Биологическая активность
GJG057 is a LTC4S ингибитор. GJG057 exhibits мощный cytotoxic effects against various human cancer клетка lines, including SGC-7901, HGC-27, and MCF-7, with IC₅₀ values of 20.5 ± 5.93 μM, 3.3 ± 2.53 μM, and 16.6 ± 0.75 μM, respectively. Notably, GJG057 shows high selectivity towards cancer cells over normal cells. Mechanistic investigations revealed that GJG057 induces apoptosis in a concentration-dependent manner and downregulates the expression of HIF-1α, VEGF, and PKM2, leading to decreased lactate production. Furthermore, GJG057 effectively inhibits tubulin assembly, suggesting its potential as a multi-target anti-tumor agent.
Оригинал на английском
GJG057 is a LTC4S inhibitor. GJG057 exhibits potent cytotoxic effects against various human cancer cell lines, including SGC-7901, HGC-27, and MCF-7, with IC₅₀ values of 20.5 ± 5.93 μM, 3.3 ± 2.53 μM, and 16.6 ± 0.75 μM, respectively. Notably, GJG057 shows high selectivity towards cancer cells over normal cells. Mechanistic investigations revealed that GJG057 induces apoptosis in a concentration-dependent manner and downregulates the expression of HIF-1α, VEGF, and PKM2, leading to decreased lactate production. Furthermore, GJG057 effectively inhibits tubulin assembly, suggesting its potential as a multi-target anti-tumor agent.
Химические свойства
- CAS №
- 2761767-18-2
- Брутто-формула
- C₂₁H₂₁F₅N₄O₂
- Мол. масса
- 456.42 г/моль
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.