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BMVC

目录号 : GC68021

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。

BMVC Chemical Structure

Cas No.:627810-06-4

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10mg
¥4,320.00
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25mg
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50mg
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Sample solution is provided at 25 µL, 10mM.

Description

IC50: ~0.2 μM (Telomerase)[1]
G-quadruplex[1]
IC50: ~2.5 μM (Taq DNA polymerase)[1]

BMVC is a potent G-quadruplex (G4) stabilizer and a selective Telomerase inhibitor with an IC50 of ~0.2 μM. BMVC inhibits Taq DNA polymerase with an IC50 of ~2.5 μM. BMVC increases the melting temperature of G4 structure of telomere and accelerates telomere length shortening. Anticancer activities[1][2].

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.

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.

[1]. Huang FC, et al. G-quadruplex stabilizer 3,6-bis(1-methyl-4-vinylpyridinium)carbazole diiodide induces accelerated senescence and inhibits tumorigenic properties in cancer cells. Mol Cancer Res. 2008 Jun;6(6):955-64.
[2]. Jen-Fei Chu, et al. A Novel Method for Screening G-quadruplex Stabilizers to Human Telomeres. Journal of the Chinese Chemical Society, 2011, 58, 296-300.

化学性质

Cas No. 627810-06-4 SDF Download SDF
分子式 C28H25I2N3 分子量 657.33
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1 mM 1.5213 mL 7.6065 mL 15.2131 mL
5 mM 0.3043 mL 1.5213 mL 3.0426 mL
10 mM 0.1521 mL 0.7607 mL 1.5213 mL
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