Histone Methyltransferase

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Catalog No. Product Name Application Product Information


PRMTs Inhibitor
AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 ??M and 8.8 ??M for yeast Hmt1p and human PRMT1, respectively.


HMT Inhibitor
Chaetocin is a histone methyltransferase SUV39H1 inhibitor (IC50 = 0.8 μM). Induces apoptosis in myeloma cell lines in vitro; exhibits antiproliferative activity in a mouse myeloma model in vivo.


EZH2 inhibitor
CPI-1205 is a highly potent (biochemical IC50 = 0.002 ??M, cellular EC50 = 0.032 uM) and selective inhibitor of EZH2.
A15920 SALE


EZH2 inhibitor
CPI-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.


EZH1 inhibitor
CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.


EZH2 Inhibitor
3 Deazaneplanocin A (DZNep) is a cyclopentenyl analog of 3-deazaadenosine, originally synthesized as an inhibitor of S-adenosyl-L-homocysteine hydrolase.


EZH2 inhibitor
EI1 is a potent and selective small molecule inhibitor of EZH2 with IC50 values of 15 nM and 13 nM for wild type EZH2 and EZH2 Y641F mutant, respectively.
A12735 SALE


DOT1L Inhibitor‎
EPZ-5676 is a small molecule inhibitor of histone methyltransferase with potential antineoplastic activity.
A12712 SALE

EPZ-6438 (Tazemetostat)

EZH2 inhibitor
EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. It induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells.


DOT1L inhibitor
EPZ004777 is a potent, selective inhibitor of DOT1L. EPZ004777 selectively inhibits cellular H3K79 methylation and inhibits expression of key MLL fusion target genes.


EZH2 inhibitor
EPZ005687 is a potent inhibitor of EZH2 (K(i) of 24 nM)


EZH2 Inhibitor
EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.
A11757 SALE


EZH2 inhibitor
GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes.
A13114 SALE


EZH2 inhibitor
GSK343 is a potent histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor (IC= 4 nM). Diplays 1000-fold selectivity for other HMTs except EZH1 (60-fold selectivity). GSK343 inhibits H3K27 methylation in HCC1806 cells with an IC of <200nM (measured by immunofluorescence).


EZH2 Inhibitor
GSK-503 is a potent EZH2 inhibitor with potential anticancer activity.
A14374 SALE


PRMT5 inhibitor
GSK591 is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 11 nM.
A12585 SALE


type I PRMT inhibitor
MS023 is a potent inihbitor of PRMTs 1,3,4,6,and 8 (IC50 = 30, 119, 83, 8, and 8 nM, respectively), which are responsible for asymmetric dimethylation of arginine residues.
A12941 SALE

SGC 0946

DOT1L inhibitor
SGC 0946 is a potent DOT1L methyltransferase inhibitor that blocks H3K79 methylation in A431 cells and MCF10A cells.
A13690 SALE

UNC 0638

HMT inhibitor
UNC 0638 is a selective inhibitor of G9a and GLP histone lysine methyltransferases.
A13166 SALE


Ezh2/Ezh1 Inhibitor
UNC1999 is the first orally bioavailable inhibitor that has high in vitro potency for wildtype and mutant EZH2 as well as EZH1.


G9a HMTase inhibitor
UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date
A12947 SALE


G9a/GLP HMTase inhibitor
UNC0638 is an inhibitor of protein lysine methyltransferases G9a(IC50<15 nM) and GLP(IC50=19 nM) with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets.
A13194 SALE


G9a HMTase inhibitor
UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50 values are 6 nM and 15 nM for G9a and GLP, respectively).

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