small-molecule antagonist of the MDM2 (murine double minute 2) protein, which negatively regulates the tumor suppressor protein p53.
By inhibiting the MDM2-p53 interaction, Nutlin 3 can activate p53 and induce cell cycle arrest and apoptosis in p53-proficient cancer cells.
This compound has been extensively studied as a potential cancer therapeutic, with applications in a variety of solid tumors and hematological malignancies.
PubCompare.ai's AI-driven platform can help researchers optimize Nutlin 3 research protocols for reproducibility and accuracy, by identifying the best options from the literature, preprints, and patents, and comparing them to ensure relibale results.

Most cited protocols related to «Nutlin 3»

1
Chemoresistant cancer cell line establishment
Cited 30 times
The N-myc-amplified neuroblastoma cell lines UKF-NB-2, UKF-NB-3, and UKF-NB-6 were established from stage 4 neuroblastoma patients.31 (link), 32 (link), 33 (link) The alveolar rhabdomyosarcoma cell line UKF-Rhb-1 was established from a bone marrow metastasis.11 (link) The melanoma cell lines Colo-679 and Mel-HO were obtained from the DSMZ (Braunschweig, Germany).
Parental chemosensitive cell lines were adapted to growth in the presence of anti-cancer drugs by continuous exposure of these cell lines to the increasing concentrations of these drugs as described before.31 (link), 32 (link)The following chemoresistant UKF-NB-3 sublines were derived from the resistant cancer cell line (RCCL) collection: UKF-NB-3rCDDP1000 (adapted to CDDP), UKF-NB-3rDAC8 (DAC), UKF-NB-3rDOX20 (DOX), UKF-NB-3rGEMCI10 (GEMCI), UKF-NB-3rIRINO800 (IRINO), UKF-NB-3rMEL400 (MEL), UKF-NB-3rOXALI2000 (OXALI), UKF-NB-3rPCL20 (PCL), UKF-NB-3rTOPO15 (TOPO), UKF-NB-3rVCR10 (VCR), and UKF-NB-3rVINOR20 (VINOR).
The following chemoresistant UKF-NB-2 sublines were derived from the RCCL collection: UKF-NB-2rCDDP1000, UKF-NB-2rDOX20, and UKF-NB-2rVCR10.
The following chemoresistant UKF-Rhb-1 sublines were derived from the RCCL collection: UKF-Rhb-1rCDDP1000 and UKF-Rhb-1rDOCE10 (DOCE), UKF-Rhb-1rDOX10, UKF-Rhb-1rGEMCI10, UKF-Rhb-1rIRINO200, UKF-Rhb-1rMEL400, UKF-Rhb-1rOXALI1000, and UKF-Rhb-1rVCR10Moreover, the following melanoma sub-lines were derived from the RCCL collection: Colo-679rVCR20, Colo-679rPLX403210 μM (PLX4032, vemurafenib), MelHOrVCR20, MelHOrCDDP1000, MelHOrDAC20, and MelHOrPLX403210 μM.
The corresponding IC50 values for the parental cells and their drug-resistant sublines are provided in Supplementary Table 4.
All cells were propagated in IMDM supplemented with 10% FBS, 100 IU/ml penicillin and 100 mg/ml streptomycin at 37 °C. Cells were routinely tested for mycoplasma contamination and authenticated by short tandem repeat profiling.
Standard molecular cloning techniques were used to generate lentiviral vectors based on Lentiviral Gene Ontology vector technology (see http://www.lentigo-vectors.de), and cell transduction was performed as described before.11 (link), 18 (link), 34 (link)
Michaelis M., Rothweiler F., Barth S., Cinatl J., van Rikxoort M., Löschmann N., Voges Y., Breitling R., von Deimling A., Rödel F., Weber K., Fehse B., Mack E., Stiewe T., Doerr H.W., Speidel D, & Cinatl J j.r. (2011). Adaptation of cancer cells from different entities to the MDM2 inhibitor nutlin-3 results in the emergence of p53-mutated multi-drug-resistant cancer cells. Cell Death & Disease, 2(12), e243-.
Publication 2011
Alveolar Epithelial Cells Alveolar Rhabdomyosarcoma Antineoplastic Agents Bone Marrow Cell Lines Cells Cisplatin Cloning Vectors Lentigo LINE-1 Elements Malignant Neoplasms Melanoma Mycoplasma Neoplasm Metastasis Neuroblastoma Parent Patients Penicillins Pharmaceutical Preparations PLX4032 Rhabdomyosarcoma Rhabdomyosarcoma 1 Short Tandem Repeat Streptomycin Topotecan Vemurafenib
2
Functional and Genetic TP53 Status in Cell Lines
Cited 15 times
