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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V20662 | EPZ011989 | 1598383-40-4 | EPZ011989 (EPZ-011989) is a potent, orally bioavailable EZH2 inhibitor with high anticancer activity. |
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V75865 | EPZ011989 hydrochloride | 2095432-26-9 | EPZ011989 HCl is an orally bioactive EZH2 inhibitor (antagonist) with Ki <3 nM. |
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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. |
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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. |
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V2602 | EPZ020411 | 1700663-41-7 | EPZ020411 (EPZ-020411) is a selective PRMT6 (protein arginine methyltransferase) inhibitor with antitumor effects. |
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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. |
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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. |
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V75873 | EPZ031686 | 2095161-11-6 | EPZ031686 is a potent orally bioactive SMYD3 inhibitor (antagonist) with IC50 of 3 nM. |
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V52104 | EZH2-IN-14 | 1979157-17-9 | EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor (antagonist) with IC50 of 12 nM. |
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V56082 | EZH2-IN-15 | 2098545-98-1 | EZH2-IN-15 (SHR2554) is an EZH2 inhibitor. |
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V75869 | EZH2-IN-17 | 2489672-09-3 | EZH2-IN-17 (compound 28) is a potent orally bioactive EZH2 inhibitor (antagonist) with IC50 of 0.95 nM. |
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V52103 | EZH2-IN-4 | 2088132-99-2 | EZH2-IN-4 is an orally bioactive EZH2 inhibitor (antagonist) with IC50 of 0.923 nM and 2.65 nM for wild-type and mutant 5-mer EZH2, respectively. |
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V52102 | EZH2-IN-5 | 1403258-69-4 | EZH2-IN-5 is a potent EZH2 inhibitor (antagonist) with IC50s of 1.52 nM and 4.07 nM for wild-type and mutant Tyr641 EZH2, respectively. |
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V53080 | EZM0414 TFA (SETD2-IN-1 TFA) | 2411759-92-5 | EZM0414 TFA is a specific and orally bioactive inhibitor of the human histone methyltransferase SETD2. |
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V20887 | EZM2302 (GSK-3359088) | 1628830-21-6 | EZM 2302 is a coactivator-related arginine methyltransferase 1 (CARM1) preparation with IC50 of 6 nM. |
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V0391 | GSK126 (GSK2816126; GSK 2816126A) | 1346574-57-9 | GSK126 (GSK-2816126; GSK-2816126A) is a selective and SAM (S-adenosyl-methionine)-competitive inhibitor of EZH2 (Enhancer of zeste homolog 2) methyltransferase with anticancer activity. |
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V3142 | GSK3326595 (EPZ-015938) | 1616392-22-3 | GSK3326595 (EPZ015938) is a novel, potent,orally bioactive,and selective inhibitor ofprotein arginine methyltransferase 5 (PRMT5). |
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V32454 | GSK3368715 | 1629013-22-4 | GSK3368715 (GSK-3368715; EPZ-019997; EPZ019997) is a novel, orally bioactive, and reversible inhibitor of type I PRMTs (protein arginine methyltransferases) with potential antitumor activity. |
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V32456 | GSK3368715 dihydrochloride | 1628925-77-8 | GSK3368715 dihydrochloride (GSK-3368715; EPZ-019997;EPZ019997), the dihydrochloride salt of GSK3368715, is a potent and orally bioavailable inhibitor oftype I PRMTs (protein arginine methyltransferases)with potential anticancer activity. |
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V21306 | GSK3368715 trihydrochloride (EPZ019997 trihydrochloride) | 2227587-26-8 | GSK3368715 tri HCl (EPZ019997) is an orally bioactive, reversible, noncompetitive SAM type I protein arginine methyltransferase (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). |
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