MLN120B dihydrochloride
Based on 28 publication(s) in Google Scholar
MLN120B dihydrochloride (ML120B dihydrochloride) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.45%
- CAS 番号: 1782573-78-7
- 分子式: C19H17Cl3N4O2
- 分子量:439.72
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 MLN120B dihydrochloride
More- Signal Transduct Target Ther. 2020 Oct 9;5(1):235. [Abstract]
- Cancer Cell. 2024 Feb 12;42(2):238-252.e9. [Abstract]
- Nature. 2022 Oct;610(7931):366-372. [Abstract]
- Blood. 2023 Nov 2.
- Blood. 2015 Nov 12;126(20):2291-301. [Abstract]
- Blood. 2015 Sep 10;126(11):1324-35. [Abstract]
- Sci Transl Med. 2021 Jan 27;13(578):eaba7308. [Abstract]
- Theranostics. 2020 Apr 6;10(11):5029-5047. [Abstract]
- Cell Death Dis. 2016 Dec 1;7(12):e2505. [Abstract]
- Acta Pharmacol Sin. 2021 May;42(5):814-823. [Abstract]
- Aging Cell. 2021 Jul;20(7):e13426. [Abstract]
- Cell Rep. 2020 Mar 31;30(13):4370-4385.e7. [Abstract]
- Cell Prolif. 2023 Sep;56(9):e13442. [Abstract]
- J Invest Dermatol. 2017 Dec;137(12):2532-2543. [Abstract]
- Biochem Pharmacol. 2018 Jun:152:45-59. [Abstract]
- Int Immunopharmacol. 2024 Nov 15:141:113013. [Abstract]
- Sci Rep. 2021 Jul 28;11(1):15319. [Abstract]
- Int J Cancer. 2017 Mar 1;140(5):1147-1158. [Abstract]
- J Biol Chem. 2015 Apr 24;290(17):11061-74. [Abstract]
- Viruses. 2021 May 25;13(6):976. [Abstract]
- Cytokine. 2026 May:201:157135. [Abstract]
- Exp Ther Med. 2021 Feb;21(2):122. [Abstract]
- bioRxiv. 2025 February 22.
- University of Strathclyd. 2024
- bioRxiv. 2024 Mar 28.
- bioRxiv. 2023 Mar 23.
- Patent. US20220025002A1.
- SSRN. 2022 Jan 26.
Customer Validation & Images
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生物活性
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 [3H]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 IC50 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM.1S cells
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Concentration:5 μM; 10 μM; 20 μM
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Incubation Time:90 mintues
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Result:Inhibited p-IκB and p-P65 expression in a dose-dependent manner.
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Cell Line:Myeloma cell lines: MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells
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Concentration:0-40 μM
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Incubation Time:72 hours
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Result:Inhibited proliferation of multiple myeloma cell lines.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice implanted with human fetal bone chips and then INA6 cells are directly injected into mice[1]
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Dosage:50 mg/kg
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Administration:Oral administration; twice daily; 3 weeks
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Result:Inhibited human multiple myeloma cell growth in vivo.
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Animal Model:Two-month-old female Lewis rats[2]
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Dosage:30 mg/kg, 10 mg/kg, 3 mg/kg, or 1 mg/kg
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Administration:Oral administration; twice daily; 3 weeks
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Result:Protected against bone and cartilage destruction in a rat model.
