Gsk2795039

Manufactured by Merck Group

Sourced in United States, United Kingdom

GSK2795039 is a laboratory equipment product. It is a device used for scientific research and analysis purposes. The core function of this product is to facilitate specific laboratory procedures or measurements, though the exact details of its intended use are not available.

Automatically generated - may contain errors

Lab products found in correlation

Hydrogen peroxide, by Thermo Fisher Scientific (1 mentions) Difmup, by Thermo Fisher Scientific (1 mentions) N acetyl cysteine (nac), by Merck Group (1 mentions) Rotenone, by Merck Group (1 mentions) Shp099, by Selleck Chemicals (1 mentions) Gkt137831, by Selleck Chemicals (1 mentions) Alexidine dihydrochloride, by Merck Group (1 mentions) P akt ser473, by Cell Signaling Technology (1 mentions) Cycloheximide (chx), by Selleck Chemicals (1 mentions) γh2ax, by Cell Signaling Technology (1 mentions) Pou2f1, by Abcam (1 mentions) Trim21, by Abcam (1 mentions) Horseradish peroxidase hrp conjugated goat anti rabbit igg, by Beyotime (1 mentions) Goat anti mouse igg, by Beyotime (1 mentions) Mg132, by Selleck Chemicals (1 mentions) Bcl 2, by Proteintech (1 mentions) α tubulin, by Proteintech (1 mentions) Gsk1016790a, by Merck Group (1 mentions) Endothelin 1 et 1, by Merck Group (1 mentions) Hc067047, by Bio-Techne (1 mentions)

7 protocols using gsk2795039

Molecular Inhibitors in Cellular Assays

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Rotenone, NAC, GSK2795039,Ebselen, DPI, GSK2795039 and alexidine dihydrochloride were purchased from Sigma-Aldrich. Glutamine L-[5-14C] was from ARC. SHP099 and GKT137831 was purchased from Selleckchem. TCS401, ML090 was purchased from CAYMAN.GLX351322 was purchased from MCE. Mito-TEMPO, DiFMUP and hydrogen peroxide were purchase from Fisher Scientific. Si-IDH1, Si-NOX1, si-NOX3, si-SHP-2 were purchase from Sigma. si-PTP1B and si-PTPMT1 were purchased from Qiagen. si-NOX2 was synthesized by IDT. Primers was synthesized by IDT (The Sequence of siRNA are listed in Key Resources Table).

Zhang R., Chen D., Fan H., Wu R., Tu J., Zhang F.Q., Wang M., Zheng H., Qu C.K., Elf S.E., Faubert B., He Y.Y., Bissonnette M.B., Gao X., DeBerardinis R.J, & Chen J. (2022). Cellular signals converge at the NOX2-SHP-2 axis to induce reductive carboxylation in cancer cells. Cell chemical biology, 29(7), 1200-1208.e6.

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Immunoblotting Assay for Signaling Pathways

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The specific reagents included the primary antibodies against AKT, POU2F1, and TRIM21 (Abcam, London, UK); against PI3K^p100α, γ-H₂AX, 53BP1 and p-AKT^Ser473 (Cell Signaling Technology, Danvers, MA, USA); against α-tubulin, BCL-2 and BAX (Proteintech, Chicago, USA); horseradish peroxidase (HRP)-conjugated goat anti-rabbit IgG or goat anti-mouse IgG (Beyotime, Shanghai, China). GSK2795039, 3-MA and DADS (oil, ≥98%, and 1.008 g/mL) were purchased from Sigma, (Saint Louis, Missouri, USA), and the DADS was fully dissolved in Tween 80 and diluted at 1:100 in physiological saline and stored in a -20°C freezer. Additionally, 740Y-P, LY49002, MG132, AG activator 1 and cycloheximide as well as AV-153, an antimutagenic molecule were obtained from Selleckchem, Houston, USA and MedChenExpress, Monmouth Junctio, USA, respectively.

Xia L., Lin J., Peng M., Jiang X., Peng Q., Cui S., Zhang W., Li S., Wang J., Oyang L., Tan S., Hu Z., Wu N., Tang Y., Luo X., Ren Z., Shi Y., Liao Q, & Zhou Y. (2024). Diallyl disulfide induces DNA damage and growth inhibition in colorectal cancer cells by promoting POU2F1 ubiquitination. International Journal of Biological Sciences, 20(4), 1125-1141.

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Endothelin-1 Signaling Pathway Modulation

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GSK1016790A, GSK2795039, SNP, and Endothelin-1 (ET-1) were obtained from Sigma-Aldrich. GKT1372831 was obtained from MCE MedChemExpress. HC067047 was obtained from Tocris Bioscience. All other chemicals were purchased from Sigma. Stock solutions were prepared in DMSO (1000× or higher). ET-1 stock was prepared in saline solution supplemented with 1% BSA. Working stocks were freshly prepared in distilled water.

Xie Y., Nishijima Y., Zinkevich N.S., Korishettar A., Fang J., Mathison A.J., Zimmermann M.T., Wilcox D.A., Gutterman D.D., Shen Y, & Zhang D.X. (2022). NADPH oxidase 4 contributes to TRPV4-mediated endothelium-dependent vasodilation in human arterioles by regulating protein phosphorylation of TRPV4 channels. Basic research in cardiology, 117(1), 24.

