MLN120B is a potent and effective, ATP competitive IKKβ inhibitor with IC50 value of 20 μM. MLN120B inhibits both baseline and tumor necrosis factor-α-induced nuclear factor-κB activation, associated with down-regulation of IκBα and p65 nuclear factor-κB phosphorylation in multiple myeloma cells. 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.
In vivo, MLN120B (50 mg/kg, p.o.) inhibits human multiple myeloma cell growth. 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.
|Cell lines||Multiple myeloma cells|
|Preparation method||MLN-120B is dissolved in DMSO. Multiple myeloma cells are cultured with MLN-120B, 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.|
|Animal models||Rat adjuvant-induced arthritis model (Two-month-old female Lewis rats)|
|Dosages||3 mg/kg, 10 mg/kg, 30 mg/kg|
|Administration||orally as a suspension delivered via a gavage needle|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 20 mg/mL|
Imaging pulmonary NF-kappaB activation and therapeutic effects of MLN120B and TDZD-8.
Ansaldi D, et al. PLoS One. 2011;2011. PMID: 21966423.
MLN120B, a novel IkappaB kinase beta inhibitor, blocks multiple myeloma cell growth in vitro and in vivo.
Hideshima T, et al. Clin Cancer Res. 2006 Oct 1;12(19):5887-94. PMID: 17020997.
IKKbeta inhibition protects against bone and cartilage destruction in a rat model of rheumatoid arthritis.
Schopf L, et al. Arthritis Rheum. 2006 Oct;54(10):3163-73. PMID: 17009244.
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