化合物MLN120B TQ0306

Product Introduction
Bioactivity


英文名: MLN120B

描述: MLN120B 是一种ATP 竞争性的、有效的、具有口服活性的IKKβ抑制剂，IC50=60 nM。它在体内外抑制多发性骨髓瘤细胞生长，也可用于研究类风湿关节炎。

细胞实验: Multiple myeloma cells are cultured with MLN120B, harvested, washed, and lysed using lysis buffer [50 mM Tris-HCl (pH 7.4), 150 mM NaCl, 1% NP40, 5 mM EDTA, 5 mM NaF, 2 mM Na3VO4, 1 mM phenylmethylsulfonyl fluoride, 5 μg/mL leupeptin, 5 μg/mL aprotinin]. Whole-cell lysates are subjected to Western blotting using phosphorylated IκBα, IκBα, phosphorylated p65 NF-κB, and p65 NF-κB antibodies [1].

动物实验: Human fetal long bone grafts are implanted into SCID mice (SCID-hu mice). Approximately 4 weeks following bone implantation, 2.5×10^6 INA6 multiple myeloma cells in 50 μL PBS is injected directly into human bone within SCID-hu hosts. Soluble human IL-6 receptor (shuIL-6R) released from INA6 cells is assessed in mouse sera by ELISA as in our prior studies. Mice are treated orally with vehicle alone or MLN120B 50 mg/kg (twice daily) for 3 weeks after the detection of measurable shuIL-6R in mouse sera [1].

体外活性: MLN120B几乎完全阻断了MM.1S、U266和INA6细胞的生长刺激，以及由于多发性骨髓瘤细胞与BMSCs粘附所诱导的BMSCs中IL-6的分泌[1]。此外，MLN120B对由LPS引起的RAW267.4细胞中NF-κB激活显示出抑制效果。对于转染了NF-κB2-luc2、IL8-luc2或TNF-AIP3-luc2报告基因的细胞，MLN120B的IC50值分别为1.4、14.8或27.3 μM[3]。

体内活性: MLN120B（50 mg/kg，口服）在体内抑制人类多发性骨髓瘤细胞的生长[1]。MLN120B（12 mg/kg，每日两次，口服）以剂量依赖的方式抑制爪肿胀，并显著防止因关节炎引起的体重减轻以及软骨和骨骼侵蚀[2]。

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

溶解度: DMSO : 30 mg/mL (81.78 mM)
H2O : Insoluble


关键字: MLN120B | ML120B | Inhibitor | I kappa B kinase | inhibit | IKK | IκB kinase | MLN-120B

相关产品: IKK-IN-1 | WS3 | BAY-985 | Dehydroglyasperin C | Physalin O | Vinpocetine | TRAM-34 | Neoechinulin A | Goshonoside F5 | TBK1/IKKε-IN-5

相关库: Anti-Prostate Cancer Compound Library | Anti-Liver Cancer Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Anti-Ovarian Cancer Compound Library | Kinase Inhibitor Library | Inhibitor Library | Hematonosis Compound Library | Target-Focused Phenotypic Screening Library | Bioactive 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