783348-36-7
783348-36-7 structure
- Name: MLN120B
- Chemical Name: N-(6-chloro-7-methoxy-9H-pyrido[3,4-b]indol-8-yl)-2-methylpyridine-3-carboxamide
- CAS Number: 783348-36-7
- Molecular Formula: C19H15ClN4O2
- Molecular Weight: 366.801
- Catalog: Signaling Pathways NF-κB IKK
- Create Date: 2018-12-10 18:01:48
- Modify Date: 2024-01-14 07:45:17
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MLN120B is a specific, ATP competitive IKKβ inhibitor with an IC50 of 60 nM.
| Name | N-(6-chloro-7-methoxy-9H-pyrido[3,4-b]indol-8-yl)-2-methylpyridine-3-carboxamide |
|---|---|
| Synonyms |
cs-1291
ml-120b mln-120b 3-Pyridinecarboxamide, N-(6-chloro-7-methoxy-9H-pyrido[3,4-b]indol-8-yl)-2-methyl- N-(6-Chloro-7-methoxy-9H-β-carbolin-8-yl)-2-methylnicotinamide MLN120B |
| Description | MLN120B is a specific, ATP competitive IKKβ inhibitor with an IC50 of 60 nM. |
|---|---|
| Related Catalog | |
| Target |
IKKβ:60 nM (IC50) |
| In Vitro | 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[1]. MLN120B shows an inhibitory effect on LPS induced NF-κB activation in RAW267.4 cells. The IC50 values of MLN120B is 1.4, 14.8 or 27.3 µM for NF-κB2-luc2, IL8-luc2 or TNF-AIP3-luc2 reporter transfected cells, respectively[3]. |
| 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[2]. |
| 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. |
| Animal Admin | Human fetal long bone grafts are implanted into SCID mice (SCID-hu mice) as described previously. Approximately 4 weeks following bone implantation, 2.5×106 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 detection of measurable shuIL-6R in mouse sera. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 545.0±50.0 °C at 760 mmHg |
| Molecular Formula | C19H15ClN4O2 |
| Molecular Weight | 366.801 |
| Flash Point | 283.4±30.1 °C |
| Exact Mass | 366.088348 |
| PSA | 83.39000 |
| LogP | 3.84 |
| Vapour Pressure | 0.0±1.5 mmHg at 25°C |
| Index of Refraction | 1.752 |
| Storage condition | 2-8℃ |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H302 |
| RIDADR | NONH for all modes of transport |
| HS Code | 2933990090 |
| HS Code | 2933990090 |
|---|---|
| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |