| 货号 | 13945-25mg |
| 描述 | WD-repeat protein 5 (WDR5) is a scaffold protein commonly involved in the formation of nucleosome-modifying protein complexes with histones.1 For example, WDR5 is a component of a mixed-lineage leukemia (MLL) methyltransferase complex that targets histone 3.2 WDR5 can also be a component of histone acetyltransferase complexes and can directly bind methylated as well as unmodified histones.3,1 WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro(IC50 = 39 µM).4,5 |
| 别名 | WD-Repeat Protein 5-0103; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Migliori, V.,Mapelli, M. and Guccione, E. On WD40 proteins: Propelling our knowledge of transcriptional control? Epigenetics 7(8), 815-822 (2012). 2.Guccione, E.,Bassi, C.,Casadio, F., et al. Methylation of histone H3R2 by PRMT6 and H3K4 by an MLL complex are mutually exclusive. Nature 449, 933-937 (2007). 3.Guelman, S.,Kozuka, K.,Mao, Y., et al. The double-histone-acetyltransferase complex ATAC is essential for mammalian development. Molecular and Cellular Biology 29(5), 1176-1188 (2009). 4.Senisterra, G.,Wu, H.,Allali-Hassani, A., et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochemistry Journal 449(1), 151-159 (2013). 5.Wigle, T.J. and Copeland, R.A. Drugging the human methylome: An emerging modality for reversible control of aberrant gene transcription. Current Opinion in Chemical Biology 17(3), 369-378 (2013). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 383.4 |
| 分子式 | C21H25N3O4 |
| CAS号 | 890190-22-4 |
| 稳定性 | ≥ 2 years |
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