The functional and genetic TP53 status of 966 cell lines was determined using the Cancer Cell Line Encyclopedia (CCLE; see URLs)44 , Genomics of Drug Sensitivity in Cancer (GDSC; see URLs)45 , Cancer Target Discovery and Development (CTD2; see URLs)46 , and The Cancer Genome Atlas (TCGA accessed via cBioPortal; see URLs)47 databases. Cell lines were first separated into two functional classes by considering nutlin-3 sensitivity data from GDSC and CTD2, and a p53 target gene expression signature48 computed using CCLE data. Each cell line was provisionally considered as p53 functional if the functional score (calculated as [Target Genes CCLE Z-score] - [Nutlin-3 CTD2 Z-score] - [Nutlin-3 Sanger Z-score]) was above 0, and provisionally considered as p53 non-functional if this value was below 0. Cell lines in the p53 functional class were declared p53 wild-type (WT) if no TP53 alterations were detected by CCLE, GDSC, or TCGA (n = 252), and discarded as ambiguous if any TP53 alterations were found (n = 104). Cell lines in the p53 non-functional class were declared p53 mutant if any genetic TP53 alteration was found (n = 528) and discarded as ambiguous if no TP53 alterations were found (n = 82). The p53 mutant class was further divided into four subclasses: a loss-of-function (LOF) subclass, comprising cell lines with nonsense mutations, frameshift mutations, or homozygous deletions; a missense subclass; a splice-site subclass; and an in-frame insertion/deletion subclass. Cell lines with multiple TP53 alterations were classified using the following precedence order: missense > in-frame > splice site > LOF. Refer to Supplementary Table 1 for the full classification matrix.
Giacomelli A.O., Yang X., Lintner R.E., McFarland J.M., Duby M., Kim J., Howard T.P., Takeda D.Y., Ly S.H., Kim E., Gannon H.S., Hurhula B., Sharpe T., Goodale A., Fritchman B., Steelman S., Vazquez F., Tsherniak A., Aguirre A.J., Doench J.G., Piccioni F., Roberts C.W., Meyerson M., Getz G., Johannessen C.M., Root D.E, & Hahn W.C. (2018). Mutational processes shape the landscape of TP53 mutations in human cancer. Nature genetics, 50(10), 1381-1387.
Publication 2018
Cell Lines Frameshift Mutation Gene Deletion Genes Genome Homozygote Hypersensitivity INDEL Mutation Malignant Neoplasms Mutation Mutation, Nonsense nutlin 3 Pharmaceutical Preparations Reading Frames TP53 Gene TP53 protein, human
3
ID8 Cell Culture and Cytotoxicity Assay
Cited 12 times
ID8 cells, obtained from Dr Katherine Roby (University of Kansas Medical Center, KS), were cultured in DMEM supplemented with 4% fetal calf serum, 100µg/ml penicillin, 100µg/ml streptomycin and ITS (5 µg/ml insulin, 5µg/ml transferrin and 5ng/ml sodium selenite). As ID8 was obtained directly from their original source, separate STR validation was not performed. For cytotoxicity assays, cells were plated onto 24 plates (3x103 cells/well) in triplicate. Survival was assessed by MTT assay (Nutlin-3) or sulphorhodamine B assay (rucaparib) after 72 hours.
Walton J., Blagih J., Ennis D., Leung E., Dowson S., Farquharson M., Tookman L.A., Orange C., Athineos D., Mason S., Stevenson D., Blyth K., Strathdee D., Balkwill F.R., Vousden K., Lockley M, & McNeish I.A. (2016). CRISPR/Cas9-mediated Trp53 and Brca2 knockout to generate improved murine models of ovarian high grade serous carcinoma. Cancer research, 76(20), 6118-6129.
Publication 2016
Biological Assay Cells Cytotoxin Fetal Bovine Serum Insulin lissamine rhodamine B nutlin 3 Penicillins rucaparib Selenite, Sodium Streptomycin Transferrin
4
MTT Assay for Cell Viability
Cited 11 times
Cell viability was tested by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide dye reduction assay after 120 h of incubation, modified as described before.11 (link), 18 (link)
Michaelis M., Rothweiler F., Barth S., Cinatl J., van Rikxoort M., Löschmann N., Voges Y., Breitling R., von Deimling A., Rödel F., Weber K., Fehse B., Mack E., Stiewe T., Doerr H.W., Speidel D, & Cinatl J j.r. (2011). Adaptation of cancer cells from different entities to the MDM2 inhibitor nutlin-3 results in the emergence of p53-mutated multi-drug-resistant cancer cells. Cell Death & Disease, 2(12), e243-.
Publication 2011
Biological Assay Bromides Cell Survival
5
Regulation of Cell Proliferation by Tsc2 and Sesn2
Cited 9 times

