52934-83-5
中文名称
七尾霉素
英文名称
NANAOMYCIN A
CAS
52934-83-5
分子式
C16H14O6
分子量
302.28
MOL 文件
52934-83-5.mol
更新日期
2023/03/17 20:03:07
52934-83-5 结构式
基本信息
中文别名
那罗星七尾霉素
英文别名
os-3966-arosanomycina
(1s-e)-10-dioxo
OS-3966-A
ROSANOMYCINA
1h-naphtho(2,3-c)pyran-3-aceticacid,3,4,5,10-tetrahydro-9-hydroxy-1-methyl-5,
(1S)-3,4,5,10-Tetrahydro-9-hydroxy-1-methyl-5,10-dioxo-1H-naphtho[2,3-c]pyran-3β-acetic acid
(1S,3R)-3,4,5,10-Tetrahydro-9-hydroxy-1-methyl-5,10-dioxo-1H-naphtho[2,3-c]pyran-3-acetic acid
Antibiotic OS 3966A, Nanafrocin, 1H-Naphtho[2,3-c]pyran-3-acetic acid,3,4,5,10-tetrahydro-9-hydroxy-1-methyl-5,10-dioxo-(1S,3R)-
物理化学性质
熔点179°C
沸点363.32°C (rough estimate)
密度1.2514 (rough estimate)
折射率1.4600 (estimate)
储存条件−20°C
溶解度insoluble in H2O; ≥15.1 mg/mL in DMSO; ≥31.07 mg/mL in EtOH with ultrasonic
形态固体
颜色Yellow to orange
常见问题列表
生物活性
Nanaomycin A 是第一个选择性 DNMT3B 抑制剂，IC50 为 500 nM。Nanaomycin A 是一种醌类抗生素，可重新激活人类癌细胞中沉默的抑癌基因。Nanaomycin A 抑制人疟原虫恶性疟原虫的体外生长，IC80 值为 33.1 nM。靶点
|
DNMT3B 500 nM (IC 50 ) |
体外研究
Nanaomycin A (10-10000 nM; 72 hours) has a distinct cytotoxic effect in all three cell lines.
Nanaomycin A (0.5, 5 μM; 72 hours) reveals induction of RASSF1A protein expression in A549 cells.
Nanaomycin A (5 μM; 72 hours) has an 18-fold relative induction.
Nanaomycin A not affects the enzymatic activity of DNMT1.
Cell Cytotoxicity Assay
| Cell Line: | HCT116 (colon), A549 (lung), and HL60 (bone marrow) human tumor cell lines |
| Concentration: | 10, 100, 1000, 10000 nM |
| Incubation Time: | 72 hours |
| Result: | Had a distinct cytotoxic effect in all three cell lines. |
Western Blot Analysis
| Cell Line: | A549 cells |
| Concentration: | 0.5, 5 μM |
| Incubation Time: | 72 hours |
| Result: | Revealed induction of RASSF1A protein expression. |
RT-PCR
| Cell Line: | A549 cells |
| Concentration: | 5 μM |
| Incubation Time: | 72 hours |
| Result: | Had an 18-fold relative induction. |