BRD32048

BRD32048

CAT N°: 16516
Price:

From 66.00 56.10

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.{26964} The ETV1 transcription factor is phosphorylated downstream of MAPK signaling and is acetylated at lysines 33 and 116 by the histone acetyltransferase p300.{26964} 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.{26612} At 20-100 µM, BRD32048 can dose-dependently prevent invasion of ETV1-reliant cancer cells in in vitro models.{26612}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N2-(4-methoxyphenyl)-6-(1-piperidinylmethyl)-1,3,5-triazine-2,4-diamine
  • Correlated keywords
    • oncogenes ETS variants 1 ETV1 transcription factors cancers E26 transformation-specific genes inhibitors p300 acetylation BRD 32048 BRD-32048 ETV-1 inhibits oncoproteins
  • Product Overview:
    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.{26964} The ETV1 transcription factor is phosphorylated downstream of MAPK signaling and is acetylated at lysines 33 and 116 by the histone acetyltransferase p300.{26964} 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.{26612} At 20-100 µM, BRD32048 can dose-dependently prevent invasion of ETV1-reliant cancer cells in in vitro models.{26612}

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