Home Epigenetics Histone Methyltransferase antagonist - WDR5 antagonist OICR-9429 For research use only.

OICR-9429

OICR-9429 is a potent antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3 and reduces viability of acute myeloid leukemia cells in vitro. It binds to WDR5 with high affinity (KD = 93 ± 28 nM.

OICR-9429 Chemical Structure

OICR-9429 Chemical Structure

CAS No. 1801787-56-3

Purity & Quality Control

OICR-9429 Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BL21(DE3)-V2R-pRARE2 Function assay Binding affinity to human poly His-tagged WDR5 (1 to 334 residues) expressed in Escherichia coli BL21(DE3)-V2R-pRARE2 cells by surface plasmon resonance analysis, Kd=0.03μM 26958703
BL21(DE3)-V2R-pRARE2 Function assay Inhibition of human poly His-tagged WDR5 (1 to 334 residues) interaction with MLL1 assessed as displacement of fluorescein isothiocyanate labelled 9-Ala-FAM peptide substrate from WDR5 expressed in Escherichia coli BL21(DE3)-V2R-pRARE2 cells by fluorescen, K=0.06μM 26958703
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Biological Activity

Description OICR-9429 is a potent antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3 and reduces viability of acute myeloid leukemia cells in vitro. It binds to WDR5 with high affinity (KD = 93 ± 28 nM.
Targets
Wdr5-MLL interaction [1] WDR5 [1]
93 nM(Kd)
In vitro
In vitro

OICR-9429 binds WDR5 with high affinity (Kd=93±28 nM) and competitively disrupts its interaction with a high-affinity Wdr5-interacting (WIN) peptide of MLL (Kdisp=64±4 nM)[1].
Cell Research Cell lines Primary human AML cells
Concentrations 5 μM
Incubation Time 72 h
Method

20,000 viable, actively proliferating primary human AML cells per well were seeded in 96-well plates in triplicates and treated with 0.05% DMSO or OICR-9429. Cell viability was measured using the Cell Titer-Glo luminescent cell viability assay on a VICTOR X4 luminometer after 72 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Wdr5 / MLL / RbBP5 26167872
In Vivo
In vivo

OICR-9429, a potent WDR5 inhibitor, suppressed proliferation, metastasis and PD-L1-based immune evasion while enhancing apoptosis and chemosensitivity to cisplatin in bladder cancer by blocking the WDR5-MLL complex mediating H3K4me3 in target genes.
Animal Research Animal Models Male BALB/c nude mice
Dosages 30 or 60 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 555.59 Formula

C29H32F3N5O3
CAS No. 1801787-56-3 SDF Download OICR-9429 SDF
Smiles CN1CCN(CC1)C2=C(C=C(C=C2)C3=CC=CC(=C3)CN4CCOCC4)NC(=O)C5=CNC(=O)C=C5C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 41 mg/mL ( (73.79 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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