|VTP-50469 is a novel, potent, selective, orally-available MeninMLL1 inhibitor, being effectively against MLL-rearranged and NPM1c+ leukemia, selectively killing cell lines with MLLrearrangements and NPM1c+ mutations.
|UNC 0638 hydrate
|UNC0638 is an inhibitor of protein lysine methyltransferases G9a and GLP with IC50 of < 15 nM, 19 nM, respectively.
|TP-064 is a potent and selective PRMT4 inhibitor. The in vitro activity of TP-064 includes inhibition of PRMT4 with IC50 < 10nM for methylation of H3 (1-25) and greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In cellular assays, TP-064 inhibits the methylation of MED12 with IC50 = 43 nM.
|TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor.
|Ryuvidine is an inhibitor of SETD8 with cellular activity. It also acts as a CDK4 inhibitor and inducer of the DNA damage response.
|PRMT5 inhibitor C17 is a potent, selective, and cell active protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50 = 0.33 μM) exhibited a broad selectivity against a panel of other methyltransferases.
|PF-06726304 is a potent and selective EZH2 inhibitor with Ki value of 0.7 nM.
|NSD2-PWWP1 antagonist 3f can bind to the NSD2-PWWP1 domain with Kd value of 3.4μM and abrogates histone H3K36me2 binding to the PWWP1 domain in cells.
|MS37452 compete against H3K27me3 binding through interactions with key residues in the methyl-lysine binding pocket of CBX7ChD. It derepresses transcription of Polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells.
|MS1943 is a first-in-class EZH2 selective degrader that effectively reduces EZH2 levels in cells.
|MS049 2HCl is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.
|MM-589 trifluoroacetate is a potent inhibitor of the WD repeat domain 5 protein (WDR5)–mixed lineage leukemia (MLL) interaction, and may yield a therapy for acute leukemia.
|MM-589 is a potent inhibitor of the WD repeat domain 5 protein (WDR5)–mixed lineage leukemia (MLL) interaction, and may yield a therapy for acute leukemia.
|M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with IC50 values of 1 nM and 4 nM in MV4;11 cells and MOLM-13 cells, respectively.
|LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.
|JQEZ5 is a potent and selective SAM-competitive EZH2 lysine methyltransferase inhibitor with IC50 of 11 nM.
|JNJ-64619178 is a selective, orally active, and pseudo-irreversible inhibitor of protein arginine methyltransferase 5 (IC50: 0.14 nM). It has effective activity In lung cancer.
|GSK3368715, aslo known as EPZ019997, is a potent, reversible type I PRMT inhibitor with anti-tumor effects in human cancer models. Inhibition of PRMT5, the predominant type II PRMT, produces synergistic cancer cell growth inhibition when combined with GSK3368715. Interestingly, deletion of the methylthioadenosine phosphorylase gene (MTAP) results in accumulation of the metabolite 2-methylthioadenosine, an endogenous inhibitor of PRMT5, and correlates with sensitivity to GSK3368715 in cell lines.
|GSK3368715 dihydrochloride is a novel potent type-I protein arginine methyltransferases (PRMTs) inhibitor.
|GSK3368715 2HCl is a novel potent type-I protein arginine methyltransferases (PRMTs) inhibitor.
|GSK3326595 is a potent, specific and reversible PRMT5 inhibitor which can decrease the levels of both monomethylated and dimethylated arginine residues in histones H2A, H3 and H4.
|GSK2807 Trifluoroacetate is a SMYD3 SAM-competitive inhibitor with Ki of 14 nM.
|Furamidine, also known as DB75, is a cell-permeable inhibitor of protein arginine methyltransferase 1 (PRMT1) that is selective for PRMT1. Furamidine (DB75) binds to strings of AT base pair sequences in DNA′s minor groove. Furamidine was originally developed as an anti-parasitic compound for a variety of diseases including Chagas′ disease. Furamidine targets the enzyme active site and is primarily competitive with the substrate and noncompetitive toward the cofactor. Furthermore, cellular studies revealed that 1 is cell membrane permeable and effectively inhibits intracellular PRMT1 activity and blocks cell proliferation in leukemia cell lines with different genetic lesions.
|Furamidine 2HCl is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with IC50 of 9.4 μM.
|for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated.
|EZM 2302 is the first potent and selective inhibitor of CARM1 enzymatic activity with IC50 value of 6 nM.
|EZH2-IN-2 is a EZH2 inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC50 of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity.
|EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 nM and 1.1 nM respectively.
|EPZ020411 2HCl is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.
|EPZ011989 HCl is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of < 3 nM.
|EBI-2511 is a Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin’s Lymphoma. EBI-2511 showed enzymatic activity and cellular activity of 4.0 and 6.0nM, respectively. EBI-2511 demonstrated excellent in vivo efficacy in Pfeiffer tumor Xenograft models in mouse and is under preclinical development for the treatment of cancers associated with EZH2 mutations.
|CMP5 is a potent and selective PRMT5 Inhibitor. CMP5 showed to occupy hPRMT5 catalytic site and block symmetrically dimethylated S2Me-H4R3 & S2Me-H3R8 with no effect on the asymmetric methylation of H4R3 in lymphoblastoid cell lines at 40 µM. CMP-5 shows promise as a novel therapeutic approach for B-cell lymphomas.
|CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected.
|Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU (VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 μM.
|CARM1-IN-1 HCl is a potent and specific CARM1 (Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 μM and shows very low activity against PRMT1 and SET7 (IC50 > 600 μM).
|BCI-121 (BCI121) is a substrate-competitive inhibitor of SMYD3 that inhibits SMYD3-substrate interaction and chromatin recruitment It can significantly reduce the proliferation of various cancer cells.
|BAY-598 is an inhibitor of SMYD2. It can inhibit in vitro methylation of p53 at lysine 370 with IC50 value of 27 nM.
|AMI-1 free acid
|AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
|A-893 is a potent and selective SMYD2 inhibitor (IC50: 2.8 nM).
|A-395 is a antagonist of Polycomb repressive complex 2 (PRC2) protein–protein interactions that potently inhibits the trimeric PRC2 complex (EZH2–EED–SUZ12) with an IC50 of 18 nM.
|A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50s of 25 and 144 nM respectively.