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Submit ReviewYM 58483
Description: Inhibitor of SOCE in non-excitable cells
Alternative Names: Btp2
Chemical Name: N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-1,2,3-thiadiazole-5-carboxamide
Purity: ≥99% (HPLC)
Biological Activity for YM 58483
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.
Compound Libraries for YM 58483
YM 58483 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for YM 58483
| M. Wt | 421.32 |
| Formula | C15H9F6N5OS |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 223499-30-7 |
| PubChem ID | 2455 |
| InChI Key | XPRZIORDEVHURQ-UHFFFAOYSA-N |
| Smiles | O=C(C3=C(C)N=NS3)NC1=CC=C(N2N=C(C(F)(F)F)C=C2C(F)(F)F)C=C1 |
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.
Solubility Data for YM 58483
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.13 | 100 | |
| ethanol | 42.13 | 100 |
Preparing Stock Solutions for YM 58483
The following data is based on the product molecular weight 421.32. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.37 mL | 11.87 mL | 23.73 mL |
| 5 mM | 0.47 mL | 2.37 mL | 4.75 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.37 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
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Product Datasheets for YM 58483
References for YM 58483
References are publications that support the biological activity of the product.
Ishikawa et al (2003) A pyrazole derivative, YM-58483, potently inhibits store-operated sustained Ca2+ influx and IL-2 production in T lymphocytes. J.Immunol. 170 4441 PMID: 12707319
Zitt et al (2004) Potent inhibition of Ca2+ release-activated Ca2+ channels and T-lymphocyte activation by the pyrazole derivative BTP2. J.Biol.Chem. 26 12427 PMID: 14718545
Ohga et al (2008) Characterization of YM-58483/BTP2, a novel store-operated Ca2+ entry blocker, on T cell-mediated immune responses in vivo. Int.Immunopharmocol. 8 1787 PMID: 18793756
If you know of a relevant reference for YM 58483, please let us know.
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Keywords: YM 58483, YM 58483 supplier, YM58483, inhibitor, inhibits, CRAC, SOCE, store-operated, channel, calcium, Ca2+, release, activated, entry, channels, inhibitors, Btp2, Other, Calcium, Channels, General, Signaling, Agents, STIM-Orai, 3939, Tocris Bioscience
10 Citations for YM 58483
Citations are publications that use Tocris products. Selected citations for YM 58483 include:
Faten et al (2021) Targeting CAMKK2 and SOC Channels as a Novel Therapeutic Approach for Sensitizing Acute Promyelocytic Leukemia Cells to All-Trans Retinoic Acid. Cells 10 PMID: 34943872
Olivier et al (2021) TRAIL Triggers CRAC-Dependent Calcium Influx and Apoptosis through the Recruitment of Autophagy Proteins to Death-Inducing Signaling Complex. Cells 11 PMID: 35011619
Robert J et al (2021) PAR-2-activated secretion by airway gland serous cells: role for CFTR and inhibition by Pseudomonas aeruginosa. Am J Physiol Lung Cell Mol Physiol 320 L845-L879 PMID: 33655758
Silvia et al (2021) RGS10 physically and functionally interacts with STIM2 and requires store-operated calcium entry to regulate pro-inflammatory gene expression in microglia. Cell Signal 83 109974 PMID: 33705894
Gao et al (2015) A store-operated calcium channel inhibitor attenuates collagen-induced arthritis. Br J Pharmacol 172 2991 PMID: 25651822
Martin et al (2017) Molecular Phenotyping Combines Molecular Information, Biological Relevance, and Patient Data to Improve Productivity of Early Drug Discovery. Cell Chem Biol 24 624-634.e3 PMID: 28434878
Gao et al (2013) Potent analgesic effects of a store-operated calcium channel inhibitor. Pain 154 2034 PMID: 23778292
Yanfeng et al (2022) Enhanced Orai1-mediated store-operated Ca2+ channel/calpain signaling contributes to high glucose-induced podocyte injury. J Biol Chem 298 101990 PMID: 35490782
Jeremy et al (2020) Calcium-stimulated disassembly of focal adhesions mediated by an ORP3/IQSec1 complex. Elife 9 PMID: 32234213
Gregory R et al (2020) Distinct pharmacological profiles of ORAI1, ORAI2, and ORAI3 channels. Cell Calcium 91 102281 PMID: 32896813
Do you know of a great paper that uses YM 58483 from Tocris? Please let us know.
Reviews for YM 58483
Average Rating: 4 (Based on 3 Reviews.)
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Inhibits calcium entry in mast cells..
By
ANANTH KUMAR KAMMALA on 01/30/2021
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: LAD2 - mast cells
YM 58483 was used to study the role of the MRGPRX2 receptor in store-operated calcium entry using human mast cells (LAD2 cells). At a concentration of 0.3 and 1 uM of YM58483 inhibited the calcium entry induced by cortistatin in mast cells.
BTP2 attenuates store-operated Ca2+ entry.
By
Anonymous on 07/10/2019
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: HEK293
HEK293 cells were incubated with intracellular Ca2+ sensitive dye, Fura-2AM in normal tyrode solution for 40 min, washed and kept aside for 20 min. Fura2-loaded cells were excited alternately at 340 and 380 nm and fluorescence at 510 nm was expressed as 340/380 ratio. Intracellular Ca2+ stores were depleted with 30 μM BHQ which promotes store-operated Ca2+ entry into the cells upon addition of 1 mM extracellular Ca2+. Preincubation of cells with 10 μM BTP2 (YM 58483) for 10 min attenuates this Ca2+ entry.
Store-operated calcium entry blocker.
By
Anonymous on 01/31/2018
Assay Type: Ex Vivo
Species: Mouse
Cell Line/Tissue: Brain slice
Used to block SOCE mechanism but no effect was seen. Unsure about efficacy of the compound, it might be a lack of SOCE involvement in the biological process studied here.