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GSK-2816126

GSK-2816126 is a novel small molecule that has shown promise in preclinical studies for the treatment of various disease conditions.
This compound targets a specific biological pathway and may have therapeutic potential in areas such as oncology, inflammation, and metabolic disorders.
Researchers can leverage PubCompare.ai's AI-driven analysis to efficiently locate and compare protocols from the literature, preprints, and patents related to GSK-2816126, enabling them to make informed decisions and drive their research forward with confidence.
Experiene the future of protocol comparison today with PubCompare.ai and gain valuable insights to enhance your understanding of this promising therapeutic candidate.

Most cited protocols related to «GSK-2816126»

1
3D Culture of Ovarian Cancer Cell Lines
Cited 4 times
OVISE, TOV21G, RMG1 and OVTOKO cell lines were all obtained from Japanese Collection of Research Bioresources. SKOV3 cell line was obtained from American Type Culture Collection. OVCA429 and KK cell lines were obtained from Dr. Ie-Ming Shih. All cell lines were cultured according to instructions and in 3D conditions using Matrigel unless otherwise specified. All cell lines were used within 6 months of culture after receiving them, but were not tested. 3D culture was adapted from previously published methods 31 (link) using growth factor reduced-Matrigel (GFR-Matrigel; BD Biosciences). In the 3D culture models, GSK126 treatment was started at the time of assay setup. Briefly, a single cell suspension was plated in 8-well chambers covered with Matrigel. Matrigel media with either vehicle control (DMSO) or drug was changed every 4 days and cells were grown for 12 days. Each of the experiments was performed in duplicate in three independent experimental repeats.
Biter B.G., Aird K.M., Garipov A., Li H., Amatangelo M., Kossenkov A.V., Schultz D.C., Liu Q., Shih I.M., Conejo-Garcia J.R., Speicher D.W, & Zhang R. (2015). Targeting EZH2 methyltransferase activity in ARID1A mutated cancer cells is synthetic lethal. Nature medicine, 21(3), 231-238.
Publication 2015
Biological Assay Cell Lines Cells Growth Factor GSK-2816126 Japanese matrigel Pharmaceutical Preparations Sulfoxide, Dimethyl
2
Preparation and Dilution of Small Molecule Inhibitors
Cited 3 times
UNC1999 was produced at Icahn School of Medicine at Mount Sinai (9 (link)) and was diluted in DMSO to a stock of 10 mmol/L for cell culture experiments. For in vivo experiments, UNC1999 was slowly dissolved in 5% DMSO in corn oil with vigorous vortex followed by rotation to achieve a homogenous suspension of 60 or 100 mg/mL. GSK126 was purchased from CHEMIETEK and was diluted in DMSO to a stock of 20 mmol/L. Bortezomib and carfilzomib for cell culture experiments were obtained from Selleck Chemicals and were diluted in DMSO to stocks of 100 μmol/L. Bortezomib was purchased from Janssen Pharmaceutical KK for in vivo experiments and was diluted in normal saline to a 1 mg/mL stock. MG132 was obtained from Cayman Chemical and was diluted in DMSO to a stock of 10 mmol/L.
Rizq O., Mimura N., Oshima M., Saraya A., Koide S., Kato Y., Aoyama K., Nakajima-Takagi Y., Wang C., Chiba T., Ma A., Jin J., Iseki T., Nakaseko C, & Iwama A. (2017). Dual Inhibition of EZH2 and EZH1 Sensitizes PRC2-Dependent Tumors to Proteasome Inhibition. Clinical cancer research : an official journal of the American Association for Cancer Research, 23(16), 4817-4830.