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Publication 2008
Biological Assay Camptothecin Cells Cloning Vectors Doxycycline Fibroblasts Glucose Glutamine Growth Factor IGF1 protein, human Insulin Lipofectamine MCF-7 Cells nutlin 3 Penicillins Plasmids Pressure Retroviridae Infections Serum Sirolimus Streptomycin Transfection Tuberous Sclerosis 2

Most recents protocols related to «Nutlin 3»

1
Real-Time Migration Assay of ARPE-19 Cells
ARPE-19 real time migration was assessed using an xCELLigence RTCA DP Instrument (F. Hoffmann-La Roche SA, Basel, Switzerland), using the specific CIM-Plates (Agilent, Santa Clara, CA, USA), electronically integrated Boyden Chambers. In particular, the xCELLigence RTCA DP Instrument registers, in real time, impedance values that are related to cell migration, and then converts them into an adimensional parameter, that is the “Cell Index” (CI). For migration experiments, ARPE-19 cells were treated for 24 h in 6 wells in complete DMEM/F-12 medium with different concentrations of Nutlin-3 or LIPO0.5-NUT, using untreated cells as controls. After treatments, cells were starved from FBS for 2 h before being detached, accurately counted and then seeded in the upper chamber of the CIM-Plates (4 × 104 cells/well), following the manufacturer’s instructions. Finally, plates were inserted into the instruments and migration data were recorded every 5 min.
Esposito E., Pozza E., Contado C., Pula W., Bortolini O., Ragno D., Toldo S., Casciano F., Bondi A., Zauli E., Secchiero P., Zauli G, & Melloni E. (2024). Microfluidic Fabricated Liposomes for Nutlin-3a Ocular Delivery as Potential Candidate for Proliferative Vitreoretinal Diseases Treatment. International Journal of Nanomedicine, 19, 3513-3536.
Publication 2024
2
Nutlin-3-a Synthesis and Characterization
Nutlin-3-a ((-)-4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl) piperazin-2-one, NUT, 98% ee) was synthesized following the procedure reported in the literature [27 (link),28 (link)]. Polysorbate 80 (polyoxyethylenesorbitan monooleate, tween 80, T80) was purchased from Sigma-Aldrich (St Louis, MO, USA). The soybean lecithin (PC) (90% phosphatidylcholine) was Epikuron 200 from Lucas Meyer (Hamburg, Germany). STRAT-M® membranes (STRAT-M) were purchased from Merck-Sigma Aldrich (Milan, Italy). Solvents were of HPLC grade, and all other chemicals were of analytical grade.
Esposito E., Ferrara F., Drechsler M., Bortolini O., Ragno D., Toldo S., Bondi A., Pecorelli A., Voltan R., Secchiero P., Zauli G, & Valacchi G. (2024). Nutlin-3 Loaded Ethosomes and Transethosomes to Prevent UV-Associated Skin Damage. Life, 14(1), 155.
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Publication 2024
