BRD32048
货号：
16516-500ug 基本售价：
490.0 元 规格：
500 ug
产品信息
概述| 货号 | 16516-500ug |
| 描述 | 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 (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 vitromodels.2 |
性能| 供应商 | Cayman |
| 应用文献 |
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).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 314.4 |
| 分子式 | C16H22N6O |
| CAS号 | 433694-46-3 |
| 稳定性 | ≥ 2 years |
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