Publication 2017
Bortezomib Caimans carfilzomib Cell Culture Techniques Corn oil GSK-2816126 Homozygote MG 132 Normal Saline Pharmaceutical Preparations Sulfoxide, Dimethyl UNC1999
3
Murine Ovarian Cancer Model and Therapeutic Evaluation
Cited 3 times
ID8 mouse ovarian cancer cells were described originally 34 (link). ID8 cells (5 x 105) were injected into peritoneal cavity of NSG mice or C57BL/6 mice (6–8 weeks old, Jackson Lab) 11 (link),32 (link). Tumor progression was monitored 2 ~ 3 times per week by Xenogen IVIS® Spectrum in vivo Bioluminescence imaging system (PerkinElmer). Tumor volume was calculated based on the total flux (photons per second). Tumor-bearing mice were treated (i. p) with 5 mg/kg DZNep (SML0305, Sigma), 50 mg/kg EPZ6438 (E-7438, Active Biochem), 0.2 mg/kg 5-AZA dC (A3656, Sigma), or 10 mg/kg anti-PD-L1 (B7-H1, clone 10F.9G2, BE0101, Bio X Cell) three times per week for two weeks. In some cases, tumor was dissected for the analysis of chemokine production or T cells infiltration as indicated.
In adoptive T cell therapeutic model, human TAA-specific CD8+ T cells were generated in vitro and primary human ovarian cancer cells were inoculated subcutaneously into the flanks of NSG mice 11 (link),32 (link). TAA-specific CD8+ T cells (7 X 106) were intravenously transfused into tumor-bearing mice. DZNep (5 mg/kg), GSK126 (30 mg/kg), and 5-AZA dC (0.2 mg/kg) treatments were started before T cell transfusion by intraperitoneal administration 3 times per week. In some cases, mice received CD8+ T cells which were preincubated with anti-CXCR3 for 1 hour before in vivo transfusion, followed by intraperitoneal administration of 500 μg anti-CXCR3 for 3 times per week. Tumor growth was monitored and recorded. Tumor cells and tumor infiltrating immune cells were isolated and studied by FACS, real-time PCR and/or immunohistochemistry. All animal protocols were approved by the University of Michigan Committee on Use and Care of Animals (UCUCA).
Peng D., Kryczek I., Nagarsheth N., Zhao L., Wei S., Wang W., Sun Y., Zhao E., Vatan L., Szeliga W., Kotarski J., Tarkowski R., Dou Y., Cho K., Hensley-Alford S., Munkarah A., Liu R, & Zou W. (2015). Epigenetic silencing of Th1 type chemokines shapes tumor immunity and immunotherapy. Nature, 527(7577), 249-253.
Publication 2015
3-deazaneplanocin Animals Azacitidine Blood Transfusion CD8-Positive T-Lymphocytes CD274 protein, human Cells Chemokine Clone Cells CXCR3 protein, human Disease Progression E 7438 EPZ-6438 GSK-2816126 Homo sapiens Immunohistochemistry Injections, Intraperitoneal Mice, Inbred C57BL Mus Neoplasms Ovarian Neoplasm Peritoneal Cavity Real-Time Polymerase Chain Reaction T-Lymphocyte
4
Molecular Screening Assay Reagents
Cited 3 times
Small molecules utilized in the screen were all obtained from the Molecular Screening Facility at The Wistar Institute. GSK126 was obtained from Xcess Biosciences and Active Biochem. UNC1999 was obtained from Selleckchem. The following antibodies from the indicated suppliers were used: anti-EZH2 (BD Bioscience, Cat. No: 612666, 1:1000), anti-EZH2 (Cell Signaling, Cat. No: 5246, 1:100), anti-ARID1A (Sigma, Cat. No: HPA005456, 1:1000), anti-H3K27Me3 (Cell Signaling, Cat. No: 9733, 1:1000), anti-β-actin (Sigma, Cat. No: A5441, 1:10,000), anti-ARID1A (Santa Cruz, Cat. No: sc-32761, 1:500), anti-Ki67 (Cell Signaling, Cat. No: 9449, 1:1000), anti-PIK3IP1 (Santa Cruz, Cat. No: sc-86785, 1:500), anti-Histone H3 (Millipore, Cat. No: 06-755, 1:1000), anti-GAPDH (Millipore, Cat. No: MAB374, 1:10,000), anti-cleaved caspase 3 (Cell Signaling, Cat. No: 9661, 1:10,000), anti-PI3K (p110alpha) (Cell Signaling, Cat. No: 4255, 1:1000), anti-pAKT (T308, Cell Signaling, Cat. No: 13038, 1:1000), anti-AKT (Cell Signaling, Cat. No: 9272, 1:1000) and anti-H3K9Me3 (Abcam, Cat. No: ab8898, 1:1000). pBabe-Myr-PIK3CA143V plasmid was obtained from Addgene. pBabe-EZH2, pBabe-EZH2 ΔSET and pQCXIP-PIK3IP1 plasmids were generated by standard molecular cloning protocols, and details are available upon request. Growth factor reduced Matrigel was purchased from BD Bioscience.
