Size | Price | Stock | Qty |
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1mg |
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5mg |
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Other Sizes |
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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].
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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].
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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. |
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 |
Typically exists as solids (or liquids in special cases) at room temperature
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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.