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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.
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MLN120B purchased from AbMole
| Cell Experiment | |
|---|---|
| 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. |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Rat adjuvant-induced arthritis model (Two-month-old female Lewis rats) |
| Formulation | |
| Dosages | 3 mg/kg, 10 mg/kg, 30 mg/kg |
| Administration | orally as a suspension delivered via a gavage needle |
| Molecular Weight | 366.8 |
| Formula | C19H15ClN4O2 |
| CAS Number | 783348-36-7 |
| Solubility (25°C) | DMSO: ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related IκB/IKK Products |
|---|
| BAY 11-7082
BAY 11-7082 is an inhibitor of cytokine-induced IκB-α phosphorylation (IC50 ~ 10 μM). BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). |
| SC-514
SC-514 is a selective and reversible inhibitor of IκB kinase 2 (IKK2) with IC50 of 3-12 μM. |
| TPCA-1
TPCA-1 is an inhibitor of IKK-2 with IC50 of 17.9 nM. |
| BMS-345541 hydrochloride
BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IC50 values of 0.3 μM and 4 μM for IKK-2 and IKK-1 respectively). BMS-345541 binds at an allosteric site of IKK. |
| Bardoxolone Methyl
Bardoxolone Methyl is an IKK inhibitor with potent pro-apoptotic and anti-inflammatory activities, as well as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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