Histone Methyltransferase
Histone modifications play critical roles in regulating both global and stage-specific gene expression. Methylation on histones H3K4, H3K36 and H3K79 is generally associated with gene activation, whereas methylation on histones H3K9 and H3K27 is generally associated with gene repression. Histone lysine methylation is dynamically regulated by site-specific methyltransferases and demethylases. EZH2 (the catalytic subunit of PRC2) is responsible for the methylation of H3K27 in cells.
DOT1L is a histone H3 lysine 79 methyltransferase whose inhibition increases the yield of induced pluripotent stem cells (iPSCs). EPZ-5676 is a potent and selective DOT1L inhibitor.
Crucial to PRC2 activity, the histone methyltransferase enhancer of zeste homolog 2 (EZH2) tri-methylates lysine 27 of histone 3 (H3K27me3), leading to chromatin condensation and transcriptional repression.
Histone Methyltransferase Isoform Specific Products
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Histone Methyltransferase
(369)
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EZH1
(11)
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EZH2
(85)
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DOT1L
(21)
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SMYD2
(9)
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SMYD3
(9)
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SUV39H2/
KMT1B (4)View all products
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EHMT2/
G9a/ (32)KMT1C View all products
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EHMT1/
GLP/ (20)KMT1D View all products
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ASH1L/
KMT2H (4)View all products
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SETDB1/
KMT2G (4)View all products
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SETD2/
KMT3A (5)View all products
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NSD2/
MMSET/ (16)WHSC1 View all products
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NSD3/
WHSC1L1 (4)View all products
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SETD7/
KMT7 (6)View all products
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SETD8/
KMT5A (5)View all products
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PRMT1
(24)
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PRMT3
(17)
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PRMT4
(19)
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PRMT5
(63)
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PRMT6
(23)
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PRMT7
(8)
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PRMT8
(13)
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All Product Categories
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Histone Methyltransferase Inhibitors
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Histone Methyltransferase Agonists
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Histone Methyltransferase Antagonists
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Histone Methyltransferase Activators
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Histone Methyltransferase Modulators
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Histone Methyltransferase Chemical
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Histone Methyltransferase Inducers
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Histone Methyltransferase Degraders
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Histone Methyltransferase Controls
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Histone Methyltransferase Ligands
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Histone Methyltransferase Related Products (686)
Related Products (686)
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Antibodies (84)
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Histone Methyltransferase Isoform Comparison
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AMI-1 (Standard)
0 ImagesCat. No.: HY-18962RCAS No.: 20324-87-2AMI-1 (Standard) is the analytical standard of AMI-1. This product is intended for research and analytical applications. AMI-1 is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
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Piribedil maleate
0 ImagesCat. No.: HY-12707BCAS No.: 937719-94-3Piribedil maleate is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil maleate is also a α2-adrenoceptors antagonist. Piribedil maleate can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil maleate has the potential for the research of parkinson's disease, circulatory disorders, cancers.
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MRK-740-NC
0 ImagesCat. No.: HY-176820CAS No.: 2421146-31-6
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CM-272 (Standard)
0 ImagesCat. No.: HY-101925RCAS No.: 1846570-31-7CM-272 (Standard) is the analytical standard of CM-272 (HY-101925). This product is intended for research and analytical applications. CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death.
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EBI-2511 (Standard)
0 ImagesCat. No.: HY-111418RCAS No.: 2098546-05-3EBI-2511 (Standard) is the analytical standard of EBI-2511 (HY-111418). This product is intended for research and analytical applications. EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively.
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EED226 (Standard)
0 ImagesEED226 (Standard) is the analytical standard of EED226 (HY-101117). This product is intended for research and analytical applications. EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model. EED226 is a potent, selective, and orally bioavailable EED inhibitor. EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays.
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GSK343 (Standard)
0 ImagesCat. No.: HY-13500RCAS No.: 1346704-33-3GSK343 (Standard) is the analytical standard of GSK343. This product is intended for research and analytical applications. GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
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UNC0321 (Standard)
0 ImagesCat. No.: HY-10930RCAS No.: 1238673-32-9UNC0321 (Standard) is the analytical standard of UNC0321 (HY-10930). This product is intended for research and analytical applications. UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 has anti-apoptotic activity and has potential application in diabetic vascular complications.
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CPI-905
0 ImagesCat. No.: HY-111085CAS No.: 931078-17-0CPI-905 is a potent, selective, and cell-active EZH2 inhibitor.
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Valemetostat tosylate (Standard)
0 ImagesCat. No.: HY-109108ARCAS No.: 1809336-93-3Synonyms: DS-3201 tosylate (Standard)Valemetostat tosylate (Standard) is the analytical standard of Valemetostat (tosylate) (HY-109108A). This product is intended for research and analytical applications. Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma.
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HLCL-61 hydrochloride (Standard)
0 ImagesCat. No.: HY-100025ARCAS No.: 1158279-20-9HLCL-61 (hydrochloride) (Standard) is the analytical standard of HLCL-61 (hydrochloride) (HY-100025A). This product is intended for research and analytical applications. HLCL-61 hydrochloride is a first-in-class inhibitor of protein arginine methyltransferase 5 (PRMT5).
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GSK926
0 ImagesCat. No.: HY-116605CAS No.: 1346704-13-9
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SKI-73
0 ImagesCat. No.: HY-114206CAS No.: 2206744-61-6
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GSK591 hydrochloride
0 ImagesCat. No.: HY-100235ACAS No.: 2320953-89-5Synonyms: EPZ015866 hydrochloride; GSK3203591 hydrochlorideGSK591 (EPZ015866) hydrochloride is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM.
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MS049 (Standard)
0 ImagesCat. No.: HY-100360RCAS No.: 1502816-23-0MS049 (Standard) is the analytical standard of MS049 (HY-100360). This product is intended for research and analytical applications. MS049, a chemical probe, is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells.
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DCE_42
0 ImagesCat. No.: HY-122115CAS No.: 669749-45-5DCE_42 is a potent EZH2 inhibitor with an IC50 value of 22.6 µM. DCE_42 inhibits cell proliferation and has the potential for the research of lymphoma.
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BI-9466
0 ImagesCat. No.: HY-142048CAS No.: 2538293-52-4BI-9466 (Compound 2) is a nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd of 144 µM. BI-9466 is a negative control compound of BI-9321 (HY-114208). BI-9466 has no inhibitory activity against NSD3-PWWP1 domain by introduction of a much basic nitrogen heterocycle at the 5-position of BI-9321.
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Fagaronine chloride
0 ImagesCat. No.: HY-122532CAS No.: 52259-64-0Fagaronine chloride is an alkaloid with inhibitory activity against reverse transcriptase and topoisomerase I. Fagaronine chloride can effectively inhibit the reverse transcriptase of RSii tumor virus at a concentration of 6-60 μg/mL. Fagaronine chloride rapidly blocks the synthesis of DNA polymerase by interacting with the template primer. Fagaronine chloride has shown anti-tumor potential, especially in the study of retroviral infection.
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Piribedil (Standard)
0 ImagesPiribedil (Standard) is the analytical standard of Piribedil. This product is intended for research and analytical applications. Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a α2-adrenoceptors antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers.
