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 |
|---|---|---|---|---|
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V51747 | DDO-2093 | 2250024-74-7 | DDO-2093 is a potent activator of MLL1 and WDR5 protein-protein reactions (IC50=8.6 nM; Kd=11.6 nM) with anti-tumor activity. |
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V77097 | DDO-2093 dihydrochloride | DDO-2093 di-HCl is a potent inhibitor of MLL1 and WDR5 protein-protein interaction (IC50=8.6 nM; Kd=11.6 nM) with anti-tumor activity. | |
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V25158 | DM-01 | 2355280-00-9 | DM-01 is a potent and specific EZH2 inhibitor that may be utilized in the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL) and SNF5/INI-1/SMARCB1 gene-related solid tumors. |
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V77073 | Dot1L-IN-1 TFA | Dot1L-IN-1 TFA is a highly efficient and selective Dot1L inhibitor (antagonist) with Ki of 2 pM and IC50<0.1 nM. | |
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V2483 | Dot1L-IN-4 | 2565705-02-2 | Dot1L-IN-4 is a potent DOT1L (telomere silencing disruptor-like 1) inhibitor (antagonist) with IC50 SPA DOT1L of 0.11 nM. |
|
V75871 | Dot1L-IN-5 | 2565705-03-3 | Dot1L-IN-5 is a potent DOT1L (telomere silencing disruptor-like 1) inhibitor (antagonist) with IC50 of 0.17 nM. |
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V75866 | Dot1L-IN-6 | 2565705-01-1 | Dot1L-IN-6 is a potent DOT1L (telomere silencing disruptor-like 1) inhibitor (antagonist) with IC50 SPA DOT1L of 0.19 nM. |
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V20268 | DS-437 | 1674364-87-4 | DS-437 (DS437) is a novel and potent dual PRMT5 and PRMT7 inhibitor with anticancer activity. |
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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. |
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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. |
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V56084 | EEDligand 1 | 2762275-20-5 | EED ligand 1 is a versatile and potent inhibitor that targets the EED subunit of the methyltransferase PRC2. |
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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. |
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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. |
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V78566 | EML734 | EML734 is a potent and specific PRMT7/9 inhibitor (antagonist) with IC50s of 315 nM and 0.89 μM respectively. | |
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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. |
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V0402 | Entacapone (OR611) | 130929-57-6 | Entacapone (OR-611) is an approved anti-PD/Parkinsons Diseasemedication acting as a specific and peripherally active catechol-O-methyltransferase (COMT) inhibitor (IC50 = 151 nM). |
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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. |
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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. |
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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. |
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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. |
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