3
Antiproliferative Assay for Cisplatin and Nutlin-3
Either 24 h after cell seeding in 96-well plates (5000 cells/well) or after spheroid aggregation, cultures were treated with 2 μM, 10 μM, and 20 μM Cisplatin or 8 μM and 30 μM of nutlin-3, respectively. Viability was assessed by continuous monitoring of the GFP and mCherry fluorescence of the cultures for 120 h, using the JuLI Stage fluorescent live-cell imaging system (NanoEntek, Seoul, Republic of Korea). Cisplatin (Cat. No: Vnr461201) was obtained from Accord Healthcare, UK; nutlin-3 (Cat. No: 3984/10) was obtained from Tocris Bioscience (Bristol, UK).
Vajda F., Szepesi Á., Erdei Z., Szabó E., Várady G., Kiss D., Héja L., Német K., Szakács G, & Füredi A. (2024). Mesenchymal Stem Cells Increase Drug Tolerance of A431 Cells Only in 3D Spheroids, Not in 2D Co-Cultures. International Journal of Molecular Sciences, 25(8), 4515.
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Publication 2024
4
Nutlin-3 Synthesis and Characterization
Nutlin-3 (rel-4-[[(4R,5S)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]-2-piperazinone) was purchased from Cayman Chemicals (Ann Arbor, MI, USA). Nutlin-3a ((-)-4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl) piperazin-2-one, NUT, 98% ee) was synthesized following the procedure reported in the literature.14 (link),27 (link) The soybean lecithin PC (94% phosphatidylcholine) was Epikuron 200 from Lucas Meyer (Hamburg, Germany). Polytetrafluoroethylene (PTFE) membranes (pore size 0.22 μm), and 5(6)-Carboxy-X-rhodamine (Rho) were purchased from Merck-Sigma Aldrich (Milan, Italy). Solvents were of HPLC grade, and all other chemicals were of analytical grade.
Esposito E., Pozza E., Contado C., Pula W., Bortolini O., Ragno D., Toldo S., Casciano F., Bondi A., Zauli E., Secchiero P., Zauli G, & Melloni E. (2024). Microfluidic Fabricated Liposomes for Nutlin-3a Ocular Delivery as Potential Candidate for Proliferative Vitreoretinal Diseases Treatment. International Journal of Nanomedicine, 19, 3513-3536.
Publication 2024
5
Ferroptosis Inducers and Inhibitors
Nutlin-3 (N6287), tert-butyl hydroperoxide (TBH, 458139), N-acetyl-L-cysteine (NAC, A7250), tert-butylhydroquinone (tBHQ, 112941), 1S,3R-RSL-3 (RSL-3, SML2234), and ferrostatin-1 (Ferr-1, SML0583) were obtained from Sigma-Aldrich. Imidazole ketone erastin (IKE, HY-114481) was obtained from MedChemExpress.
Wang Z., Yang X., Chen D., Liu Y., Li Z., Duan S., Zhang Z., Jiang X., Stockwell B.R, & Gu W. (2024). GAS41 modulates ferroptosis by anchoring NRF2 on chromatin. Nature Communications, 15, 2531.
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Publication 2024

