Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. - 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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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. -
PRMT5 Inhibitor
HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
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G9a inhibitor
CPUY074020 is a potent G9a inhibitor with an IC50 of 2.18 μM, and possesses anti-proliferative activity . -
PRMT6 Inhibitor
EPZ020411 dihydrochloride is a selective inhibitor of protein arginine methyltransferase 6 (PRMT6) with a robust IC50 of 0.010 μM. This compound effectively blocks PRMT6-mediated methylation of histone H3 at arginine 2, which enhances cellular oxidative stress responses by reducing reactive oxygen species (ROS) production and inhibiting apoptosis. EPZ020411 dihydrochloride has significant implications for research in fields including neuropathic pain, colorectal cancer, ototoxicity, hearing loss, and glioblastoma. -
Prodrug Of KMT9 Inhibitor
KMT9-IN-1 is a prodrug of the KMT9 inhibitor that releases the active compound 7b upon hydrolysis by cellular esterases. This compound effectively targets KMT9, resulting in a reduction of H4K12me1 levels. KMT9-IN-1 exhibits notable antitumor activity against colon cancer and can be employed in research focused on prostate cancer and hepatocellular carcinoma. -
DNMT1 Degrader
MS9024 is a selective degrader of DNA methyltransferase 1 (DNMT1), facilitating its degradation in HCT116 cells through the ubiquitin-proteasome pathway, achieving a DC50 of 35 nM. In additional cell lines, such as MDA-MB-468 and H1299, MS9024 shows DC50 values of 254 nM and 101 nM, respectively. Furthermore, it exhibits inhibitory activity against DNMT1 with an IC50 of 0.43 μM, making it a valuable tool for studying the role of DNMT1 in epigenetic regulation and its implications in cancer research. -
EZH2 PROTAC
PROTAC EZH2 Degrader-41 is a PROTAC designed to target EZH2 by recruiting cIAP E3 ubiquitin ligase. This compound facilitates the ubiquitination and subsequent proteasomal degradation of EZH2, thereby exerting significant antiproliferative effects in lymphoma cells. PROTAC EZH2 Degrader-41 is a valuable tool for investigating the role of EZH2 in lymphoma research and its potential as a therapeutic target. -
EZH2 Inhibitor
TDI-6118 is a potent inhibitor of the histone methyltransferase EZH2, known for its ability to penetrate the blood-brain barrier. This compound exhibits significant biological activity in targeting EZH2, making it a valuable tool for investigating central nervous system malignancies. Its application in research may contribute to a better understanding of the molecular mechanisms underlying various brain cancers. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-12 is a CRBN-recruiting PROTAC designed to selectively degrade the EZH2 protein, exhibiting an IC50 of 3.90 nM for EZH2 and an IC50 of 5.24 μM for EZH1. This compound facilitates targeted protein degradation, making it a valuable tool for research focused on epigenetic regulation and cancer biology. Its ability to modulate the expression of key oncogenic factors positions it as a significant reagent for therapeutic investigations targeting EZH2-dependent pathways. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-24 is an innovative molecule designed to target EZH2 by utilizing a PROTAC-mediated degradation mechanism. This compound exhibits potent EZH2 methyltransferase inhibitory activity, facilitating the selective degradation of the EZH2 protein. Research applications include studies on epigenetic regulation and therapeutic strategies for cancers with aberrant EZH2 activity. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-30 is a PROTAC protein degrader specifically designed to target the enhancer of zeste homolog 2 (EZH2) with an IC50 of 6.22 μM in SU-DHL-6 cells. This compound is instrumental in research applications focusing on diffuse large B-cell lymphoma by promoting the degradation of EZH2 and thereby modulating epigenetic regulation. The inclusion of ligands for both EZH2 and MDM2, coupled with a linker, facilitates targeted protein degradation and offers a valuable tool for investigating therapeutic strategies in cancer biology. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-43 is a targeted PROTAC protein degrader that specifically degrades the EZH2 protein, exhibiting an IC50 of 21.73 μM in SU-DHL-6 cells. This compound is valuable for investigating the role of EZH2 in lymphoma research and understanding its mechanistic function in histone methylation. The dual ligand design incorporates a histone methyltransferase ligand and a VHL ligand, promoting efficient substrate recognition and recruitment for proteasomal degradation.
