同义名 :	-
	CAS号 :	1801787-56-3
	货号 :	A225196
	分子式 :	C29H32F3N5O3
	纯度 :	99%+
	分子量 :	555.59
	MDL号 :	MFCD28411621
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

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]. OICR-9429 binds to WDR5 with high affinity and competitively disrupts its interaction with a high-affinity Wdr5-INteracting (WIN) peptide of MLL. It disrupted the C/EBPα p30-Wdr5 interaction at 10μM. OICR-9429 selectively inhibited proliferation and induced differentiation in p30-expressing human AML cells and induced the up-regulation of myeloid marker genes in 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]

实验方案
	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

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.