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AG-490

AG-490 is a tyrosine kinase inhibitor with potential therapeutic applications in various fields, including oncology and immunology.
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Most cited protocols related to «AG-490»

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Publication 2010
AG-490 Carbohydrates Diet Diet, High-Fat Enzyme-Linked Immunosorbent Assay Fat-Restricted Diet Freezing Hormones Insulin Leptin Mice, Inbred C57BL Mus Neoplasms Neoplasms, Liver Pharmaceutical Preparations Proteins Serum Tissues TNFRSF1A protein, human Transplantation
All reagents were high grade and were purchased from Sigma with the following exceptions. RPMI, DMEM, Calcein and ethidium homodimer and other culture reagents were purchased from Invitrogen Inc (Grand Island, NY, USA) and the UCSF cell culture facility (UCSF, San Francisco, CA). Fetal bovine Serum Defined (FBS) was purchased from Hyclone Laboratories (Logan, UT, USA). PD98059, a MEK inhibitor; SP600 125, a JNK inhibitor; wortmanin an inhibitor of PI3 kinase and pyrrolidinecarbodithoic acid (PDTC), a NF-κB inhibitor); AG490, a JAK2-STAT inhibitor were purchased from Calbiochem (San Diego, CA). LPS (Escherichia coli, O26:B6), aminoguandine, apocynin, allopurinol, minocycline, N(omega)-hydroxy-L-arginine (NOHA), indomethacin and amino-3-morpholinyl-1,2,3-oxadiazolium chloride (SIN-1) were purchased from Sigma (St Louis, MO). Drugs were dissolved in DMSO or ethanol and stored at -20°C and either used (final concentration of vehicle 0.1% (v/v or dried down and resuspended in PBS/0.1% bovine serum albumin (BSA). Mitogen activated kinase (MAPK) Anti-phospho-ERK monoclonal antibody (mAb), anti-ERK polyclonal antibody (#4370), anti-phospho-p38 MAPK mAb (# 4631), anti-phospho-JNK/SAPK mAb (#4668) were from Cell Signaling Technology (Danvers, MA); anti-NF-κBp65 (# SC-8008), anti-IκBα (# SC-1643) and respective horseradish peroxidase-coupled secondary antibodies were purchased from Santa Cruz (Santa Cruz, CA) and. Antibodies against iNOS ( # 61043), iNOS positive control lysates (#611473) were from BD Biosciences (BD Biosciences, Lexington, KY).
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Publication 2011
1-Phosphatidylinositol 3-Kinase acetovanillone Acids AG-490 Allopurinol alpha, NF-KappaB Inhibitor Antibodies Antibodies, Anti-Idiotypic Arginine Cell Culture Techniques Chlorides Escherichia coli Ethanol ethidium homodimer fluorexon Horseradish Peroxidase I-kappa B Proteins Indomethacin JAK2 protein, human Minocycline Mitogens Monoclonal Antibodies NOS2A protein, human PD 98059 Pharmaceutical Preparations Phosphotransferases prolinedithiocarbamate Serum Albumin, Bovine Sulfoxide, Dimethyl
3T3-L1 preadipocytes were maintained in DMEM containing 10% calf serum (Hyclone Laboratories, South Logan, UT). Two day postconfluent 3T3-L1 cells (designated day 0) were induced to differentiate by addition of a standard cocktail composed of 0.5 mM IBMX, 1 μM Dex, and 10 μg/ml insulin in 10% FBS for 2 days (designated as MDI cocktail). The cells were then cultured in DMEM supplemented with 10% FBS and 5 μg/ml insulin. The medium was replaced with fresh medium every 2 days. For the AG490 experiments, cells were preincubated with 10 μM AG490 for 1 h and then treated with 10 ng/ml IL-4. For cell counting, cells were harvested and stained with trypan blue (0.5%; Biological Industries, Kibbutz Beit Haemek, Israel), and viable cells were counted with the use of a hemocytometer (Lauda-Königshofen, Marienfeld-Superior, Germany).
