- Voies de signalisation
- Epigenetics
- Histone Methyltransferase
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
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EZH1
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EZH2
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DOT1L
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SMYD2
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SMYD3
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SUV39H2/KMT1B
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EHMT2/G9a/KMT1C
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EHMT1/GLP/KMT1D
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ASH1L/KMT2H
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SETDB1/KMT2G
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SETD2/KMT3A
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NSD2/MMSET/WHSC1
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NSD3/WHSC1L1
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SETD7/KMT7
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SETD8/KMT5A
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PRMT1
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PRMT3
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PRMT4
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PRMT5
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PRMT6
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PRMT7
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PRMT8
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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 Produits associés (653)
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Anticorps (84)
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Histone Methyltransferase Isoform Comparison
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Tazemetostat
0 ImagesSynonyms: EPZ-6438; E-7438Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells. -
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- GSK126
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- Pinometostat
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GSK3326595
0 ImagesSynonyms: EPZ015938GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma. -
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Navlimetostat
0 ImagesSynonyms: MRTX-1719; BMS-986504Navlimetostat 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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EZM8266
0 ImagesEZM8266 is an orally active and selective G9a (EHMT2) histone methyltransferase inhibitor with a human EHMT2 IC50 of 1 pM. EZM8266 reduces repressive H3K9me2 marks at immune-stimulatory gene and endogenous retroviral element promoters. EZM8266 reduces colony formation, migration, and invasion of cancer cells. EZM8266 enhances IFN-γ response, increases MHC class I expression, and enhances CXCL10-mediated T cell recruitment in cancer cells. EZM8266 can be used for the research of hepatocellular carcinoma. -
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LLC0424N
0 ImagesCat. No.: HY-185557CAS No.: 3063448-59-6LLC0424N is a negative control compound designed by methylating the thalidomide moiety of LLC0424 (HY-161574). LLC0424N shows does not induce NSD2 degradation and inhibit growth of acute lymphoblastic leukemia cells with NSD2 mutation. LLC0424N can be used for the research of acute lymphoblastic leukemia. -
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WX2-43
0 ImagesWX2-43 is a PRMT5-KLF4 inhibitor (Kd of 11.0 nM). WX2-43 binds to the region between amino acids L400-M500 on PRMT5. WX2-43 efficiently intercepts the interaction between KLF4 and PRMT5, and blocks KLF4 methylation. WX2-43 decreases p21 levels and increases Bax levels. WX2-43 suppresses triple negative breast tumor progression. WX2-43 can be used in the research of triple-negative breast cancer and colorectal cancer. -
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- GSK343
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EZM0414 TFA
0 ImagesCat. No.: HY-136328CAS No.: 2411759-92-5Synonyms: SETD2-IN-1 TFAEZM0414 (SETD2-IN-1) TFA is the TFA salt form of EZM0414 (HY-144858). EZM0414 TFA is a potent, selective, orally active inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 TFA can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma. -
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- 3-Deazaneplanocin A
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Valemetostat
0 ImagesSynonyms: DS-3201Valemetostat (DS-3201), a first-in-class EZH1/2 dual inhibitor with IC50 values <10 nM. Valemetostat can be used for the research of relapsed/refractory peripheral T-cell lymphoma. -
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BIX-01294
0 ImagesBIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells. -
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UNC0642
0 ImagesUNC0642, a chemical probe, is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC50 of <2.5 nM for G9a. -
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- AMG-193
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Chaetocin
0 ImagesChaetocin is a specific inhibitor of the histone methyltransferase (HMT) SU(VAR)3-9 with an IC50 of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 μM. -
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3-Deazaneplanocin A hydrochloride
0 ImagesSynonyms: DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities. -
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EED226
0 ImagesEED226 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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- MS023
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EPZ004777
0 ImagesEPZ004777 is an effective and selective DOT1L inhibitor, with IC50 being 0.4 nM. EPZ004777 reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 can be used for the study of leukemia. -
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Sorry. There is currently no product that acts on isoform Bcl-2, Bcl-W and Bim together.Please
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