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CAS No. : 978-62-1
MCE 国际站:IMD-0354
产品活性:IMD-0354 (IKK2 Inhibitor V) 是一种选择性 IKKβ 抑制剂,抑制 NF-κB 活性。IMD0354 抑制 TNF-α 诱导的 NF-κB 转录活性,IC50 为 1.2 μM。
研究领域:NF-κB
作用靶点:IKK
In Vitro: IMD-0354 inhibits NF-κB activity in HMC-1 cells, resulting in complete repression of growth factor-independent proliferation of mast cells. When the DNA-binding activity of NF-κB is inhibited by treatment with IMD-0354, cell proliferation is completely suppressed. HMC-1 cells are incubated with increasing concentrations of IMD-0354 or STI571 for 24, 48, and 72 hours, and numbers and viability of cells are determined by a dye exclusion test and an MTT assay. IMD-0354 suppresses cell proliferation in a time- and dose-dependent manner. The inhibitory effect of IMD-0354 is remarkable, even at lower concentrations, when compared with that of STI571. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC 50 of 1.2±0.3 uM.
In Vivo: Daily administration with 5 mg/kg IMD-0354 significantly suppresses tumor expansion in nude mice implanted with established MDA-MB-231 tumors. In mice treated with IMD-0354, tumor progression is restrained. The number of infiltrating cells in aqueous humor is 53.6±9.8×105, 72.5±17.0×105, 127.25±32.0×105, and 132.0±25.0×105 cells/mL in rats treated with 30, 10, 3, or 0 mg/kg of IMD-0354, respectively. The total protein concentrations of aqueous humor are 92.6±3.1 mg/mL, 101.5±6.8 mg/mL, 112.6±1.9 mg/mL, and 117.33±1.8 mg/mL in rats treated with 30, 10, 3, and 0 mg/kg of IMD-0354, respectively.
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | NF-κB Signaling Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Targeted Diversity Library | Anti-Liver Cancer Compound Library | Human Metabolite Library | Anti-Prostate Cancer Compound Library | Cancer Stem Cells Compound Library | Pain-Related Compound Library | Highly Selective Inhibitors Library | TBK1/IKKε-IN-4 | Isophysalin A | GS143 | PS-1145 | Glabrescone C | Ertiprotafib | IKK-IN-4 | Resveratrol | NF-κB-IN-1 | HPN-01 | BAY32-5915 | Oxaprozin | TBK1/IKKε-IN-1 | LY2409881 | Tizoxanide | Bay 65-1942 (R form) | (Rac)-BAY-985 | Lucidone | IKK 16 hydrochloride | (Rac)-PF-184 | BOT-64 | Malachite green oxalate | AZD3264 | IKKβ-IN-1 | PHA 408 | Resveratrol-d4 | GSK319347A
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货号: HY-10172
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