BMVC 是一种有效的 G-四联体 (G4) 稳定剂和选择性的端粒酶 (telomerase) 抑制剂，IC50约为 0.2 μM。BMVC 抑制 Taq DNA 聚合酶，IC50约为 2.5 μ M。BMVC 提高了端粒G4结构的熔化温度，并加速了端粒长度的缩短。抗癌活性。
| 生物活性 | BMVC is a potentG-quadruplex(G4)stabilizer and a selectivetelomeraseinhibitor with anIC50of ~0.2 μM. BMVC inhibits Taq DNA polymerase with anIC50of ~2.5 μM. BMVC increases the melting temperature ofG4structure of telomere and accelerates telomere length shortening. Anticancer activities[1][2]. |
| IC50& Target | IC50: ~0.2 μM (Telomerase)[1]
G-quadruplex[1]
IC50: ~2.5 μM (Taq DNA polymerase)[1] |
体外研究
(In Vitro) | BMVC (0.5 μM; 0-18 days; H1299 cells) treatment markedly increases the percentage of sub-G1-phase cells after 18 days[1].
BMVC (0.5 μM; 0-18 days; H1299 cells) long-term treatment leads to ceasing of cell growth and eventually cell death through apoptosis. The long-term BMVC treatment induces senescence program in H1299 cells[1].
In BMVC-treated cancer cells, hallmarks of senescence, including morphologic changes, detection of senescence-associated β-galactosidase activity, and decreasesd bromodeoxyuridine incorporation, are detected. The BMVC-induced senescence phenotype is accompanied by progressive telomere shortening and detection of the DNA damage foci, indicating that BMVC caused telomere uncapping after long-term treatments[1].
BMVC also suppresses the tumor-related properties of cancer cells, including cell migration, colony-forming ability, and anchorage-independent growth[1].
Cell Cycle Analysis[1] | Cell Line: | H1299 cells | | Concentration: | 0.5 μM | | Incubation Time: | 0 day, 6 days, 12 days, 18 days | | Result: | The percentage of sub-G1-phase cells was markedly increased after 18 days. |
Apoptosis Analysis[1] | Cell Line: | H1299 cells | | Concentration: | 0.5 μM | | Incubation Time: | 0 day, 6 days, 12 days, 18 days | | Result: | Increased apoptotic cells. |
|
体内研究
(In Vivo) | BMVC (1 mg/kg; intraperitoneal injection; every 3 day; BALB/cAnN.Cg-Foxn1nu/CrlNarl mice) treatment delays tumorigenic potential of cancer cells in vivo[1].
| Animal Model: | BALB/cAnN.Cg-Foxn1nu/CrlNarl mice injected with H1299 cells[1] | | Dosage: | 1 mg/kg | | Administration: | Intraperitoneal injection; every 3 day | | Result: | The growth rates of tumors in animals were significantly slower than that of control animals. The tumor cells of the mice were indeed entering apoptosis. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
m.cnreagent.com