BRD32048

  • 化学数据
CAS号 433694-46-3 货号 BCP30330
中文名 BRD32048
英文名 BRD32048
中文别名
英文别名 BRD-32048; BRD 32048;
分子式 C16H22N6O 分子量 314.39
  • 用途
生物活性 BRD32048 is an inhibitor of the ETV1 transcription factor oncoprotein.ETS variant 1 (ETV1) is a transcription factor oncogene implicated in several cancers where it has been altered by chromosomal translocation, gene amplification, or lineage dysregulation.The ETV1 transcription factor is phosphorylated downstream of MAPK signaling and is acetylated at lysines 33 and 116 by the histone acetyltransferase p300.Both of these events increase the protein half-life of ETV1 and enhance its transcriptional activity. BRD32048 is a substituted [1,3,5]triazine derivative that inhibits ETV1 transcriptional activity by binding to ETV1 (KD = 17.1 µM in vitro), which reduces p300-dependent acetylation and stability of ETV1 and, thereby, promotes its degradation.2 At 20-100 µM, BRD32048 can dose-dependently prevent invasion of ETV1-reliant cancer cells in in vitro models.
信号通路 MAPK Pathway 

结构式

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