BRD32048 |
| Catalog No.GC42975 |
BRD32048 est un liant direct d'ETV1 avec un KD de 17,1 μM. BRD32048 module À la fois l'activité transcriptionnelle induite par ETV1 et l'invasion des cellules cancéreuses induites par ETV1. BRD32048 inhibe l'acétylation d'ETV1 et favorise sa dégradation. BRD32048 agit comme un perturbagène ETV1 candidat de premier plan.
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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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