Histone Methyltransferase

Histone Methyltransferase

Histone modifications are essential for controlling both overall gene expression and stage-specific gene expression. While histones H3K9 and H3K27 are typically associated with gene repression, methylation on histones H3K4, H3K36, and H3K79 is typically associated with gene activation. Site-specific methyltransferases and demethylases dynamically control the methylation of histone lysines. The methylation of H3K27 in cells is carried out by EZH2 (the catalytic subunit of PRC2).
Inhibiting DOT1L, a histone H3 lysine 79 methyltransferase, improves the production of induced pluripotent stem cells (iPSCs). A powerful and specific DOT1L inhibitor, EPZ-5676.

The histone methyltransferase enhancer of zeste homolog 2 (EZH2) trimethylates histone 3's lysine 27 (H3K27me3), which results in chromatin condensation and transcriptional repression and is essential for PRC2 activity.

Histone Methyltransferase related products

Structure Cat No. Product Name CAS No. Product Description
V2603 UNC0638 1255580-76-7 UNC0638 (UNC-0638) is a selective and cell-permeable inhibitor of G9a histone methyltransferaseand GLP with IC50 of<15 nM and 19 nM, respectively.
V3137 UNC0642 1481677-78-4 UNC0642 (UNC-0642) is a novel, potent, selective, dual inhibitor ofG9a/GLP (histone methyltransferases) with antitumor activity.
V2057 UNC0646 1320288-17-2 UNC0646 is a novel, potent and selective histone methyltransferase G9a inhibitor with IC50 of 6 nM.
V0427 UNC1215 1415800-43-9 UNC1215 (UNC-1215) is a potent and selectiveantagonist of L3MBTL3, a member of the MBT (malignant brain tumor) family of methyllysine (Kme) reading domain, with potential antineoplastic activity.
V0385 UNC1999 1431612-23-5 UNC1999 (UNC-1999) is an orally bioavailable, cell-permeable, selective, SAM-competitive and dual inhibitor of EZH2/EZH1 (Enhancer of zeste homolog) with antineoplastic activity.
V35160 UNC2399 2412791-72-9 UNC2399, a biotinylated UNC1999, is a selective EZH2 inhibitor (antagonist) with high in vitro potency against EZH2 with IC50 of 17 nM.
V2605 UNC3866 1872382-47-2 UNC3866 is a novel and potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains with Kd of 100 nM as determined by AlphaScreen.
V75864 UNC4976 2920299-34-7 UNC4976 is a nucleic acid-binding PAM (positive allosteric modulator) peptidomimetic of the CBX7 chromatin domain.
V76388 UNC4976 TFA UNC4976 TFA is a nucleic acid-binding PAM (positive allosteric modulator) peptidomimetic of the CBX7 chromatin domain.
V40758 UNC6852 UNC6852 is a selective PRC2 degrader based on PROTAC technology.
V35159 UNC6852 2688842-08-0 UNC6852 is a selective PRC2 degrader based on PROTAC technology.
V53045 UNC6934 2561494-77-5 UNC6934 is a chemical probe targeting the PWWP domain of NSD2, which localizes to the nucleolus.
V75870 UNC8153 TFA 2929304-61-8 UNC8153 TFA is a potent and specific nuclear receptor binding SET domain-containing 2 (NSD2) targeted degrader with a Kd of 24 nM.
V22727 Urea J Acid 134-47-4 Urea J Acid (AMI-1; AMI 1) is a selective inhibitor of Histone Methyltransferase (HMT) with anti-inflammatory activity.
V50975 UZH2 2756566-45-5 UZH2 is a potent and specific METTL3 inhibitor (antagonist) with IC50 of 5 nM.
V27912 Valemetostat 1809336-39-7 Valemetostat (formerly known as DS-3201; DS-3201b; Ezharmia) is a first-in-class,investigational and oral EZH1/2 dual inhibitor with anticancer activity.
V32192 Valemetostat tosylate 1809336-93-3 Valemetostat tosylate (DS3201; DS3201b; Ezharmia), thetosylate salt ofValemetostat, is an investigational and orally bioavailable dual EZH1/2 inhibitor with potential anticancer activity.
V28182 WDR5-0103 890190-22-4 WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 µM).
V56078 WDR5-IN-4 2407457-36-5 WDR5-IN-4 is a WIN site inhibitor of chromatin-associated WD repeat domain 5 protein (WDR5) with a Kd of 0.1 nM.
V75862 WDR5-IN-4 TFA 2749300-35-2 WDR5-IN-4 TFA is a WIN site inhibitor of chromatin-associated WD repeat domain 5 protein (WDR5) with a Kd of 0.1 nM.
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