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Publication 2014
1-Methyl-3-isobutylxanthine 3T3-L1 Cells AG-490 Biopharmaceuticals Cells Insulin Interleukin-10 Serum Trypan Blue
The generation of the GFAP-GFP mouse used in this study has been described previously (Zhou et al., 1997) and CD1 mice were obtained from Charles River Labs (Wilmington, MA). All mouse colonies were maintained in the animal facility of Children’s National Medical Center, and all animal procedures complied with the guidelines of the National Institute of Health, and with the Children’s Research Institute Institutional Animal Care and Use Committee (IACUC) guidelines. Male mice were placed in a chamber containing 10.5 ± 0.5% O2 from P3 to P11 as previously described (Ment et al., 1998 ; Fagel et al., 2006 (link)). Strain-matched and age-matched animals reared in normal oxygen levels were used as controls (normoxia). For studies examining proliferation, BrdU (Sigma; 50μg per gram body weight) was administered 2hr prior to sacrifice. Mice were sacrificed at the given time point after hypoxia and perfused transcardially with phosphate buffered saline followed by 4% paraformaldehyde (PFA) and post fixed overnight in PFA followed by 20% glycerol and stored at 4°C. Treatment of mice with the JAK/STAT inhibitor AG490 has been previously described (Zhou et al., 2011 (link); Xu et al., 2011 ). Briefly, CD1 mice were treated with AG490 (10 mg/kg i.p.) or DMSO (control) twice daily (injections were ~8–10 hours apart) from P6 to P11. At P11 the white matter was carefully dissected out and lysed as described below, followed by Western blot analysis.
Publication 2011
AG-490 Animals Body Weight Bromodeoxyuridine Child Glial Fibrillary Acidic Protein Glycerin Hypoxia Institutional Animal Care and Use Committees Kinase Inhibitor, Janus Males Mice, House Oxygen paraform Phosphates Rivers Saline Solution Strains Sulfoxide, Dimethyl trestolone Western Blot White Matter
Normal aCSF (35 °C) and normal pipette solution were used in electrophysiological recording (Ibrahim et al., 2003 (link)) (Supplemental Methods). When the cationic blocker La3+ was added to the bath, a HEPES-buffered CSF solution was utilized (Zhang et al., 2008 (link)). In some experiments, low Na+ (5 mM) HEPES-buffered CSF solution and Ca2+ free extracellular CSF solution were used, where N-methyl-D-glucamine (NMDG) replaced Na+, and Mg2+ replaced Ca2+, respectively. For experiments measuring the ramp current-voltages (I–Vs) , K+-gluconate in the normal internal solution was replaced with Cs+-gluconate (pH 7.35 with CsOH), and the extracellular solution contained Na+, K+, Ih (HCN), Ca2+ and GABAA channel blockers (in mM: NaCl, 126; 4-aminopyridine, 5; KCl, 2.5; MgCl2, 1.2; CsCl, 2; CaCl2, 1.4; CoCl2, 1; nifedipine, 0.01; HEPES, 20; NaOH, 8; glucose, 10; tetrodotoxin, 0.001; picrotoxin, 0.1). Ramp I-Vs were also recorded in a solution that both Na+ and K+ were replaced with same concentration of Cs+(pH 7.35 with CsOH).
All drugs were purchased from Calbiochem (La Jolla, CA) unless otherwise specified. Leptin was provided by Dr. Parlow (Harbor-UCLA Medical Center, Torrance, California, USA) through the National Hormone and Peptide Program. The Jak2 inhibitor (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl) acrylamide a-Cyano-(3,4-dihydroxy)-N-benzylcinnamide Tyrphostin B42 (AG 490), the PLC inhibitor U73122, the less active analog U73343 and the PI3 kinase inhibitor wortmannin (Alomone Laboratories) were dissolved in dimethylsulfoxide (DMSO) as stock solutions. The selective PLCγ inhibitor 1-O-Octadecyl-2-O-methyl-rac-glycero-3-phosphorylcholline (ET-18-OCH3) was dissolved in H2O. 1, 2-Bis-(o-aminophenoxyethane)-N, N, N', N'-tetra-acetic acid (BAPTA) tetrasodium salt was dissolved in the internal solution at a 10 mM concentration. The ion channel blockers/activators used were as follows: 1-[β-[3-(4-methoxyphenyl) propoxy]-4-methoxyphenethyl]-1H-imidazole hydrochloride (SKF96365); 2-aminoethyl diphenylborinate (2-APB); flufenamic acid (FFA) and 1-(cis-9-Octadecenoyl)-2-acetyl-sn-glycerol, 2-Acetyl-1-oleoyl-sn-glycerol (OAG), all were dissolved in DMSO. LaCl3 was dissolved in H2O.
