- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Bioactive Molecules
- Anti-infection
- Apoptosis
- Autophagy
- Cell Cycle/DNA Damage
- Cytoskeleton
- Epigenetics
- GPCR/G Protein
- Immunology/Inflammation
- JAK/STAT Signaling
- MAPK/ERK Pathway
- Membrane Transporter/Ion Channel
- Metabolic Enzyme/Protease
- Neuronal Signaling
- NF-κB
- PI3K/Akt/mTOR
- PROTAC
- Protein Tyrosine Kinase/RTK
- Stem Cell/Wnt
- TGF-beta/Smad
- Vitamin D Related/Nuclear Receptor
- Others
- Methylation
- Cytoskeletal Signaling
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 783348-36-7] MLN120B
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15473 |
| Brand: | MCE |
| CAS: | 783348-36-7 |
Overview
| MDL | MFCD17392835 |
|---|---|
| Molecular Weight | 366.80 |
| Molecular Formula | C19H15ClN4O2 |
| SMILES | O=C(C1=CC=CN=C1C)NC2=C(OC)C(Cl)=CC3=C2NC4=C3C=CN=C4 |
18 Publications Citing Use of MCE
- [1]Nature. 2022 Oct;610(7931):366-372.
- [2]Blood. 2015 Nov 12;126(20):2291-301.
- [3]Blood. 2015 Sep 10;126(11):1324-35.
- [4]Sci Transl Med. 2021 Jan 27;13(578):eaba7308.
- [5]Signal Transduct Target Ther. 2020 Oct 9;5(1):235.
- [6]Theranostics. 2020 Apr 6;10(11):5029-5047.
- [7]Cell Rep. 2020 Mar 31;30(13):4370-4385.e7.
- [8]Aging Cell. 2021 Jun 29;e13426.
- [9]J Invest Dermatol. 2017 Dec;137(12):2532-2543.
- [10]Cell Death Dis. 2016 Dec 1;7(12):e2505.
- [11]Int J Cancer. 2017 Mar 1;140(5):1147-1158.
- [12]Acta Pharmacol Sin. 2020 Aug 27.
- [13]Biochem Pharmacol. 2018 Jun;152:45-59.
- [14]J Biol Chem. 2015 Apr 24;290(17):11061-74.
- [15]Sci Rep. 2021 Jul 28;11(1):15319.
- [16]Viruses. 2021, 13(6), 976.
- [17]Exp Ther Med. 2021 Feb;21(2):122.
- [18]Patent. US20220025002A1.
Summary
IC50 & Target
|
IKKβ 60 nM (IC 50 ) |
In Vitro
MLB120B (0-20 μM; 90 minutes) inhibits phosphorylation and degradation of IκB in RPMI 8226 and INA6 cells; however, no significant inhibition is observed in MM.1S cells
[1]
.
MLB120B (1.25-20 μM; 90 minutes) completely abrogates TNF-a-induced phosphorylation and degradation of IκB in a dosedependent fashion. Phosphorylation of p65 NF-κB induced by TNF-a is also blocked by MLN120B
[1]
.
MLN120B inhibits proliferation of multiple myeloma cell lines. MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells. Five percent to fifty percent and 18% to 70% inhibition in proliferation is observed at doses >20 uM and [
3
H]thymidine uptake, respectively[1].
MLN120B (1.25-40 μM; 72 hours) 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 IC
50
values of MLN120B is 1.4 µM, 14.8 µM or 27.3 µM for NF-κB2-luc2, IL8-luc2 or TNF-AIP3-luc2 reporter transfected cells, respectively[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | MM.1S cells |
| Concentration: | 1.25-20 μM |
| Incubation Time: | 90 minutes |
| Result: | Inhibited p- IκB and p-P65 expression in a dose-dependent manner. |
Cell Viability Assay [1]
| Cell Line: | Multiple myeloma cell lines: MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells |
| Concentration: | 1.25 μM-20 μM |
| Incubation Time: | 72 hours |
| Result: | Inhibits proliferation of multiple myeloma cell lines. |
In Vivo
MLN120B (oral administration; 50 mg/kg; twice daily; 3 weeks) induces a reduction of shuIL-6R, marker of tumor growth, marker of tumor growth. It also leads to a rend toward prolonged survival in animals treated versus control
[1]
.
MLN120B (oral administration; 1-30 mg/kg; twice daily; 3 weeks) 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 also reduced after MLN120B administration
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Two-month-old female Lewis rats [2] |
| Dosage: | 30 mg/kg, 10 mg/kg, 3 mg/kg, or 1 mg/kg |
| Administration: | Oral administration; twice daily; 3 weeks |
| Result: | Protected against bone and cartilage destruction in a rat model. |
| Animal Model: | SCID mice implanted with human fetal bone chips and then INA6 cells are directly injected into mice [1] |
| Dosage: | 50 mg/kg |
| Administration: | Oral administration; twice daily; 3 weeks |
| Result: | Inhibited human multiple myeloma cell growth in vivo. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 31 mg/mL ( 84.51 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7263 mL | 13.6314 mL | 27.2628 mL |
| 5 mM | 0.5453 mL | 2.7263 mL | 5.4526 mL |
| 10 mM | 0.2726 mL | 1.3631 mL | 2.7263 mL |
References
- [1] Hideshima T, et all. MLN120B, a novel IkappaB kinase beta inhibitor, blocks multiple myeloma cell growth in vitro and in vivo. Clin Cancer Res. 2006 Oct 1;12(19):5887-94.
- [2] Schopf L, et al. IKKbeta inhibition protects against bone and cartilage destruction in a rat model of rheumatoid arthritis. Arthritis Rheum. 2006 Oct;54(10):3163-73.
- [3] Ansaldi D, et al. Imaging pulmonary NF-kappaB activation and therapeutic effects of MLN120B and TDZD-8. PLoS One. 2011;6(9):e25093.
- [4] Nagashima K, et al. Rapid TNFR1-dependent lymphocyte depletion in vivo with a selective chemical inhibitor of IKKbeta. Blood. 2006 Jun 1;107(11):4266-73.
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.