SB203580

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	兔	豚鼠	仓鼠	狗
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K_m系数（3），再除以大鼠的K_m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

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

• 

  Mar Drυgs. 2020 Aug 17;18(8):429.

  Comparison of Physicochemical Characteristics and Macrophage Immunostimulatory Activities of Polysaccharides from Chlamys farreri
  SB203580购买自AbMole

• 

  Int J Oncol. 2020 Jul;57(1):197-212.

  G6PD Facilitates Clear Cell Renal Cell Carcinoma Invasion by Enhancing MMP2 Expression Through ROS‑MAPK Axis Pathway
  SB203580购买自AbMole

• 

  Toxicol Appl Pharmacol. 2020 May 15;395:114981.

  Exposure to Diisononyl Phthalate Promotes Atopic March by Activating of NF-κB and p38 MAPK
  SB203580购买自AbMole

• 

  Front Immunol. 2019 Apr 26;10:913.

  IL-12 Expands and Differentiates Human Vγ2Vδ2 T Effector Cells Producing Antimicrobial Cytokines and Inhibiting Intracellular Mycobacterial Growth.
  SB203580购买自AbMole

• 

  Food Chem Toxicol. 2018 Feb 12;114:78-87.

  Exposure to diisodecyl phthalate exacerbated Th2 and Th17-mediated asthma through aggravating oxidative stress and the activation of p38 MAPK
  SB203580购买自AbMole

• 

  Nat Commun. 2015 Jan 19;6:6018.

  Increased atrial arrhythmia susceptibility induced by intense endurance exercise in mice requires TNFα.
  SB203580购买自AbMole

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.