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CAS No.: 890190-22-4

WDR5-0103 Catalog No. CSN17252

Synonyms: WD-Repeat Protein 5-0103

WDR5-0103 is a selective antagonist of WD repeat-containing protein 5 (WDR5) with Kd of 450 nM.

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靶点选择性

生物活性

实验方案

技术信息

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 K_d 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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6080 mL
- 13.0398 mL
- 26.0796 mL
- 5 mM
- 0.5216 mL
- 2.6080 mL
- 5.2159 mL
- 10 mM
- 0.2608 mL
- 1.3040 mL
- 2.6080 mL

技术信息

CAS号

890190-22-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H25N3O4

运输

蓝冰

分子量

383.44

别名

WD-Repeat Protein 5-0103

溶解度

DMSO	77.0 mg/mL (200.8 mM)
Water	Insoluble
Ethanol	20.0 mg/mL (52.2 mM)

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