17β-羟基渥曼青霉素
重组PI 3-激酶和mTOR的抑制剂
有货
基本信息
| 产品名称 | 17β-羟基渥曼青霉素 |
|---|---|
| 英文名称 | 17β-hydroxy Wortmannin |
| 运输条件 | 超低温冰袋运输 |
一般描述
17β-hydroxy Wortmannin 是渥曼青霉素的类似物。它不可逆地结合PI 3-激酶，并有效阻断中性粒细胞中由fMLP刺激的呼吸爆发（IC | 50 | = 5 nM）。17β-羟基Wortmannin抑制重组PI 3-激酶和mTOR（分别为IC | 50 | = 2.7和193 nM）并阻止LNCap前列腺癌细胞的生长（IC | 50 | = 1.46μM）。17-羟基已用于进一步修饰该化合物，例如通过聚乙二醇化和与雷帕霉素缀合。
17β-hydroxy Wortmannin is an analog of wortmannin . It irreversibly binds PI 3-kinase and potently blocks fMLP-stimulated respiratory burst in neutrophils (IC|50|= 5 nM). 17β-hydroxy Wortmannin inhibits recombinant PI 3-kinase and mTOR (IC|50|= 2.7 and 193 nM, respectively) and prevents the growth of LNCap prostate cancer cells (IC|50|= 1.46 μM). The 17-hydroxyl group has been used to further modify this compound, e.g., by pegylation and conjugation with rapamycin .
相关属性
| CAS编号 | 58053-83-1 |
|---|---|
| 折光率 | n20D1.60 (Predicted) |
| 熔点 | 239.2° C (Predicted) |
| 沸点 | 615.4° C at 760 mmHg (Predicted) |
| 溶解性 | Soluble in 1:9 EtOH:PBS (pH 7.2) (~0.1 mg/mL), ethanol (~0.15 mg/mL), DMSO (~2.5 mg/mL), and DMF (~3 mg/mL). |
| 储存温度 | -20°C储存 |
| 密度 | 1.39 g/cm3(Predicted) |
| 分子量 | 430.4 |
| 分子式 | C₂₃H₂₆O₈ |
| 品牌 | Jinpan |
| Smiles | COC[C@H]1OC(=O)c2coc3C(=O)C4=C([C@H](OC(=O)C)C[C@H]5(C)[C@@H](O)CCC45)[C@H]1(C)c23 |
| IC50 | Blocks fMLP-stimulated respiratory burst: IC₅₀= 5 nM (neutrophils); Recombinant PI3K: IC₅₀= 2.7 nM; Recombinant mTOR: IC₅₀= 193 nM; Growth of LNCap prostate cancer cells: IC₅₀= 1.46 μM |