Publication 2010
1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid 1-Phosphatidylinositol 3-Kinase 2-aminoethyl diphenylborinate Acetic Acid Acrylamide ACTR protein, human AG-490 alpha-cyano-(3,4-dihydroxy)-N-benzylcinnamide Bath Cations cesium chloride Dalfampridine Flufenamic Acid gluconate Glucose Glycerin HEPES Hormones imidazole Ion Channel JAK2 protein, human Leptin Magnesium Chloride N-benzylcinnamide Nifedipine Peptides Pharmaceutical Preparations Picrotoxin PLCG2 protein, human SK&F 96365 Sodium Chloride Sulfoxide, Dimethyl Tetragonopterus Tetrodotoxin U 73122 Wortmannin

Most recents protocols related to «AG-490»

The chemosensitivity of the cells to a variety of conventional chemotherapeutic drugs, small molecule inhibitors, and natural products was determined using an MTT assay. The choice of chemotherapeutic agents was motivated by the desire to compare cell response between two models, 3D cells in the present study and semi-solid Matrigel-embedded cells in our previous study (22 (link)). Standard chemotherapeutic agents that target proliferating cell mechanisms, as well as drugs with multi-targeted actions that do not rely on the proliferative status of the cells, were used. Doxorubicin, etoposide, vinblastine, paclitaxel, 2-deoxyglucose (2-DG), emodin, apigenin, resveratrol, caffeic acid phenethyl ester (CAPE), curcumin, capsaicin, shikonin, and dihydroxybenzaldehyde (DHBZ) were purchased from MilliporeSigma. Cucurbitacin I (CBC-I), AG-490, and BAY 11-7085 were purchased from Calbiochem. Chrysin was kindly provided by Dr Sirivan Athikomkulchai (Faculty of Pharmacy, Srinakharinwirot University, Nakhon Nayok, Thailand). Briefly, 100 µl of the cell suspension was seeded into each well of a 96-well plate (1×104 cells), then 100 µl of cytotoxic agents in a range of concentrations or a vehicle (cell culture media) were added. After 48 h of incubation, each well was replaced with 100 µl of 0.5 mg/ml MTT solution (MilliporeSigma) and incubated for another 2 h at 37°C. Absorbance was measured at 550 nm (650 nm was subtracted as the reference wavelength) using a microplate reader. The IC50 value for each cytotoxic drug (the drug concentration exhibiting 50% cell viability) was calculated.
Publication 2023
AG-490 Antineoplastic Agents Apigenin BAY 11-7085 Biological Assay caffeic acid phenethyl ester Capsaicin Cell Culture Techniques Cells Cell Survival chrysin cucurbitacin I Culture Media Curcumin Cytotoxin Doxorubicin Drug Delivery Systems Emodin Etoposide Faculty, Pharmacy inhibitors matrigel Natural Products Paclitaxel Pharmaceutical Preparations Pharmacotherapy Resveratrol shikonin Vinblastine
KSHV-positive PEL cell lines, BC3 (ATCC, CRL-2277) and BCBL1 (kindly supplied by Prof. P. Monini, National AIDS center, Istituto Superiore di Sanità, Rome, Italy), were grown in RPMI 1640 medium (Sigma-Aldrich, Burlington, MA, USA), supplemented with 10% fetal bovine serum (FBS) (Sigma-Aldrich, Burlington, MA, USA), L-glutamine (2 mM) (Aurogene, Rome, Italy), and streptomycin/penicillin (100 μg/mL) (Aurogene, Rome, Italy) (complete medium) at 37 °C, in a 5% CO2 humified setting. Cells were seeded into 6-well plates, at a density of 4 × 105 per well, in a final volume of 2 mL in complete RPMI medium, and they were treated for 24 h with J2 (10–20 µM) (MedChemExpress, Monmouth Junction, NJ, USA; cat n. HY-124653), PES-Cl (10–20 µM) (Calbiochem, San Diego, CA, USA; cat n. 5.31067), 17-AAG (0.1–1 µM) (Selleckem, Planegg, Germany; cat. n. S1141) or AG490 (100 µM) (Calbiochem, San Diego, CA, USA; cat n. 658411), inhibitors of HSP27, HSP70, HSP90 and STAT3, respectively. All the drugs were dissolved in DMSO, and the control cells were supplemented with DMSO in the same amount used for the other samples. To evaluate if HSPs or STAT3 inhibitors could sensitize PEL cells to the cytotoxic effect of PARP inhibitor, the cell lines were pre-treated for 1 h with HSP27, 70, 90 inhibitor (inHSP) or AG490 and then supplemented with AZD2461 (AZD, 40 μM) (Sigma-Aldrich, Burlington, MA, USA, cat n. SML1858) for 24 h. Untreated cells were used as a control group (CT).
