YM-58483 (BTP2)

Catalog No.S8380

Molecular Weight(MW): 421.32

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

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5mg	USD 97	In stock
25mg	USD 327	In stock
100mg	USD 977	In stock
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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

Cell Research: ^[2]	+ Expand 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. (Only for Reference)
Animal Research: ^[1]	+ Expand Animal Models: Male C57BL/6, BDF1((C57BL/6×DBA2)F1), DBA2 and Balb/c mice Formulation: 0.5% methylcellulose solution Dosages: 1-30 mg/kg Administration: p.o. (Only for Reference)

Cell Research:

^[2]

+ Expand

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.

(Only for Reference)

Animal Research:

^[1]

+ Expand

Animal Models: Male C57BL/6, BDF1((C57BL/6×DBA2)F1), DBA2 and Balb/c mice
Formulation: 0.5% methylcellulose solution
Dosages: 1-30 mg/kg
Administration: p.o.
(Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	84 mg/mL (199.37 mM)
	Ethanol	84 mg/mL (199.37 mM)
	Water	Insoluble
In vivo	Add solvents individually and in order: 1% CMC Na	30mg/mL

* 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.

Chemical Information Download YM-58483 (BTP2) SDF

Molecular Weight	421.32
Formula	C₁₅H₉F₆N₅OS
CAS No.	223499-30-7
Storage	3 years -20°C powder
Synonyms	N/A

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