1. MAPK/ERK Pathway Protein Tyrosine Kinase/RTK Epigenetics TGF-beta/Smad
  2. p38 MAPK Src PKC
  3. SB 220025

SB 220025 是一种可逆的、口服有效的、具有细胞渗透性、ATP 竞争性和选择性的人 p38 MAPK 抑制剂 (IC50 = 60 nM)。SB 220025 还能抑 p56LckPKC,其 IC50 值分别为 3.5 和 2.89 µM。SB 220025 能抑制响应球型脂联素 (gAd) 的 IL-8 基因的表达,并减少炎症细胞因子的产生并抑制血管生成。SB 220025 在慢性炎症疾病模型中有效地阻止关节炎的进展,可用于炎症的研究。

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SB 220025 Chemical Structure

SB 220025 Chemical Structure

CAS No. : 165806-53-1

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  • 生物活性

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生物活性

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].

IC50 & Target[1]

p38

60 nM (IC50)

p56-Lck

3.5 μM (IC50)

PKC

2.89 μM (IC50)

体外研究
(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]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[1]

Cell Line: HUVEC cells
Concentration: 20 μM
Incubation Time: 6 h
Result: Inhibited MCP-1 gene expression.
体内研究
(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]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
分子量

338.38

Formula

C18H19FN6

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SB 220025
目录号:
HY-112291
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