货号：P3807
储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。
产品描述
Deubiquitinating enzymes (DUBs) remove ubiquitin from their substrates and, together with ubiquitin ligases, play an important role in the regulation of protein expression. PR-619 is a broad-range UDB inhibitor that led to cell morphological changes, the upregulation of HSPs and accumulation of ubiquitinated protein species. PR-619 exhibits concentration dependent cytotoxicity in very narrow concentration range of 7 - 10 μM to OLN 93 cells. Treatment with 9 μM PR-619 causes an increase in the abundance of ubiquitinated protein, and proteasomal activity reduce to 50% within 24 h. PR-619 promotes the association of tau, ubiquitin and p62 with microtubules and alter their solubility. In addition, Treatment with the PR-619 increased caspase-8 ubiquitination and caspase-8 enzymatic activity and sensitized normal fibroblasts to TRAIL-mediated apoptosis. In vivo, administered daily with 100 μg PR-619 improves renal histopathological changes in mice with unilateral ureteral obstruction. Administration of PR-619 also attenuated renal fibrosis with downregulation of mesenchymal markers, extracellular matrix proteins, matrix metalloproteinases, apoptosis, macrophage infiltration, and the TGF-β1 mRNA level.
靶点:
DUB
EC50:1-20μM
储存液制备 | 质量 | 1 mg | 5 mg | 10 mg |
1 mM | 1.4580 mL | 7.2898 mL | 14.5796 mL | |
5 mM | 0.2916 mL | 1.4580 mL | 2.9159 mL | |
10 mM | 0.1458 mL | 0.7290 mL | 1.4580 mL |
产品性质
CAS号 | 2645-32-1 | |
分子式 | C7H5N5S2 | |
分子量 | 223.28 | |
溶解度 | DMSO | 22.0 mg/mL (98.5 mM) warming |
Water | insoluble | |
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