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MLN120B
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MLN120B图片
CAS NO:783348-36-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 366.81
Formula C19H15ClN4O2
CAS No. 783348-36-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 30mg/mL
Water: N/A
Ethanol: N/A
Chemical Name N-{6-chloro-7-methoxy-9H-pyrido[3,4-b]indol-8-yl}-2-methylpyridine-3-carboxamide
Synonyms MLN 120B; MLN-120B; ML-120B; ML120B; MLN120B; ML 120B.
实验参考方法
In Vitro

In vitro activity: MLN120B inhibits both baseline and tumor necrosis factor-alpha-induced nuclear factor-kappaB activation, associated with down-regulation of IkappaBalpha and p65 nuclear factor-kappaB phosphorylation. MLN120B triggers 25% to 90% growth inhibition in a dose-dependent fashion in multiple myeloma cell lines and significantly augments tumor necrosis factor-alpha-induced cytotoxicity in MM.1S cells. MLN120B augments growth inhibition triggered by doxorubicin and melphalan in both RPMI 8226 and IL-6-dependent INA6 cell lines. Neither IL-6 nor IGF-1 overcomes the growth-inhibitory effect of MLN120B. MLN120B inhibits constitutive IL-6 secretion by BMSCs by 70% to 80% without affecting viability. Importantly, MLN120B almost completely blocks stimulation of MM.1S, U266, and INA6 cell growth, as well as IL-6 secretion from BMSCs, induced by multiple myeloma cell adherence to BMSCs. MLN120B overcomes the protective effect of BMSCs against conventional (dexamethasone) therapy.


Kinase Assay: MLN120B is a novel, potent, specific and ATP competitive IKKβ (IκB kinase beta subunit) inhibitor with an IC50 of 60 nM.


Cell Assay: 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.

In Vivo MLN120B (50 mg/kg, p.o.) inhibits human multiple myeloma cell growth in vivo[1]. MLN120B (12 mg/kg twice daily, p.o.) inhibits paw swelling in a dose-dependent manner and offers significant protection against arthritis-induced weight loss as well as cartilage and bone erosion. NF-κB activity in arthritic joints is reduced after MLN120B administration
Animal model SCID mice
Formulation & Dosage 50 mg/kg, p.o.
References Clin Cancer Res. 2006 Oct 1;12(19):5887-94.