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1.2μM。

CAS号：978-62-1
纯度：99.77%
分子式：C₁₅H₈ClF₆NO₂
分子量：383.67
结构式：

储存条件：-20℃，有效期2年，溶入溶剂后-20℃请尽量在一个月内使用。

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 72hours,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 IC₅₀ of 1.2±0.3μM。

In Vivo：
Daily administration with 5mg/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 0mg/kg of IMD-0354,respectively.The total protein concentrations of aqueous humor are 92.6±3.1mg/mL,101.5±6.8mg/mL,112.6±1.9mg/mL,and 117.33±1.8mg/mL in rats treated with 30,10,3,and 0mg/kg of IMD-0354,respectively