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SB203580

目录号 M1781 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


SB203580是一种p38 MAPK抑制剂,IC50为0.3-0.5 μM,与SAPK3(106T)和SAPK4(106T)相比选择性低10倍,且抑制PKB磷酸化,IC50为3-5 μM。

SB203580结构式

别名:RWJ 64809, PB 203580

包装 价格 库存状态
10mM*1mL 原价 ¥ 650
促销价 ¥ 617.5
中国库存现货
10mg 原价 ¥ 600
促销价 ¥ 570
中国库存现货
50mg 原价 ¥ 1380
促销价 ¥ 1311
中国库存现货
100mg 原价 ¥ 2320
促销价 ¥ 2204
中国库存现货
其他规格数量报价?

质量控制及产品安全说明书
生物活性

SB203580是一种p38 MAPK抑制剂,IC50为0.3-0.5 μM,与SAPK3(106T)和SAPK4(106T)相比选择性低10倍,且抑制PKB磷酸化,IC50为3-5 μM。SB203580作用于人类T细胞,鼠CT6 T细胞, 或BAF F7 B细胞,抑制IL-2诱导的增殖,IC50为3-5 μM。SB203580也抑制IL-2诱导的p70S6K激活, IC50 > 10 μM。SB203580也抑制PDK1活性,IC50为3-10 μM,这种抑制存在剂量依赖性。

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验
细胞系 CT6 cells,BA/F3 cells and PBMC/T cells
方法 2–5 × 106 rested CT6 cells were resuspended in 2 ml of RPMI, 5% fetal calf serum and preincubated with inhibitors or vehicle control as indicated in figure legends. Cells were then stimulated with 20 ng/ml recombinant human IL-2 for 5 min at 37 °C and pelleted in a minifuge for 30 s, medium was aspirated, and the pellet was lysed in the appropriate buffer. BA/F3 cells stably expressing deletion mutants of IL-2 receptor β chain (a generous gift from Professor T. Taniguchi, Tokyo, Japan) were maintained in glutamine containing RPMI further supplemented with 5% fetal calf serum and 0.2 μg/ml G418 (Calbiochem-Novabiochem) as described previously. Human peripheral blood mononuclear cells were prepared from buffy coat leukophoresis residues (North London Blood Transfusion Service, Colindale, London UK) and activated with 50 ng/ml OKT3 for 48 h. The cells were then washed extensively, rested overnight, and washed again before activating with IL-2; such cell preparations were >90% T cells . Cellular proliferation assays were performed by measurement of [3H]thymidine incorporation as described previously.
浓度 0~30 µm
处理时间 24 h
动物实验
动物模型 Systemic lupus erythematosus (SLE) model (female MRL/lpr mice and female C57BL/6 mice)
配制 Dissolved in drinking water (250 μM)
剂量 0.1 M/day
给药处理 orally
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。

化学数据
分子量 377.43
分子式 C21H16FN3OS
CAS号 152121-47-6
纯度 99.97%
溶解性(25°C) DMSO 43 mg/mL
储存和运输条件 固体粉末: -20°C 冷藏长期储存
常温运输及临时存放
储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.6495 mL 13.2475 mL 26.495 mL
5 mM 0.5299 mL 2.6495 mL 5.299 mL
10 mM 0.2649 mL 1.3247 mL 2.6495 mL
使用AbMole产品发表的文献
客户产品验证及相关生物数据
数据来源 Food Chem Toxicol (2018). Figure 6. SB203580 (Abmole Bioscience, Houston, TX, USA)
方法 i.p.
细胞系 SPF (specific pathogen free) male BALB/c mice
浓度 5 mg/kg
处理时间 0 to 20 days
实验结果 To clarify the underlying mechanism of DIDP exposure on Th17 type asthmatic lesions, SB203580 was used to block the p38 MAPK signaling pathway.
数据来源 Nat Commun (2015). Figure 7. SB203580 (AbMole Bioscience)
方法 atrial arrhythmia induction and picrosirius red-stained atrial sections
细胞系
浓度 i.p.4 mg/kg
处理时间 6 weeks
实验结果 Treatment of mice with the p38 inhibitor SB203580 during the 6-week exercise period completely prevented AF as well as atrial fibrosis.
参考文献

Induction of autophagy in hepatocellular carcinoma cells by SB203580 requires activation of AMPK and DAPK but not p38 MAPK.
Zhang H, et al. Apoptosis. 2012 Apr;17(4):325-34. PMID: 22170404.

SB203580, a specific inhibitor of p38-MAPK pathway, is a new reversal agent of P-glycoprotein-mediated multidrug resistance.
Barancík M, et al. Eur J Pharm Sci. 2001 Aug;14(1):29-36. PMID: 11457647.

The MAP kinase inhibitors, PD098059, UO126 and SB203580, inhibit IL-1beta-dependent PGE(2) release via mechanistically distinct processes.
Newton R, et al. Br J Pharmacol. 2000 Jul;130(6):1353-61. PMID: 10903976.

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