PR-39 TFA
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 4833.76 |
| Molecular Formula | C231H347F3N70O42 |
| SMILES | - |
Summary
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] .
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Sealed storage, away from moisture
| Powder | -80°C | 2 years |
|---|---|---|
| -20°C | 1 year |
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 100 mg/mL ( 20.69 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (10.34 mM); Clear solution; Need ultrasonic
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.