產(chǎn)品描述: | 20S Proteasome activator 1 是一種有效的 20S 蛋白酶激活劑,對胰蛋白酶樣位點(diǎn)、胰凝乳蛋白酶樣位點(diǎn)和半胱天冬酶位點(diǎn)的 IC50 分別為 0.3 μM、0.7 μM 和 1.8 μM。20S Proteasome activator 1 能在細(xì)胞系統(tǒng)中翻譯,防止致病性 α-synuclein A53T 突變體積累。20S Proteasome activator 1 可用于神經(jīng)退行性疾病的研究。 |
靶點(diǎn): |
IC50: 0.3 μM (trypsin-like site), 0.7 μM (chymotrypsin-like site), 1.8 μM (caspase-like site);Proteasome |
體外研究: |
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. 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. |
參考文獻(xiàn): |
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. |
溶解性: |
soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.029 ml |
10.143 ml |
20.285 ml |
5 mM |
0.406 ml |
2.029 ml |
4.057 ml |
10 mM |
0.203 ml |
1.014 ml |
2.029 ml |
50 mM |
0.041 ml |
0.203 ml |
0.406 ml |
|
注意: |
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