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CAS No.: 978-62-1

IMD-0354 Catalog No. CSN16069

Synonyms: IKK2 Inhibitor V

IMD-0354 is a synthetic selective NF-kB inhibitor and blocks IκBα phosphorylation in NF-κB pathway.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The NF-kB pathway plays a key role in multiple cellular processes, including immune signaling, inflammation, development, proliferation and survival. The activation of the upstream molecule, IKKα or β (IkB kinase), is required for NF-kB pathway and regulates NF-kB pathway via phosphorylation by specific IKK kinases and by autophosphorylation. IMD-0354 is an IKKβ inhibitor, which can inhibit the NF-κB pathway. Slight decrease of p-IκB level and block of NF-κB nuclear translocation induced by TNF-α could be observed in cardiomyocytes exposure to 1μM IMD-0354. The suppression of IL-1β and MCP-1 induced by TNF-α could be suppressed by IMD-0354. Treatment with 1μM IMD-0354 for 24h could decrease the binding of NF-κB to DNA and its activity of transcription in HMC-1 cells. Intraperitoneal injection with 20mg/kg IMD-0354 twice a day for 28 days suppressed the thickened intima induced by injured arteries with decreased inflammatory factors on mRNA level compared with control, including COX-2, ICAM-1, IL-6, MCP-1 and MMP-3.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HFF cells	-	Function assay	72 h	Antiapicomplexan activity against Toxoplasma gondii RH tachyzoites expressing yellow fluorescent protein infected in HFF cells after 72 hrs by fluorescence assay, IC50=0.016 μM	22970937

动物研究
剂量
Mice: 0.23 mg/kg - 0.92 mg/kg^[3] (i.p.) Rat: 3 mg/kg - 30 mg/kg^[4] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 0.23 mg/kg - 0.92 mg/kg^[3] (i.p.) Rat: 3 mg/kg - 30 mg/kg^[4] (i.p.)
给药途径	i.p.

[1] Sugita A, Ogawa H, et al. Antiallergic and anti-inflammatory effects of a novel I kappaB kinase beta inhibitor, IMD-0354, in a mouse model of allergic inflammation. Int Arch Allergy Immunol. 2009;148(3):186-98.
[2] Tanaka A, Konno M, et al. A novel NF-kappaB inhibitor, IMD-0354, suppresses neoplastic proliferation of human mast cells with constitutively activated c-kit receptors. Blood. 2005 Mar 15;105(6):2324-31.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6064 mL
- 13.0319 mL
- 26.0639 mL
- 5 mM
- 0.5213 mL
- 2.6064 mL
- 5.2128 mL
- 10 mM
- 0.2606 mL
- 1.3032 mL
- 2.6064 mL

技术信息

CAS号

978-62-1

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H8ClF6NO2

运输

蓝冰

分子量

383.67

别名

IKK2 Inhibitor V

溶解度

DMSO	10.0 mg/mL (26.1 mM)
Water	Insoluble
Ethanol	77.0 mg/mL (200.7 mM)

动物实验配方

2% DMSO+5% Tween 80+0.5% CMC Na +water

3 mg/mL

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