中文名称 | 成球菌素 |
---|---|
英文名称 | Conglobatin |
CAS号 | 72263-05-9 |
分子式 | C28H38N2O6 |
分子量 | 498.61 |
外观 | White to grayish white powder |
储存条件 | Store at -20°C |
Conglobatin is a dimeric macrolide dilactone originally isolated from S. conglobatus. It disrupts binding of heat shock protein 90 (Hsp90) to the co-chaperone Cdc37 complex and induces downregulation of client protein expression in SK-BR-3 breast cancer cells. It also inhibits cell proliferation in HER2+ breast cancer cell lines (IC50s = 12.9-61.5 uM, respectively) and decreases the number of invasive cells in vitro. When combined with lapatinib , tumor growth of SK-BR-3 mouse xenografts was reduced to a greater degree than with conglobatin alone. Conglobatin has various anticancer effects in esophageal squamous cell carcinoma (ESCC) models as well, including an inhibition of cell proliferation in KYSE510 cells (IC50 = 9.31 uM). It also inhibits β1 integrin activation leading to a loss of cellular adhesion.
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