硫链丝菌素
中文名称:
硫链丝菌素
中文同义词:
硫链丝菌素, 来源于链霉菌;硫链丝菌肽;硫链丝菌肽(-20`C);硫活素;硫链丝菌素A;硫链丝霉素;藓霉素;硫链丝霉素、硫酸丝菌肽
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;Inhibitors;BETAPACE;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;antibiotic;RNA-Protein Translation InhibitorsMore...Close...
Mol文件:
1393-48-2.mol
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
Soluble in DMSO or chloroform
形态
Off-white powder
酸度系数(pKa)
10.43±0.46(Predicted)
水溶解性
0.24g/L(28 ºC)
Merck
13,9440
生物活性
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。
体外研究
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.
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.
体内研究
Thiostrepton (i.p.; 17 mg/kg) reduces the tumorigenicity of Ewings 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.
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.
危险品标志
Xn
危险类别码
22
安全说明
22-24/25
WGK Germany
3
RTECS号
XN6300100
F
10-21
海关编码
29419090
毒性
LD50 oral in mouse: > 1gm/kg
