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 |
|---|---|---|---|---|
|
V20268 | DS-437 | 1674364-87-4 | DS-437 (DS437) is a novel and potent dual PRMT5 and PRMT7 inhibitor with anticancer activity. |
|
V52145 | E67-2 | 1364914-62-4 | As an E67 analogue, E67-2 is a low-toxic, selective KIAA1718 Jumonji domain inhibitor (antagonist) with IC50 of 3.4 µM. |
|
V3760 | EBI-2511 | 2098546-05-3 | EBI-2511 is anovel and orally available benzofuran derived EZH2 inhibitors that was discovered through a scaffold hopping approach based on the clinical compound of EPZ-6438. |
|
V56084 | EEDligand 1 | 2762275-20-5 | EED ligand 1 is a versatile and potent inhibitor that targets the EED subunit of the methyltransferase PRC2. |
|
V52142 | EEDi-5285 | 2488952-40-3 | EEDi-5285 is a very potent and orally bioactive inhibitor of embryonic ectoderm development (EED), binding to EED protein with IC50 of 0.2 nM and having anti-cancer activity. |
|
V0393 | EI1 (KB145943; EI 1) | 1418308-27-6 | EI1(KB-145943; EI-1) is a potent and selective inhibitor of EZH2 (Enhancer of zeste homolog 2) with potential antitumor activity. |
|
V78566 | EML734 | 3031795-11-3 | EML734 is a potent and specific PRMT7/9 inhibitor (antagonist) with IC50s of 315 nM and 0.89 μM respectively. |
|
V52130 | EML741 | 2328074-38-8 | EML741 is a histone methyltransferase (G9a/GLP) inhibitor (antagonist) with IC50 and Kds of 23 nM and 1.13 μM for G9a, respectively. |
|
V88886 | EPIC-0628 | EPIC-0628 is an inhibitor of HOTAIR-EZH2 interaction and promotes ATF3 expression. | |
|
V0390 | EPZ015666 (GSK3235025) | 1616391-65-1 | EPZ015666 (GSK-3235025), an analog ofEPZ-015866, is a potent, selective and orally bioavailable inhibitor of PRMT5 (protein arginine methyltransferase) with antineoplastic activity. |
|
V52935 | EPZ-719 | 2697176-16-0 | EPZ-719 is a novel and potent inhibitor of SETD2 (IC50 = 0.005 μM) with high selectivity compared to other histone methyltransferases. |
|
V0401 | EPZ004777 | 1338466-77-5 | EPZ004777 (EPZ-004777) is a potent and selective inhibitor of DOT1 Like Histone Lysine Methyltransferase (DOT1L) inhibitor with antineoplastic activity. |
|
V33044 | EPZ004777 hydrochloride | 1380316-03-9 | EPZ004777 hydrochloride, the hydrochloride salt ofEPZ-004777, is a novel and potent DOT1L inhibitor with an IC50 value of 400 pM. |
|
V0379 | EPZ005687 | 1396772-26-1 | EPZ005687 (EPZ-005687) is a novel, potent and selective inhibitor of EZH2 (a histone lysine N-methyltransferase) with anticancer activity. |
|
V20662 | EPZ011989 | 1598383-40-4 | EPZ011989 (EPZ-011989) is a potent, orally bioavailable EZH2 inhibitor with high anticancer activity. |
|
V75865 | EPZ011989 hydrochloride | 2095432-26-9 | EPZ011989 HCl is an orally bioactive EZH2 inhibitor (antagonist) with Ki <3 nM. |
|
V2940 | EPZ015866 (GSK591; GSK3203591) | 1616391-87-7 | EPZ015866 (also known as EPZ-015866; GSK-3203591; GSK-591) is an orally bioavailable and selective inhibitor ofPRMT5 (protein arginine methyltransferase 5) with potential anticancer activity. |
|
V2602 | EPZ020411 | 1700663-41-7 | EPZ020411 (EPZ-020411) is a selective PRMT6 (protein arginine methyltransferase) inhibitor with antitumor effects. |
|
V31817 | EPZ020411 hydrochloride | 2070015-25-5 | EPZ020411 (EPZ-020411) HCl, the hydrochloride salt of EPZ020411, is a novel and selective inhibitor of PRMT6 (protein arginine methyltransferase, IC50 =10 nM) with therapeutic utility in the treatment of cancer. |
|
V20667 | EPZ031686 | 1808011-22-4 | EPZ-031686 (EPZ031686) is a potent, selective andorally bioavailable SMYD3 (Set and Mynd Domain containing 3) inhibitor with potential antitumor activity. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
