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WDR5-0103

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Chemical Structure| 890190-22-4 同义名 : WD-Repeat Protein 5-0103
CAS号 : 890190-22-4
货号 : A651436
分子式 : C21H25N3O4
纯度 : 99%+
分子量 : 383.441
MDL号 : MFCD07086826
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(130.4 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 WDR5 (WD40 repeat protein 5) is an essential component of the human trithorax-like family of SET1 (Su(var)3-9 enhancer-of-zeste trithorax 1) methyltransferase complexes that carry out trimethylation of histone 3 Lys4 (H3K4me3), play key roles in development and are abnormally expressed in many cancers. WDR5-0103 is a potent and selective WDR5 antagonist with Kd of 450 nM. At an MLL (mixed-lineage leukaemia protein) complex concentration of 0.125 μM, WDR5-0103 inhibited 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 were consistent with a mechanism of action in which WDR5-0103 antagonized the interaction of WDR5 with MLL by competing with MLL for their mutual binding site on WDR5[2].
作用机制 The methoxyphenyl and ester groups of WDR5-0103 increase shape complementarity with the binding pocket[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.04mL

2.61mL

1.30mL

26.08mL

5.22mL

2.61mL
参考文献

[1]Senisterra G, Wu H, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem J. 2013 Jan 1;449(1):151-9.

[2]Senisterra G, Wu H, Allali-Hassani A, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem J. 2013;449(1):151-159