Catalog No.
Product Name
Application
Product Information
Citations
-
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.- Tianzhi Huang, .et al. , Mol Cell, 2021, Mar 18;81(6):1276-1291 PMID: 33539787
- Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase in human erythrocytes, also used as an antimalarial and anti-inflammatory agent.
-
PRMT5 inhibitor
PF-06855800 (PF06855800) is a potent, selective, SAM competitive, BBB-penetrant, orally active inhibitor of protein arginine methyltransferase PRMT5 with Ki of 0.02 nM. -
Histone Methyltransferase inhibitor
JNJ-64619178 is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties. -
PRMT5 inhibitor
GSK3326595 is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 6.2 nM. -
EZH2 inhibitor
PF-06726304 is a potent and SAM-competitive EZH2 (Enhancer of Zeste Homolog 2) lysine methyltransferase inhibitor. -
SMYD3 inhibitor
SMYD3-IN-1 (compound 29) is an irreversible and selective inhibitor of SMYD3 (SET and MYND domain containing 3), with an IC50 of 11.7 nM. -
SUV39H2 inhibitor
OTS186935 is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM.- Jennings Luu, .et al. , Hum Mol Genet, 2020, Jul 21;ddaa158 PMID: 32691052
-
PRMT inhibitor
GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). -
virion mRNA(guanine-7-)-methyltransferase inhibitor
Sinefungin is a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication. -
EHMT inhibitor
EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disease or cancer. -
SMYD2 inhibitor
SMYD2-IN-1 is a SMYD2 inhibitor extracted from patent WO2016166186A1, compound example 1.1, has an IC50 of 4.45 nM. -
EHMT inhibitor
EHMT2-IN-1 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disorder or cancer. -
Dot1L inhibitor
Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively. -
EZH1/2 dual inhibitor
Valemetostat (DS-3201) is a first-in-class EZH1/2 dual inhibitor, used in the research of relapsed/refractory peripheral T-cell lymphoma. -
EZH2 inhibitor
PF-06821497 (compound 23a) is a potent, selective and orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition. -
EZH1/2 dual inhibitor
Valemetostat tosylate (DS-3201 tosylate) is a first-in-class EZH1/2 dual inhibitor, used in the research of relapsed/refractory peripheral T-cell lymphoma. -
SMYD3 inhibitor
GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM and an IC50 of 130 nM. -
PRMT inhibitor
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). -
EZH2 inhibitor
Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective and orally available EZH2 inhibitor. -
DOT1L inhibitor
EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM. -
PRMT6 inhibitor
EPZ020411 hydrochloride is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ??10 fold selectivity for PRMT6 over PRMT1 and PRMT8. -
histone lysine methyltransferase inhibitor
BIX-01338 hydrate is a histone lysine methyltransferase inhibitor. -
SETD8 inhibitor
UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM; selective over 15 other methyltransferases. -
CARM1 inhibitor
SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with IC50 of 50 nM. -
EZH2 inhibitor
Gambogenic acid is an active ingredient in gamboge, with anticancer activity. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination. -
Menin-MLL inhibitor
SNDX-5613 is a potent and specific Menin-MLL inhibitor. -
PRMT7 inhibitor
SGC8158 is a potent inhibitor of PRMT7, useful for investigating PRMT7's cellular functions. It reduces monomethylarginine levels on Hsp70, a key PRMT7 substrate. SGC8158 exhibits growth inhibitory effects in various cancer cells, including multidrug-resistant (MDR) cancer cells, with IC50 values ranging from 2 to 9 μM. -
PRMT5-MTA complex inhibitor
MRTX9768 is a highly potent, selective, and orally bioavailable first-in-class inhibitor of the PRMT5-MTA complex, demonstrating targeted inhibition of protein arginine methyltransferase 5 (PRMT5) in MTAP-deleted tumors with potential antineoplastic activity.
