Bioactivity | 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]. |
Invitro | 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: |
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: |
Name | SB 220025 |
CAS | 165806-53-1 |
Formula | C18H19FN6 |
Molar Mass | 338.38 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |