| Description | PR 39 (porcine) acetate is a noncompetitive, reversible and allosteric proteasome inhibitor. PR 39 (porcine) acetate reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. |
| In vitro | PR-39 (100 nM) 阻断了 TNF-α (1 ng/mL; 20 分钟) 在人脐静脉内皮细胞 (HUVEC) 中激活 VCAM-1 (2 小时) 和 ICAM-1 (8 小时) 表达的能力[2]。PR-39 (10 μM) 对 ECV304 细胞的增殖能力没有影响。PR39 能够抑制 IκBα 的降解，而不显著影响细胞中总体蛋白的降解[2]。 |
| In vivo | PR-39促进血管生成，抑制炎症反应，并在小鼠中显著减小心肌梗死面积。PR-39（10 mg/kg，静脉注射；在Caerulein 50μg/kg, 腹腔注射前1小时）阻止小鼠急性胰腺炎诱导后IκBα的降解和NF-κB依赖的转录。PR-39（1 μg/kg/天；7天腹腔内持续注射）在C57BL/6小鼠中显著减少梗死面积[2]。 |
| molecular weight | N/A |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Maria Gaczynska, et al. Proline- and arginine-rich peptides constitute a novel class of allosteric inhibitors of proteasome activity. Biochemistry. 2003 Jul 29;42(29):8663-70. 2. Y Gao, et al. Inhibition of ubiquitin-proteasome pathway-mediated I kappa B alpha degradation by a naturally occurring antibacterial peptide. J Clin Invest. 2000 Aug;106(3):439-48. |