Gsk4112

Manufactured by Bio-Techne

Sourced in United Kingdom

GSK4112 is a small molecule compound that acts as an agonist for the nuclear receptor REV-ERB. It is used in research applications to modulate the activity of REV-ERB, which plays a role in circadian rhythm and metabolic regulation.

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Lab products found in correlation

Sr8278, by Bio-Techne (2 mentions) Penicillin streptomycin glutamine (psg), by Thermo Fisher Scientific (2 mentions) Fetal bovine serum (fbs), by Thermo Fisher Scientific (2 mentions) F 12k medium, by Thermo Fisher Scientific (1 mentions) Hfl 1 cells, by American Type Culture Collection (1 mentions) Penicillin, by Thermo Fisher Scientific (1 mentions) Streptomycin, by Thermo Fisher Scientific (1 mentions) Rabbit anti opa1 antibody, by Abcam (1 mentions) P drp1 ser637, by Cell Signaling Technology (1 mentions) Rev erbα, by Cell Signaling Technology (1 mentions) P drp1 ser616, by Cell Signaling Technology (1 mentions) Gapdh, by Cell Signaling Technology (1 mentions) Trypsin edta, by Thermo Fisher Scientific (1 mentions) Sinapic acid, by Merck Group (1 mentions) Staurosporine, by Bio-Techne (1 mentions) Sr1001, by Bio-Techne (1 mentions) Sr1078, by Bio-Techne (1 mentions)

4 protocols using gsk4112

TGF-β and Cigarette Smoke Exposure in HFL-1 Cells

Cited 1 time

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HFL-1 cells were purchased from ATCC, and cultured in DMEM: F12K medium (11320033; Thermo Fisher Scientific) with 10% FBS (10082147; Thermo Fisher Scientific), 1% Penicillin-Streptomycin-Glutamine (10378016; Thermo Fisher Scientific), and 1% Non-Essential Amino Acids (11140076, Thermo Fisher Scientific). Before treatment, cells were serum deprived for 12 hours and then treated with 5 ng/mL TGF-β with or without 10 μM GSK4112 (3663; TOCRIS) for 3 days; or 0.1% CSE with or without 10 μM GSK4112 or 0.25% CSE for 2 days. CSE stock was always prepared freshly right before the treatment as described previously (13 (link)). In brief, CS (3R4F, University of Kentucky) was bubbling into 10 mL FBS-free DMEM: F12K medium (Phenol-red free) as 10% CSE stock. The 0.25% and 0.1% CSE working solutions were diluted from the stock CSE. Quality control of the CSE was based on the absorbance at 320 nm (1.00 ± 0.05 nm).

Wang Q., Sundar I.K., Lucas J.H., Muthumalage T, & Rahman I. (2021). Molecular clock REV-ERBα regulates cigarette smoke–induced pulmonary inflammation and epithelial-mesenchymal transition. JCI Insight, 6(12), e145200.

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Rev-erbα Agonist GSK4112 Protocol

Cited 1 time

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GSK4112 (TOCRIS, Bristol, UK) is a Rev-erbα agonist [23 (link)]. GSK4112 was dissolved in DMSO (Solaibao, Beijing, China) to 25 mM and the stock solutions were stored at −20 °C.

Chu G., Zhou X., Hu Y., Shi S, & Yang G. (2019). Rev-erbα Inhibits Proliferation and Promotes Apoptosis of Preadipocytes through the Agonist GSK4112. International Journal of Molecular Sciences, 20(18), 4524.

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Mitochondrial Dynamics in Parkinson's Disease

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Sinapic acid (SA, Cat# D7927), MPTP (Cat# M0896) and MPP⁺ (Cat# D048) were obtained from Sigma–Aldrich (St. Louis, MO, USA). SR8278 (SR, Cat# 4463) and GSK4112 (GSK, Cat# 3663) were purchased from Tocris Bioscience (Bristol, UK). DMEM and FBS were obtained from HyClone (Logan, UT, USA). Trypsin-EDTA and a mixture of penicillin and streptomycin were purchased from Gibco-BRL (Grand Island, NY, USA). Rabbit anti-TH (Cat# 2792S), REV-ERB α (Cat# 13418S), p-Drp1 Ser616 (Cat# 3455S), p-Drp1 Ser637 (Cat# 4867S), and GAPDH (Cat# 2118S) were purchased from Cell Signaling Technology Inc (Boston, MA, USA). Anti-rabbit (Cat# 7074S) and mouse (Cat# 7076S) horseradish peroxidase (HRP)-linked IgG antibodies were also obtained from Cell Signaling Technology Inc. The mouse anti-Drp1 antibody (Cat# sc-271583) was purchased from Santa Cruz Biotechnology Inc (Santa Cruz, CA, USA). The rabbit anti-OPA1 antibody (Cat# ab157457) and MFN2 (Cat# ab56889) were purchased from Abcam (Cambridge, UK).

Lee S.B, & Yang H.O. (2022). Sinapic Acid Ameliorates REV-ERB α Modulated Mitochondrial Fission against MPTP-Induced Parkinson’s Disease Model. Biomolecules & Therapeutics, 30(5), 409-417.

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Drug Compound Preparation Protocol

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GSK4112, SR8278, SR1001, SR1078, lithium chloride and staurosporine (STS) were purchased from Tocris. Drugs were dissolved in DMSO or water and stored as concentrated solutions at −80°C prior to use.

Mishra H.K., Wei H., LeRoux M., Ko I., Rohr K.E., Nievergelt C.M., Maihofer A.X., Shilling P., Alda M., Berrettini W.H., Calabrese J.R., Coryell W.H., Frye M., Gershon E., McInnis M.G., Nurnberger J., Oedegaard K.J., Zandi P.P., Kelsoe J.R, & McCarthy M.J. (2024). Differential contributions of circadian clock genes to cell survival in bipolar disorder patient derived neuronal progenitor cells distinguishes lithium responders and non-responders. Research Square.

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