20S Proteasome-IN-3

Names

[ CAS No. ]:
1803040-07-4

[ Name ]:
20S Proteasome-IN-3

Biological Activity

[Description]:

20S Proteasome-IN-3 is a 20S proteasome β5 subunit inhibitor (IC50=1.64 μM)[1][2]. 20S Proteasome-IN-3 shows anti-tumor proliferation activity[2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome

[Target]

IC50: 1.64 μM (20S proteasome β5 subunit)[1]


[In Vitro]

20S Proteasome-IN-3 (Compound 10b) (5.34-9.69 μM, 18-24 h) exhibits significant inhibition against A375, SW480, DU145, and HeLa cells[2]. Cell Proliferation Assay[2] Cell Line: A375, SW480, DU145, and HeLa cell lines Concentration: 5.34-9.69 μM Incubation Time: 18-24 hours Result: Inhibited the proliferation of SW480, DU145, A375 and HeLa cells with the IC50s of 5.34, 9.69, 5.66 and 7.03 μM, respectively.

[References]

[1]. Qi Sun, et al. Design and synthesis of tripeptidyl furylketones as selective inhibitors against the β5 subunit of human 20S proteasome. Eur J Med Chem. 2020 Apr 15;192:112160.

[2]. Qi Sun, et al. Synthesis, bioactivity, docking and molecular dynamics studies of furan-based peptides as 20S proteasome inhibitors. ChemMedChem. 2015 Mar;10(3):498-510.

Chemical & Physical Properties

[ Molecular Formula ]:
C34H43N3O8

[ Molecular Weight ]:
621.72

Related Compounds