S34186 |
20S Proteasome activator 1 |
源叶(MedMol) | 98% |
- 产品描述:
20S Proteasome activator 1 是一种有效的 20S 蛋白酶激活剂,对胰蛋白酶样位点、胰凝乳蛋白酶样位点和半胱天冬酶位点的 IC50 分别为 0.3 μM、0.7 μM 和 1.8 μM。20S Proteasome activator 1 能在细胞系统中翻译,防止致病性 α-synuclein A53T 突变体积累。20S Proteasome activator 1 可用于神经退行性疾病的研究。
- 靶点: IC50: 0.3 μM (trypsin-like site), 0.7 μM (chymotrypsin-like site), 1.8 μM (caspase-like site);Proteasome
- 体外研究:
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.
- 参考文献:
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
- 保存条件: -20℃
- 配置溶液浓度参考:
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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)