货号:A651436 同义名: 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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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
规格 | 价格 | 会员价 | 库存 | 数量 | |||
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产品名称 | Histone Methyltransferase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BRD4770 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
UNC1999 |
+++
EZH2, IC50: 2 nM EZH1, IC50: 45 nM |
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EPZ005687 |
++
EZH2, Ki: 24 nM |
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EPZ015666 |
+++
PRMT5, Ki: 5 nM |
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3-Deazaneplanocin A HCl |
++++
S-adenosylhomocysteine hydrolase, Ki: 50 pM |
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EPZ6438 |
+++
EZH2, IC50: 11 nM EZH2, Ki: 2.5 nM |
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GSK126 |
++
EZH2, IC50: 9.9 nM |
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MI-3 |
+
Menin-MLL, IC50: 648 nM |
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MM-102 |
++
MLL1, IC50: 0.4 μM |
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EI1 |
++
Ezh2 (wild-type), IC50: 15 nM EZH2 (Y641F), IC50: 13 nM |
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SGC0946 |
++++
DOT1L, IC50: 0.3 nM |
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PFI-2 HCl |
++++
SETD7, IC50: 2 nM SETD7, Ki: 0.33 nM |
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Pinometostat |
++++
DOT1L, Ki: 80 pM |
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EPZ004777 |
+++
DOT1L, IC50: 0.4 nM |
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Entacapone |
++
COMT, IC50: 151 nM |
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UNC0379 |
+
SETD8, IC50: 7.9 μM |
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Menin-MLL inhibitor MI-2 |
+
Menin-MLL, IC50: 446 nM |
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GSK343 |
+++
EZH2, IC50: 4 nM EZH1, IC50: 240 nM |
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BIX-01294 3HCl |
+
G9a, IC50: 2.7 μM |
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 890190-22-4 |
分子式 | C21H25N3O4 |
分子量 | 383.441 |
别名 | WD-Repeat Protein 5-0103 |
运输 | 蓝冰 |
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 |