Biter B.G., Aird K.M., Garipov A., Li H., Amatangelo M., Kossenkov A.V., Schultz D.C., Liu Q., Shih I.M., Conejo-Garcia J.R., Speicher D.W, & Zhang R. (2015). Targeting EZH2 methyltransferase activity in ARID1A mutated cancer cells is synthetic lethal. Nature medicine, 21(3), 231-238.
Publication 2015
Actins Antibodies ARID1A protein, human Caspase 3 EZH2 protein, human GAPDH protein, human Growth Factor GSK-2816126 Histone H3 matrigel PIK3CA protein, human PIK3CB protein, human Plasmids UNC1999
5
Molecular Screening Assay Reagents
Cited 3 times
Small molecules utilized in the screen were all obtained from the Molecular Screening Facility at The Wistar Institute. GSK126 was obtained from Xcess Biosciences and Active Biochem. UNC1999 was obtained from Selleckchem. The following antibodies from the indicated suppliers were used: anti-EZH2 (BD Bioscience, Cat. No: 612666, 1:1000), anti-EZH2 (Cell Signaling, Cat. No: 5246, 1:100), anti-ARID1A (Sigma, Cat. No: HPA005456, 1:1000), anti-H3K27Me3 (Cell Signaling, Cat. No: 9733, 1:1000), anti-β-actin (Sigma, Cat. No: A5441, 1:10,000), anti-ARID1A (Santa Cruz, Cat. No: sc-32761, 1:500), anti-Ki67 (Cell Signaling, Cat. No: 9449, 1:1000), anti-PIK3IP1 (Santa Cruz, Cat. No: sc-86785, 1:500), anti-Histone H3 (Millipore, Cat. No: 06-755, 1:1000), anti-GAPDH (Millipore, Cat. No: MAB374, 1:10,000), anti-cleaved caspase 3 (Cell Signaling, Cat. No: 9661, 1:10,000), anti-PI3K (p110alpha) (Cell Signaling, Cat. No: 4255, 1:1000), anti-pAKT (T308, Cell Signaling, Cat. No: 13038, 1:1000), anti-AKT (Cell Signaling, Cat. No: 9272, 1:1000) and anti-H3K9Me3 (Abcam, Cat. No: ab8898, 1:1000). pBabe-Myr-PIK3CA143V plasmid was obtained from Addgene. pBabe-EZH2, pBabe-EZH2 ΔSET and pQCXIP-PIK3IP1 plasmids were generated by standard molecular cloning protocols, and details are available upon request. Growth factor reduced Matrigel was purchased from BD Bioscience.
Biter B.G., Aird K.M., Garipov A., Li H., Amatangelo M., Kossenkov A.V., Schultz D.C., Liu Q., Shih I.M., Conejo-Garcia J.R., Speicher D.W, & Zhang R. (2015). Targeting EZH2 methyltransferase activity in ARID1A mutated cancer cells is synthetic lethal. Nature medicine, 21(3), 231-238.