Top products related to «Nutlin 3»

1
Nutlin 3 by Merck Group
Sourced in United States, Germany, Italy
Nutlin-3 is a small molecule compound developed by Merck Group. It is a potent and selective inhibitor of the interaction between the p53 tumor suppressor protein and the MDM2 (murine double minute 2) protein, which negatively regulates p53 activity. Nutlin-3 binds to the p53-binding pocket of MDM2, preventing p53 degradation and leading to p53 activation.
2
Nutlin 3 by Cayman Chemical
Sourced in United States
Nutlin-3 is a small molecule that inhibits the interaction between the p53 tumor suppressor protein and the MDM2 oncoprotein. This interaction is important in regulating p53 activity and stability. Nutlin-3 binds to the p53-binding pocket of MDM2, thereby preventing the degradation of p53 and leading to its accumulation and activation.
3
Nutlin 3 by Selleck Chemicals
Sourced in United States
Nutlin-3 is a small-molecule inhibitor that binds to the MDM2 protein, preventing its interaction with the p53 tumor suppressor protein. This disruption of the MDM2-p53 complex can lead to the stabilization and activation of p53, a key regulator of cell cycle arrest and apoptosis.
4
Cycloheximide (chx) by Merck Group
Sourced in United States, Germany, United Kingdom, China, Italy, Sao Tome and Principe, France, Macao, Japan, Spain, Canada, Switzerland, India, Israel, Brazil, Poland, Portugal, Australia, Morocco, Sweden, Austria, Senegal, Belgium
Cycloheximide is a laboratory reagent commonly used as a protein synthesis inhibitor. It functions by blocking translational elongation in eukaryotic cells, thereby inhibiting the production of new proteins. This compound is often utilized in research applications to study cellular processes and mechanisms related to protein synthesis.
5
Dimethyl sulfoxide (dmso) by Merck Group
Sourced in United States, Germany, United Kingdom, China, Italy, Sao Tome and Principe, France, Macao, India, Canada, Switzerland, Japan, Australia, Spain, Poland, Belgium, Brazil, Czechia, Portugal, Austria, Denmark, Israel, Sweden, Ireland, Hungary, Mexico, Netherlands, Singapore, Indonesia, Slovakia, Cameroon, Norway, Thailand, Chile, Finland, Malaysia, Latvia, New Zealand, Hong Kong, Pakistan, Uruguay, Bangladesh
DMSO is a versatile organic solvent commonly used in laboratory settings. It has a high boiling point, low viscosity, and the ability to dissolve a wide range of polar and non-polar compounds. DMSO's core function is as a solvent, allowing for the effective dissolution and handling of various chemical substances during research and experimentation.
6
Doxorubicin by Merck Group
Sourced in United States, Germany, United Kingdom, France, China, India, Italy, Poland, Macao, Japan, Sao Tome and Principe, Canada, Spain, Brazil, Australia, Belgium, Switzerland, Singapore, Israel
Doxorubicin is a cytotoxic medication that is commonly used in the treatment of various types of cancer. It functions as an anthracycline antibiotic, which works by interfering with the DNA replication process in cancer cells, leading to their destruction. Doxorubicin is widely used in the management of different malignancies, including leukemia, lymphoma, and solid tumors.
7
Nutlin 3a by Merck Group
Sourced in United States, Germany
Nutlin-3a is a chemical compound developed by Merck Group. It is a potent and selective inhibitor of the interaction between the p53 tumor suppressor protein and the MDM2 (murine double minute 2) oncoprotein. Nutlin-3a is primarily used as a research tool in cellular and biochemical studies to investigate the p53-MDM2 pathway and its role in various cellular processes.
8
Mg132 by Merck Group
Sourced in United States, Germany, China, United Kingdom, Macao, Sao Tome and Principe, France, Canada, Italy, Switzerland, Morocco, Belgium, Japan, Sweden, Australia, Austria, Israel, Spain
MG132 is a proteasome inhibitor, a type of laboratory reagent used in research applications. It functions by blocking the activity of the proteasome, a complex of enzymes responsible for the degradation of proteins within cells. MG132 is commonly used in cell biology and biochemistry studies to investigate the role of the proteasome in various cellular processes.
9
Etoposide by Merck Group
Sourced in United States, Germany, United Kingdom, Japan, France, China, Italy, Canada, Switzerland, Belgium, Macao, Portugal, Poland
Etoposide is a chemotherapeutic agent used in the treatment of various types of cancer. It is a topoisomerase inhibitor that disrupts the process of DNA replication, leading to cell death. Etoposide is available as a solution for intravenous administration.
10
Lipofectamine 2000 by Thermo Fisher Scientific
Sourced in United States, China, Germany, United Kingdom, Canada, Japan, France, Italy, Switzerland, Australia, Spain, Belgium, Denmark, Singapore, India, Netherlands, Sweden, New Zealand, Portugal, Poland, Lithuania, Hong Kong, Argentina, Ireland, Austria, Israel, Czechia, Cameroon, Taiwan, Province of China, Morocco
Lipofectamine 2000 is a cationic lipid-based transfection reagent designed for efficient and reliable delivery of nucleic acids, such as plasmid DNA and small interfering RNA (siRNA), into a wide range of eukaryotic cell types. It facilitates the formation of complexes between the nucleic acid and the lipid components, which can then be introduced into cells to enable gene expression or gene silencing studies.

More about "Nutlin 3"

Nutlin 3, MDM2, p53, cell cycle arrest, apoptosis, cancer therapeutics, solid tumors, hematological malignancies, Cycloheximide, DMSO, Doxorubicin, Nutlin-3a, MG132, Etoposide, Lipofectamine 2000, PubCompare.ai, protocol optimization, reproducibility, accuracy