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Histone Methyltransferase
Isoform-selective Products
Signaling Pathway
Histone Methyltransferase Products
- All (63)
- Histone Methyltransferase Inhibitors (59)
- Histone Methyltransferase Antagonists (3)
- New Histone Methyltransferase Products
| Catalog No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S7061 | GSK126 | GSK126 (GSK2816126A, GSK2816126) is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases. |
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| S7128 | Tazemetostat (EPZ-6438) | Tazemetostat (EPZ-6438, E7438) is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs. |
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| S7120 | DZNeP (3-deazaneplanocin A) HCl | DZNeP (3-deazaneplanocin A) HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM in a cell-free assay. |
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| S7164 | GSK343 | GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. GSK343 induces autophagy. |
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| S7062 | Pinometostat (EPZ5676) | Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1. |
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| S8006 | BIX 01294 | BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3. |
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| S7353 | EPZ004777 | EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay and demonstrates >1,200-fold selectivity for DOT1L over all other tested PMTs. EPZ004777 induces apoptosis. |
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| S7748 | EPZ015666 (GSK3235025) | EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs. |
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| S7165 | UNC1999 | UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. UNC1999 is a potent autophagy inducer. UNC1999 specifically suppresses H3K27me3/2 and induces a range of anti-leukemia effects including anti-proliferation, differentiation, and apoptosis. |
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| S8496 | EED226 | EED226 is a potent, selective, and orally bioavailable a novel allosteric Polycomb repressive complex 2 (PRC2) inhibitor with an IC50 of 23.4 nM when the H3K27me0 peptide was used as substrate and an IC50 of 53.5 nM when the mononucleosome was used as the substrate. It directly binds to the H3K27me3 binding pocket of EED. | ||
| S7004 | EPZ005687 | EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM in a cell-free assay, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases. |
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| S8068 | Chaetocin | 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. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR). | ||
| S7079 | SGC 0946 | SGC 0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM in a cell-free assay, is inactive against a panel of 12 PMTs and DNMT1. | ||
| S8664 | Pemrametostat (GSK3326595) | Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models. | ||
| S7265 | MM-102 | MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic inhibitor of the WDR5/MLL1 protein-protein interaction, which bind to WDR5 with Ki < 1 nM and IC50 =2.4nM.This product may precipitate when dissolved in saline solution or PBS solution. It is recommended to prepare the stock solution in DMSO solution. |
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| S8071 | UNC0638 | UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP histone methyltransferase with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 has anti-viral activities. | ||
| S7805 | EPZ011989 | EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM. | ||
| S7230 | UNC0642 | UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels. | ||
| S7833 | OICR-9429 | OICR-9429 is a potent antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3 and reduces viability of acute myeloid leukemia cells in vitro. It binds to WDR5 with high affinity (KD = 93 ± 28 nM. |
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| S7570 | UNC0379 | UNC0379 is a selective, substrate competitive inhibitor of N-lysine methyltransferase SETD8 with IC50 of 7.3 μM, high selectivity over 15 other methyltransferases. | ||
| S8111 | GSK591 | GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM. |
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| S8353 | Lirametostat (CPI-1205) | Lirametostat (CPI-1205) is an orally available selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM and 52 nM for EZH2 and EZH1 respectively. It has potential antineoplastic activity. | ||
| S7618 | MI-2 (Menin-MLL Inhibitor) | MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM. | ||
| S7616 | CPI-169 | 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. | ||
| S7817 | MI-503 | MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM. It shows pronounced growth suppressive activity in a panel of human MLL leukemia cell lines(GI50 at 250 nM-570 nM range), but only a minimal effect in human leukemia cell lines without MLL translocations. | ||
| S8112 | MS023 | 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. | ||
| S7983 | A-196 | A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets. | ||
| S7804 | GSK503 | GSK503 is a potent and specific EZH2 methyltransferase inhibitor. |
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| S7884 | AMI-1 | AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively. |
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| S7294 | PFI-2 HCl | PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets. | ||
| S7832 | SGC707 | SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively. | ||
| S7572 | A-366 | A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM and 38nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. | ||
| S4589 | Amodiaquine dihydrochloride dihydrate | Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase with estimated Ki of 18.6 nM. It is also used as an antimalarial and anti-inflammatory agent. | ||
| S7619 | MI-3 (Menin-MLL Inhibitor) | MI-3 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 648 nM. | ||
| S7591 | BRD4770 | BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence. | ||