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Publication 2023
Acquired Immunodeficiency Syndrome AG-490 AZD2461 Cell Lines Cells Fetal Bovine Serum Glutamine Heat-Shock Proteins 70 Heat Shock Protein 27 HSP90 Heat-Shock Proteins Human Herpesvirus 8 inhibitors Penicillins Pharmaceutical Preparations Poly(ADP-ribose) Polymerase Inhibitors STAT3 Protein Streptomycin Sulfoxide, Dimethyl tanespimycin
Recombinant human IL-6 (Peprotech, Rocky Hill, NJ, USA) was used to evaluate the effect of exogenous IL-6 on the EMT phenotype of A2780 and SKOV3 cells based on a previously established dosing regimen (A2780 cells were cultured in the presence of IL-6 (50 ng/ml) for 24 hours, whereas SKOV3 cells were cultured in the presence of IL-6 (10 ng/ml) for 48 hours). Pharmacological inhibitors of STAT3 (AG490) and HIF-1α (YC-1) were purchased from Cayman Chemical (Ann Arbor, MI, USA). Both A2780 and SKOV-3 cells were treated with YC-1 (10 μM) for 1 hour prior to the addition of exogenous IL-6. Cells were pretreated with AG490 (50 μM) 30 minutes prior to the addition of IL-6.
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Publication 2023
AG-490 Caimans Cells Homo sapiens inhibitors Phenotype STAT3 Protein Treatment Protocols
The primary myometrium and leiomyoma cells were treated with 100 ng/mL leptin for 48 h. Human adipocyte (SW872) cells were used to coculture with human primary or immortalized myometrium and leiomyoma cells [10 (link)]. We used a Transwell system using 0.4-mm porous membranes from Corning (Corning, New York, NY, USA) to coculture the cells with their respective media. We cultured the Transwell system for eight days, and changed 50% of the medium every 48 h. We then collected the myometrium and leiomyoma media for the multiplex array, and for protein quantification and analysis, we harvested the cells. For a separate series of experiments, the cultured single cells and adipocyte cocultured cells for 7 days were treated with the STAT3 inhibitor (AG490, Calbiochem, Merck Millipore, Burlington, MA, USA) at 50 μM, ERK the inhibitor (PD98059, Cell signaling, Danvers, MA, USA) at 10 μM, and the AKT inhibitor (MK2206, Cayman Chemicals, Ann Arbor, MI, USA) at 10 μM for 24 h. For the leptin treatment, we treated the cells with 100 ng/mL leptin for the first 24 h and then the combination with inhibitors for another 24 h. After 24 h of incubation, we harvested the cells for protein quantification and analysis.
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Publication 2023
Adipocytes AG-490 Caimans Cultured Cells Homo sapiens inhibitors Leptin MK 2206 Myometrium PD 98059 Proteins STAT3 Protein Tissue, Membrane Uterine Fibroids
M199 medium, Rowell Park Memorial Institute (RPMI) 1640 medium, fetal bovine serum (FBS), penicillin, and streptomycin were purchased from Life Technologies, Inc. (Grand Island, NY, USA). The RNA extraction kit was purchased from Intron Biotechnology (Seoul, Republic of Korea). FMN1, ITGA2, COL13A1, VEGFC, NRG1, and β-actin oligonucleotide primers and ITGA2 and VEGFC siRNA were purchased from Bioneer Technology (Seoul, Republic of Korea). 2-mercaptoethanol and phorbol myristate acetate (PMA) were purchased from Sigma-Aldrich Corp. (St. Louis, MO, USA). CCR2 antagonist RS102895 was obtained from Santa Cruz Biotechnology (Santa Cruz, CA, USA). CCR5 antagonist fuscin (3,4,7,9-Tetrahydroxy-6-methyl-1H-phenalen-1-one) was purchased from Adipogen Life Sciences (San Diego, CA, USA). JNK inhibitor SP600125, PI3K/Akt inhibitor LY294002, and JAK2/STAT3 inhibitor AG490 were obtained from Calbiochem (San Diego, CA, USA). Dimethyl sulfoxide (DMSO) and CellTrackerTM were obtained from Invitrogen (Grand Island, NY, USA). Recombinant human CC chemokine ligand 2 (CCL2) and CCL5 were purchased from Thermo Fisher Scientific (Waltham, MA, USA).
