||Cyproheptadine hydrochloride sesquihydrate, an antihistamine, is an antagonist of serotonin and histamine2.
||AZ505 ditrifluoroacetate is an effective and selective SMYD2 inhibitor (IC50: 0.12 μM).
||CM-579 is a dual inhibitor of G9a and DNMT( IC50:16 nM, 32 nM for G9a and DNMT). It has potent in vitro cellular activity in a wide range of cancer cells.
||CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative activity.
||The Ki value of DOT1L-in-1 is 2pm.It is a highly effective, selective and novel Dot1L inhibitor.
||Dot1l-in-2 is an effective, selective and oral bioutilization inhibitor of histone methyltransferase Dot1L, with IC50 and Ki of 0.4 nM and 0.08 nM, respectively.
||Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM.
||Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.17 nM.
||DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.DW14800 is a protein arginine methyltransferase
||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. E
||GNA002 is a highly potent, specific, and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor (IC50: 1.1 μM).
||GSK2807 Trifluoroacetate is a selective and SAM-competitive inhibitor of SMYD3 (Ki: 14 nM; IC50: 130 nM).
||GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48
||GSK3368715 dihydrochloride is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.
||PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity.
||PF-06726304 shows robust antitumor growth activity. PF-06726304 is an effective and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 (Kis: 0.7 and 3.0
||PRMT5-IN-1 is a covalent inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50 of 11 nM for PRMT5/MEP50).
||SMYD2-IN-1 is an inhibitor of SMYD2 (IC50 of 4.45 nM).
||SMYD3-IN-1 is an irreversible and selective SMYD3 (SET and MYND domain containing 3) inhibitor(IC50 of 11.7 nM).
||SNDX-5613 is a potent and specific inhibitor of Menin-MLL(Ki of 0.149 nM and a cell based IC50 of 10-20 nM). SNDX-5613 can be used for the research of MLL-rearranged (MLL-r) acute
||Valemetostat tosylate is a dual inhibitor of EZH1/2 and used in the research of relapsed/refractory peripheral T-cell lymphoma.
||MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).
||DC-05 is an inhibitor of DNA methyltransferase 1 (DNMT1) (IC50 and a Kd: 10.3 μM and 1.09 μM, respectively).
||EBI-2511 is a highly potent and orally active inhibitor of EZH2 (IC50: 6 nM in Pfeffiera cell lines).
||Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki:
||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.
||Lotilaner is a parasiticide. It is used as a potent non-competitive antagonist of insects GABACl receptors (IC50 of 23.84 nM for Drosophila melanogaster GABA receptor). It also has
||MI-538 is an interaction between menin and MLL fusion proteins inhibitor(IC50 of 21 nM).
||PBIT inhibits JARID1B histone demethylase (IC50 of about 3 μM). PBIT also inhibits JARID1A and JARID1C (IC50s of 6 μM and 4.9 μM, respectively). PBIT is a specific inhibitor of
||PRMT5-IN-2 is an inhibitor of protein arginine methyltransferase 5.
||Tazemetostat hydrobromide is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-ty
||UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3, and JMJD2E. UNC0224 is a potent and selective histone methyltransferase G9a inhibitor (Ki: 2.6 nM, an IC50 of 15 nM, and a
||UNC0321 is inactive against SET7/9, SET8/PreSET7, PRMT3, and JMJD2E. UNC0321 is an effective and selective histone methyltransferase G9a inhibitor (Ki: 63 pM) and (assay-dependent
||GSK-503, a potent EZH2 inhibitor, has potential antitumor activity.
||Tazemetostat is an orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyltransferase EZH2, with potential antineoplastic
||UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8.
||JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.
||EPZ005687 is a potent and selective inhibitor of EZH2.
||BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence.
||BIX 01294 Trihydrochloride
||BIX01294 is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.
||PFI-2 is an effective, specific and cell-active lysine methyltransferase SETD7 inhibitor (Ki/IC50: 0.33/2 nM), 1000-fold selectivity over other methyltransferases and other non-epi
||GSK126 is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).
||C-7280948 is a PRMT1 inhibitor.
||EPZ020411 is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.
||GSK3368715, a potent inhibitor of type I protein arginine methyltransferases (PRMT), could inhibit PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM.
||AMI-1 is an effective and selective Histone Methyltransferase (HMT) inhibitor (IC50: 3.0/8.8 μM, for yeast Hmt1p, and human PRMT1).
