1. Metabolic Enzyme/Protease
  2. Proteasome
  3. 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。

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Proteasome-IN-4 Chemical Structure

Proteasome-IN-4 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE 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].

MCE 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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Proteasome-IN-4
目录号:
HY-144369
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