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氨基酸及其衍生物 抑制剂 常见氨基酸及蛋白质类药
SU 9516
发布者:信康   浏览次数:
  • 产品名称:SU 9516
  • CAS:377090-84-1
  • 别名:
  • 英文名:SU 9516
    • 储存条件 Store at +4°C
    • 溶解度 DMSO: ~17 mg/mL
    • 形态crystalline
    • 颜色brown
    • 生物活性SU9516是一种3位取代的吲哚酮类CDK抑制剂,对CDK2,CDK1,和CDK4的IC50分别为22 nM,40 nM,和200 nM。
    • 体外研究SU9516 decreases cdk2-specific phosphorylation of the retinoblastoma protein pRB, increases caspase-3 activation, and alters cell cycle in RKO and SW480 cells. SU9516 also inhibits the cell proliferation, and induces cell apoptosis in both cell lines. SU9516 kills leukemic cells through inhibition of RNA Pol II CTD phosphorylation, oxidative damage and transcriptional down-regulation of Mcl-1. In human T-cell leukemia Jurkat cells, SU9516 significantly enhances sensitivity to methotrexate. In addition, SU9516 also suppresses Aurora-A centrosomal localization and consequent centrosome amplification.