Proteasome-IN-4 

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: 8.39 nM (proteasome)^[1]

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 T_1/2 of 329.21 min^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

750.97

C₄₄H₅₈N₆O₅

CCN(C1=CC=CC=C1)C(C2CCN(CC2)C(N[C@H](C(N[C@H](C(N[C@@H]3CCCC4=C3C=CC=C4)=O)CCC5=CC=CC=C5)=O)CC(NCC(C)(C)C)=O)=O)=O

Room temperature in continental US; may vary elsewhere.

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

• [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.  [Content Brief]