YM 58483

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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)
Citations (10)
Reviews (3)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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.

View Related Products by Product Action

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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:

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

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

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..
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.

PMID: 32038646 Reference
review image

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.

review image

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.