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- 2025年07月23日
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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
BMS-345541
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
445430-58-0
- 规格：
50mg/25mg/10mg/1mg/5mg
| 规格： | 50mg | 产品价格： | ￥4490.0 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ￥2790.0 |
| 规格： | 10mg | 产品价格： | ￥1390.0 |
| 规格： | 1mg | 产品价格： | ￥332.0 |
| 规格： | 5mg | 产品价格： | ￥890.0 |
| 基本信息 | |
| CAS | No.445430-58-0 |
| 英文名称 | BMS-345541 |
| 别名 | IKK Inhibitor III |
| 分子式 | C14H17N5 |
| 分子量 | 255.32 |
| 溶解性 | Soluble in Water/DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD18089812 |
| SMILES | CC1=CC2=C(C=C1)N=C(C3=NC=C(N23)C)NCCN |
| InChIKey | PSPFQEBFYXJZEV-UHFFFAOYSA-N |
| InChI | InChI=1S/C14H17N5/c1-9-3-4-11-12(7-9)19-10(2)8-17-14(19)13(18-11)16-6-5-15/h3-4，7-8H，5-6，15H2，1-2H3，(H，16，18) |
| PubChem CID | 9813758 |
| 靶点 | IKK |
| 通路 | NF-κB |
| 背景说明 | 是一种选择性的 IKK 催化亚基 IKK-1 和 IKK-2 抑制剂。 |
| 生物活性 | BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM， IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.[1-3] |
| In Vitro | BMS-345541 (4(2-aminoethyl)amino-1，8-dimethylimidazo(1，2-a)quinoxaline) was identified as a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC(50) = 0.3 microm， IKK-1 IC(50) = 4 microm). The compound failed to inhibit a panel of 15 other kinases and selectively inhibited the stimulated phosphorylation of I kappa B alpha in cells (IC(50) = 4 microm) while failing to affect c-Jun and STAT3 phosphorylation， as well as mitogen-activated protein kinase-activated protein kinase 2 activation in cells. Consistent with the role of IKK/NF-kappa B in the regulation of cytokine transcription， BMS-345541 inhibited lipopolysaccharide-stimulated tumor necrosis factor alpha， interleukin-1 beta， interleukin-8， and interleukin-6 in THP-1 cells with IC(50) values in the 1- to 5-microm range.[1] |
| 细胞实验 | BMS-345541 was also shown to have excellent pharmacokinetics in mice， and peroral administration showed the compound to dose-dependently inhibit the production of serum tumor necrosis factor alpha following intraperitoneal challenge with lipopolysaccharide.[1] |
| 细胞实验 | SK-MEL-5 cells are treated with BMS-345541 at different concentrations (0， 1.0， 10， and 100 μM) for different time periods. The cells are collected by trypsinization， fixed in 70% ethanol for 2 hours on ice and stained with PI solution (PBS containing 2 μg/mL PI， 0.1% Triton X-100， and 125 units/mL RNase A) at 37°C for 30 minutes. Cell fluorescence is measured by flow cytometry with 488 nm excitation and 620 nm emission filters and resulting data are analyzed using the software program MultiCycle[2]. |
| 动物实验 | Mice[1] BMS-345541 is administered either by intravenous tail vein injection or by peroral gavage to groups of three 18-22 g female BALB/c mice. BMS-345541 is formulated as a 2 mg/mL solution in 3% Tween 80， water. Mice receive either a 2 mg/kg (1 mL/kg) intravenous bolus or a 10 mg/kg (5 mL/kg) peroral gavage. Whole blood samples are taken from individual mice by orbital bleed and cardiac puncture at 0， 0.05， 0.25， 0.5， 1.0， 3.0， 6.0， and 8.0 h after dosing. Whole blood is centrifuged at 20×103×g for 5 min. Serum is stored at -20°C until analysis. |
| 激酶实验 | Assays measuring the enzyme-catalyzed phosphorylation of GST-IκBα are performed by adding enzyme (IKK-2， IKK-1， or IKK-ε， typically to a final concentration of 0.5 μg/mL) at 30°C to solutions of 100 μg/mL GST-IκBα and 5 μM [33P]ATP in 40 mM Tris-HCl， pH 7.5， containing 4 mM MgCl2， 34 mM sodium phosphate， 3 mM NaCl， 0.6 mM potassium phosphate， 1 mM KCl， 1 mM dithiothreitol， 3% (w/v) glycerol， and 250 μg/mL bovine serum albumin. The specific activity of [33P]ATP used in the assay is 100 Ci/mmol. After 5 min， the kinase reactions are stopped by the addition of 2× LaemmLi sample buffer and heat-treated at 90°C for 1 min. The samples are then loaded on to NuPAGE 10% BisTris gels. After completion of SDS-PAGE， gels are dried on a slab gel dryer. The bands are then detected using a 445Si PhosphorImager， and the radioactivity is quantified using ImageQuant software. Under these conditions， the degree of phosphorylation of GST-IκBα is linear with time and concentration of enzyme[1]. |
| 数据来源文献 | [1]. Burke JR， et al. BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice. J Biol Chem， 2003， 278(3)， 1450-1456. [2]. Yang J， et al. BMS-345541 targets inhibitor of kappaB kinase and induces apoptosis in melanoma: involvement of nuclear factor kappaB and mitochondria pathways. Clin Cancer Res， 2006， 12(3 Pt 1)， 950-960. [3]. MacMaster JF， et al. An inhibitor of IkappaB kinase， BMS-345541， blocks endothelial cell adhesion molecule expression and reduces the severity of dextran sulfate sodium-induced colitis in mice. Inflamm Res， 2003， 52(12)， 508-511. |
| 单位 | 瓶 |
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IB3400 BMS-345541 抑制剂/拮抗剂/激动剂 索莱宝
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