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PP242

PP242 is a small-molecule inhibitor that targets the mammalian target of rapamycin (mTOR) kinase. mTOR is a serine/threonine protein kinase that regulates cell growth, proliferation, motility, and survival in response to nutrient and growth factor signals.
PP242 has been studied for its potential therapeutic applications in cancer, neurological disorders, and other conditions invovling dysregulation of the mTOR pathway.
Reseach on PP242 may provide insights into the complex signaling networks controling cellular processes and identify novel drug targets for improved treatment strategies.

Most cited protocols related to «PP242»

Structural Studies of mTOR-mLST8 Complexes

Cited 20 times

Crystals were grown by the hanging-drop vapour diffusion method at 4 °C. Apo-crystals of the mTOR^ΔN–mLST8 complex were grown from 100 mM Tris-Cl, 6-8% (w/v) polyethylene glycol (PEG) 8000, 500 mM NaCl, 10% (v/v) glycerol, 10 mM DTT, pH 8.5. Crystals of the mTOR^ΔN-mLST8 bound to ADP-MgF₃-Mg₂ were grown similarly, except the well-buffer contained 10 mM MgCl₂, 3 mM ADP, and 20 mM NaF. The mTOR^ΔN-mLST8-ATPγS-Mg₂ complex was prepared by soaking apo-crystals for one hour in a stabilization buffer of 50 mM Tris-Cl, pH 8.5, 10 mM Tris-Cl, 8.0, 10% PEG8000, 0.1 M NaCl, 6% glycerol, supplemented with 5 mM MgCl₂ and 1 mM ATPγS. The mTOR^ΔN-mLST8-AMPPNP-Mn₂ complex was prepared by soaking apo-crystals similarly, except the stabilization buffer had a pH of 7.5 and it was supplemented with 1 mM AMPPNP and 2 mM MnCl₂, and the data was collected at the Manganese absorption edge. Crystals of mTOR^ΔN-mLST8-Torin2 and mTOR^ΔN-mLST8-PI-103 were prepared by mixing 1 mM of the inhibitors with the protein. Co-crystals appeared from the same condition as the apo-crystals. Crystals of mTOR^ΔN-mLST8-PP242 were prepared by soaking apo-crystals for 2.5 hours in the stabilization buffer supplemented with 0.2 mM PP242. Apo-crystals were harvested in stabilization buffer, transferred to 50 mM Tris-Cl, pH 8.5, 10 mM Tris-Cl, pH 8.0, 0.1 M NaCl, 14% (w/v) PEG8000, 22% (v/v) glycerol, and were flash-frozen in liquid nitrogen. Crystals with ADP-MgF₃-Mg₂, ATPγS-Mg_2, Torin2, PI103 and PP242 were flash-frozen similarly, except for the presence of the corresponding cofactors or inhibitors (0.1 mM) in the buffers. Diffraction data were collected at -170 °C at the ID24C and ID24E beamlines of the Advanced Photon Source, and they were processed with the HKL suite⁴⁹.

Yang H., Rudge D.G., Koos J.D., Vaidialingam B., Yang H.J, & Pavletich N.P. (2013). mTOR kinase structure, mechanism and regulation by the rapamycin-binding domain. Nature, 497(7448), 217-223.

Publication 2013

adenosine 5'-O-(3-thiotriphosphate) Adenylyl Imidodiphosphate Buffers Diffusion Freezing Glycerin inhibitors Magnesium Chloride Manganese manganese chloride MLST8 protein, human Nitrogen PI103 polyethylene glycol 8000 PP242 Proteins Sodium Chloride Tromethamine

Autophagy Induction and Inhibition Assays

Cited 12 times

To induce autophagy, HeLa, HEK293, and OVCAR8 cells were treated with PP242 (2 to 20 μM) for 0 to 24 h. K562 cells were incubated with imatinib (either 1 or 2 μM) or PP242 (10 μM) for 0 to 22 h. To induce autophagy by starvation, K562 or HEK293 cells were washed 3 times with PBS (137 mM NaCl, 2.7 mM KCl, 10 mM Na₂HPO₄, 1.8 mM KH₂PO₄) and incubated in Earle's Balanced Salt Solution (Life Technologies Corporation, 14155063) for various time points. To block autophagy flux, cells were incubated with chloroquine (2.5 to 20 μM) for 0.5 to 6 h.

