YM-58483 (BTP2)

Catalog No.S8380 Batch:S838001

Technical Data

Formula	C₁₅H₉F₆N₅OS
Molecular Weight	421.32	CAS No.	223499-30-7
Solubility (25°C)*	In vitro	DMSO	84 mg/mL (199.37 mM)
		Ethanol	42 mg/mL (99.68 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

YM-58483/BTP2 is a blocker of store-operated Ca2+ entry (SOCE), which regulates the activation of non-excitable cells such as lymphocytes.

Targets

SOCE ^[1]

In vitro

YM-58483 (also known as BTP2) is a selective SOCE blocker that inhibits anti-CD3 antibody-induced sustained Ca2+ influx in Jurkat T cells. YM-58483 does not cross-react with voltage-operated Ca2+ entry, K+ channels, or Cl− channels. It suppresses the CRAC, TRPC3, and TRPC5 channels, and also facilitates the TRPM4 channel. YM-58483 suppresses cytokine production (IL-2, IL-4, IL-5, IFN-γ, etc.) and proliferation in T cells in vitro. YM-58483 inhibits the spleen cell proliferation associated with MLR by suppressing NF-AT activation via sustained influx of extracellular Ca2+^[1]. YM-58483 potently inhibits IL-2 production and NF-AT-driven promoter activity, but not AP-1-driven promoter activity in Jurkat cells^[2].

In vivo

YM-58483 exhibits inhibitory effects on several types of allergic asthma models, such as airway hyperresponsiveness, early and late bronchoconstriction, and antigen-induced airway eosinophilia, with the reduction of IL-4 and leukotriene levels in the airways of rats and guinea pigs. YM-58483 also inhibits the anti-host CTL response, donor T cell expansion, and IFN-γ production in GVHD mice. YM-58483 selectively inhibits storeoperated Ca2+ influx, it does not affect baseline intracellular Ca2+ levels. YM-58483 caused no apparent change in general activity in mice at doses up to 30 mg/kg, p. o^[1].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Jurkat cells Concentrations 0.03-3 μM Incubation Time 30 min Method Jurkat cells (1×10⁷ cells/ml) were tested with varying concentration of compounds for 30 min at 37°C. The cells were stimulated with 1 μM ionomycin for 30 min at 37°C. After stimulation, the cells were centrifuged at 200×g for 2 min, and were solubilized in 100 μl of Triton X-100 lysis buffer. The cell lysate was centrifuged at 15,000×g for 20 min; the clarified lysate was subjected to SDS-PAGE; and NF-ATc2 was detected by Western blotting with anti-NF-ATc2 mAb.
Animal Study:^{^[1]}	Animal Models Male C57BL/6, BDF1((C57BL/6×DBA2)F1), DBA2 and Balb/c mice Dosages 1-30 mg/kg Administration p.o.

Cell Assay:^{^[2]}

Cell lines
Jurkat cells
Concentrations
0.03-3 μM
Incubation Time
30 min
Method
Jurkat cells (1×10⁷ cells/ml) were tested with varying concentration of compounds for 30 min at 37°C. The cells were stimulated with 1 μM ionomycin for 30 min at 37°C. After stimulation, the cells were centrifuged at 200×g for 2 min, and were solubilized in 100 μl of Triton X-100 lysis buffer. The cell lysate was centrifuged at 15,000×g for 20 min; the clarified lysate was subjected to SDS-PAGE; and NF-ATc2 was detected by Western blotting with anti-NF-ATc2 mAb.

Animal Study:^{^[1]}

Animal Models
Male C57BL/6, BDF1((C57BL/6×DBA2)F1), DBA2 and Balb/c mice
Dosages
1-30 mg/kg
Administration
p.o.

References

Selleck's YM-58483 (BTP2) has been cited by 5 publications

Lysosomal Ca2+ as a mediator of palmitate-induced lipotoxicity [ Cell Death Discov, 2023, 9(1):100]	PubMed: 36944629
Sensing plasma membrane pore formation induces chemokine production in survivors of regulated necrosis [ Dev Cell, 2022, S1534-5807(21)01035-2]	PubMed: 35016014
Mannan-Binding Lectin Reduces Epithelial-Mesenchymal Transition in Pulmonary Fibrosis via Inactivating the Store-Operated Calcium Entry Machinery [ J Innate Immun, 2022, 1-13]	PubMed: 35671705
Ang II Promotes Cardiac Autophagy and Hypertrophy via Orai1/STIM1 [ Front Pharmacol, 2021, 12:622774]	PubMed: 34079454
Epithelial Sodium Channel Regulates Adult Neural Stem Cell Proliferation in a Flow-Dependent Manner. [ Cell Stem Cell, 2018, 22(6):865-878]	PubMed: 29779889

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SHIPPING AND STORAGE
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