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Publication 2023
2-Mercaptoethanol Actins AG-490 beta-Chemokines CCL5 protein, human CCR5 protein, human Fetal Bovine Serum fuscin Homo sapiens Introns JAK2 protein, human Ligands LY 294002 NRG1 protein, human Oligonucleotide Primers Penicillins phenalen-1-one PIK3CG protein, human RNA, Small Interfering SP600125 STAT3 protein, human Streptomycin Sulfoxide, Dimethyl Tetradecanoylphorbol Acetate VEGFC protein, human

Top products related to «AG-490»

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AG490 is a lab equipment product manufactured by Merck Group. It functions as a tyrosine kinase inhibitor.
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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.
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AG490 is a chemical compound used in laboratory research. It functions as a selective inhibitor of the JAK2 protein tyrosine kinase. The core function of AG490 is to modulate cellular signaling pathways in experimental settings.
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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.
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LY294002 is a chemical compound that functions as a specific inhibitor of phosphoinositide 3-kinase (PI3K). It is commonly used in laboratory research settings to investigate the role of PI3K signaling pathways.
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Tyrphostin AG490 is a small-molecule inhibitor that selectively targets the Janus kinase 2 (JAK2) enzyme. It is commonly used in laboratory research to study the signaling pathways involving JAK2.
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AG490 is a small molecule inhibitor that targets the Janus kinase 2 (JAK2) enzyme. It is commonly used in cell-based research applications to study the role of JAK2 signaling pathways.
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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.
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AG490 is a selective tyrosine kinase inhibitor. It functions by inhibiting the JAK2/STAT3 signaling pathway.
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RPMI 1640 is a common cell culture medium used for the in vitro cultivation of a variety of cells, including human and animal cells. It provides a balanced salt solution and a source of essential nutrients and growth factors to support cell growth and proliferation.

More about "AG-490"

AG-490 is a tyrosine kinase inhibitor that has shown potential therapeutic applications in various fields, including oncology and immunology.
This small molecule compound, also known as Tyrphostin AG490, works by inhibiting the Janus kinase (JAK) signaling pathway, which plays a crucial role in cell growth, differentiation, and immune response regulation.
In cancer research, AG-490 has demonstrated the ability to suppress tumor cell proliferation, induce apoptosis, and enhance the efficacy of other anticancer agents.
It has been studied in the context of various malignancies, such as leukemia, lymphoma, and solid tumors.
Additionally, AG-490 has exhibited immunomodulatory effects, making it a potential candidate for therapeutic applications in autoimmune disorders and inflammatory conditions.
To facilitate efficient and reproducible AG-490 research, the AI-powered platform PubCompare.ai has been developed.
This innovative tool leverages advanced artificial intelligence (AI) algorithms to assist researchers in identifying relevant protocols from published literature, preprints, and patents.
By performing comprehensive comparisons, PubCompare.ai helps researchers easily locate the most suitable protocols, enhancing the accuracy and reproducibility of their AG-490 studies.
In the lab, AG-490 is commonly dissolved in the organic solvent DMSO (dimethyl sulfoxide) and used in cell culture experiments, often in combination with cell culture media like RPMI 1640 and FBS (fetal bovine serum).
Researchers may also utilize transfection reagents like Lipofectamine 2000 to introduce AG-490 or related constructs into cell lines.
Additionally, the PI3K/Akt inhibitor LY294002 has been used in conjunction with AG-490 to investigate the interplay between these signaling pathways.
By leveraging the insights and tools provided by PubCompare.ai, researchers can streamline their AG-490 investigations, leading to more informed and efficient research outcomes.