Histone Methyltransferase Antagonists

Cat.No.	Product Name	Information	Product Use Citations
S2184	WDR5-0103	WDR5-0103 (WD-Repeat Protein 5-0103) is a small-molecule antagonist of WDR5 (WD40 repeat protein 5) with Kd of 450 nM.	Cell Reports, September 26, 2023, 113145 Journal of Clinical Investigation, July 3, 2023, e169993 Frontiers in Immunology, August 9, 2022, 938944
S8359	UNC3866	UNC3866 is a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. This compound binds the chromodomains of CBX4 and CBX7 most potently, with a K(d) of ∼100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains.	Leukemia, 2021, 2299-2310 Leukemia, 2021, 10.1038/s41375-021-01121-8 International Journal of Molecular Sciences, 2021, 619
S7833	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.	FASEB J, 2025, 39(8):e70543 Mol Cell, 2024, 84(8):1475-1495.e18 PLoS Biol, 2024, 22(3):e3002240

Cat.No.

Product Name

Information

Product Use Citations

Product Validations

S2184

WDR5-0103

WDR5-0103 (WD-Repeat Protein 5-0103) is a small-molecule antagonist of WDR5 (WD40 repeat protein 5) with Kd of 450 nM.

Cell Reports, September 26, 2023, 113145

Journal of Clinical Investigation, July 3, 2023, e169993

Frontiers in Immunology, August 9, 2022, 938944

S8359

UNC3866

UNC3866 is a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. This compound binds the chromodomains of CBX4 and CBX7 most potently, with a K(d) of ∼100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains.

Leukemia, 2021, 2299-2310

Leukemia, 2021, 10.1038/s41375-021-01121-8

International Journal of Molecular Sciences, 2021, 619

S7833

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.

FASEB J, 2025, 39(8):e70543

Mol Cell, 2024, 84(8):1475-1495.e18

PLoS Biol, 2024, 22(3):e3002240