PR-39 TFA
目录号 : GC63964PR-39 TFA 是富含脯氨酸和精氨酸的天然抗菌肽,是一种非竞争性,可逆和变构的蛋白酶体 (proteasome) 抑制剂。PR-39 TFA 可逆地结合到蛋白酶体的 α7 亚基上,并通过泛素-蛋白酶体途径阻断 NF-κB 抑制剂 IκBα 的降解。PR-39 TFA 刺激小鼠的血管生成,抑制炎症反应并显着减小心肌梗死面积。
Sample solution is provided at 25 µL, 10mM.
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice[1][2].
PR-39 TFA, shown to selectively affect proteasomemediated protein degradation in vivo, alters the shape of the 20S and 26S cylinder and affects the binding of 19S caps in a reversible manner. PR-39 TFA specifically blocks degradation of IκBα and HIF-1α by the proteasome[1]. PR-39 TFA (100 nM) blocks TNF-α-induced (1 ng/mL; for 20 minutes) activation of VCAM-1 (2 hours) and ICAM-1 (8 hours) expression in human umbilical vein endothelial cells (HUVEC)[2]. PR-39 TFA (10 μM) does not affect the ability to proliferate of ECV304 cell. PR39 is able to inhibit IκBα degradation without significantly affecting overall protein degradation in cells[2].
PR-39 TFA (10 mg/kg, intravenously; 1 hour before Caerulein of 50 μg/kg, ip) blocks IκBα degradation and NF-κB-dependent transcription in the mouse pancreas after induction of acute pancreatitis[2]. PR-39 TFA (1 μg/kg/day; 7-day intraperitoneal infusion) demonstrates significantly small infarct in C57BL/6 mice[2].
[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.
Cas No. | SDF | Download SDF | |
分子式 | C231H347F3N70O42 | 分子量 | 4833.76 |
溶解度 | Water : 100 mg/mL (20.69 mM; Need ultrasonic) | 储存条件 | -20°C, away from moisture |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 0.2069 mL | 1.0344 mL | 2.0688 mL |
5 mM | 0.0414 mL | 0.2069 mL | 0.4138 mL |
10 mM | 0.0207 mL | 0.1034 mL | 0.2069 mL |
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% DMSO % % Tween 80 % saline | ||||||||||
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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