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Catalog No.
Product Name
Application
Product Information
Citations
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EZH2 inhibitor
Lirametostat (CPI-1205) is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2.
- George L.Joun, .et al. , bioRxiv, 2025, Jan 8
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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
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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.- Jingzhou Chen, .et al. , Nat Commun, 2026, Jan 19;17(1):1874 PMID: 41554751
- Xinxin Chai, .et al. , International Journal of Cancer, 2025, Dec 09 PMID: 41363617
- Afifa Yaqub, .et al. , Pakistan Journal of Zoology, 2022, 54(6)
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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.- Linna Han, .et al. , Biochem J, 2023, Mar 31;480(6):421-432 PMID: 36896918
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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.- Lucy E. Dawson, .et al. , Sarcoma, 2020, 2020: 8647981 PMID: 32300280
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Dupret B, .et al. , Biochim Biophys Acta Gene Regul Mech, 2017, Oct;1860(10):1079-1093 PMID: 28887218
- Theresa Baker, .et al. , Oncotarget, 2015, Oct 20; 6(32): 32646-32655 PMID: 26360609
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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
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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).- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
- Nie L, .et al. , Nat Commun, 2019, Nov 8;10(1):5114 PMID: 31704972
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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.- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
- Wang Z, .et al. , J Cell Mol Med, 2019, May 13 PMID: 31087496
- Theresa Baker, .et al. , Oncotarget, 2015, Oct 20; 6(32): 32646-32655 PMID: 26360609
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DOT1L Inhibitor
EPZ-5676 is a small molecule inhibitor of histone methyltransferase with potential antineoplastic activity.- Yoo H, .et al. , Cell Death Dis, 2020, Jan; 11(1): 14 PMID: 31908356
- Guang Bai, .et al. , Epigenetics of Chronic Pain, 2019, Pages 1-48
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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. -
PRMT4 inhibitor
EPZ0025654 (GSK3536023) is a potent inhibitor of protein arginine methyltransferase 4 (PRMT4, also known as CARM1), with an IC50 of 3 nM. -
HDAC1/DNA Methyltransferase Inhibitor
Psammaplin A, a marine-derived metabolite, is a potent inhibitor of HDAC1 (IC50: 45 nM), DNA methyltransferases (IC50: 18.6 nM), and aminopeptidase N (IC50: 18 μM). It also suppresses DNA topoisomerase and farnesyl protein transferase activities. As a PPARγ activator, Psammaplin A induces apoptosis and exhibits antitumor, anti-inflammatory, and anti-angiogenic properties. Additionally, it demonstrates antibacterial activity against Gram-positive bacteria by inhibiting DNA synthesis and DNA -
PRMT5/7 inhibitor
DS-437 is a dual inhibitor of PRMT5 and PRMT7, with IC₅₀ values of 6 μM for both enzymes. It exhibits high selectivity over 29 other human methyltransferases, including protein, DNA, and RNA methyltransferases. DS-437 functions as a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5 and also inhibits DNMT3A and DNMT3B with IC₅₀ values of 52 μM and 62 μM, respectively. Additionally, DS-437 inhibits the methylation of FOXP3, making it a useful tool for studying epigenetic regulation and immune modulation. -
PRMT5 inhibitor
PRT543 (PRMT5-IN-35) is a potent, selective, and orally active inhibitor of protein arginine methyltransferase 5 (PRMT5), with an IC₅₀ value of 1 nM. It effectively targets PRMT5-mediated epigenetic regulation and demonstrates strong potential for use in cancer research, particularly in malignancies driven by dysregulated arginine methylation. -
PRMT5 inhibitor
TNG908 is a MTAP (methylthioadenosine phosphorylase)-synergistic inhibitor of PRMT5 (protein arginine methyltransferase 5). It is orally active and capable of crossing the blood–brain barrier, making it suitable for targeting both systemic and central nervous system tumors. TNG908 selectively exploits MTAP deletion—a common alteration in cancers—to enhance its antitumor efficacy, making it a promising agent for cancer research and precision oncology. -
PRMT5/MTA inhibitor
Navlimetostat is a potent, orally active, and selective inhibitor of the PRMT5-MTA complex. It exhibits IC₅₀ values of 3.6 nM for the PRMT5-MTA complex and 20.5 nM for PRMT5 alone. Navlimetostat binds to the PRMT5-MTA complex with exceptionally high affinity (K\_D = 0.14 pM). It demonstrates strong antineoplastic activity both in vitro and in vivo, making it a promising candidate for cancer research and therapeutic development targeting PRMT5-driven malignancies. -
PRMTs inhibitor
AMI-1 free acid is a potent, cell-permeable, and reversible inhibitor of protein arginine N-methyltransferases (PRMTs). It inhibits human PRMT1 and yeast Hmt1p with IC₅₀ values of 8.8 μM and 3.0 μM, respectively. AMI-1 functions by blocking the binding of peptide substrates to PRMTs, making it a useful tool for studying arginine methylation and its role in gene regulation, signal transduction, and disease. -
PRMTs inhibitor
MS023 dihydrochloride is a potent, selective, and cell-permeable inhibitor of type I protein arginine methyltransferases (PRMTs). It exhibits strong inhibitory activity with IC₅₀ values of 30 nM for PRMT1, 119 nM for PRMT3, 83 nM for PRMT4, 4 nM for PRMT6, and 5 nM for PRMT8. MS023 is a valuable tool for studying PRMT-dependent epigenetic regulation and has potential applications in cancer and other PRMT-associated diseases. -
PRMT5 inhibitor
LLY-284 is the diastereomer of LLY-283 and exhibits significantly reduced activity compared to LLY-283. While LLY-283 is a potent inhibitor of protein arginine methyltransferase 5 (PRMT5) with strong anticancer potential, LLY-284 serves primarily as a less active control compound in studies evaluating PRMT5-targeted cancer therapeutics. -
PRMT5 inhibitor
BRD0639 is a first-in-class inhibitor that disrupts the interaction between protein arginine methyltransferase 5 (PRMT5) and its substrate adaptor proteins. It functions as a PRMT5 binding motif (PBM)-competitive agent, selectively interfering with PBM-dependent PRMT5 activities. BRD0639 is a valuable chemical probe for studying PRMT5-mediated methylation and its role in epigenetic regulation and disease. -
EZH1/EZH2 inhibitor
Tulmimetostat (CPI-0209) is an orally active, dual inhibitor of EZH1 and EZH2, key enzymatic components of the polycomb repressive complex 2 (PRC2) involved in histone methylation and gene silencing. By targeting EZH2, Tulmimetostat effectively suppresses aberrant gene repression associated with tumorigenesis. It exhibits antitumor activity and is currently being investigated in studies involving a variety of solid tumors and hematologic malignancies. -
Menin-KMT2A inhibitor
Bleximenib (JNJ-75276617) is an orally active and highly selective menin–KMT2A (MLL) interaction inhibitor, with IC50 values of 0.1 nM in humans, 0.045 nM in mice, and ≤0.066 nM in dogs. It effectively inhibits the proliferation of tumor cells and induces apoptosis and differentiation, particularly in malignancies driven by KMT2A rearrangements. Bleximenib is a promising therapeutic candidate for the study and treatment of leukemia and other menin-dependent cancers.
