Биологическая активность
Hsp90 ингибитор 5b is a first-in-class, малая молекула ингибитор of the C-terminal (CTD) Hsp90 dimerization with KD of 3.42 uM, IC50 of 1.3 uM against leukemia клетка line K562.Hsp90 ингибитор 5b inhibits Hsp90 chaperone function, does not show any interaction with the NTD of Hsp90.Hsp90 ингибитор 5b down-regulated the phospho-BCR-ABL1 and total-BCR-ABL1 levels, as well as the related downstream signaling pathways, additionally reduced the expression of client proteins associated with Hsp90 chaperone activity, involving Akt, Stat5, and c-Myc.Hsp90 ингибитор 5b inhibited leukemic клетка lines (K562, KCL22 and HL60) proliferation and induced apoptosis in a caspase 3/7 enzyme-dependent assay.Hsp90 ингибитор 5b is effective against resistant leukemia cells and in the zebrafish xenotransplantation model.
Оригинал на английском
Hsp90 inhibitor 5b is a first-in-class, small molecule inhibitor of the C-terminal (CTD) Hsp90 dimerization with KD of 3.42 uM, IC50 of 1.3 uM against leukemia cell line K562.Hsp90 inhibitor 5b inhibits Hsp90 chaperone function, does not show any interaction with the NTD of Hsp90.Hsp90 inhibitor 5b down-regulated the phospho-BCR-ABL1 and total-BCR-ABL1 levels, as well as the related downstream signaling pathways, additionally reduced the expression of client proteins associated with Hsp90 chaperone activity, involving Akt, Stat5, and c-Myc.Hsp90 inhibitor 5b inhibited leukemic cell lines (K562, KCL22 and HL60) proliferation and induced apoptosis in a caspase 3/7 enzyme-dependent assay.Hsp90 inhibitor 5b is effective against resistant leukemia cells and in the zebrafish xenotransplantation model.
Химические свойства
- CAS №
- 1542130-29-9
- Брутто-формула
- C₃₉H₄₂N₁₀O₈
- Мол. масса
- 778.83 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.