WDR5-0103 , 97% , 一个有效的含WD重复序列蛋白5 (WDR5) 选择性拮抗剂, Kd值为450 nM
WDR5-0103, 97%, a potent and selective WD repeat-containing protein 5 (WDR5) antagonist
分子式: C21H25N3O4
分子量: 383.44
纯度: 97%
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基本信息
英文别名WD-repeat protein 5-0103 |
安全信息
存储条件Freezer -20℃ | Symbol   |
Hazard StatementsH302 H410 | |
Precautionary StatementsP264 P270 P330 P501 P273 P391 P301+P317 | |
UN3077 | Hazard Class9 |
Packing GroupIII | |
化学和物理性质
产品描述
产品描述
WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM. IC50 value: 450 nM (Kd) Target: WDR5 in vitro: WDR5-0103 inhibits MLL catalytic activity with an IC50 value of 39±10 μM. An increase in MLL complex concentration resulted in proportional increase in IC50 values for WDR5-0103 (83±10 and 280±12 μM at concentrations of 500 and 1000 nM of the core trimeric MLL complex respectively). These data are consistent with a mechanism of action in which WDR5-0103 antagonizes the interaction of WDR5 with MLL by competing with MLL for their mutual binding site on WDR5.
靶点（IC50 & Targe）
WDR5,
体外研究
体内研究
激酶实验
细胞实验
动物实验
参考文献
[1]. Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem J. 2013 Jan 1;449(1):151-159.