Guo S., Liang Y., Murphy S.F., Huang A., Shen H., Kelly D.F., Sobrado P, & Sheng Z. (2015). A rapid and high content assay that measures cyto-ID-stained autophagic compartments and estimates autophagy flux with potential clinical applications. Autophagy, 11(3), 560-572.

Publication 2015

Autophagy Cardiac Arrest Cells Chloroquine HEK293 Cells HeLa Cells Imatinib K562 Cells PP242 Sodium Chloride

Breast Cancer Cell Lines and Compound Evaluation

Cited 12 times

We obtained AU565, HCC1954 and T47D breast cancer cell lines and MCF10A mammary epithelial cells from the American Type Culture Collection (ATCC). We cultured AU565 and HCC1954 cells in RPMI 1640 (ATCC) supplemented with 10% fetal bovine serum (FBS), T47D cells in RPMI 1640 supplemented with 10% FBS and insulin (0.2 U/ml), and MCF10A cells in DMEM/F12 (Invitrogen) supplemented with 5% horse serum, EGF (20 ng/ml), insulin (10 μg/ml), hydrocortisone (0.5 μg/ml), and cholera toxin (100 ng/ml). We added penicillin (50 U/ml) and streptomycin (50 μg/ml) to all growth media.
We purchased dactolisib (BEZ235), GSK1059615 and PP242 from Selleck Chemicals. All compounds were at least 97% pure as evaluated by HPLC and MS analysis. All compounds were dissolved in DMSO as 10 mM stock solutions. For dose-response experiments, we plated cells in 2 replicates at 7,000 cells per well in 96-well plates (Corning) in full growth media for 24 hr and then treated them with 9 doses in serial dilutions (10⁻¹⁰ to 10⁻⁵ M) of each compound for 6, 24 and 72 hr.

Fallahi-Sichani M., Honarnejad S., Heiser L.M., Gray J.W, & Sorger P.K. (2013). Metrics other than potency reveal systematic variation in responses to cancer drugs. Nature chemical biology, 9(11), 708-714.

Publication 2013

BEZ235 Breast Cells Cholera Toxin Culture Media dactolisib Epithelial Cells Equus caballus Fetal Bovine Serum High-Performance Liquid Chromatographies Hydrocortisone Insulin MCF-7 Cells Penicillins PP242 Serum Streptomycin Sulfoxide, Dimethyl Technique, Dilution

RNA-Seq Protocol for Gene Expression Analysis

Cited 4 times

For gene expression analysis, total RNA was extracted from 3 biological replicates for each ligand treatment using Trizol reagent and further cleaned using the RNAeasy kit (QIAGEN). For time course studies, MCF-7 cells were treated with Veh (0.1% EtOH), 10 nM E2 or 1 μM PaPE for 4 h and 24 h. For inhibitor studies, MCF-7 cells were pretreated with Ctrl (0.1% DMSO), 1 μM PP242 or 1 μM AZD6244 for 30 min and then treated with Veh, 10 nM E2 or 1 μM PaPE-1 in the presence or absence of inhibitors for 4 h. Once the sample quality and replicate reproducibility were verified, 2 samples from each group were subjected to sequencing. RNA at a concentration of 100 ng/μL in nuclease-free water was used for library construction. cDNA libraries were prepared with the mRNA-TruSeq Kit (Illumina, Inc.). Briefly, the poly-A containing mRNA was purified from total RNA, RNA was fragmented, double-stranded cDNA was generated from fragmented RNA, and adapters were ligated to the ends.
The paired-end read data from the HiSeq 2000 were processed and analyzed through a series of steps. Base calling and de-multiplexing of samples within each lane were done with Casava 1.8.2. FASTQ files were trimmed using FASTQ Trimmer (version 1.0.0). TopHat2 (version 0.5) (55 (link)) was employed to map paired RNA-Seq reads to version hg19 of the Homo sapiens reference genome in the UCSC genome browser (56 (link)) in conjunction with the RefSeq genome reference annotation (57 (link)). Gene expression values (raw read counts) from BAM files were calculated using StrandNGS (version 2.1) Quantification tool. Partial reads were considered and option of detecting novel genes and exons was selected. Default parameters for finding novel exons and genes were specified. DESeq normalization algorithm using default values was selected. Differentially expressed genes were then determined by fold-change and p-value with Benjamini and Hochberg multiple test correction for each gene for each treatment relative to the vehicle control (9 (link)). We considered genes with fold-change >2 and Benjamini-Hochberg adjusted p-value less than or equal to 0.05 as statistically significant, differentially expressed. All RNA-Seq datasets have been deposited with the NCBI under GEO accession number GSE73663.

