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CAS号 | 433694-46-3 | 货号 | BCP30330 |
中文名 | BRD32048 | ||
英文名 | BRD32048 | ||
中文别名 | |||
英文别名 | BRD-32048; BRD 32048; | ||
SMILES | COC1=CC=C(C=C1)NC2=NC(=NC(=N2)N)CN3CCCCC3 | ||
化学名称 | |||
分子式 | C16H22N6O | 分子量 | 314.39 |
纯度 | 98% | 配送 | 惯例下常温包邮 |
产品描述 | BRD32048 is an inhibitor of the ETV1 transcription factor oncoprotein.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.2 At 20-100 µM, BRD32048 can dose-dependently prevent invasion of ETV1-reliant cancer cells in in vitro models. |
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