| Description |
SB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 also inhibits p56Lck and PKC with IC50 values of 3.5 and 2.89 µM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation[1][2].
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| Related Catalog |
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| Target |
p38:60 nM (IC50)
p56-Lck:3.5 μM (IC50)
PKC:2.89 μM (IC50)
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| In Vitro |
SB 220025 (20 μM; 6 h) 显着降低 HUVEC 细胞中响应球型脂联素 (gAd) 的 IL-8 基因表达[1]。 RT-PCR[1] Cell Line: HUVEC cells Concentration: 20 μM Incubation Time: 6 h Result: Inhibited MCP-1 gene expression.
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| In Vivo |
SB 220025 (3-50 mg/kg; p.o.; single) 可抑制体内炎症细胞因子的产生[2]。 SB 220025 (5, 30, 50 mg/kg; i.p.; bid) 抑制小鼠气囊肉芽肿模型的血管生成[2]。 SB 220025 (30 mg/kg; p.o.; twice a day for 3, 5, 7 or 14 days) 防止小鼠气囊血管生成模型第 3 天后发生的血管生成增加[2]。 SB 220025 (50 mg/kg; p.o.; b.i.d.; 10 days) 在慢性炎症疾病模型中有效地阻止关节炎的进展[2]。 Animal Model: Acute model of LPS-induced TNF-a expression[2]. Dosage: 3-50 mg/kg Administration: Oral administration; single; 30 min before challenge with LPS. Result: Dosedependently inhibited TNF-a production with an ED50 value of 7.5 mg/kg, and showed more than 80% inhibition when at 50 mg/kg. Animal Model: Murine air pouch granuloma model[2]. Dosage: 5, 30, 50 mg/kg Administration: Intraperitoneal injection; bisindie (bid, twice a day). Result: Caused a dose-dependent reduction in angiogenesis. Animal Model: Murine air pouch granuloma model[2]. Dosage: 30 mg/kg Administration: Oral administration; twice a day from day 0 until removal of granuloma tissue at days 3, 5, 7 or 14. Result: Did not affect the initial burst of angiogenesis but did prevent the increase in angiogenesis that occurs after day 3.
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| References |
[1]. Tomizawa A, et al. Induction of gene expression in response to globular adiponectin in vascular endothelial cells. Life Sci. 2009 Sep 9;85(11-12):457-61. [2]. Jackson JR, et al. Pharmacological effects of SB 220025, a selective inhibitor of P38 mitogen-activated protein kinase, in angiogenesis and chronic inflammatory disease models. J Pharmacol Exp Ther. 1998 Feb;284(2):687-92.
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