化合物YM58483 T3651

Product Introduction
Bioactivity


英文名: YM-58483

描述: YM-58483 (BTP2) 是一种特异性有效的 CRAC 通道和随后的 Ca2+ 信号抑制剂，可阻断钙池操纵的阳离子内流 (SOCE)。

细胞实验: 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)

激酶实验: HCT-116 cells are washed with PBS and then homogenized with a 27-gauge syringe in binding buffer (10 mm Tris-HCl (pH 7.4), 50 mm KCl, 5 mm MgCl2, 1 mm EDTA, and 0.1 mm Na3VO4). The cell lysate is centrifuged at 13,000 rpm for 30 min at 4°C, and the supernatant is collected. The HCT-116 cell lysate supernatant is precleared by incubating with Dynabeads M-280 streptavidin for 30 min at 4°C and captured by magnet separation. The cleared supernatants are incubated with biotinyl-KRIBB11 compound. After overnight incubation at 4°C, proteins associated with the biotinyl-KRIBB11 compound are precipitated with Dynabeads M-280 streptavidin. Precipitated samples are separated by a magnet. Samples are washed with 1 mL of ishing buffer containing 50 mm HEPES (pH 7.5), 50 mm NaCl, 1 mm EDTA, 1 mm EGTA, 0.1% Tween 20, 10% (v/v) glycerol, 1 mm NaF, 0.1 mm Na3VO4, and protease inhibitor mixture tablets (1 tablet/10 mL). Samples are boiled in SDS-PAGE sample buffer, separated by 10% polyacrylamide gel, and immunoblotted with antibodies against HSF1, HSF2, HSP90, or CDK9.

体外活性: 在多种过敏性哮喘模型,如气道高反应、早期和晚期支气管狭窄、抗原诱导的气道嗜酸性粒细胞中,YM-58483均有抑制效果,在大鼠和豚鼠器官中还出现白三烯、IL-4水平的降低.在GVHD小鼠中,YM-58483还可抑制抗宿主CTL反应、供体T细胞扩张及IFN-γ的产生.YM-58483（30 mg/kg,p.o.）对小鼠的一般活动没有明显影响[1].

体内活性: 作为选择性SOCE阻滞剂,YM-58483在Jurkat T细胞中抑制anti-CD3抗体所诱导的持续性钙离子流入。它抑制CRAC、TRPC3和TRPC5通道、促进TRPM4通道,抑制细胞因子的产生（IL-2, IL-4, IL-5, IFN-γ等）及T细胞的增殖。通过抑制NF-AT的激活,YM-58483可抑制MLR相关的脾细胞增殖[1]。YM-58483对IL-2的产生和NF-AT驱动的启动子活性也有明显的抑制作用,但不影响Jurkat细胞中AP-1驱动的启动子活性[2]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 78 mg/mL (185.1 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 78 mg/mL (185.1 mM)


关键字: inhibit | CRAC Channel | Ca2+ release-activated Ca2+ channels | YM58483 | Calcium release-activated channels | BTP 2 | YM-58483 | BTP-2 | Inhibitor

相关产品: FS-2 | CP-060 | Calciseptin | TTA-A8 | Levosemotiadil | Atherosperminine | NS-638 | Nilvadipine | Nicardipine | LY393615

相关库: Ion Channel Inhibitor Library | Anti-Hypertension Compound Library | Bioactive Lipid Compound Library | Calcium Channel Compound Library | Membrane Protein-targeted Compound Library | Anti-Metabolism Disease Compound Library | Inhibitor Library | Metabolism Compound Library | Anti-Cardiovascular Disease Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途