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Alzheimer's Disease Mouse Model Treatment

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Drugs were administered 1-month post-surgery to avoid surgery side effects. Mice were allocated to three groups: control (n = 6), Aβ (n = 5), and Aβ + GSK2795039 (n = 6). Injections were made i.c.v. through the guide cannula (1 μl/min) to awake mice. All substances were injected in equal volumes (1 μl) and the guide cannula was closed by a plunger. Mice in the Aβ + GSK2795039 group received GSK2795039 (MedChemExpress Europe; 4.5 mg/ml in DMSO) and oligomeric Aβ_1-42 (Sigma-Aldrich, 1 mg/ml in 1.0% NH4OH) on the first day, and daily GSK2795039 further for 14 days. Mice in the Aβ group received Aβ_1-42 on the first day and daily DMSO for the following 14 days. Mice in the сontrol group received daily DMSO for 15 days.

Malkov A., Popova I., Ivanov A., Jang S.S., Yoon S.Y., Osypov A., Huang Y., Zilberter Y, & Zilberter M. (2021). Aβ initiates brain hypometabolism, network dysfunction and behavioral abnormalities via NOX2-induced oxidative stress in mice. Communications Biology, 4, 1054.

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ACE Inhibition and Oxidative Stress Response

Cited 1 time

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Inhibitor treatment assays were performed on serum-starved primary monocytes or THP-1 cells. ACE ligand Angiotensin I (#1563/1, R&D) was added at a concentration of 1μM both alone and in combination with the following inhibitors: 1μM of ACE inhibitor lisinopril (21CEC PX Pharm Ltd., Sussex, UK), 10μM of the NADPH oxidase 2 (NOX2) inhibitor GSK2795039 (#SML2770G, Sigma Aldrich), and 20μM of type 1 angiotensin receptor (AGTR1) inhibitor Irbesartan (#I2286, Sigma Aldrich). Based on an established protocol in the THP-1 cell line (24 (link)), cells were exposed to 5 Gy irradiation at 2 hours following inhibitor treatment. At 24 hours post-irradiation, THP-1 or CD14⁺ peripheral blood cells were assessed as described below for ACE activation, MCP-1 ELISA, intracellular ROS generation, or endothelial cell adhesion.

Sharma G.P., Fish B.L., Frei A.C., Narayanan J., Gasperetti T., Scholler D., Pierce L., Szalewski N., Blue N., Medhora M, & Himburg H.A. (2022). Pharmacological ACE-inhibition Mitigates Radiation-Induced Pneumonitis by Suppressing ACE-expressing Lung Myeloid Cells. International journal of radiation oncology, biology, physics, 113(1), 177-191.

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Necroptosis Inhibitor Compounds Evaluation

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PF-573-228 and necrostatin-1 were purchased from MedChem Express (Monmouth, NJ), while necrostatin-1s was purchased from New England Biolabs (Ipswich, MA). GSK-872 was purchased from Tocris (Toronto, Canada). Necrosulfonamide (NSA), N-acetyl cysteine (NAC), PF-562-271, and GSK2795039 were purchased from Millipore Sigma.

Afriyie-Asante A., Dabla A., Dagenais A., Berton S., Smyth R, & Sun J. (2021). Mycobacterium tuberculosis Exploits Focal Adhesion Kinase to Induce Necrotic Cell Death and Inhibit Reactive Oxygen Species Production. Frontiers in Immunology, 12, 742370.

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Reconstitution and Preparation of Bioactive Compounds

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1% bovine serum albumin (BSA) solution was used to dissolve endothelin-1 (Millipore Sigma, St. Louis, MO, USA). Methanol (MeOH) and 0.3M NaOH solution were used to reconstitute S1P (Millipore Sigma, St. Louis, MO, USA and Cayman Chemical, Ann Arbor, MI, USA) according to the manufacturer’s recommendations. W146 (Cayman Chemical & Tocris Bioscience, Minneapolis, MN, USA) was reconstituted in MeOH and 0.03M NaOH. CAY10444 and c-PTIO (Cayman Chemical) were dissolved in dimethylformamide and water, respectively. GKT137831 (Cayman Chemical) and GSK2795039 (Millipore Sigma) were both dissolved in ethanol. Apocynin and PEG-Catalase (Millipore Sigma) were dissolved in MeOH and water, respectively. Acetylcholine (Millipore Sigma) was diluted in water. S1P receptor antibodies were purchased from Invitrogen by Thermo Fisher (Thermo Fisher Scientific, Waltham, MA, USA). ROS-ID® NO Detection kit (Enzo Life Sciences, Enzo Biochem, Farmingdale, New York) was dissolved in HEPES buffer at the time of the experiment.

Katunaric B., SenthilKumar G., Schulz M.E., De Oliveira N, & Freed J.K. (2022). Sphingosine-1-Phosphate-Induced Vasodilation in Human Resistance Arterioles During Health and Disease. Hypertension (Dallas, Tex. : 1979), 79(10), 2250-2261.

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