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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A-395 (Standard)
0 ImagesCat. No.: HY-101512RCAS No.: 2089148-72-9A-395 (Standard) is the analytical standard of A-395 (HY-101512). This product is intended for research and analytical applications. A-395, a chemical probe, is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM.
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(1-Nitroethene-1,2-diyl)dibenzene
0 ImagesSynonyms: alpha-Nitrostilbene; α-Nitrostilbene; NSC 385(1-Nitroethene-1,2-diyl)dibenzene (alpha-Nitrostilbene; α-Nitrostilbene) is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC50=11 μM in histone H4 methylation assay). It also inhibits histone H4 methylation by PRMT8, but not histone H3.1 methylation by CARM1 or Set7/9, at concentrations of 10 and 100 μM.
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EPZ030456
0 ImagesCat. No.: HY-122223CAS No.: 1808011-23-5
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Navlimetostat (Standard)
0 ImagesCat. No.: HY-139611RCAS No.: 2630904-45-7Synonyms: MRTX-1719 (Standard); BMS-986504 (Standard)Navlimetostat (Standard) is the analytical standard of Navlimetostat (HY-139611). This product is intended for research and analytical applications. Navlimetostat is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat binds to the PRMT5-MTA complex, with Kd value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study.
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EZM 2302 (Standard)
0 ImagesCat. No.: HY-111109RCAS No.: 1628830-21-6EZM 2302 (Standard) is the analytical standard of EZM 2302 (HY-111109). This product is intended for research and analytical applications. EZM 2302 is a potent and orally active CARM1 inhibitor with an IC50 value of 6 nM. EZM 2302 shows antiproliferative activity and anti-tumor activity. EZM 2302 inhibits PABP1 and SMB expression.
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MC3629
0 ImagesCat. No.: HY-164500CAS No.: 1375163-30-6MC3629 is an inhibitor of histone methyltransferase (EZH2) with anti-tumor activity. MC3629 inhibits SHH MB cancer cell proliferation and self-renewal and induces apoptosis. MC3629 can be used to study drug resistance in tumor aggressiveness.
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Amodiaquine dihydrochloride (Standard)
0 ImagesSynonyms: Amodiaquin dihydrochloride (Standard)Amodiaquine (dihydrochloride) (Standard) is the analytical standard of Amodiaquine (dihydrochloride). This product is intended for research and analytical applications. Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
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4-Methoxycinnamyl alcohol
0 ImagesCat. No.: HY-168164CAS No.: 53484-50-74-Methoxycinnamyl alcohol is an anticancer compound with cytotoxic activity against MCF-7, HeLa, and DU145 cancer cell lines with IC50 values of 14.24, 7.82, and 22.10 μg/mL, respectively. 4-Methoxycinnamyl alcohol showed the ability to induce cell necrosis, rather than apoptosis, after a 48-hour DNA fragmentation assay. 4-Methoxycinnamyl alcohol was isolated from Foeniculum vulgare.
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MAK683 (Standard)
0 ImagesMAK683 (Standard) is the analytical standard of MAK683 (HY-103663). This product is intended for research and analytical applications. MAK683 is an embryonic ectoderm development (EED) inhibitor extracted from patent US20160176882 A1, compound example 2. MAK683 exhibits IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay.
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(R)-BAY-598
0 ImagesCat. No.: HY-19546ACAS No.: 1906920-28-2(R)-BAY-598 ((R)-4) is a potent inhibitor of protein-lysine methyltransferase SMYD2, with the IC50 of 1.7 μM.
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3-Deazaneplanocin A (Standard)
0 ImagesCat. No.: HY-10442RCAS No.: 102052-95-9Synonyms: DZNep (Standard); 3-Deazaneplanocin (Standard)3-Deazaneplanocin A (Standard) is the analytical standard of 3-Deazaneplanocin A (HY-10442). This product is intended for research and analytical applications. 3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity.
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Metoprine (Standard)
0 ImagesSynonyms: BW 197U (Standard)Metoprine (Standard) is the analytical standard of Metoprine. This product is intended for research and analytical applications. Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT. Metoprine is an antifolate and antitumor agent.
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UNC0642 (Standard)
0 ImagesUNC0642 (Standard) is the analytical standard of UNC0642. This product is intended for research and analytical applications. UNC0642 is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC50 of <2.5 nM for G9a.
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DC-S100
0 ImagesCat. No.: HY-125105CAS No.: 178803-91-3DC-S100 is a potent SET7 inhibitor with an IC50 of 30.04 μM. DC-S100 binds to the cofactor (SAM) binding site of SET7 and forms hydrogen bonds and hydrophobic interactions with residues at this site. DC-S100 is applicable to biological studies of epigenetics and related diseases.
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Onametostat (Standard)
0 ImagesCat. No.: HY-101564RCAS No.: 2086772-26-9Synonyms: JNJ-64619178 (Standard)Onametostat (Standard) is the analytical standard of Onametostat (HY-101564). This product is intended for research and analytical applications. Onametostat (JNJ-64619178) is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. Onametostat has potent activity in lung cancer.
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GSK126 (Standard)
0 ImagesCat. No.: HY-13470RCAS No.: 1346574-57-9Synonyms: GSK2816126A (Standard)
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Furamidine dihydrochloride (Standard)
0 ImagesCat. No.: HY-110137RCAS No.: 55368-40-6Synonyms: DB75 dihydrochloride (Standard); NSC 305831 dihydrochloride (Standard)Furamidine (dihydrochloride) (Standard) is the analytical standard of Furamidine (dihydrochloride). This product is intended for research and analytical applications. Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent.
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LLY-284 (Standard)
0 ImagesCat. No.: HY-107777ARCAS No.: 2226515-75-7LLY-284 (Standard) is the analytical standard of LLY-284 (HY-107777A). This product is intended for research and analytical applications. LLY-284 is the diastereomer of LLY-283 with much less active. LLY-283 is a potent inhibitor of PRMT5. LLY-284 has the potential for the research of cancer diseases.
