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Histone Methyltransferase

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Catalog No. Product Name Application Product Information
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.


Hmt1p/PRMT1 Inhibitor
AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 uM and 8.8 uM for yeast Hmt1p and human PRMT1, 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.
A14374 SALE


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


EZH2 Inhibitor
GSK-503 is a potent EZH2 inhibitor with potential anticancer activity.
A12585 SALE


PRMT1 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.


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
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.
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.

MI-2 (Menin-MLL inhibitor 2)

Menin-MLL interaction inhibitor
MI-2 (Menin-MLL inhibitor 2) specifically binds to Menin and inhibits Menin??s interaction with MLL fusion proteins in cells. It can effectively reverse MLL fusion protein?Cmediated leukemic transformation by downregulating the expression of target genes downstream of MLL fusion protein oncogenic activity. MI-2 is a new tool for better understanding MLL-mediated leukemogenesis and represents a new approach for studying the role of Menin as an oncogenic cofactor of MLL fusion proteins.
A15450 SALE

SGC 707

PRMT3 Inhibitor
SGC 707 is a potent allosteric inhibitor of PRMT3 (IC50 = 50 nM) with >100-fold selectivity over other methyltransferases and other non-epigenetic targets.
A15813 SALE


SMYD2 inhibitor
LLY-507 is a cell-active, small molecule inhibitor of SMYD2 with IC50 of= 15 nM.


PRMT3 inhibitor
XY1 is a negative control of SGC 707 . SGC 707 (Adooq Catalog# A15450) is a potent, selective allosteric inhibitor of PRMT3 (IC50 = 50 nM).


WDR5 antagonist
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 M).


PRMT5 Inhibitor
HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.

TC-E 5003

PRMT1 inhibitor
TC-E 5003 is a selective inhibitor of PRMT1 with IC50 value of 1.5 uM .


PRMT6 inhibitor
EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has >10 fold selectivity for PRMT6 over PRMT1 and PRMT8.


SMYD3/ MEKK2 inhibitor
EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively.


EZH2 inhibitor
CPI-1205 is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2.

AZ505 ditrifluoroacetate

SMYD2 inhibitor
AZ505 ditrifluoroacetate is a potent and highly selective inhibitor of the oncogenic protein SMYD2(IC50=0.12 uM) with potential anticancer activity, >600 fold than SMYD3(IC50>83.3 uM); DOT1L(IC50>83.3 uM);EZH2(IC50>83.3 uM).


SMYD2 inhibitor
AZ505 is a potent and highly selective inhibitor of the oncogenic protein SMYD2(IC50=0.12 μM) with potential anticancer activity, >600 fold than SMYD3(IC50>83.3 μM); DOT1L(IC50>83.3 μM);EZH2(IC50>83.3 μM).


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.

UNC 2400

EZH1/EZH2 inhibitor
UNC 2400, a close analogue of UNC1999, is a negative control of UNC1999 that inhibits EZH2 and EZH1.


CBX4 /CBX7 chromodomains antagonist
UNC3866 is a potent antagonist of CBX4 and CBX7 chromodomains with a Kd of ~100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains.
A15969 SALE


G9a/GLP inhibitor
A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 value of 3.3 nM.
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.
A15487 SALE


G9a/GLP inhibitor
UNC0642 is a potent and selective G9a and GLP histone lysine methyltransferase inhibitor (IC50 < 2.5 nM). It reduces H3K9 dimethylation levels in MDA-MB-231 cells (IC50 = 110 nM). Displays modest brain penetration in vivo.
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.


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

Opicapone (BIA 9-1067)

COMT inhibitor
opicapone is a novel catechol-O-methyltransferase inhibitor
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).


G9a inhibitor
UNC-0631 is a novel G9a inhibitor with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity.
A13194 SALE


G9a/GLP 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).


SUV39H 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.
A12735 SALE

EPZ-5676 (Pinometostat)

DOT1L Inhibitor‎
EPZ-5676 is a small molecule inhibitor of histone methyltransferase with potential antineoplastic activity.
A11763 SALE

BIX 01294

G9a/GLP HMT inhibitor
BIX 01294 is a G9a-like protein and G9a histone lysine methyltransferase inhibitor.


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.
A12941 SALE

SGC 0946

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


MLL1 inhibitor
MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 uM.

UNC 0224

G9a inhibitor
UNC0224 is a potent and selective G9a inhibitor with IC50 of 15 nM in in the G9a Thioglo assay.


G9a inhibitor
BRD4770 is a novel histone methyltransferase inhibitor.

3-deazaneplanocin A HCl (DZNep HCl)

EZH2 inhibitor
3-deazaneplanocin A, also known as DZNep, is a well-known histone methyltransferase inhibitor, which disrupts polycomb-repressive complex 2 (PRC2), and induces apoptosis, while inhibiting proliferation and metastasis, in cancer cells, including acute myeloid leukemia, breast cancer and glioblastoma.
A14320 SALE


SETD8 HMTase inhibitor
UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. Its affinity to SETD8 was confirmed by ITC (isothermal titration calorimetry) and SPR (surface plasmon resonance) studies.
A14216 SALE


SETD7 inhibitor
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.


menin-MLL interaction inhibitor
MI-3 is a potent menin-MLL interaction inhibitor with IC50 of 648 nM.
A13690 SALE

UNC 0638

G9a/GLP inhibitor
UNC 0638 is a selective inhibitor of G9a and GLP histone lysine methyltransferases.


PRMT1 inhibitor
C7280948 is an inhibitor of histone arginine methyltransferase PRMT1 with IC50 values of 12.75 uM.


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

Amodiaquine 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.

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