| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
PR-39 TFA targets the proteasome, specifically the alpha7 subunit of the 20S core particle. It acts as a noncompetitive, reversible, and allosteric inhibitor, blocking the degradation of the NF-kappaB inhibitor IkappaBalpha. Additionally, as a peptide, it can target bacterial membranes through its amphipathic, proline- and arginine-rich structure, leading to antimicrobial effects.
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| ln Vitro |
PR-39 TFA modifies the 20S and 26S cylinder shape and reversibly impacts the binding of 19S caps. It has been demonstrated to specifically impact proteasome-mediated protein degradation in vivo. IκBα and HIF-1α degradation by the proteasome is selectively inhibited by PR-39 TFA[1]. HRUVECs' production of VCAM-1 (two hours) and ICAM-1 (eight hours) is activated by TNF-α at a concentration of 1 ng/mL for 20 minutes, while PR-39 TFA (100 nM) prevents this[2]. The proliferative ability of ECV304 cells is not affected by 10 μM of PR-39 TFA. While having minimal effect on the total amount of protein degradation in cells, PR39 can prevent IκBα degradation[2].
In vitro, PR-39 TFA has several activities. It functions as a noncompetitive, reversible, and allosteric proteasome inhibitor. It binds to the alpha7 subunit of the proteasome and blocks the degradation of IkappaBalpha. It also has antibacterial activity against both Gram-positive and Gram-negative bacteria and can stimulate angiogenesis. It influences immune and inflammatory responses. |
| ln Vivo |
In the mouse pancreas following the formation of acute pancreatitis, PR-39 TFA (10 mg/kg, intravenously administered; one hour prior to Caerulein of 50 μg/kg, ip) inhibits IκBα degradation and NF-κB-dependent transcription[2]. In C57BL/6 mice, PR-39 TFA (1 μg/kg/day; 7-day intraperitoneal infusion) greatly reduces the size of the infarct[2].
In vivo, PR-39 TFA has been shown to stimulate angiogenesis and modulate inflammatory responses. Its ability to block the degradation of IkappaBalpha and activate NF-kappaB is expected to play a role in tissue repair and immune modulation. It functions in the inflammatory milieu not only to kill bacteria but also to aid in modulating the viability of inflammatory cells by regulating apoptosis. |
| Enzyme Assay |
A cell-free proteasome inhibition assay is performed using purified 20S proteasome and a fluorogenic peptide substrate (e.g., Suc-LLVY-AMC). PR-39 TFA is added at varying concentrations to the proteasome in assay buffer. The reaction is initiated by adding the substrate. The increase in fluorescence (ex/em = 380/460 nm) is measured over time. The IC50 is calculated from the inhibition curve.
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| Cell Assay |
RAW 264.7 macrophages or endothelial cells are seeded in 96-well plates. For angiogenesis assays, HUVECs are plated on Matrigel and treated with PR-39 TFA; tube formation is quantified. For antibacterial assays, bacteria are grown in liquid culture with the peptide. For NF-kappaB activation, cells are treated, lysed, and IkappaBalpha degradation and NF-kappaB p65 nuclear translocation are measured by Western blot and immunofluorescence.
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| Animal Protocol |
A standard in vivo protocol for PR-39 TFA involves a mouse wound healing model. Male C57BL/6 mice (8-10 weeks) are anesthetized, and a full-thickness excisional wound (6 mm) is created. PR-39 TFA (10-100 uM in sterile PBS) is applied topically to the wound. Wound closure is measured daily. Tissue is collected for histology and measurement of angiogenesis (CD31 staining) and inflammatory markers.
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| ADME/Pharmacokinetics |
PR-39 TFA is a 39-amino acid peptide with a molecular weight of 4833.76. The TFA salt form enhances solubility. As a peptide, its plasma half-life is expected to be short (<30 minutes) due to rapid proteolytic degradation. For in vivo use, it is often applied topically or used as a research tool for ex vivo experiments. Systemic use may require frequent dosing.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for PR-39 TFA are not available. As a naturally occurring peptide, it is expected to have low toxicity at physiological concentrations. High concentrations may cause hemolysis. Standard laboratory safety precautions for handling peptides should be followed. It is for research use only.
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| References |
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| Additional Infomation |
PR-39 TFA is a research-grade peptide and is not approved for clinical use. It is a natural proline- and arginine-rich antibacterial peptide and a noncompetitive, reversible, allosteric proteasome inhibitor. It is a multi-functional tool for studying angiogenesis, innate immunity, inflammation, and proteasome biology. The TFA salt is the standard commercial form.
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| Molecular Formula |
C231H347F3N70O42
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|---|---|
| Molecular Weight |
4833.76
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| Related CAS # |
PR-39;139637-11-9
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O :~100 mg/mL (~20.69 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (10.34 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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