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.
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. |