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My CartCAS：152121-47-6
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to light yellow Solid
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| CAS | 152121-47-6 |
| Name | SB-203580 |
| Molecular Formula | C21H16FN3OS |
| Molecular Weight | 377.43 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to light yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00922198 |
| SMILES | O=S(C1=CC=C(C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)C=C1)C |
| Target Point | p38 MAPK，LCK，GSK3β,PKBα，Autophagy, Mitophagy |
| Passage | MAPK;PI3K/Akt/mTOR;Stem Cells;Protein Tyrosine Kinase/RTK;Autophagy |
| Background | SB-203580 is a selective, ATP-competitive inhibitor of p38 MAPK that also inhibits LCK, GSK3β and PKα. SB-203580 is an activator of autophagy and mitophagy. |
| Biological Activity | SB 203580是一种广泛使用的 p38 MAPK 抑制剂， IC50 介于 0.3-0.5μM 之间。 对 p38 MAPK 的选择性比 PKB, LCK, 和 GSK-3β 高100倍。SB 203580能够以剂量依赖性方式抑制PDK1的活性，IC50在3-10μM范围内。[1-5] |
| In Vitro | SB 203580抑制IL-2驱动的T细胞增殖，IC50为3-5μM，SB 203580能够以剂量依赖性方式抑制PDK1的活性，IC50在3-10μM范围内[1]。浓度为1μM的SB 203580足以抑制TF-1细胞中的p38激酶活性。 5和10μM的SB 203580增强NF-κB介导的基因转录，而与p65亚基的反式激活结构域上的磷酸化无关。 10μM的SB 203580增强了ERK1/2和JNK的磷酸化[1]。 |
| In Vivo | 所有动物用NS(未感染的对照)攻击并用SB203580或安慰剂治疗存活。与安慰剂相比，在大肠杆菌前1小时用最高剂量的SB203580(100mg/kg)预处理增加了死亡的危害比。对于大肠杆菌，与安慰剂相比，在48小时但不是24小时，低剂量和高剂量SB203580降低磷酸化的p38MAPK和磷酸化与总p38的比率。高剂量SB203580在24小时时在组织学上降低肺中性粒细胞的趋势接近显著性(p = 0.09)并且在48小时时显著增加(p = 0.01)，其模式随时间不同[3]。在几种细胞因子抑制和炎性疾病模型中评估SB 203580。显然，它是小鼠和大鼠中炎性细胞因子产生的有效抑制剂，IC50值为15至25mg/kg [4]。 |
| Cell Experiment | 通过蛋白质印迹分析p38，JNK1/2和ERK1/2的磷酸化。简而言之，将TF-1细胞在含有0.1％FBS的RPMI 1640中培养16小时，随后用培养基或OA(30ng/mL)或SB 203580(1μM，5μM，10μM)加刺激不同时间段。 OA。收获后，通过将细胞重悬于500μL1×样品缓冲液(含有2％SDS，10％甘油，2％β-巯基乙醇，60mM Tris-HCl(pH6.8)和溴酚蓝)中并裂解来制备总细胞提取物。将细胞通过23G1针头(三次)。将细胞提取物直接煮沸10分钟并储存在-20℃。在上样之前，将样品再次煮沸5分钟，并通过在SDS/12.5％PAGE凝胶(丙烯酰胺：双丙烯酰胺为173：1)上运行1/10体积来分离细胞提取物并转移至纤维素硝酸盐膜。用抗体进行免疫印迹通过标准程序进行并进行检测[2]。 |
| Animal Experiment | 小鼠[3]在存活研究中，将体重为20g至30g的C57BL/6J小鼠用异氟烷短暂麻醉并用0.05mL IT生理盐水(NS，未感染对照)或大肠杆菌(15×109CFU/kg)攻击。 。在NS攻击前1小时，小鼠(n = 24)接受腹膜内SB203580(100mg/kg，0.25mL)或仅稀释剂(安慰剂)。受感染的动物在IT大肠杆菌(n = 241)之前1小时接受剂量为100，10，1或0.1mg/kg的SB203580或安慰剂; SB203580 100或0.1 mg/kg或安慰剂在大肠杆菌后1小时(n = 121);在大肠杆菌(n = 72)后12小时或SB203580 100mg/kg或安慰剂。所有动物在攻击后4小时开始接受头孢曲松(100mg/kg，0.1mL，皮下)4天和NS(0.5mL，皮下)1天。最初48小时每2小时观察动物，48小时至72小时每4小时观察一次动物，72小时至96小时每8小时观察动物，然后每天观察两次直至研究完成(168小时)[3]。 |
| Data Literature Source | [1]. Lali FV，et al. The pyridinyl imidazole inhibitor SB203580 blocks phosphoinositide-dependent protein kinase activity，protein kinase B phosphorylation，and retinoblastoma hyperphosphorylation in interleukin-2-stimulated T cells independently of p38 mitogen-activated protein kinase. J Biol Chem. 2000 Mar 10;275(10):7395-402. [2]. Birkenkamp KU，et al. The p38 MAP kinase inhibitor SB203580 enhances nuclear factor-kappa B transcriptional activity by a non-specific effect upon the ERK pathway. Br J Pharmacol. 2000 Sep;131(1):99-107. [3]. Su J，et al. SB203580，a p38 inhibitor，improved cardiac function but worsened lung injury and survival during Escherichia coli pneumonia in mice. J Trauma. 2010 Jun;68(6):1317-27. [4]. Badger AM，et al. Pharmacological profile of SB 203580，a selective inhibitor of cytokine suppressive binding protein/p38 kinase，in animal models of arthritis，bone resorption，endotoxin shock and immune function. J Pharmacol Exp Ther. 1996 Dec;279(3):1453-61. [5]. Lin Y，et al. Critical role of astrocytic interleukin-17 A in post-stroke survival and neuronal differentiation of neural precursor cells in adult mice. Cell Death Dis. 2016 Jun 23;7(6):e2273 |
| Unit | Piece |
| Specification | 10mg 20mg 50mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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Alfhili MA, et. . Int J Occup Med Environ Health. 2022 Feb 15;35(1):1-11. doi: 10.13075/ijomeh.1896.01814.
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