Madak-Erdogan Z., Kim S.H., Gong P., Zhao Y.C., Zhang H., Chambliss K.L., Carlson K.E., Mayne C.G., Shaul P.W., Korach K.S., Katzenellenbogen J.A, & Katzenellenbogen B.S. (2016). Design of pathway-preferential estrogens that provide beneficial metabolic and vascular effects without stimulating reproductive tissues. Science signaling, 9(429), ra53.

Publication 2016

AZD 6244 Biopharmaceuticals cDNA Library DNA, Complementary DNA Library DNA Replication Ethanol Exons Gene Expression Gene Expression Profiling Genes Genome Homo sapiens inhibitors Ligands MCF-7 Cells mRNA, Polyadenylated PP242 RNA, Messenger RNA-Seq Sulfoxide, Dimethyl trizol

Axon Protein Synthesis Inhibition Assay

Cited 3 times

After 48 hours, axons were severed from their cell bodies and subsequently treated with 2 μM puromycin (Sigma-Aldrich) for 10 minutes. After treatment, the cultures were fixed in 2% formaldehyde/7.5% sucrose in PBS for 20 minutes at RT, washed 3 times in PBS + 0.001% Triton-X-100, permeabilized for 3-5 minutes with 0.1% Triton-X-100 and blocked in 5% heat-inactivated goat serum in PBS for 30 minutes at RT and subsequently labeled with Alexa Fluor 647-conjugated mouse anti-puromycin antibody (1:250, MABE343-AF647, Millipore) overnight. For experiments involving pharmacological treatments, axons were pre-treated with 50μM CHX (Sigma-Aldrich) for 20 minutes, 50μM dynasore (Sigma-Aldrich) for 20 minutes, 50μM Chloroquine (Sigma-Aldrich) or 2.5μM PP242 for 10 minutes before puromycin administration.

Cioni J.M., Lin J.Q., Holtermann A.V., Koppers M., Jakobs M.A., Azizi A., Turner-Bridger B., Shigeoka T., Franze K., Harris W.A, & Holt C.E. (2019). Late Endosomes Act as mRNA Translation Platforms and Sustain Mitochondria in Axons. Cell, 176(1-2), 56-72.e15.

Publication 2019

Alexa Fluor 647 Antibodies, Anti-Idiotypic Axon Cell Body Chloroquine Formaldehyde Goat Mus N'-(3,4-dihydroxybenzylidene)-3-hydroxy-2-naphthahydrazide Pharmacotherapy PP242 Puromycin Serum Sucrose Triton X-100

Most recents protocols related to «PP242»

Histological and Immunohistochemical Analysis of Spinal Cord Injury

To analyze the effect of EGCG, PP242, or the combined therapy on injured spinal cords, 15 cross-sections (5 μm thickness) per spinal cord were selected at 1-mm intervals along the cranio-caudal axis, including the lesion center. Cresyl violet-Luxol fast blue staining was performed to distinguish the white and gray matter (WM/GM) of the injured spinal cord. The total area and distribution of sparse white/gray matter and cavity size were analyzed using ImageJ software (NIH, Bethesda, MD, USA) [41 (link)].
All 71 rats were used for histological and immunohistochemical analyses. A total of 47 animals underwent transcardial perfusion with 4% paraformaldehyde in the eighth week after SCI, and 24 animals were transcardially perfused 7 days after SCI. Concisely, anesthetic pentobarbital (150 mg/kg. Penbital, Bioveta, Ivanovice na Hane, Czech Republic) was injected intraperitoneally to overdose the animals. After thoracotomy, transcardial perfusion was started with a phosphate buffer followed by 4% paraformaldehyde in the phosphate buffer. Rat’s spines were removed and placed in 4% paraformaldehyde for additional overnight fixation. The following day, spinal cords were dissected (2 cm superior and 2 cm inferior from the lesion) and left in 4% paraformaldehyde for the following procedures.
Paraffin-embedded and serially sectioned spinal cords (5 μm cross-sections, 1 mm interval) were used for further morphometric and immunohistochemical analyses. Luxol Fast Blue histological staining was chosen for sparing areas of white and gray matter analysis. Axioskop 2 plus microscope (Zeiss, Oberkochen, Germany) and Image J software (Wayne Rasband, NIH, Bethesda, MD, USA) were used for capturing and analyzing images [41 (link)].
A series of spinal cords were immunostained for detection of astrogliosis and axonal sprouting. Immunostaining for astrogliosis was performed using primary anti-GFAP antibody conjugated to CY3 (MAB3402C3, 1:200, Sigma, St, Louis, MO, USA). Axonal sprouting was detected by a primary antibody against GAP-43 (AB5220, 1;1000 Millipore, Billerica, MA, USA) and a secondary antibody goat anti-mouse IgG conjugated to Alexa-Fluor 488 (ab150113, 1:500, Abcam, Bristol, UK). Images were captured with a LEICA CTR6500 with FAXS 4.2.6245.1020 software (TissueGnostics, Vienna, Austria). For immunohistochemistry, images were analyzed using Image J software (Wayne Rasband, NIH, Bethesda, MD, USA) for astrogliosis and HistoQuest 4.0.4.0154 software (TissueGnostics, Vienna, Austria) for axonal sprouting [8 (link)].

