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.¹ The ETV1 transcription factor is phosphorylated downstream of MAPK signaling and is acetylated at lysines 33 and 116 by the histone acetyltransferase p300.¹ 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 (K_D = 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.²

≥98%

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1.Oh, S.,Shin, S. and Janknecht, R. ETV1, 4 and 5: An oncogenic subfamily of ETS transcription factors. Biochim.Biophys.Acta. 1826(1), 1-12 (2012).

2.Pop, M.S.,Stransky, N.,Garvie, C.W., et al. A small molecule that binds and inhibits the ETV1 transcription factor oncoprotein. Molecular Cancer Therapeutics 13(6), 1492-1502 (2014).