| S7575 | LLY-507 | LLY-507 is a cell-active, potent, and selective inhibitor of protein-lysine Methyltransferase SMYD2. | ||
| S8624 | Onametostat (JNJ-64619178) | Onametostat (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. | ||
| S2184 | WDR5-0103 | WDR5-0103 (WD-Repeat Protein 5-0103) is a small-molecule antagonist of WDR5 (WD40 repeat protein 5) with Kd of 450 nM. | ||
| S7611 | EI1 | EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively. |
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| S4021 | Tolcapone | Tolcapone (Ro 40-7592) is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM. | ||
| S8359 | UNC3866 | UNC3866 is a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. UNC3866 binds the chromodomains of CBX4 and CBX7 most potently, with a K(d) of ∼100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains. | ||
| S7820 | EPZ020411 2HCl | EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM. | ||
| S7816 | MI-463 | MI-463 is a potent inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM. | ||
| S8209 | HLCL-61 HCL | HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia. | ||
| S8983 | MAK683 | MAK683 (EED inhibitor-1, example 2) is an inhibitor of embryonic ectoderm development (EED). MAK683 exhibits IC50 of 59 nM, 89 nM and 26 nM in EED Alphascreen binding, LC-MS and ELISA assay, respectively. | ||
| S7815 | MI-136 | MI-136 can specifically inhibit the menin-MLL interaction. It inhibits DHT-induced expression of androgen receptor (AR) target genes. | ||
| S3147 | Entacapone | Entacapone (OR-611) inhibits catechol-O-methyltransferase(COMT) with IC50 of 151 nM. Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders. | ||
| S8147 | MS049 | MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. | ||
| S7868 | SAH (S-Adenosyl-L-homocysteine) | SAH (S-Adenosyl-L-homocysteine) is an inhibitor for (Methyltransferase Like 3-14) METTL3-METTL14 heterodimer complex (METTL3-14) with IC50 of 0.9 μM. | ||
| S8934 | VTP50469 | VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction with Ki of 104 pM. VTP50469 exhibits anti-leukemia activity. | ||
| S8494 | PF-06726304 | PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM. | ||
| S7656 | CPI-360 | CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases. | ||
| S8607 | JQ-EZ-05 (JQEZ5) | JQ-EZ-05 (JQEZ5) is a specific and reversible EZH1/2 inhibitor. | ||
| S8340 | SGC2085 | SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs. | ||
| S7020 | UNC0646 | UNC0646 is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP with IC50 of 6 nM and 15 nM , respectively, with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity. | ||
| E1163New | MS177 | MS177 is an EZH2-targeting PRTOAC degrader and a potent inhibitor of enzymatic EZH2, that effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukemia cell growth inhibition, apoptosis, and cell cycle progression arrest. | ||
| E1728New | STC-15 | STC-15 is an oral, small-molecule inhibitor of RNA methyltransferase METTL3. It inhibits tumor growth through the activation of anti-cancer immune responses associated with increased interferon signaling and synergizes with T-cell checkpoint blockade. | ||
| S5445 | AMI-1 (free acid) | AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively. | ||
| S8918 | MS1943 | MS1943 is an orally bioavailable EZH2 selective degrader that effectively reduces EZH2 levels in cells with IC50 of 120 nM for inhibiting EZH2 methyltransferase activity. | ||
| E2911 | UZH2 | UZH2 is a potent and selective METTL3 inhibitor with an IC50 value of 5 nM in TR-FRET assay. | ||
| S8702 | EBI-2511 | EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G). | ||
| S9659 | UNC6852 | UNC6852 is a selective degrader that targets polycomb repressive complex 2 (PRC2) with IC50 of 247 nM for EED. UNC6852 is based on PROTAC and contains an EED226-derived ligand and a ligand for VHL. | ||
| E1967New | ORIC-944 | ORIC-944 is a potent and selective allosteric inhibitor of the polycomb repressive complex 2 (PRC2) via the embryonic ectoderm development (EED) subunit. It exhibits anti-tumor activity in vivo prostate cancer models. | ||
| S7061 | GSK126 | GSK126 (GSK2816126A, GSK2816126) is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases. |
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| S7128 | Tazemetostat (EPZ-6438) | Tazemetostat (EPZ-6438, E7438) is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs. |
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| S7120 | DZNeP (3-deazaneplanocin A) HCl | DZNeP (3-deazaneplanocin A) HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM in a cell-free assay. |
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| S7164 | GSK343 | GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. GSK343 induces autophagy. |
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| S7062 | Pinometostat (EPZ5676) | Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1. |
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| S8006 | BIX 01294 | BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3. |
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| S7353 | EPZ004777 | EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay and demonstrates >1,200-fold selectivity for DOT1L over all other tested PMTs. EPZ004777 induces apoptosis. |
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| S7748 | EPZ015666 (GSK3235025) | EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs. |
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| S7165 | UNC1999 | UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. UNC1999 is a potent autophagy inducer. UNC1999 specifically suppresses H3K27me3/2 and induces a range of anti-leukemia effects including anti-proliferation, differentiation, and apoptosis. |
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| S7004 | EPZ005687 | EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM in a cell-free assay, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases. |
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|
| S8068 | Chaetocin | 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. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR). | ||