Machova Urdzikova L., Cimermanova V., Karova K., Dominguez J., Stepankova K., Petrovicova M., Havelikova K., D. Gandhi C., Jhanwar-Uniyal M, & Jendelova P. (2023). The Role of Green Tea Catechin Epigallocatechin Gallate (EGCG) and Mammalian Target of Rapamycin (mTOR) Inhibitor PP242 (Torkinib) in the Treatment of Spinal Cord Injury. Antioxidants, 12(2), 363.

Publication 2023

alexa fluor 488 Anesthetics Angioedemas, Hereditary Animals anti-IgG Axon Buffers cresyl violet Dental Caries Drug Overdose epigallocatechin gallate Epistropheus Glial Fibrillary Acidic Protein Gliosis Goat Gray Matter Growth Associated Protein 43 Immunoglobulins Immunohistochemistry Luxol Fast Blue MBS Mice, House Microscopy Paraffin paraform Pentobarbital Perfusion Phosphates PP242 Psychotherapy, Multiple Spinal Cord Thoracotomy Vertebral Column

Spinal Cord Injury Treatment in Rats

Male Wistar rats, 10 weeks old, (n = 71; Breeding facility of the Physiological institute CAS, Prague, Czech Republic), weighing approximately 300 ± 15 g, were used in this study. Rats were housed in pairs in individually ventilated cage systems (Tecniplast, Buguggiate, Italy), and provided with food and water ad libitum. Immediately following SCI, all animals were randomly divided into 4 subgroups for behavioral examinations: control (n = 13), PP242 (n = 13), EGCG (n = 11), and PP242 + EGCG (n = 10). PP242 (5 mg/kg; Apex BIO, Houston, MA, USA) [38 (link)], EGCG (50 mg/kg; Merck, Branchburg, NJ, USA) [8 (link)], combination of PP242 (5 mg/kg) + EGCG (50 mg/kg,), or vehicle in controls was administered intraperitoneally. The rats received treatment daily for 5 consecutive days, starting from the second day after SCI. The rats (n = 47) survived for 9 weeks after SCI surgery. The rats were behaviorally tested according to the protocol and their spinal cord tissue was removed for histological evaluation of white and gray matter, astrogliosis, and axonal sprouting. In addition, immunohistological analysis for mTOR signaling molecule pS6 and PCR analysis for cytokines were also performed. A total of 24 rats survived for 7 days after SCI, and their spinal cords were used for immunohistochemistry (n = 6, each group). The number of animals were estimated according to the power analysis based on the data from our previous experiments. All the experiments were performed in accordance with the European Communities Council Directive of 22 September 2010 (2010/63/EU) regarding the use of animals in research and approved by the Ethics Committee of the Institute of Experimental Medicine CAS and subsequently by the Section Committee of Czech Academy of Sciences, Prague, Czech Republic (Project No. 54/2017, approved 14 July 2017). The number of animals was statistically optimized to achieve refinement and reduction.

