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 |
|---|---|---|---|---|
|
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. |
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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. |
|
V56085 | WM-586 | 2894832-05-2 | WM-586 is a covalent WDR5 inhibitor that disrupts the binding of WDR5 to MYC. |
|
V51746 | WM-662 | 1308257-47-7 | WM-662 is a WDR5-MYC responsive reagent with IC50 of 18 μM. |
|
V28304 | XY1 | 1624117-53-8 | XY1 is an analog of SGC707 used as a negative control of SGC-707, which is a potent, selective allosteric inhibitor of PRMT3 (IC50 = 50 nM). |
|
V2265 | ZINC30303842 | 1210906-48-1 | MR837 is an inhibitor of NSD2-PWWP1. |
|
V78899 | ZZM-1220 | ZZM-1220 is a covalent inhibitor of histone lysine methyltransferase G9a/GLP with IC50 of 458 nM and 924 nM respectively. |
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