BMVC

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

BMVC 

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

BMVC Chemical Structure

CAS No. : 627810-06-4

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生物活性

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].

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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

657.33

Formula

C28H25I2N3

CAS 号

627810-06-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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.

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