化学情報
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CAS 番号 1782573-78-7
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性状 Solid
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分子量 439.72
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分子式 C19H17Cl3N4O2
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Color Off-white to light yellow
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SMILES
ClC1=C(C(NC(C2=CC=CN=C2C)=O)=C3C(C4=C(N3)C=NC=C4)=C1)OC.Cl.Cl
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別名
ML120B dihydrochloride
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (28)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
2020 Oct 9;5(1):235. PMID: 33037188 -
Cancer Cell
Response to Bruton's tyrosine kinase inhibitors in aggressive lymphomas linked to chronic selective autophagy. [Abstract]2024 Feb 12;42(2):238-252.e9. PMID: 38215749 -
Nature
2022 Oct;610(7931):366-372. PMID: 36198801 -
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Blood
ATM deficiency promotes development of murine B-cell lymphomas that resemble diffuse large B-cell lymphoma in humans. [Abstract]2015 Nov 12;126(20):2291-301. PMID: 26400962 -
Blood
NF-κB and AKT signaling prevent DNA damage in transformed pre-B cells by suppressing RAG1/2 expression and activity. [Abstract]2015 Sep 10;126(11):1324-35. PMID: 26153519 -
Sci Transl Med
A chimeric antigen receptor with antigen-independent OX40 signaling mediates potent antitumor activity. [Abstract]2021 Jan 27;13(578):eaba7308. PMID: 33504651 -
Theranostics
2020 Apr 6;10(11):5029-5047. PMID: 32308766 -
Cell Death Dis
2016 Dec 1;7(12):e2505. PMID: 27906189 -
Acta Pharmacol Sin
Activation of unfolded protein response overcomes Ibrutinib resistance in diffuse large B-cell lymphoma. [Abstract]2021 May;42(5):814-823. PMID: 32855532 -
Aging Cell
2021 Jul;20(7):e13426. PMID: 34187082 -
Cell Rep
SFTSV Infection Induces BAK/BAX-Dependent Mitochondrial DNA Release to Trigger NLRP3 Inflammasome Activation. [Abstract]2020 Mar 31;30(13):4370-4385.e7. PMID: 32234474 -
Cell Prolif
2023 Sep;56(9):e13442. PMID: 37086012 -
J Invest Dermatol
The Unknown Aspect of BAFF: Inducing IL-35 Production by a CD5+CD1dhiFcγRIIbhi Regulatory B-Cell Subset in Lupus. [Abstract]2017 Dec;137(12):2532-2543. PMID: 28844943
MLN120B dihydrochloride purchased from MedChemExpress. Usage Cited in: J Invest Dermatol. 2017 Dec;137(12):2532-2543. [Abstract]
MZ B cells are pre-treated with different concentrations of MLN120B, which selectively inhibit NF-κB1 pathway, the expression of p35 and Ebi3 significantly reduced.
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Biochem Pharmacol
Canagliflozin exerts anti-inflammatory effects by inhibiting intracellular glucose metabolism and promoting autophagy in immune cells. [Abstract]2018 Jun:152:45-59. PMID: 29551587
MLN120B dihydrochloride purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Jun:152:45-59. [Abstract]
Effects of NF-κB inhibitor (10 μM MLN120B) is measured on p62 protein in LPS-induced RAW264.7 cells.
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Int Immunopharmacol
Inflammatory factor-mediated miR-155/SOCS1 signaling axis leads to Treg impairment in systemic lupus erythematosus. [Abstract]2024 Nov 15:141:113013. PMID: 39213866 -
Sci Rep
A phenotypic high-content, high-throughput screen identifies inhibitors of NLRP3 inflammasome activation. [Abstract]2021 Jul 28;11(1):15319. PMID: 34321581 -
Int J Cancer
Synergy of interleukin 10 and toll-like receptor 9 signalling in B cell proliferation: Implications for lymphoma pathogenesis. [Abstract]2017 Mar 1;140(5):1147-1158. PMID: 27668411 -
J Biol Chem
Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain. [Abstract]2015 Apr 24;290(17):11061-74. PMID: 25762719 -
Viruses
Activation of the STAT3 Signaling Pathway by the RNA-Dependent RNA Polymerase Protein of Arenavirus. [Abstract]2021 May 25;13(6):976. PMID: 34070281 -
Cytokine
The LA-NF-κB-ILC2 axis exacerbates intestinal milk protein allergy in mice by promoting ILC2 activation. [Abstract]2026 May:201:157135. PMID: 41780286 -
Exp Ther Med
Proteomic and microRNA-omic profiles and potential mechanisms of dysfunction in pancreatic islet cells primed by inflammation. [Abstract]2021 Feb;21(2):122. PMID: 33335585 -
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溶剤 & 溶解度
DMSO : 16.67 mg/mL (37.91 mM; ultrasonic and warming and adjust pH to 8 with NaOH and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[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. [Content Brief]
[3]. Ansaldi D, et al. Imaging pulmonary NF-kappaB activation and therapeutic effects of MLN120B and TDZD-8. PLoS One. 2011;6(9):e25093. [Content Brief]
[4]. [3].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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2742 mL | 11.3709 mL | 22.7417 mL | 56.8544 mL |
| 5 mM | 0.4548 mL | 2.2742 mL | 4.5483 mL | 11.3709 mL | |
| 10 mM | 0.2274 mL | 1.1371 mL | 2.2742 mL | 5.6854 mL | |
| 15 mM | 0.1516 mL | 0.7581 mL | 1.5161 mL | 3.7903 mL | |
| 20 mM | 0.1137 mL | 0.5685 mL | 1.1371 mL | 2.8427 mL | |
| 25 mM | 0.0910 mL | 0.4548 mL | 0.9097 mL | 2.2742 mL | |
| 30 mM | 0.0758 mL | 0.3790 mL | 0.7581 mL | 1.8951 mL |
MLN120B dihydrochloride 関連分類
HY-15473A 関連分類
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