Биологическая активность
GSK2194069 is a мощный and specific ингибитор of the β-ketoacyl reductase (KR) activity of human fatty acid synthase (hFAS) с IC50 of 7.7 nM (CoA release); shows an IC50 of 29 nM versus hFAS with acetoacetyl-CoA as the substrate, but shows little or no inhibition with β-hydroxybutyrylCoA and crotonyl-CoA (IC50 >1,000 nM), also does not inhibit the partial activities of the KS domain; decreases phosphatidylcholine levels in A549 cells с IC50 of 15.5 nM without effect on FAS protein levels, reduced A549 клетка growth with EC50 of 15 nM.
Оригинал на английском
GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of human fatty acid synthase (hFAS) with IC50 of 7.7 nM (CoA release); shows an IC50 of 29 nM versus hFAS with acetoacetyl-CoA as the substrate, but shows little or no inhibition with β-hydroxybutyrylCoA and crotonyl-CoA (IC50 >1,000 nM), also does not inhibit the partial activities of the KS domain; decreases phosphatidylcholine levels in A549 cells with IC50 of 15.5 nM without effect on FAS protein levels, reduced A549 cell growth with EC50 of 15 nM.
Химические свойства
- CAS №
- 1332331-08-4
- Брутто-формула
- C₂₅H₂₄N₄O₃
- Мол. масса
- 428.48 г/моль
- Синонимы
- GSK 2194069; GSK-2194069
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.