Ym254890

Manufactured by MedChemExpress

Sourced in United States

YM254890 is a laboratory reagent that acts as a selective antagonist for the Gq protein. It inhibits the activity of Gq, a class of heterotrimeric G proteins involved in signal transduction pathways. YM254890 can be used in in vitro and cell-based assays to study Gq-mediated cellular processes.

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Lab products found in correlation

2 protocols using ym254890

Characterization of Signaling Pathways

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Isoproterenol, formoterol, GO6983, GO6976, RO32–0432, GF109203X, H89, PSB603, ESI-09, TPPB, NECA (adenosine-5′-N-ethyluronamide), MRS5698 and MRS2365 ([[(1R,2R,3S,4R,5S)-4-[6-amino-2-(methylthio)-9H-purin-9-yl]-2,3-dihydroxybicyclo[3.1.0]hex-1-yl]methyl] diphosphoric acid monoester trisodium salt) were purchased from Tocris (Ellisville, MO). CGS21680">CGS21680, carbachol, cholera toxin (CTX) and PTX were from Sigma (St. Louis, MO). YM254890, enzastaurin, LY333531, VTX-27 and AB928 were purchased from MedChemExpress (Monmouth Junction, NJ, USA). BAY60-6583 (LUF6210, termed hereafter ‘BAY’) was synthesized at Leiden/Amsterdam Center for Drug Research and was provided by Ad IJzerman (Leiden, The Netherlands). All compounds were dissolved in DMSO except that CTX and PTX were in water, and proper controls were included in all experiments. AlphaScreen cAMP kit, SureFire p-ERK1/2 (Thr202/Tyr204) Assay Kit and AlphaScreen SureFire p-Akt 1/2/3 (p-Ser473) Assay Kit were purchased from PerkinElmer (Waltham, MA). G_s-null and G_q/11-null HEK293 cells were generated at Tohoku University, Sendai, Japan. HEK293 human embryonic kidney, PC-3 human prostate cancer, NIH-3T3 mouse fibroblast, and H9C2 rat cardiomyoblast cells were from ATCC (Manassas, VA); all other reagents were from standard commercial sources and of analytical grade.

Gao Z.G., Levitan I.M., Inoue A., Wei Q, & Jacobson K.A. (2023). A2B adenosine receptor activation and modulation by protein kinase C. iScience, 26(7), 107178.

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Islet Insulin Secretion Dynamics

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For each experiment, 20 islets were perfused with a physiological solution (in mM) of 140 NaCl, 3.6 KCl, 2 NaHCO₃, 0.5 NaH₂PO₄, 0.5 MgSO₄, 5 HEPES, and 2.5 CaCl₂ with different glucose concentrations (2, 5, and 10 mM) at 37°C. The flow rate was set to 200 μL/min and the fractions collected every 2 minutes using an automated system. Insulin concentration in the fractions was measured with an ultrasensitive sandwich ELISA protocol. GLP-1 (1 nM; Bachem) and YM-254890 (100 nM; MedChemExpress) were added where indicated. To allow a direct comparison between different experiments, the insulin release per islet and unit of time was calculated based on islet area (87 (link)) and flow rate respectively. A picture of all the islets was obtained before the experiment using the Moticam 2500 camera connected to a fixed-focus dissection microscope. The area was calculated using the proprietary Moticam software that incorporates a calibrated distance measurement. The insulin concentration was multiplied by the correction factor representing the relative difference in islet area compared with the area of the largest islet group measured in all experiments.

Jacobo-Piqueras N., Theiner T., Geisler S.M, & Tuluc P. (2024). Molecular mechanism responsible for sex differences in electrical activity of mouse pancreatic β cells. JCI Insight, 9(6), e171609.

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