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 Frontiers in Immunology, August 9, 2022, 938944 Protein Cell, 2025, 16(6):439-457
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

Frontiers in Immunology, August 9, 2022, 938944

Protein Cell, 2025, 16(6):439-457

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