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Adezmapimod (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  


Adezmapimod (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。Adezmapimod 不抑制 JNK 活性,是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 激活剂。

Adezmapimod (SB203580)结构式

别名:RWJ 64809; PB 203580; Adezmapimod

规格 价格 库存状态
Free Sample (0.5-1 mg)  ¥ 0 中国库存现货
10mM*1mL in DMSO ¥ 600 中国库存现货
5mg ¥ 400 中国库存现货
10mg ¥ 550 中国库存现货
50mg ¥ 1300 中国库存现货
100mg ¥ 2200 中国库存现货
其他规格数量报价?

质量标准及产品资料
生物活性

Adezmapimod (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。Adezmapimod 不抑制 JNK 活性,是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 激活剂。

使用AbMole产品发表的文献
产品使用成果展示
数据来源 Food Chem Toxicol (2018). Figure 6. SB203580 (Abmole Bioscience, Houston, TX, USA)
方法 i.p.
细胞系/动物模型 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/动物模型
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.
实验参考
体外实验*
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

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

体内实验*
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

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

化学性质
分子量 377.43
分子式 C21H16FN3OS
CAS号 152121-47-6
溶解性(25°C) DMSO 20 mg/mL (ultrasonic and warming)
储存条件 粉末型式       -20°C   3年;4°C   2年
溶于溶剂       -80°C   6个月;-20°C   1个月
运输方式 冰袋运输,根据产品的不同,可能会有相应调整。
储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。

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
不同实验动物依据体表面积的等效剂量转换表(参考来源于公开文献
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,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Zhang H, et al. Apoptosis. Induction of autophagy in hepatocellular carcinoma cells by SB203580 requires activation of AMPK and DAPK but not p38 MAPK.

[2] Barancík M, et al. Eur J Pharm Sci. SB203580, a specific inhibitor of p38-MAPK pathway, is a new reversal agent of P-glycoprotein-mediated multidrug resistance.

[3] Newton R, et al. Br J Pharmacol. The MAP kinase inhibitors, PD098059, UO126 and SB203580, inhibit IL-1beta-dependent PGE(2) release via mechanistically distinct processes.

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