Биологическая активность
DDO-5936 is a мощный PPI ингибитор targeting Hsp90-Cdc37 protein-protein interaction (PPI) as Orally Active Inhibitors for the Treatment of Colorectal Cancer. DDO-5936 disrupted the Hsp90-Cdc37 PPI both in vitro and in vivo via связывание to a previously unknown site on Hsp90 involving Glu47, one of the связывание determinants for the Hsp90-Cdc37 PPI, leading to селективный down-regulation of Hsp90 киназы clients in HCT116 cells. In addition, inhibition of Hsp90-Cdc37 complex formation by DDO-5936 resulted in a remarkable cyclin-dependent киназы 4 decrease and consequent inhibition of клетка proliferation through Cdc37-dependent клетка cycle arrest.
Оригинал на английском
DDO-5936 is a potent PPI inhibitor targeting Hsp90-Cdc37 protein-protein interaction (PPI) as Orally Active Inhibitors for the Treatment of Colorectal Cancer. DDO-5936 disrupted the Hsp90-Cdc37 PPI both in vitro and in vivo via binding to a previously unknown site on Hsp90 involving Glu47, one of the binding determinants for the Hsp90-Cdc37 PPI, leading to selective down-regulation of Hsp90 kinase clients in HCT116 cells. In addition, inhibition of Hsp90-Cdc37 complex formation by DDO-5936 resulted in a remarkable cyclin-dependent kinase 4 decrease and consequent inhibition of cell proliferation through Cdc37-dependent cell cycle arrest.
Химические свойства
- CAS №
- 2355377-13-6
- Брутто-формула
- C₂₅H₂₉N₅O₄S
- Мол. масса
- 495.59 г/моль
- SMILES
- C1CCCN1C1N=C(C=CN=1)NC1=CC=C(C=C1)N(S(=O)(=O)C1C(=CC(=CC=1C)C)C)CC(=O)O
- Синонимы
- N-[4-[[2-(1-Pyrrolidinyl)-4-pyrimidinyl]amino]phenyl]-N-[(2,4,6-trimethylphenyl)sulfonyl]glycine
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Хранение и физические свойства
- Условия хранения
- Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.