Publication 2023

Animals Axon Cytokine epigallocatechin gallate Food FRAP1 protein, human Gliosis Gray Matter Immunohistochemistry Males Operative Surgical Procedures Physical Examination physiology PP242 Rats, Wistar Rattus norvegicus Spinal Cord Tissues

Statistical Analysis of Neuroprotective Compounds

All the raw data from behavioral testing, histological, and immunohistochemical parts of the study were summarized in Excel (Office 2010, Microsoft). The statistical comparison of the four tested groups (EGCG, PP242, combination of the two, and vehicle-treated tested group) was accomplished with several statistical tests in the GraphPad Prism for Windows software (version 5.03, GraphPad Software, Boston, MA, USA). For evaluation of the normality of the raw data, Kolmogorov–Smirnov test was used. For behavioral testing, the two-way repeated measurement ANOVA was applied, except for the Ladder walking test, where the one-way ANOVA was used. Immunohistochemical GFAP analysis was analyzed with the two-way ANOVA mixed-effects model (REML). The Bonferroni correction test was used as a post hoc pair-to-pair test. The tests were selected according to the distribution of the data for each investigation.
All graphs in the results part display as arithmetical means with standard error of the mean. The statistical significance in the graphs as well as in the text is signposted by a scheme; * p < 0.05, ** p < 0.01, *** p < 0.001.

Publication 2023

epigallocatechin gallate Glial Fibrillary Acidic Protein neuro-oncological ventral antigen 2, human PP242 prisma Walk Test

Nucleolar Morphology Analysis of HCT-15 Cells

To analyze nucleolar morphology of HCT-15 cells, we performed high speed imaging with optimum focusing capabilities. We seeded 20,000 cells in a 384 well-plate (Greiner) and the next day, we treated cells with 500 nM of pp242, 1 μM of MG132, and 1 μM of Rotenone for 24 h. Cells were fixed with 4% PFA, permeabilized by 1% Triton X-100 for 1 h, blocked with goat serum, incubated with anti-L7a antibody overnight, and detected using Alexa 488-conjugated secondary antibody. Nuclei were stained with DAPI. At least 200 cell nuclei were analyzed with four repeats. Cells were imaged on an IC200 high-throughput image cytometer (VALA Sciences) using a plan APO 40× objective. A single plane was acquired for the DAPI channel, and a z stack series (10 μm, 1 μm increment) was acquired for the GFP channel. Image analysis was performed using a custom-made algorithm developed in MATLAB. We analyzed two fields-of-view (FOV) per well (average of 46 cells per FOV). For each FOV, DAPI-labelled nuclei were segmented using a watershed transform strategy. For nucleolus segmentation, the best focused GFP-labelled nucleoli plane was selected, and objects were identified by first performing morphological top-hat filtering, followed by computing the regional maxima of the H-maxima transform. The mean number of nucleoli per nucleus, average size of nucleoli, and mean fluorescence intensity of nucleoli were then calculated.

Shaiken T.E., Grimm S.L., Siam M., Williams A., Rezaeian A.H., Kraushaar D., Ricco E., Robertson M.J., Coarfa C., Jain A., Malovannaya A., Stossi F., Opekun A.R., Price A.P, & Dubrulle J. (2023). Transcriptome, proteome, and protein synthesis within the intracellular cytomatrix. iScience, 26(2), 105965.

Publication 2023

Antibodies, Anti-Idiotypic Cell Nucleolus Cell Nucleus Cells DAPI Fluorescence Goat Immunoglobulins MG 132 PP242 Rotenone Serum Triton X-100

Single-Molecule FISH for Ribosomal S6 mRNA

To detect ribosomal S6 (RPS6) mRNA, we performed single-molecule FISH using Stellaris RNA FISH probes conjugated to CAL Fluor Red 610 targeting Human RPS6 (VSMF-20680-5), Biosearch technologies, Petaluma, CA). Control and pp242 treated HCT-15 cells on cover glasses were fixed in PBS containing 3.7% (v/v) formaldehyde and permeabilized with 70% (v/v) ethanol for 1 h at 4°C. The cells were then washed with 10% formamide buffer (Stellaris Wash Buffer A) before hybridizing with the probe set in Stellaris Hybridization Buffer (SMF-HB1-10). The hybridizations were performed overnight in a moist chamber at 37°C. The following day, the cells on cover glasses were transferred to Stellaris Wash buffer A (SMF-WA1-60) and incubated for 30 min. For nuclear staining, we incubated cells with DAPI (5 ng/ml) for 30 min in the dark in Wash buffer A, washed with Stellaris Wash buffer B (SMF-WB1-20) for 5 min and mounted. Images were obtained using a deconvolution microscope (GE Healthcare, Olympus IX71).

