Description
BMVC is a potent G-quadruplex (G4) stabilizer and a selective telomerase inhibitor with an IC 50 of ~0.2 µM. BMVC inhibits Taq DNA polymerase with an IC 50 of ~2.5 µM. BMVC increases the melting temperature of G4 structure of telomere and accelerates telomere length shortening. Anticancer activitiesIn VitroBMVC (0.5 µM; 0-18 days; H1299 cells) treatment markedly increases the percentage of sub-G1-phase cells after 18 days. 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. 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. BMVC also suppresses the tumor-related properties of cancer cells, including cell migration, colony-forming ability, and anchorage-independent growth. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell 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 AnalysisCell Line: H1299 cells Concentration: 0.5 µM Incubation Time: 0 day, 6 days, 12 days, 18 days Result: Increased apoptotic cells.In VivoBMVC (1 mg/kg; intraperitoneal injection; every 3 day; BALB/cAnN.Cg-Foxn1 nu /CrlNarl mice) treatment delays tumorigenic potential of cancer cells in vivo. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/cAnN.Cg-Foxn1 nu /CrlNarl mice injected with H1299 cells 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.Form:SolidIC50& Target:IC50: ~0.2 µM (Telomerase), G-quadruplex, IC50: ~2.5 µM (Taq DNA polymerase)