化合物IMD 0354 T6141

Product Introduction
Bioactivity


英文名: IMD-0354

描述: IMD-0354 (IKK2 Inhibitor V) 是一种选择性IKKβ抑制剂，能够抑制 NF-κB 活性。它能够抑制 TNF-α 诱导的 NF-κB 转录活性，IC50=1.2 μM。

细胞实验: Cells (2×105 cells/mL) are incubated in phenol red free α-MEM containing 10% FCS (for HMC-1 and IC-2 cells) or 5% FCS (for CBhCMCs), and antibiotics with or without various concentrations of IMD-0354, STI571, or PDTC. IC-2WT cells and CBhCMCs are incubated in the presence of 100 ng/mL recombinant rat or recombinant human SCF. One hundred microliters of cell suspension is applied to each well of 96-well culture plates and are incubated for 24, 48, and 72 hours. Before 4 hours from the end of the culture, 10 μL of 5 mg/mL 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide (MTT) dissolves in PBS is added to each well. The reaction is stopped with the addition of 100 μL of 10% SDS in 0.01 N HCl. Absorbance is measured at 577 nm with ImmunoMini NJ-2300.(Only for Reference)

激酶实验: In vitro mTOR kinase assays : The reaction mixture consisted of the following components in 10 μL assay buffer (50 mM Hepes pH 7.5, 10 mM MgCl 2, 3 mM MnCl 2, 1 mM EGTA, 2 mM DTT, 0.01%Tween-20): 0.10 μg/mL of in-house generated mTOR enzyme, 0.05 μM ULight-eIF4E-binding protein 1 (Thr37/46) peptide and 10 μM ATP. The mixture is incubated for 60 min at room temperature. 10 μL of Detection mixture consisted of 16 mM EDTA, 0.004 mM Eu-W1024-labeled Anti-Phospho-eIF4E-binding protein 1-(Thr37/46) antibody and 1X LANCE? Detection Buffer is then added and incubated for 60 min.

体外活性: IMD-0354（<5 μM）抑制了HMC-1细胞中NF-κB的表达以及NF-κB向细胞核的转移。IMD-0354以时间和剂量依赖的方式抑制HMC-1细胞的增殖。IMD-0354（0.5 μM）几乎完全抑制了IC-2 g559细胞和IC-2V814细胞的增殖。IMD-0354（0.5 μM）导致HMC-1细胞周期在G0/G1阶段停滞。IMD-0354（1 μM）增加了HMC-1细胞中具有低二倍体DNA含量的细胞数。IMD-0354（<1 μM）降低了HMC-1细胞中处于S和G2/M阶段的细胞比例。IMD-0354（1 μM）降低了HMC-1细胞中Cyclin D3表达以及pRb磷酸化水平，且这一作用随时间依赖增加。在高浓度下，IMD-0354（<10 μM）对HMC-1细胞中STAT3和STAT6的信号无影响，而STAT1和STAT5的磷酸化略有抑制。在剂量依赖的方式下，IMD-0354抑制了CBhCMCs中NF-κB向细胞核的转移，持续24小时。[1]在HepG2细胞中，IMD-0354以10 μg/ml的浓度抑制了98.5%的NF-κB活性。[2]IMD-0354（1 μM）改善了在同时给予TNFα（6 nM）和胰岛素（100 nM）的情况下，TNFα引起的3T3-L1脂肪细胞星化12小时后培养基中的脂联素浓度下降，以及TNFα治疗下调的Akt磷酸化恢复。[3]IMD-0354（1 μM）抑制了由肿瘤坏死因子-α（TNF-α）引起的IκBα磷酸化和NF-κB核内转移，在培养的心肌细胞中显著减少TNF-α诱导的白介素-1β和单核细胞趋化蛋白-1的产生。[4]

体内活性: IMD-0354 at 5 mg/kg also significantly decreases NF-κB, but the magnitude of the decrease is lower than with 20 mg/kg IMD-0354 in lungs of OVA-sensitized mice. IMD-0354 (20 mg/kg) ameliorates airway hyperresponsiveness and reduces the numbers of bronchial eosinophils and mucus-producing cells in OVA-sensitized mice. IMD-0354 (20 mg/kg) also reduces the total numbers of cells and eosinophils in bronchoalveolar lavage fluid in OVA-sensitized mice. IMD-0354 (20 mg/kg) inhibits the production of Th2 cytokines such as interleukin (IL)-5 and IL-13 and eotaxin in the airways and/or lungs of OVA-sensitized mice, but it does not affect the restoration of Th1 cytokines such as IL-12 and interferon-gamma under the same experimental conditions. IMD-0354 (20 mg/kg) results in a partial decrease in serum IgE concentration in OVA-sensitized mice. [2] IMD-0354 significantly decreases the plasma glucose levels in KKAy mice treated with and fed an HF diet in an dose-dependent manner without influence of body weight. [3] IMD-0354 (10 mg/kg) results in a significant dose-dependent reduction of the infarction area/area at risk ratio and the preservation of fractional shortening ratio. [4]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 38.4 mg/mL (100 mM)
Ethanol : 38.4 mg/mL (100 mM)


关键字: IκB kinase | IMD-0354 | Inhibitor | I kappa B kinase | IKK | IMD0354 | inhibit

相关产品: Bay 11-7085 | GSK319347A | TBK1/IKKε-IN-2 | WS6 | MRT67307 | MLN120B | Bakkenolide IIIa | NF-κB-IN-1 | BAY 11-7082 | 7,8-Didehydrocimigenol

相关库: Drug Repurposing Compound Library | Pyroptosis Compound Library | ReFRAME Related Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途