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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Dot1L inhibitor
Dot1L-IN-1 is a highly potent, selective and structurally novel Dot1L inhibitor with a Ki of 2 pM. -
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. -
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). -
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. -
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. -
KDM1/CDK1 Inhibitor
KDM1/CDK1-IN-1 is a potent inhibitor of both KDM1 and CDK1, exhibiting IC50 values of 0.096 μM and 0.078 μM, respectively. This compound effectively induces cell cycle arrest at the G2/M phase and promotes apoptosis in HOP-92 cancer cells. Additionally, KDM1/CDK1-IN-1 demonstrates significant cytotoxic effects against a range of cell lines, including CCRF-CEM, HOP-92, and Hep-G2, with IC50 values of 16.34 μM, 3.45 μM, and 7.79 μM, respectively. Its ability to target critical regulators of the cell cycle makes KDM1/CDK1-IN-1 valuable for cancer research applications. -
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. -
SMYD3 inhibitor
EM127 (compound 11c) is a highly selective, covalent SMYD3 inhibitor with a KD of 13 μM and site-specific binding. It potently inhibits ERK1/2 phosphorylation, suppresses transcriptional regulation of SMYD3 target genes, and provides sustained inhibition of methyltransferase activity. EM127 is suitable for cancer research, particularly in SMYD3-positive tumors.
