硫链丝菌素
| 中文名称 | 硫链丝菌素 |
|---|---|
| 中文同义词 | 硫活素;硫链丝霉素;藓霉素;硫链丝菌素;硫链丝菌素(>97%,BC);硫链丝菌素A;硫酸丝菌肽;硫链丝菌肽 |
| 英文名称 | THIOSTREPTON |
| 英文同义词 | Thiostrepton (200 mg);BryaMycin, Thiactin, AlaninaMide, X 146, A 8506, 6761-31;Thiostrepton, froM StreptoMyces sp.;x146;THIOSTREPTON;Alaninamide, L-threonyl-(4S)-2-(1Z)-1-amino-1-propenyl-4,5-dihydro-4-thiazolecarbonyl-2-(1S,2S,3R)-1-amino-2,3-dihydroxy-2-methylbutyl-4-thiazolecarbonyl-2-(5R,6S)-6-2-(1S,2R)-1-amino-2-hydroxypropyl-4-thiazolyl-5-N-(7R,8S)-2-carboxy-7,8-dihydro-8-hydroxy;THIOSTREPTION;thiostrepton from streptomyces azureus |
| CAS号 | 1393-48-2 |
| 分子式 | C72H85N19O18S5 |
| 分子量 | 1664.89 |
| EINECS号 | 215-734-9 |
| 相关类别 | 抗生素、生物碱;抗生素;微生物代谢物;生化试剂;小分子抑制剂;抗生素类;小分子抑制剂，天然产物;医药原料;通用生化试剂-抗生素;抗体;Organics;Antibacterial;Antibiotics;Antibiotics A to;Antibiotics by Application;Antibiotics T-ZAntibiotics;Chemical Structure Class;Gene Regulation and Expression;Genetic Marker SelectionAntibiotics;Interferes with Protein SynthesisSpectrum of Activity;L - ZAntibiotics;Mechanism of Action;PeptidesCell Signaling and Neuroscience;Peptide Synthesis/Antibiotics;Amino Acids & Derivatives;Intermediates & Fine Chemicals;Pharmaceuticals;BETAPACE;antibiotic;Inhibitors;RNA-Protein Translation InhibitorsMore...Close... |
| Mol文件 | 1393-48-2.mol |
| 结构式 |  |
硫链丝菌素 性质
| 熔点 | 248-257°C (dec.) |
|---|---|
| 比旋光度 | D23 -98.5° (glacial acetic acid); -61° (dioxane); -20° (pyridine) |
| 密度 | 1.0824 (rough estimate) |
| 折射率 | 1.6700 (estimate) |
| 储存条件 | Sealed in dry,Store in freezer, under -20°C |
| 溶解度 | 溶于DMSO或氯仿 |
| 形态 | 类白色粉末 |
| 酸度系数(pKa) | 10.43±0.46(Predicted) |
| 颜色 | 米白色 |
| 水溶解性 | 0.24g/L(28 ºC) |
| Merck | 13,9440 |
| 稳定性 | 从购买之日起 2 年内保持稳定。 DMSO 中的溶液可在 -20℃ 下保存长达 1 周。 |
Thiostrepton 是一种抗生素，可选择性抑制 FOXM1。FOXM1 与 YAP/TEAD 复合物结合。YAP/TEAD/FOXM1 复合物在控制细胞周期的基因调控区域结合可能会影响细胞增殖。
Thiostrepton (0.01-1000 μM; 48 hours) suppresses cell viability in A2780 and HEC-1A.
Cell Viability Assay
| Cell Line: | A2780 and HEC-1A cells |
| Concentration: | 0.01, 0.1, 1, 10, 100, 1000 μM |
| Incubation Time: | 48 hours |
| Result: | The IC 50 s are 1.10 μM in A2780 and 2.22 μM in HEC-1A, respectively. |
Thiostrepton (i.p.; 17 mg/kg) reduces the tumorigenicity of Ewing's sarcoma (EWS) cells. Tumor volumes in control mice have increased ~6-fold from the initiation of treatment, while their Thiostrepton-treated counterparts increase only ~1.7-fold, exhibiting a ~3.5-fold reduction, relative to controls.
| Animal Model: | Athymic (BALB/c nu/nu) nude mice bearing A4573 cells |
| Dosage: | 17 mg/kg |
| Administration: | Administered i.p. |
| Result: | Treatment inhibited the growth of EWS-derived tumors in vivo. |
安全信息
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英文
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