P11
| 中文名称 | P11 |
|---|---|
| 中文同义词 | HSDVHK-NH2;H-HIS-SER-ASP-VAL-HIS-LYS-NH2;抑制剂多肽P11 |
| 英文名称 | HSDVHK-NH2 |
| 英文同义词 | L-Lysinamide, L-histidyl-L-seryl-L-α-aspartyl-L-valyl-L-histidyl- (9CI);P11 ( (trifluoroacetate salt) |
| CAS号 | 848644-86-0 |
| 分子式 | C30H48N12O9 |
| 分子量 | 720.79 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 848644-86-0.mol |
| 结构式 |  |
P11 性质
| 沸点 | 1380.0±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.381±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C, protect from light |
| 溶解度 | 在 20% 乙腈 - 0.1% 乙酸中溶解度为 1 mg/ml |
| 形态 | 粉末 |
| 酸度系数(pKa) | 4.17±0.10(Predicted) |
| 颜色 | 白色至米白色 |
| 序列 | H-His-Ser-Asp-Val-His-Lys-NH2 |
HSDVHK-NH2 是整合素 αvβ3-玻璃体结合蛋白的互作抑制剂，其 IC50 值为 1.74 pg/mL (2.414 pM)。
纯度(HPLC) ≥98.0%
醋酸根含量≤12.0%
水分含量≤8.0%
肽含量≥80.0%
内毒素≤50EU/mg
氨基酸组成分析≤±10%
|
αvβ3 2.74 nM (IC 50 ) |
HSDVHK significantly inhibited bFGF-induced cell migration compared to the PBS control group.
The Arg-Gly-Asp (RGD)-binding site recognition by HSDVHK-NH2 (P11) is site specific because the HSDVHK-NH2 (P11) is inactive for the complex formation of a denatured form of integrin–vitronectin. HSDVHK-NH2 (P11) shows a strong antagonism against avb3-GRGDSP interaction with an IC
50
value of 25.72 nM.
HSDVHK-NH2 (P11) inhibits the HUVEC proliferation due to the induction of HUVEC cell death through caspases activations and its mechanism is related with increased p53 expression.
Cell Proliferation Assay
| Cell Line: | HUVEC cells. |
| Concentration: | 0.1, 1, 10, and 100 μg/mL. |
| Incubation Time: | 72 h. |
| Result: | Significantly inhibited HUVEC proliferation on denatured collagen-coated plates in a dose-dependent manner. |
参考质量标准
外观:白色粉末纯度(HPLC) ≥98.0%
醋酸根含量≤12.0%
水分含量≤8.0%
肽含量≥80.0%
内毒素≤50EU/mg
氨基酸组成分析≤±10%