1. Metabolic Enzyme/Protease
  2. Proteasome
  3. Proteasome-IN-4

Proteasome-IN-4 

Cat. No.: HY-144369
Handling Instructions

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.

For research use only. We do not sell to patients.

Proteasome-IN-4 Chemical Structure

Proteasome-IN-4 Chemical Structure

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Description

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]

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.
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.
Molecular Weight

750.97

Formula

C44H58N6O5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Product Name:
Proteasome-IN-4
Cat. No.:
HY-144369
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