2761578-18-9

2761578-18-9 structure
2761578-18-9 structure
  • Name: 20S Proteasome activator 1
  • Chemical Name: 20S Proteasome activator 1
  • CAS Number: 2761578-18-9
  • Molecular Formula: C27H19ClF2N2OS
  • Molecular Weight: 492.97
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Proteasome
  • Create Date: 2022-09-01 12:52:25
  • Modify Date: 2024-02-14 16:43:01
  • 20S Proteasome activator 1 is a potent 20S proteasome activator with EC200 values of 0.3 μM, 0.7 μM and 1.8 μM for trypsin-like site, chymotrypsin-like site and caspase-like site. 20S Proteasome activator 1 translates well in a cellular system, preventing the accumulation of the pathogenic A53T mutant of α-synuclein. 20S Proteasome activator 1 can be used for researching neurodegenerative diseases[1].

Name 20S Proteasome activator 1
Description 20S Proteasome activator 1 is a potent 20S proteasome activator with EC200 values of 0.3 μM, 0.7 μM and 1.8 μM for trypsin-like site, chymotrypsin-like site and caspase-like site. 20S Proteasome activator 1 translates well in a cellular system, preventing the accumulation of the pathogenic A53T mutant of α-synuclein. 20S Proteasome activator 1 can be used for researching neurodegenerative diseases[1].
Related Catalog
Target

IC50: 0.3 μM (trypsin-like site), 0.7 μM (chymotrypsin-like site), 1.8 μM (caspase-like site)[1]

In Vitro 20S Proteasome activator 1 (compound 19) (2.5-15 μM; 45 min) degrades 73% α-synuclein at 10 μM, and over 80% at 15 μM[1]. 20S Proteasome activator 1 (5-15 μM; 24 h) reduces 25% A53T mutant, and dose-dependently reduces enhancement of α-synuclein in Hek-293T cells (transiently transfected with an A53T mutant α-synuclein plasmid) at 5 μM; decreases 67% A53T α-synuclein at 15 μM[1].
References

[1]. Staerz SD, et al. Design, Synthesis, and Biological Evaluation of Potent 20S Proteasome Activators for the Potential Treatment of α-Synucleinopathies. J Med Chem. 2022 May 12;65(9):6631-6642.

Molecular Formula C27H19ClF2N2OS
Molecular Weight 492.97