MLN120B dihydrochloride(Synonyms: ML120B dihydrochloride)

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MLN120B dihydrochloride (Synonyms: ML120B dihydrochloride)

MLN120B dihydrochloride (ML120B dihydrochloride) 是一种有效的、ATP 竞争性的和具有口服活性的 IKKβ抑制剂，IC50 为 60 nM。MLN120B 在体内外抑制多发性骨髓瘤细胞生长，也可用于类风湿关节炎的相关研究。

MLN120B dihydrochloride(Synonyms: ML120B dihydrochloride)

MLN120B dihydrochloride Chemical Structure

CAS No. : 1782573-78-7

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MLN120B dihydrochloride 的其他形式现货产品:

MLN120B

生物活性

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[1][2].

体外研究
(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 [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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MM.1S cells
Concentration: 5 μM; 10 μM; 20 μM
Incubation Time: 90 mintues
Result: Inhibited p-IκB and p-P65 expression in a dose-dependent manner.

Cell Viability Assay[1]

Cell Line: Myeloma cell lines: MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells
Concentration: 0-40 μM
Incubation Time: 72 hours
Result: Inhibited proliferation of multiple myeloma cell lines.

体内研究
(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; 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[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

分子量

439.72

Formula

C19H17Cl3N4O2
CAS 号

1782573-78-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

    [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]. [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.

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