Биологическая активность
TAS4464 is a highly мощный and селективный ингибитор of NEDD8 (IC50 of 0.955 nM). TAS4464 selectively inhibited NAE relative to the other E1s UAE and SAE. TAS4464 treatment inhibited cullin neddylation and subsequently induced the accumulation of CRL substrates such as CDT1, p27, and phosphorylated IκBα in human cancer клетка lines. TAS4464 showed greater inhibitory effects than those of the known NAE ингибитор MLN4924 both in enzyme assay and in cells.
Оригинал на английском
TAS4464 is a highly potent and selective inhibitor of NEDD8 (IC50 of 0.955 nM). TAS4464 selectively inhibited NAE relative to the other E1s UAE and SAE. TAS4464 treatment inhibited cullin neddylation and subsequently induced the accumulation of CRL substrates such as CDT1, p27, and phosphorylated IκBα in human cancer cell lines. TAS4464 showed greater inhibitory effects than those of the known NAE inhibitor MLN4924 both in enzyme assay and in cells.
Химические свойства
- CAS №
- 1848959-10-3
- Брутто-формула
- C₂₁H₂₃FN₆O₆S
- Мол. масса
- 506.51 г/моль
- SMILES
- CCOC1=C(C#CC2C3=C(N=CN=C3N)N(C=2)[C@H]4[C@H](O)[C@H](O)[C@@H](CNS(=O)(N)=O)O4)C(F)=CC=C1
- Синонимы
- TAS4464; 7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 7-[5-[(aminosulfonyl)amino]-5-deoxy-beta-D-ribofuranosyl]-5-[2-(2-ethoxy-6-fluorophenyl)ethynyl]-; BDBM320991; US10174040, Example 55; 4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-(2-ethoxy-6-fluoro-phenyl)ethynyl]pyrrolo[2,3-d]pyrimidine
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.