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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)。
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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)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 278 | 现货 | |
2 mg | ¥ 393 | 现货 | |
5 mg | ¥ 659 | 现货 | |
10 mg | ¥ 1,050 | 现货 | |
25 mg | ¥ 2,220 | 现货 | |
50 mg | ¥ 3,820 | 现货 | |
100 mg | ¥ 5,680 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 615 | 现货 |
产品描述 | YM-58483 (BTP2) is a specific and effective inhibitor of CRAC channels and subsequent Ca2+ signals. |
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]。 |
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. |
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) |
别名 | YM 58483, BTP2 |
分子量 | 421.32 |
分子式 | C15H9F6N5OS |
CAS No. | 223499-30-7 |
Smiles | Cc1nnsc1C(=O)Nc1ccc(cc1)-n1nc(cc1C(F)(F)F)C(F)(F)F |
密度 | 1.63 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: 78 mg/mL (185.1 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 78 mg/mL (185.1 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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