IMD-0354

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Chemical Structure| 978-62-1 同义名 : IKK2 Inhibitor V
CAS号 : 978-62-1
货号 : A232738
分子式 : C15H8ClF6NO2
纯度 : 99%+
分子量 : 383.673
MDL号 : MFCD00218820
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(273.67 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+5% Tween 80+0.5% CMC Na +water 3 mg/mL

生物活性
描述 IMD-0354, also known as IKK2 Inhibitor V, is a selective inhibitor of IKKβ that suppresses the activity of the NF-κB pathway through IKKβ inhibition[1]. IMD0354 inhibits TNF-α-induced NF-κB transcriptional activity with an IC50 of 1.2 µM[2]. IMD-0354 inhibits NF-κB activity in HMC-1 cells, thereby completely suppressing growth factor-dependent proliferation of mast cells. Cell proliferation is entirely inhibited when IMD-0354 treatment suppresses the DNA binding activity of NF-κB. IMD-0354 inhibits cell proliferation in a time- and dose-dependent manner. Compared to STI571, the inhibitory effect of IMD-0354 is significant even at lower concentrations[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HFF cells Function assay 72 h Antiapicomplexan activity against Toxoplasma gondii RH tachyzoites expressing yellow fluorescent protein infected in HFF cells after 72 hrs by fluorescence assay, IC50=0.016 μM 22970937
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.03mL

2.61mL

1.30mL

26.06mL

5.21mL

2.61mL
参考文献

[1]Tanaka A, et al. A novel NF-kappaB inhibitor, IMD-0354, suppresses neoplastic proliferation of human mast cells with constitutively activated c-kit receptors. Blood. 2005 Mar 15;105(6):2324-31.

[2]Li YR, et al. Study of the inhibitory effects on TNF-α-induced NF-κB activation of IMD0354 analogs. Chem Biol Drug Des. 2017 Dec;90(6):1307-1311.

[3]Tanaka A, et al. A new IkappaB kinase beta inhibitor prevents human breast cancer progression through negative regulation of cell cycle transition. Cancer Res. 2006 Jan 1;66(1):419-26.