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- 详细信息
- 文献和实验
- 技术资料
- CAS号:
873225-46-8
- 规格:
1mg/1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg/50mg/100mg
| 规格: | 1mg | 产品价格: | ¥254.0 |
|---|---|---|---|
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥626.0 |
| 规格: | 2mg | 产品价格: | ¥352.0 |
| 规格: | 5mg | 产品价格: | ¥601.0 |
| 规格: | 10mg | 产品价格: | ¥872.0 |
| 规格: | 25mg | 产品价格: | ¥1496.0 |
| 规格: | 50mg | 产品价格: | ¥2984.0 |
| 规格: | 100mg | 产品价格: | ¥4248.0 |
Product Introduction
Bioactivity
| 名称 | IKK 16 |
| 描述 | IKK 16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM, respectively. |
| 细胞实验 | IKK 16 is prepared in DMSO and stored, and then diluted with appropriate medium before use[2]. Human umbilical vein vascular endothelial cells line (HUVECs) are cultured in DMEM supplemented with 10% fetal bovine serum, streptomycin, and penicillin. The cells is grown at 37°C in a humidified 5% CO2 atmosphere. Cells are pretreated with IKK 16 (10 μmol/mL) for 1 hr. The cells are then cultured with TGF-β1 (20 ng/mL) and AT-RvD1 (20 ng/mL). After incubation, the gene expressions of Nrf2 and Smad7 are determined by RT-PCR. The protein expression of Nrf2 and IκBα are determined by Western blot[2]. |
| 动物实验 | IKK 16 is prepared in DMSO and diluted with saline or PBS.Rats and MiceIKK 16 is tested in two animal models. First, its efficacy to inhibit TNFα release into plasma upon LPS-challenge in the rat is determined. IKK 16 is dosed sc (30 mg/kg) or orally (30 mg/kg) 1 h prior to the LPS-challenge. Four hours after the challenge, plasma is collected and the systemic TNFα levels are analyzed using a commercially available ELISA kit. Both routes of administration of IKK 16 at the indicated dose results in a significant inhibition of 86% (sc) and 75% (p.o.). In a second experiment, IKK 16 is also active in the thioglycollate-induced peritonitis model in the mouse. The maximal inhibition of neutrophil extravasation in this model is about 50% at a dose of 10 mg/kg sc. MiceTwo-month-old male C57BL/6 mice receive LPS (9 mg/kg body weight) and PepG (3 mg/kg body weight) in 0.9% saline (5 mL/kg body weight) intraperitoneally. Sham mice are not subjected to LPS/PepG, but are otherwise treated the same way. At 1 hour after LPS/PepG co-administration, mice are treated either with IKK 16 (1 mg/kg body weight i.v.) or vehicle (5 mL/kg body weight 10% DMSO i.v.). At 24 hours the experiment is terminated and organ and blood samples are collected for quantification of organ dysfunction and/or injury. Mice are randomly allocated into four different groups: (1) sham+vehicle (n=10); (2) sham+IKK 16 (n=3); (3) LPS/PepG+vehicle (n=9); (4) LPS/PepG+IKK 16 (n=10).They are for reference only. |
| 体外活性 | IKK-16 inhibits TNFα-stimulated expression of the adhesion molecules E-selectin, ICAM-1, and VCAM-1 in HUVEC cells. Although IKK-16 shows activity in the IFNγ-induced expression of β2 microglobulin or HLA-DR, its potency in these assays is 4- to 10-fold weaker. [1] |
| 体内活性 | IKK-16 is orally bio-available in rats and mice, and it inhibits LPS-induced TNF-α release in vivo and neutrophil extravasion in thioglycollate-induced peritonitis.[1] |
| 存储条件 | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (6.82 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 23.64 mg/mL (48.88 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 关键字 | LRRK2 | Leucine-rich repeat kinase 2 | IκB kinase | IκB | Inhibitor | inhibit | IKK2 | IKK1 | IKK 16 | IKK | IkB/IKK | IkB | I kappa B kinase |
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| 相关库 | Inhibitor Library | Bioactive Compound Library | Bioactive Compounds Library Max | Autophagy Compound Library | Kinase Inhibitor Library | Anti-Fibrosis Compound Library | Anti-Aging Compound Library | Anti-Liver Cancer Compound Library | NO PAINS Compound Library | Anti-Ovarian Cancer Compound Library | Anti-Neurodegenerative Disease Compound Library | Immunology/Inflammation Compound Library |
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文献和实验网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广,其数量几乎占已知有机化合物的三分之一,用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等,都含有杂环化合物的结构。生物碱多是中草药的有效成分,绝大多数是含氮的杂环化合物。本章内容与医学关系密切,具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式(Ⅰ)和(Ⅱ)两种结构的高能化合物。其作用为贮藏能量(例如 ATP、肌酸磷酸)和作为产生 ATP源的中间代谢产物(例如磷酸烯醇丙酮酸)以及合成反应的中间物质(例如酰基辅酶 A),在蛋白质的结构( conformation)变化周期的第一阶段上(例如钠钾 ATP酶的羧基磷酸中间体)也具有重要作用。多数高等化合物具有磷酸基,但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质,不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开,而必须用化学方法才能分离。
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