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 |
---|---|---|---|---|
V0384 | 3-deazaneplanocin A (DZNeP; NSC 617989) HCl | 120964-45-6 | 3-deazaneplanocin A HCl (known also asDZNep; C-c3Ado; NSC-617989), the hydrochloride salt of 3-deazaneplanocin A which is an adenosineanalog, is a novel and competitive inhibitor of S-adenosylhomocysteine hydrolase and also an EZH2(histone methyltransferase) inhibitor with anticancer activity. | |
V2032 | 5WKS | 1350752-07-6 | G9a-IN-1 (Compound 113) is a G9a protein inhibitor. | |
V3067 | A-196 | 1982372-88-2 | A-196 (A196) is a potent, selective and first-in-class inhibitor of SUV420H1 and SUV420H2 (IC50= 25 and 144 nM) with anticancer activity. | |
V9842 | A-366 | 1527503-11-2 | A-366 (A366) is a novel, potent and peptide-competitive inhibitor of thehistone methyltransferase G9a with anticancer activity. | |
V0388 | AMI-1 disodium salt | 20324-87-2 | AMI-1 (AMI 1) disodium saltis a novel, cell-permeable and selective inhibitor of Histone Methyltransferase (HMT) with anti-inflammatory activity. | |
V6409 | Amodiaquin HCl hydrate | 6398-98-7 | Amodiaquin dihydrochloride(trade names Camoquin, Flavoquine)isa potent and orally bioactive inhibitor of the Ebola virus, acts by targeting the viral protein 35 (VP35). | |
V56266 | Amodiaquine-d10 | 1189449-70-4 | Amodiaquine-d10 is the deuterium labelled form of Amodiaquine. | |
V78961 | Anticancer agent 126 | Anticancer agent 126 (compound 12) is a WDR5 inhibitor (antagonist) with anticancer effects. | ||
V79864 | Antiproliferative agent-25 | antiproliferation agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50= 0.11 μM). | ||
V34821 | Antitumor agent-101 | 2848632-52-8 | Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferase G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. | |
V52392 | AS-85 | 2323623-80-7 | AS-85 is a potent ASH1L inhibitor (IC50=0.6 µM) with anti-leukemia activity. | |
V78137 | AS-99 | AS-99 is a first-in-class, potent and specific ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) and has anti-leukemia activity. | ||
V77240 | AS-99 TFA | AS-99 TFA is a first-in-class, potent and specific ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemia activity. | ||
V12013 | AZ-505 2TFA salt | 1035227-44-1 | AZ-505(AZ505) 2TFA, the ditrifluoroacetate salt ofAZ-505, is an SMYD2 (SET and MYND domain-containing protein 2)inhibitor with anticancer activity. | |
V52369 | AZ506 | 2043321-54-4 | AZ506 is a potent SMYD2 inhibitor (antagonist) with IC50 of 17 nM. | |
V4167 | BAY-598 | 1906919-67-2 | BAY-598 (BAY598 S-isomer) is novel, potent, selective and peptide-competitive small molecule inhibitor of lysine methyltransferaseSMYD2 with potential antitumor activity. | |
V52360 | BBDDL2059 | 2691174-27-1 | BBDDL2059 is a selective covalent inhibitor of the histone methyltransferase EZH2 with IC50 of 1.5 nM for EZH2-Y641F. | |
V6240 | BCI-121 | 432529-82-3 | BCI-121 is a SMYD3 inhibitor that can suppress cancer/tumor cell growth/proliferation. | |
V0381 | BIX 01294 | 935693-62-2 | BIX01294 is a novel and potent inhibitor of G9a histone methyltransferase with anticancer activity. | |
V3451 | BIX01294 triHCl | 1392399-03-9 | BIX01294 triHCl (the tri-hydrochloride salt of BIX01294) is a novel and potent inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay. |