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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 |
|---|
| ACHP
ACHP is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. |
| BMS-066
BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively. |
| Ainsliadimer A
Ainsliadimer A is a novel guaiacolide sesquiterpene dimer isolated from Ainsliaea macrocephala.Ainsliadimer A can block the NF-κB signaling pathway by binding to IKK α/β, and possesses anti-tumor and anti-inflammatory activities.Meanwhile, Ainsliadimer A can also Ainsliadimer A can also directly target peroxidase 1 and 2 (PRDX1 and PRDX2) and significantly inhibit their enzymatic activities. In addition, Ainsliadimer A can cause mitochondrial dysfunction by altering the permeability of mitochondrial membrane potential, inhibiting mitochondrial respiration and ATP production, inhibiting cell proliferation, promoting cell cycle arrest in G2/M phase, and inducing apoptosis. |
| IKK2-IN-4
IKK2-IN-4 is a potent IKK-2 inhibitor, with an IC50 of 25 nM. |
| MRT67307 dihydrochloride
MRT67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. |
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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