Publication 2015
Actins Antibodies ARID1A protein, human Caspase 3 EZH2 protein, human GAPDH protein, human Growth Factor GSK-2816126 Histone H3 matrigel PIK3CA protein, human PIK3CB protein, human Plasmids UNC1999

Most recents protocols related to «GSK-2816126»

1
Cytotoxicity of EZH2 Inhibitor GSK126
The 3D4/21 cells were seeded into a 96-well cell culture plate. When they reached about 60% confluency, the EZH2 inhibitor GSK126 was added to the medium with different concentrations (i.e., 5, 10, 20, 30, 40 μmol), and the samples were collected after 24 h of treatment for the CCK-8 assay. The same volume of DMSO was used as the untreated control. The CCK-8 assay was performed according to the instructions provided with the Cell Counting Kit-8 kit (CK04, Dojindo, Japan).
Zhang L., Jin J., Qin W., Jiang J., Bao W, & Sun M.A. (2023). Inhibition of EZH2 Causes Retrotransposon Derepression and Immune Activation in Porcine Lung Alveolar Macrophages. International Journal of Molecular Sciences, 24(3), 2394.
Full text: Click here
Publication 2023
Biological Assay Cell Culture Techniques Cells EZH2 protein, human GSK-2816126 Sincalide Sulfoxide, Dimethyl
2
EZH2 inhibitor treatment of 3D4/21 alveolar macrophages
Porcine 3D4/21 alveolar macrophages were purchased from ATCC and cultured with RPMI-1640 medium (SH30809.01, Cytiva, USA) supplemented with 10% FBS (Sigma-Aldrich, USA) and 1% anti-anti (15240062, Gibco, USA) in a constant-temperature incubator at 37 °C with 5% CO2 and saturated humidity. When 3D4/21 cells reached about 50–60% confluency, the EZH2 inhibitor GSK126 (S7061, Selleck chem, USA) was added at desired time points (e.g., 3, 12, 24, 48 h before sample collection) to the medium to a concentration of 5 μmol to begin treatment. The same volume of DMSO (21985023, Gibco, USA) was added 48 h before sample collection as the untreated control. After the desired time of treatment, all samples were collected for subsequent experiments.
Zhang L., Jin J., Qin W., Jiang J., Bao W, & Sun M.A. (2023). Inhibition of EZH2 Causes Retrotransposon Derepression and Immune Activation in Porcine Lung Alveolar Macrophages. International Journal of Molecular Sciences, 24(3), 2394.
Full text: Click here
Publication 2023
Aftercare Cells EZH2 protein, human GSK-2816126 Humidity Macrophages, Alveolar Pigs Specimen Collection Sulfoxide, Dimethyl
3
Profiling chromatin regulator inhibitors
96-well plates were coated with 2% ECM-supplemented medium (Millipore Sigma, E0282) which was allowed to solidify for 4 hours. Cells were seeded at approximately 1.0E4 per well. Drugs were brought to 10 mM in DMSO. 24 hours after seeding, 50 µL of diluted compound was added to each cell sample to generate final concentrations of EZH2 inhibitors GSK126 (5.7 µM; Sigma, 5005800001) or GSK343 (9.5 µM; Sigma, SML0766), BMI1 inhibitors PTC209 (4.3 µM; Selleck Chemicals, S7372) or PTC596 (20.8 µM; Selleck Chemicals S8820), and CBX4/7 inhibitor UNC3866 (30 µM; Sigma, SML2408). Cells were harvested for RNA at 72 hours after application of inhibitors. RNA was isolated using a RNeasy Micro Kit (Qiagen, 74004). The Nanostring assay was performed at the Emory Integrated Genomics Core (EIGC) using a custom codeset that included 177 protein-coding genes and three housekeeping control genes (ACTB, CHMP2A, GAPDH).
Williams N.L., Hong L., Jaffe M., Shields C.E, & Haynes K.A. (2023). PIC recruitment by synthetic reader-actuators to polycomb-silenced genes blocks triple-negative breast cancer invasion. bioRxiv.
