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Histone Methyltransferase Histone methyltransferase

Cat.No.  Name Information
M2358 3-Deazaneplanocin A 3-deazaneplanocin A (DZNeP), an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.
M9150 MI-463 MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the Menin-MLL interaction, with an IC50 value of 15.3 nM.
M9145 MI-2 MI-2 (Menin-MLL Inhibitor 2) is a potent menin-MLL interaction inhibitor with IC50 of 446±28 nM.
M9004 WDR5-0103 WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 µM).
M8989 BIX-01294 BIX-01294 is a potent chemical inhibitor of G9a methyltransferase that catalyzes the mono-and di-methylation of the lysine 9 residue of histone H3, with IC50 of 1.9 μM.
M8933 EPZ011989 EPZ011989 is a potent, orally-available EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646.
M8529 A-366 A-366 is a potent and highly selective peptide-competitive inhibitor of histone methyltransferase G9a, with IC50s of 3.3 nM and 38 nM for G9a and GLP, respectively, and is more than 1,000-fold selective for G9a and GLP over 21 other methyltransferases. A-366 is also a potent inhibitor of Spindlin1-H3K4me3 interaction (IC50=182.6 nM).A-366 shows high affinity for human H3R (Ki=17 nM) and exhibits subtype selectivity between subpopulations of the histaminergic and dopaminergic receptor families. It can be used for induction and maintenance of pluripotent stem cells in mice.
M8475 OICR-9429 OICR-9429 is a cell penetrant, potent and selective antagonist of the interaction of WDR5 (WD repeat domain 5) with peptide regions of MLL and Histone 3 that potently binds to WDR5.
M8397 BRD4770 BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 inhibited the dimethylation and trimethylation of H3K9, EC50 was 5 µM, and had little effect on H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 activates the ataxic telangiectasia mutation (ATM) pathway and induces cell senescence.
M8196 Sinefungin Sinefungin blocks the methylation of bases in DNA and RNA, such as 5-methylcytosine or N6-methyladenosine, suggesting a role in gene expression.
M7578 SGC0946 SGC0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM; selectively kill mixed lineage leukaemia cells.
M7509 UNC0642 UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels.
M7508 JQ-EZ-05 JQ-EZ-05 is a specific and reversible EZH1/2 inhibitor.
M6592 Chaetocin Chaetocin 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.
M6362 A 196 A-196 is a potent selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively, and biochemically inhibits SUV4-20 in a substrate-competitive manner. In addition, A-196 is a first-in-class chemical probe for SUV4-20, which can be used to study the role of histone methyltransferases in genome integrity.
M6336 3-Deazaneplanocin A hydrochloride 3-Deazaneplanocin A hydrochloride(DZNep HCl) is a eZH2 histone methyltransferase inhibitor.
M6288 LLY-507 LLY-507 is a cell-active, potent, and selective inhibitor of protein-lysine Methyltransferase SMYD2.
M5412 Amodiaquin dihydrochloride dihydrate Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase in human erythrocytes, also used as an antimalarial and anti-inflammatory agent.
M5186 CPI-360 Cpi-360 is an effective selective EZH2 inhibitor with IC50 of 0.5 nM and 2.5 nM for WT EZH2 and Y641N EZH2, respectively.
M5128 PFI-2 PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.
M4813 UNC0379 UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8 with IC50 of 7.3±1.0 uM.




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