Proteasome-IN-4

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Proteasome-IN-4 

Proteasome-IN-4 是一种良好的非共价 proteasome 抑制剂 (IC50= 8.39 nM)。Proteasome-IN-4 对 RPMI-8226、MM-1S 和 MV-4-11 细胞系具有较强的抗增殖活性。Proteasome-IN-4 可用于癌症研究。

Proteasome-IN-4

Proteasome-IN-4 Chemical Structure

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生物活性

Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC50=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research[1].

IC50 & Target

IC50: 8.39 nM (proteasome)[1]
体外研究
(In Vitro)

Proteasome-IN-4 (compound 43) (0-20 nM; 72 hours) has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines, with IC50 of 15.290, 9.067 and 2.740 nM respectively[1].
Proteasome-IN-4 (10-1000 nM; 3 hours) causes massive accumulation of polyubiquitinated proteins at the concentration from 10 nM to 1000 nM[1].
Proteasome-IN-4 (2μM) has high metabolic stability in mouse blood, with T1/2 of 329.21 min[1].

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

Cell Proliferation Assay

Cell Line: MM-1S, RPMI 8226 and MV-4-11 cells[1]
Concentration: 0-20 nM
Incubation Time: 72 hours
Result: Displayed potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines, with IC50 of 15.290, 9.067 and 2.740 nM respectively.

Western Blot Analysis

Cell Line: MM-1S[1]
Concentration: 10, 100 and 1000 nM
Incubation Time: 3 hours
Result: Caused massive accumulation of polyubiquitinated proteins at the concentration from 10 nM to 1000 nM.

体内研究
(In Vivo)

Proteasome-IN-4 (5 mg/kg; i.v.; single) has superior activities with intracellular proteasome inhibitory rates of about 50% after administration of 1 h in model mice[1].

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

Animal Model: ICR mice (6-8 weeks)[1]
Dosage: 5 mg/kg
Administration: i.v.; single
Result: Displayed superior activities with intracellular proteasome inhibitory rates of about 50% after administration of 1 h.

分子量

750.97

Formula

C44H58N6O5
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]. Cao Y, et al. Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment. Eur J Med Chem. 2022;233:114211.

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