货号 | 5267/50 |
别名 | N-[2-(4-Methylpiperazin-1-yl)-5-[3- |
供应商 | Tocris |
生物活性 | High affinity WDR5 antagonist (Kd = 93 nM); disrupts WDR5-MLL interaction. Exhibits selectivity for WDR5 over 22 methyltransferases and a panel of kinases, GPCRs, ion channels, and transporters. Reduces viability of acute myeloid leukemia cells in vitro. Also disrupts MLL1-RbBP5 interaction. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >98 % |
计算分子量 | 555.59 |
分子式 | C29H32F3N5 |
可溶性/溶解性 | Soluble to 50 mM in DMSO |
参考文献 | Getliket al (2016) Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1). J.Med.Chem. 59 2478. PMID: 26958703. Grebienet al (2015) Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. Nat.Chem.Biol. 11 571. PMID: 26167872. |