Publication 2023

Acid Hybridizations, Nucleic Buffers Cells DAPI Ethanol Eyeglasses Fishes Formaldehyde formamide Homo sapiens Microscopy PP242 Ribosomes RNA, Messenger RNA Probes

Top products related to «PP242»

Pp242 by Merck Group

Sourced in United States, United Kingdom, Switzerland

PP242 is a molecular biology reagent produced by Merck Group. It functions as a potent and selective inhibitor of the mammalian target of rapamycin complex 1 (mTORC1). The core function of PP242 is to facilitate the study of the mTOR signaling pathway and its role in various cellular processes.

Pp242 by Selleck Chemicals

Sourced in United States

PP242 is a laboratory chemical compound. It is a small molecule with a molecular formula of C₂₃H₃₀N₄O₂. PP242 is a potent and selective inhibitor of the mammalian target of rapamycin (mTOR) kinase.

Rapamycin by Merck Group

Sourced in United States, Germany, United Kingdom, China, Italy, Macao, Israel, Sao Tome and Principe, Spain, Canada, Japan, France, Switzerland, Senegal, Belgium

Rapamycin is a macrolide compound isolated from the bacterium Streptomyces hygroscopicus. It functions as an immunosuppressant and has anti-proliferative effects.

Pp242 by Bio-Techne

Sourced in United Kingdom

PP242 is a selective and potent inhibitor of the mammalian target of rapamycin complex 1 (mTORC1). It functions by blocking the kinase activity of mTOR, a critical regulator of cell growth, proliferation, and metabolism.

Rapamycin by Selleck Chemicals

Sourced in United States, China, Germany, United Kingdom, Switzerland, Japan

Rapamycin is a macrolide compound produced by the bacterium Streptomyces hygroscopicus. It functions as an immunosuppressant and has anti-tumor properties.

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.

Rapamycin by LC Laboratories

Sourced in United States, Germany, United Kingdom, Canada, Morocco, Macao

Rapamycin is a macrolide compound produced by the bacterium Streptomyces hygroscopicus. It functions as an immunosuppressant and has been used in research applications.

Bafilomycin a1 by Merck Group

Sourced in United States, Germany, Italy, Sao Tome and Principe, United Kingdom, Macao, Japan, France, Switzerland, Belgium, Australia, China, Israel

Bafilomycin A1 is a macrolide compound that acts as a potent and specific inhibitor of vacuolar-type H+-ATPases (V-ATPases). V-ATPases are involved in the acidification of various intracellular compartments, making Bafilomycin A1 a useful tool for studying cellular processes that rely on pH regulation.

Torin1 by Bio-Techne

Sourced in United Kingdom, United States, Japan

Torin1 is a laboratory reagent manufactured by Bio-Techne. It functions as an inhibitor of the mammalian target of rapamycin (mTOR) protein. Torin1 is used for research purposes in cell and molecular biology studies.

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.

More about "PP242"

PP242 is a small-molecule inhibitor that targets the mammalian target of rapamycin (mTOR) kinase, a serine/threonine protein kinase that regulates crucial cellular processes like growth, proliferation, motility, and survival. mTOR acts as a master regulator, integrating signals from nutrients, growth factors, and other stimuli to control these fundamental mechanisms.
PP242 has shown promising potential in various therapeutic applications, particularly in cancer, neurological disorders, and other conditions involving dysregulation of the mTOR pathway.
By inhibiting mTOR, PP242 can disrupt the aberrant signaling networks that drive uncontrolled cell growth and survival, which are hallmarks of many diseases.
Rapamycin, also known as sirolimus, is a natural product that was initially discovered for its antifungal properties but has since been found to be a potent mTOR inhibitor.
Cycloheximide, on the other hand, is a protein synthesis inhibitor that can be used to study the effects of mTOR inhibition on cellular processes.
Bafilomycin A1 and Torin1 are other mTOR inhibitors that have been utilized in research, while MG132 is a proteasome inhibitor that can be used in conjunction with mTOR inhibitors to investigate the complex signaling pathways involved.
By studying the mechanisms of action and the effects of PP242 and other mTOR-targeting compounds, researchers can gain valuable insights into the intricate cellular networks that control vital functions.
This knowledge can lead to the identification of novel drug targets and the development of improved treatment strategies for a wide range of conditions, ultimately benefiting patients and advancing the field of biomedical research.