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氨基酸及其衍生物 抑制劑 常見氨基酸及蛋白質(zhì)類藥
SU 9516
發(fā)布者:信康   瀏覽次數(shù):
  • 產(chǎn)品名稱:SU 9516
  • CAS:377090-84-1
  • 別名:
  • 英文名:SU 9516
    • 儲存條件 Store at +4°C
    • 溶解度 DMSO: ~17 mg/mL
    • 形態(tài)crystalline
    • 顏色brown
    • 生物活性SU9516是一種3位取代的吲哚酮類CDK抑制劑,對CDK2,CDK1,和CDK4的IC50分別為22 nM,40 nM,和200 nM。
    • 體外研究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.