YM 58483
Chemical Name: N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-1,2,3-thiadiazole-5-carboxamide
Purity: ≥99%
Biological Activity
YM 58483 is a blocker of store-operated Ca2+ entry (SOCE), which mediates the activation of non-excitable cells (e.g. lymphocytes). Inhibits calcium release-activated calcium (CRAC) channels; suppresses thapsigargin-induced sustained Ca2+ influx (IC50 = 100 nM). Displays immuno-modulatory and anti-inflammatory effects; suppresses cytokine production and proliferation of T cells in vitro.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Functional Characterization of the Odorant Receptor 51E2 in Human Melanocytes
J Biol Chem, 2016;0(0):. -
BKCa channel regulates calcium oscillations induced by alpha-2-macroglobulin in human myometrial smooth muscle cells
M Wakle-Prab, RA Lorca, X Ma, SJ Stamnes, C Amazu, JJ Hsiao, CM Karch, KL Hyrc, ME Wright, SK England
Proc Natl Acad Sci USA, 2016;113(16):E2335-44. -
A pyrazole derivative, YM-58483, potently inhibits store-operated sustained Ca2+ influx and IL-2 production in T lymphocytes.
Ishikawa et al.
J.Immunol., 2003;170:4441
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Citations for YM 58483
The citations listed below are publications that use Tocris products. Selected citations for YM 58483 include:
10 Citations: Showing 1 - 10
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Enhanced Orai1-mediated store-operated Ca2+ channel/calpain signaling contributes to high glucose-induced podocyte injury.
Authors: Yanfeng Et al.
J Biol Chem 2022;298:101990
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RGS10 physically and functionally interacts with STIM2 and requires store-operated calcium entry to regulate pro-inflammatory gene expression in microglia.
Authors: Silvia Et al.
Cell Signal 2021;83:109974
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PAR-2-activated secretion by airway gland serous cells: role for CFTR and inhibition by Pseudomonas aeruginosa.
Authors: Robert J Et al.
Am J Physiol Lung Cell Mol Physiol 2021;320:L845-L879
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TRAIL Triggers CRAC-Dependent Calcium Influx and Apoptosis through the Recruitment of Autophagy Proteins to Death-Inducing Signaling Complex.
Authors: Olivier Et al.
Cells 2021;11
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Targeting CAMKK2 and SOC Channels as a Novel Therapeutic Approach for Sensitizing Acute Promyelocytic Leukemia Cells to All-Trans Retinoic Acid.
Authors: Faten Et al.
Cells 2021;10
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Distinct pharmacological profiles of ORAI1, ORAI2, and ORAI3 channels.
Authors: Gregory R Et al.
Cell Calcium 2020;91:102281
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Calcium-stimulated disassembly of focal adhesions mediated by an ORP3/IQSec1 complex.
Authors: Jeremy Et al.
Elife 2020;9
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Molecular Phenotyping Combines Molecular Information, Biological Relevance, and Patient Data to Improve Productivity of Early Drug Discovery.
Authors: Martin Et al.
Cell Chem Biol 2017;24:624-634.e3
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A store-operated calcium channel inhibitor attenuates collagen-induced arthritis.
Authors: Gao Et al.
Br J Pharmacol 2015;172:2991
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Potent analgesic effects of a store-operated calcium channel inhibitor.
Authors: Gao Et al.
Pain 2013;154:2034
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