20S Proteasome activator 1_product_DataBase

Bioactivity	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].
Target	IC50: 0.3 μM (trypsin-like site), 0.7 μM (chymotrypsin-like site), 1.8 μM (caspase-like site)
Invitro	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].
Name	20S Proteasome activator 1
CAS	2761578-18-9
Formula	C27H19ClF2N2OS
Molar Mass	492.97
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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