Publication Preprint 2023
Biological Assay BMI1 protein, human CBX4 protein, human Cells EZH2 protein, human GAPDH protein, human Gene Products, Protein Genes, Housekeeping GSK-2816126 GSK343 inhibitors Pharmaceutical Preparations PTC596 Sulfoxide, Dimethyl UNC3866
4
Rat Alveolar Macrophage Cell Line NR8383 Culture
The rat alveolar macrophage cell line NR8383 (purchased from National Collection of Authenticated Cell Cultures, CSTR:19375.09.3101RATGNR9) was cultured in Ham’s F12K medium supplemented with 2 mM L-glutamine, 1.5 g/L sodium bicarbonate and 20% fetal bovine serum under a humidified atmosphere of 5% CO2 at 37 °C.
The following reagents were used in some experiments: LPS (Sigma-Aldrich, St. Louis, MI, USA), AZM (HIDRAGON, HuBei, China), GSK126 (MCE, Shanghai, China) and SN50 (MCE).
In some experiments, cells were divided into groups: Control group; Vehicle group (DMSO); LPS group (LPS 2 µg/mL); AZM group (LPS 2 µg/mL + AZM 8 µg/mL); GSK126 group (LPS 2 µg/mL + GSK126 4 µg/mL); and SN50 group (LPS 2 µg/mL + SN50 8 µg/mL). To evaluate the additive inhibitory effect of AZM and two inhibitors (GSK126, SN50), we performed cell experiments using the AZM + GSK126 group (LPS 2 µg/mL + AZM 8 µg/mL + GSK126 4 µg/mL) and AZM + SN50 group (LPS 2 µg/mL + AZM 8 µg/mL + SN50 8 µg/mL). Cells were treated as indicated for 24 h and then analyzed.
Wu S., Tian X., Mao Q, & Peng C. (2023). Azithromycin attenuates wheezing after pulmonary inflammation through inhibiting histone H3K27me3 hypermethylation mediated by EZH2. Clinical Epigenetics, 15, 12.
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Publication 2023
Atmosphere Bicarbonate, Sodium Cell Culture Techniques Cell Lines Cells Culture Media Fetal Bovine Serum Glutamine GSK-2816126 inhibitors Macrophages, Alveolar Psychological Inhibition Sulfoxide, Dimethyl
5
Evaluating Cell Viability Using CCK-8
Cell Counting Kit-8 (Solarbio, Beijing, China) assay was used to examine cell viability. NR8383 cells were prepared as a single cell suspension and inoculated into 96-well plates (100 µL per well) in duplicate wells and cultured for 24 h at 37 °C, 5% CO2. Cells were then treated with LPS (0, 0.5, 1, 2, 4, 8 µg/mL), AZM (0, 2, 4, 8, 16 µg/mL), GSK126 (0, 2, 4, 8, 16 µg/mL) or SN50 (0, 2, 4, 8, 16 µg/mL) for 24 h. Finally, 10 μL CCK-8 solution was added and the cells were placed in an incubator for 2 h in the dark. The absorbance value at 450 nm was determined.
Wu S., Tian X., Mao Q, & Peng C. (2023). Azithromycin attenuates wheezing after pulmonary inflammation through inhibiting histone H3K27me3 hypermethylation mediated by EZH2. Clinical Epigenetics, 15, 12.
Full text: Click here
Publication 2023
Biological Assay Cells Cell Survival GSK-2816126 Sincalide

Top products related to «GSK-2816126»

1
Gsk126 by Selleck Chemicals
Sourced in United States, China
GSK126 is a chemical compound used in research and laboratory settings. It functions as an S-adenosylmethionine-dependent methyltransferase inhibitor.
2
Gsk126 by Cayman Chemical
Sourced in United States
GSK126 is a selective and potent inhibitor of the histone methyltransferase EZH2. It is a white crystalline solid and is used as a research tool in the study of epigenetic regulation.
3
Epz 6438 by Selleck Chemicals
Sourced in United States, Germany
EPZ-6438 is a laboratory instrument designed for chemical analysis and research. It is a versatile tool that can be used to perform various analytical tasks. The core function of EPZ-6438 is to provide accurate and reliable data for researchers and scientists working in the field of chemistry.
