WDR5 0103 是一种有效的选择性 WD 重复蛋白 5 (WDR5) 拮抗剂，Kd 为 450 nM。
| Cas No. | 890190-22-4 |
| 别名 | WD-Repeat Protein 5-0103 |
| 化学名 | methyl 3-(3-methoxybenzamido)-4-(4-methylpiperazin-1-yl)benzoate |
| Canonical SMILES | COC(C1=CC(NC(C2=CC=CC(OC)=C2)=O)=C(N3CCN(C)CC3)C=C1)=O |
| 分子式 | C21H25N3O4 |
| 分子量 | 383.44 |
| 溶解度 | ≥ 12.5mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 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: WDR5in 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. References:
[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. |
