OICR-9429
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货号：A225196
OICR-9429 is an antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3.
OICR-9429 化学结构
OICR-9429 3D分子结构
规格
价格
会员价
库存
数量
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OICR-9429 纯度/质量文件 产品仅供科研
货号：A225196
标准纯度：
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OICR-9429 质控信息
BRD4770
✔
99%+
UNC1999
+++
EZH1, IC50: 45 nM
EZH2, IC50: 2 nM
99%+
EPZ005687
++
98+%
EPZ015666
+++
99%+
3-Deazaneplanocin A HCl
++++
S-adenosylhomocysteine hydrolase, Ki: 50 pM
99%+
Tazemetostat
+++
EZH2, Ki: 2.5 nM
EZH2, IC50: 11 nM
98%
GSK126
++
99%+
MI-3
+
98%
MM-102
++
99%
EI1
++
Ezh2 (wild-type), IC50: 15 nM
EZH2 (Y641F), IC50: 13 nM
99% (HPLC)
SGC0946
++++
99%+
PFI-2 HCl
++++
SETD7, Ki: 0.33 nM
SETD7, IC50: 2 nM
99%+
Pinometostat
++++
99%+
EPZ004777
+++
99%+
Entacapone
++
95%
UNC0379
+
99%+
Menin-MLL inhibitor MI-2
+
98%
GSK343
+++
EZH1, IC50: 240 nM
EZH2, IC50: 4 nM
99%+
BIX-01294 3HCl
+
99%+
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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。
OICR-9429 生物活性
描述
OICR-9429 is a potent and selective antagonist of the WDR5-MLL1 interaction with KD value of 30nM[6] Cebpap30/p30 cells, such as C3ar1, Ccl9, Lcn2, Lilrb3 , and Lyz2 , at 20μM[5]
作用机制
OICR-9429 binds in the arginine binding site of WDR5, occupying the MLL-binding pocket of Wdr5.[5]
OICR-9429 动物研究
Dose
Mice: 1.5 mg/kg[3] [4] [1] [1]
Administration
i.p.
Pharmacokinetics
Animal
Mice[1]
Dose
3 mg/kg (i.v.)
Administration
i.v.
F
67% (i.p.)
Vd
15.6 L/kg (i.v.)
T1/2
287 min (i.v.)
Tmax
5 min (i.v.)
CL
3233 ml/h/kg (i.v.)
Cmax
697 ng/ml (i.v.)
AUC
1012 h·ng/ml (i.v.)
OICR-9429 参考文献
[1] Getlik M, Smil D, et al. Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1). J Med Chem. 2016 Mar 24;59(6):2478-96.
[2] Grebien F, Vedadi M, et al. Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. Nat Chem Biol. 2015 Aug;11(8):571-578.
[3] Shimoda H, Doi S, et al. Inhibition of the H3K4 methyltransferase MLL1/WDR5 complex attenuates renal senescence in ischemia reperfusion mice by reduction of p16INK4a. Kidney Int. 2019 Nov;96(5):1162-1175.
[4] Cao L, Wu G, et al. Genotoxic stress-triggered β-catenin/JDP2/PRMT5 complex facilitates reestablishing glutathione homeostasis. Nat Commun. 2019 Aug 21;10(1):3761.
[5] Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Skucha A, Vittori S, Kuznetsova E, Smil D, Barsyte-Lovejoy D, Li F, Poda G, Schapira M, Wu H, Dong A, Senisterra G, Stukalov A, Huber KVM, Schönegger A, Marcellus R, Bilban M, Bock C, Brown PJ, Zuber J, Bennett KL, Al-Awar R, Delwel R, Nerlov C, Arrowsmith CH, Superti-Furga G. Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. Nat Chem Biol. 2015 Aug;11(8):571-578. doi: 10.1038/nchembio.1859. Epub 2015 Jul 13. Erratum in: Nat Chem Biol. 2015 Oct;11(10):815. PMID: 26167872; PMCID: PMC4511833.
[6] Getlik M, Smil D, Zepeda-Velázquez C, Bolshan Y, Poda G, Wu H, Dong A, Kuznetsova E, Marcellus R, Senisterra G, Dombrovski L, Hajian T, Kiyota T, Schapira M, Arrowsmith CH, Brown PJ, Vedadi M, Al-Awar R. Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1). J Med Chem. 2016 Mar 24;59(6):2478-96. doi: 10.1021/acs.jmedchem.5b01630. Epub 2016 Mar 9. PMID: 26958703.
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OICR-9429 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
1.80mL
0.36mL
0.18mL
9.00mL
1.80mL
0.90mL
18.00mL
3.60mL
1.80mL
OICR-9429 技术信息
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