4
Gsk126 by Merck Group
Sourced in United States
GSK126 is a laboratory equipment product manufactured by Merck Group. It is designed for use in scientific research and analysis. The core function of GSK126 is to facilitate the study and investigation of chemical and biological processes.
5
Fetal bovine serum (fbs) by Thermo Fisher Scientific
Sourced in United States, China, United Kingdom, Germany, Australia, Japan, Canada, Italy, France, Switzerland, New Zealand, Brazil, Belgium, India, Spain, Israel, Austria, Poland, Ireland, Sweden, Macao, Netherlands, Denmark, Cameroon, Singapore, Portugal, Argentina, Holy See (Vatican City State), Morocco, Uruguay, Mexico, Thailand, Sao Tome and Principe, Hungary, Panama, Hong Kong, Norway, United Arab Emirates, Czechia, Russian Federation, Chile, Moldova, Republic of, Gabon, Palestine, State of, Saudi Arabia, Senegal
Fetal Bovine Serum (FBS) is a cell culture supplement derived from the blood of bovine fetuses. FBS provides a source of proteins, growth factors, and other components that support the growth and maintenance of various cell types in in vitro cell culture applications.
6
Gsk126 by Abcam
Sourced in United States
GSK126 is a highly potent and selective inhibitor of the EZH2 histone methyltransferase enzyme. It is used in research applications to study the role of EZH2 and epigenetic regulation.
7
Gsk126 by MedChemExpress
Sourced in United States
GSK126 is a small molecule that inhibits the enzymatic activity of EZH2, a histone methyltransferase involved in the regulation of gene expression. It is commonly used as a research tool for investigating the role of EZH2 in various cellular processes and disease models.
8
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.
9
Dznep by Cayman Chemical
Sourced in United States
DZNep is a chemical compound that functions as a histone methyltransferase inhibitor. It is used in research settings to study the role of histone methylation in various biological processes.
10
Penicillin streptomycin by Thermo Fisher Scientific
Sourced in United States, Germany, United Kingdom, China, Canada, France, Japan, Australia, Switzerland, Israel, Italy, Belgium, Austria, Spain, Gabon, Ireland, New Zealand, Sweden, Netherlands, Denmark, Brazil, Macao, India, Singapore, Poland, Argentina, Cameroon, Uruguay, Morocco, Panama, Colombia, Holy See (Vatican City State), Hungary, Norway, Portugal, Mexico, Thailand, Palestine, State of, Finland, Moldova, Republic of, Jamaica, Czechia
Penicillin/streptomycin is a commonly used antibiotic solution for cell culture applications. It contains a combination of penicillin and streptomycin, which are broad-spectrum antibiotics that inhibit the growth of both Gram-positive and Gram-negative bacteria.

More about "GSK-2816126"

GSK-2816126 is a promising new small molecule that has shown potential in preclinical studies for treating various health conditions.
This compound targets a specific biological pathway and may have therapeutic benefits in oncology, inflammation, and metabolic disorders.
Researchers can utilize PubCompare.ai's AI-driven analysis to efficiently locate and compare protocols from the literature, preprints, and patents related to GSK-2816126, enabling them to make informed decisions and drive their research forward with confidence.
PubCompare.ai's platform can help researchers discover the power of AI-driven protocol comparison.
The tool allows users to effortlessly locate protocols from the literature, preprints, and patents, and then compares them to identify the most accurate and effective options.
Leveraging advanced AI, PubCompare.ai provides valuable insights to help researchers make informed decisions and enhance their understanding of this promising therapeutic candidate.
Experiene (sic) the future of protocol comparison today with PubCompare.ai and gain valuable insights to advance your research on GSK-2816126.
The platform can also be used to explore other related compounds, such as GSK126, EPZ-6438, FBS, DMSO, DZNep, and Penicillin/streptomycin, which may play a role in the development and testing of this novel therapeutic.