SB 203580 hydrochlorideCAS号: 869185-85-3分子式: C21H16FN3OS HCl分子量: 413.9描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vivo(体内研究)参考文献
产品描述 | |
描述 |
SB 203580 hydrochloride is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM, also blocks PKB phosphorylation with IC50 of 3-5 μM. |
纯度 |
98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
RWJ 64809 hydrochloride
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外观 |
Powder
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可溶性/溶解性 |
Soluble in ethanol (~30 mg/ml), DMSO (~30 mg/ml), DMF (~30 mg/ml), 1:10 solution of ethanol:PBS(pH 7.2) (~0.1 mg/ml), and water (25 mM).
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生物活性 | |
靶点 |
p38 MAPK,PKB
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In vivo(体内研究) |
SB 203580 decreases protein concentrations of IL-1β from 106.49±10.93 to 67.85±7.39 pg/mL and TNF-α from 462.54±50.16 to 252.71±44.03 pg/mL. Similarly, the protein levels of MMP-2 and MMP-9 are significantly lower in the SB 203580 than the EM group. After treatment with SB 203580, the protein levels of MMP-2 and MMP-9 decreases from 2.70±0.14 to 1.74±0.26 ng/mL and from 3.17±0.31 to 1.98±0.24 ng/mL, respectively. SB 203580 is evaluated in several models of cytokine inhibition and inflammatory disease. It is demonstrated clearly to be a potent inhibitor of inflammatory cytokine production in both mice and rats with IC50 values of 15 to 25 mg/kg.
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参考文献 | |
参考文献 |
[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 mitoge
[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]. Zhou WD, et al. SB203580, a p38 mitogen-activated protein kinase inhibitor, suppresses the development of endometriosis by down-regulating proinflammatory cytokines and proteolytic factors in a mouse model. Hum Reprod. 2010 Dec;25(12):3110-6. [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):14 [5]. Jin N, et al. The selective p38 mitogen-activated protein kinase inhibitor, SB203580, improves renal disease in MRL/lpr mouse model of systemic lupus. Int Immunopharmacol. 2011 Sep;11(9):1319-26. |
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