BRD32048 |
| Katalog-Nr.GC42975 |
BRD32048 ist ein direkter Binder von ETV1 mit einer KD von 17,1 μM. BRD32048 moduliert sowohl die ETV1-vermittelte TranskriptionsaktivitÄt als auch die Invasion von ETV1-gesteuerten Krebszellen. BRD32048 hemmt die ETV1-Acetylierung und fÖrdert deren Abbau. BRD32048 fungiert als Spitzenkandidat fÜr ETV1-StÖrungen.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 433694-46-3
Sample solution is provided at 25 µL, 10mM.
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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. At 20-100 µM, BRD32048 can dose-dependently prevent invasion of ETV1-reliant cancer cells in in vitro models.
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)
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