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Histone methyltransferase inhibitors target the enzymes that methylate lysine residues on histone tails. Lysine methyltransferases transfer methyl groups from S-adenosylmethionine to defined lysines, most often on histone H3. Methylation of lysine 27 of histone H3 (H3K27) by enhancer of zeste homolog 2 (EZH2) is linked to Polycomb gene silencing, while H3K9 methylation marks heterochromatin. Most compounds here target EZH2, including GSK126, GSK343 and tazemetostat, which compete with S-adenosylmethionine. UNC0642 inhibits G9a and G9a-like protein (GLP), pinometostat targets the H3K79 methyltransferase disruptor of telomeric silencing 1-like (DOT1L), and chaetocin acts on suppressor of variegation 3-9 homolog (SUV39H) enzymes. Inhibitors of arginine-directed enzymes are listed under Protein Arginine Methyltransferases.
UNC3866 is a potent antagonist of CBX4 and CBX7 chromodomains with a Kd of ~100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains.
A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM.
Synonyms: ZINC30303842; Z336955588; NSD2-PWWP1 antagonist 3f
ZINC30303842 is a NSD2-PWWP1 antagonist.
UNC6934 is a potent and selective chemical probe targeting the N-terminal PWWP1 domain of NSD2 (nuclear receptor-binding SET domain protein 2). It binds NSD2-PWWP1 with a Kd of 80 nM (measured by SPR) and exhibits high selectivity over 14 other PWWP domains, including NSD3-PWWP1. In U2OS cells, UNC6934 disrupts the interaction between NSD2-PWWP1 and H3K36me2-marked nucleosomes, with an IC₅₀ of 1.09 μM as determined by NanoBRET assay. It is a valuable tool for studying NSD2 chromatin interactions and epigenetic regulation.
GA001 is a potent G9a antagonist with an IC50 of 1.32 μM. This compound has been shown to induce autophagy and apoptosis, making it a valuable tool for research in breast cancer. Its ability to modulate epigenetic regulation offers significant potential in understanding cancer biology and developing therapeutic strategies.
rel-A-395 hydrochloride is an antagonist of polycomb repressive complex 2 (PRC2), specifically designed to disrupt protein-protein interactions within the trimeric PRC2 complex, comprising EZH2, EED, and SUZ12. With an IC50 value of 18 nM, this compound effectively inhibits PRC2 activity, making it a valuable tool for research on epigenetic regulation and gene expression modulation. Its application is crucial in studies aimed at understanding the role of PRC2 in oncogenesis and developmental biology.
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