BRD32048 |
| カタログ番号GC42975 |
BRD32048 は、17.1 μM の KD を持つ ETV1 の直接結合剤です。 BRD32048 は、ETV1 を介した転写活性と ETV1 が駆動する癌細胞の浸潤の両方を調節します。 BRD32048 は ETV1 のアセチル化を阻害し、その分解を促進します。 BRD32048 は、ETV1 摂動因子の最有力候補として機能します。
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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.
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