||UNC0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).
||EPZ011989 is a effective, specific orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 Y646 and EZH2 wt; 15-fold selectivity over EZH1 and >3000-fold selectivity over other
||MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
||UNC1999 is a orally bioavailable, effective and specific inhibitor of EZH2 (IC50=2 nM) and EZH1 (IC50=45).
||EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
||EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
||SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.
||SGC707 is a potent, selective, and cell-active allosteric inhibitor of PRMT3.
||EPZ5676 has been used in trials studying the treatment of Leukemia, Acute Leukemias, Acute Myeloid Leukemia, Myelodysplastic Syndrome, and Acute Lymphocytic Leukemia, among others.
||UNC0638 is an inhibitor of β-protein lysine methyltransferases G9a(IC50<15 nM) and GLP(IC50=19 nM) with excellent potency and selectivity over a wide range of epigenetic and non-e
||EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
||Potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM). Exhibits >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. Decreases le
||SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectivity over other PRMTs
||UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen.
||UNC3866 TFA(1872382-47-2 free base)
||UNC3866 TFA is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen.
||UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).
||EPZ020411 is a specific and effective inhibitor of PRMT6 (IC50=10 nM).
||EPZ020411 2HCl (1700663-41-7(free base))
||EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
||A-196 is a potent and selective inhibitor of SUV420 h1 and SUV420 h2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltr
||MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 of 34 nM and 43 nM, respectively.
||MS049 2HCl (1502816-23-0(free base))
||MS049 is a potent and selective inhibitor of PRMT4 (IC50 = 34 nM) and PRMT6 (IC50 = 43 nM). It is less active against additional type I PRMTs (IC50s = >130, >220, and 1.6 μM for P
||PFI-2 hydrochloride is a potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 (IC50: 2 nM), 500 fold active than (S)-PFI-2.
||BCI-121 is a substrate-competitive SMYD3 inhibitor that inhibits the proliferation of the cancer cell.
||EZM2302 is a selective, and orally available arginine methyltransferase CARM1 inhibitor (IC50: 6 nM).
||GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).
||GSK343, a specific and effective EZH2 inhibitor (IC50=4 nM), exhibits 60 fold specificity activity against EZH1, and >1000 fold specificity activity against other histone methyltra
||EPZ015666 is an orally available inhibitor of PRMT5 enzymatic activity.
||MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
||EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
||BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.
||CPI-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.
||GSK591, Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).
||HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
||LLY-507 is an effective, cell-active, and specific inhibitor of protein-lysine Methyltransferase SMYD2.
||MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively.
||SGC2085 is an effective and selective coactivator-associated arginine methyltransferase 1 (CARM1) inhibitor (IC50: 50 nM).
||XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), It is intended to be used as a negative control for SGC7
||JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM).
||BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, with an IC50 value of 6.3 µM
||BAY-598 is a selective inhibitor of SMYD2 with IC50 values of 27 nM.
||BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM).
||Gambogenic acid is a natural product,is an effective inhibitor of EZH2,with anticancer activity.
||CPI-1205 is a highly potent and selective inhibitor of EZH2(IC50 : 0.002 μM, EC50 : 0.032 μM) .
||MM-102 TFA is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM. MM-102 compound prevents the interaction between mixed lineage leukemia 1 (MLL1) and WD Trp-Asp repe
||CCI 007 is a selective inhibitor of MLL-r, CALM-AF10 and SET-NUP214 leukemia with IC50 of 3.5 uM against MLL-r leukemia cell line PER-485
||Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor.
||Tanshindiol B possesses a unique anti-cancer activity whose mechanism involves the inhibition of EZH2 activity and would provide chemically valuable information for designing a new
||Tanshindiol C protects macrophages from oxLDL induced foam cell formation via activation of Prdx1/ABCA1 signaling and that Prdx1 may be a novel target for therapeutic intervention
||MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM).
||MI-503 is a highly effective and orally bioavailable inhibitor of the menin-mLL interaction.
||AZ505 is an effective and specific SMYD2 inhibitor (IC50: 0.12 μM).
||UNC 0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50s: 6 nM/15 nM for G9a/GLP). UNC0646 potently blocks G9a/GLP methy
||EPZ031686 is a selective and orally available SMYD3 inhibitor (IC50: 3 nM).