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ML 120B dihydrochloride

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产品编号 T39199Cas号 1782573-78-7
别名 ML120B dihydrochloride

MLN120B dihydrochloride (ML120B dihydrochloride) is a highly potent, orally active inhibitor of IKKβ. It competitively binds to ATP and exhibits an impressive IC50 value of 60 nM. This compound effectively suppresses the growth of multiple myeloma cells both in vitro and in vivo. Furthermore, MLN120B dihydrochloride is valuable in the field of rheumatoid arthritis research.

ML 120B dihydrochloride

ML 120B dihydrochloride

Rating icon 还可以
产品编号 T39199 别名 ML120B dihydrochlorideCas号 1782573-78-7

MLN120B dihydrochloride (ML120B dihydrochloride) is a highly potent, orally active inhibitor of IKKβ. It competitively binds to ATP and exhibits an impressive IC50 value of 60 nM. This compound effectively suppresses the growth of multiple myeloma cells both in vitro and in vivo. Furthermore, MLN120B dihydrochloride is valuable in the field of rheumatoid arthritis research.

规格价格库存数量
2 mg
¥ 648
5日内发货
5 mg
¥ 1,300
5日内发货
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TargetMol 的所有产品仅用作科学研究或药证申报,不能被用于人体,我们不向个人提供产品和服务。请您遵守承诺用途,不得违反法律法规规定用于任何其他用途。
实验操作小课堂
常见问题解答
化合物带有盐酸盐离子、硫酸盐离子等是否和其本身有什么区别?盐形式和游离态有什么区别?
盐和非盐形式化合物的活性分子是一样的,在生物实验中起到的效果也一致,活性和使用方法都是一样的。只是由于呈盐不同,物理性质比如溶解度会有差异。建议您根据溶解、实验需求进行选择。
如何选择某个靶点的特异性或总的抑制剂?特异性和非特异性的区别是什么?
抑制剂按照特异性分为广谱 pan 和特异性 selective 两种。Pan 为某个靶点总的抑制剂,对所有亚型或整个家族的成员都有抑制作用。Selective 抑制剂针对某个蛋白激酶的某个亚型或家族中某个成员抑制率特别高或有特异性抑制作用。 一般评价一个抑制剂的抑制效率主要看 IC50 值,IC50 值越低,说明抑制剂效率越高。建议您根据以上几个特征进行综合选择,也可联系技术帮您推荐相关抑制剂。
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产品介绍

生物活性
产品描述
MLN120B dihydrochloride (ML120B dihydrochloride) is a highly potent, orally active inhibitor of IKKβ. It competitively binds to ATP and exhibits an impressive IC50 value of 60 nM. This compound effectively suppresses the growth of multiple myeloma cells both in vitro and in vivo. Furthermore, MLN120B dihydrochloride is valuable in the field of rheumatoid arthritis research.
体外活性
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 [ 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]. 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.
体内活性
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]. 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.
别名ML120B dihydrochloride
化学信息
分子量439.72
分子式C19H17Cl3N4O2
CAS No.1782573-78-7
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

SCI 文献

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

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