PR-39 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 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 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。
| 生物活性 | PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allostericproteasomeinhibitor. PR-39 reversibly binds to the α7 subunit of theproteasomeand blocks degradation ofNF-κB inhibitorIκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice[1][2]. |
体外研究
(In Vitro) | PR-39, 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 specifically blocks degradation of IκBα and HIF-1α by the proteasome[1].
PR-39 (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 (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].
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体内研究
(In Vivo) | PR-39 (10 mg/kg, intravenously; 1 hour before Caerulein of 50μg/kg, ip) blocks IκBα degradation and NF-κB-dependent transcription in the mouse pancreas after induction of acute pancreatitis[2].
PR-39 (1 μg/kg/day; 7-day intraperitoneal infusion) demonstrates significantly small infarct in C57BL/6 mice[2].
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| 分子量 | |
| Formula | |
| CAS 号 | |
| Sequence Shortening | RRRPRPPYLPRPRPPPFFPPRLPPRIPPGFPPRFPPRFP-NH2 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Solvent & Solubility | In Vitro: H2O Peptide Solubility and Storage Guidelines: 1. Calculate the length of the peptide. 2. Calculate the overall charge of the entire peptide according to the following table: | | Contents | Assign value | | Acidic amino acid | Asp (D), Glu (E), and the C-terminal -COOH. | -1 | | Basic amino acid | Arg (R), Lys (K), His (H), and the N-terminal -NH2 | +1 | | Neutral amino acid | Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) | 0 |
3. Recommended solution: | Overall charge of peptide | Details | | Negative (<0) | 1. Try to dissolve the peptide in water first.
2. If water fails, add NH4OH (<50 μL).
3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. | | Positive (>0) | 1. Try to dissolve the peptide in water first.
2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO. | | Zero (=0) | 1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration. |
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