Биологическая активность
GSK-J4 is a клетка permeable, мощный and селективный histone demethylase. GSK-J4 is a prodrug of GSK J1, which is the first селективный ингибитор of the H3K27 histone demethylase JMJD3 and UTX с IC50 of 60 nM in a клетка-free assay and inactive against a panel of demethylases of the JMJ family. GSK-J4 is used to probe the consequences of demethylation of H3K27me3. GSK-J4 inhibits the lipopolysaccharide-induced production of cytokines, including pro-inflammatory tumour necrosis factor (TNF).
Оригинал на английском
GSK-J4 is a cell permeable, potent and selective histone demethylase. GSK-J4 is a prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family. GSK-J4 is used to probe the consequences of demethylation of H3K27me3. GSK-J4 inhibits the lipopolysaccharide-induced production of cytokines, including pro-inflammatory tumour necrosis factor (TNF).
Химические свойства
- CAS №
- 1373423-53-0
- Брутто-формула
- C₂₄H₂₇N₅O₂
- Мол. масса
- 417.51 г/моль
- SMILES
- CCOC(=O)CCNC1=NC(=NC(=C1)N2CCC3=CC=CC=C3CC2)C4=CC=CC=N4.Cl
- Синонимы
- GSK-J4 free base; GSK-J-4; GSK-J 4; GSK-J4
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
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.