| S7079 | SGC 0946 | SGC 0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM in a cell-free assay, is inactive against a panel of 12 PMTs and DNMT1. | ||
| S8664 | Pemrametostat (GSK3326595) | Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models. | ||
| S7265 | MM-102 | MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic inhibitor of the WDR5/MLL1 protein-protein interaction, which bind to WDR5 with Ki < 1 nM and IC50 =2.4nM.This product may precipitate when dissolved in saline solution or PBS solution. It is recommended to prepare the stock solution in DMSO solution. |
|
|
| S8071 | UNC0638 | UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP histone methyltransferase with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 has anti-viral activities. | ||
| S7805 | EPZ011989 | EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM. | ||
| S7230 | UNC0642 | UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels. | ||
| S7570 | UNC0379 | UNC0379 is a selective, substrate competitive inhibitor of N-lysine methyltransferase SETD8 with IC50 of 7.3 μM, high selectivity over 15 other methyltransferases. | ||
| S8111 | GSK591 | GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM. |
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| S8353 | Lirametostat (CPI-1205) | Lirametostat (CPI-1205) is an orally available selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM and 52 nM for EZH2 and EZH1 respectively. It has potential antineoplastic activity. | ||
| S7618 | MI-2 (Menin-MLL Inhibitor) | MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM. | ||
| S7616 | CPI-169 | 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. | ||
| S7817 | MI-503 | MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM. It shows pronounced growth suppressive activity in a panel of human MLL leukemia cell lines(GI50 at 250 nM-570 nM range), but only a minimal effect in human leukemia cell lines without MLL translocations. | ||
| S8112 | MS023 | 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. | ||
| S7983 | A-196 | A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets. | ||
| S7804 | GSK503 | GSK503 is a potent and specific EZH2 methyltransferase inhibitor. |
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| S7884 | AMI-1 | AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively. |
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| S7294 | PFI-2 HCl | PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets. | ||
| S7832 | SGC707 | SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively. | ||
| S7572 | A-366 | A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM and 38nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. | ||
| S4589 | Amodiaquine dihydrochloride dihydrate | Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase with estimated Ki of 18.6 nM. It is also used as an antimalarial and anti-inflammatory agent. | ||
| S7619 | MI-3 (Menin-MLL Inhibitor) | MI-3 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 648 nM. | ||
| S7591 | BRD4770 | BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence. | ||
| S7575 | LLY-507 | LLY-507 is a cell-active, potent, and selective inhibitor of protein-lysine Methyltransferase SMYD2. | ||
| S8624 | Onametostat (JNJ-64619178) | Onametostat (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. | ||
| S7611 | EI1 | EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively. |
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| S4021 | Tolcapone | Tolcapone (Ro 40-7592) is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM. | ||
| S7820 | EPZ020411 2HCl | EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM. | ||
| S7816 | MI-463 | MI-463 is a potent inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM. | ||
| S8209 | HLCL-61 HCL | HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia. | ||
| S8983 | MAK683 | MAK683 (EED inhibitor-1, example 2) is an inhibitor of embryonic ectoderm development (EED). MAK683 exhibits IC50 of 59 nM, 89 nM and 26 nM in EED Alphascreen binding, LC-MS and ELISA assay, respectively. | ||
| S7815 | MI-136 | MI-136 can specifically inhibit the menin-MLL interaction. It inhibits DHT-induced expression of androgen receptor (AR) target genes. | ||
| S3147 | Entacapone | Entacapone (OR-611) inhibits catechol-O-methyltransferase(COMT) with IC50 of 151 nM. Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders. | ||
| S8147 | MS049 | MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. | ||
| S7868 | SAH (S-Adenosyl-L-homocysteine) | SAH (S-Adenosyl-L-homocysteine) is an inhibitor for (Methyltransferase Like 3-14) METTL3-METTL14 heterodimer complex (METTL3-14) with IC50 of 0.9 μM. | ||
| S8934 | VTP50469 | VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction with Ki of 104 pM. VTP50469 exhibits anti-leukemia activity. | ||
| S8494 | PF-06726304 | PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM. | ||
| S7656 | CPI-360 | CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases. | ||
| S8607 | JQ-EZ-05 (JQEZ5) | JQ-EZ-05 (JQEZ5) is a specific and reversible EZH1/2 inhibitor. | ||
| S8340 | SGC2085 | SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs. | ||
| S7020 | UNC0646 | UNC0646 is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP with IC50 of 6 nM and 15 nM , respectively, with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity. | ||
| E1163New | MS177 | MS177 is an EZH2-targeting PRTOAC degrader and a potent inhibitor of enzymatic EZH2, that effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukemia cell growth inhibition, apoptosis, and cell cycle progression arrest. | ||
| E1728New | STC-15 | STC-15 is an oral, small-molecule inhibitor of RNA methyltransferase METTL3. It inhibits tumor growth through the activation of anti-cancer immune responses associated with increased interferon signaling and synergizes with T-cell checkpoint blockade. | ||
| S5445 | AMI-1 (free acid) | AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively. | ||
| S8918 | MS1943 | MS1943 is an orally bioavailable EZH2 selective degrader that effectively reduces EZH2 levels in cells with IC50 of 120 nM for inhibiting EZH2 methyltransferase activity. | ||
| E2911 | UZH2 | UZH2 is a potent and selective METTL3 inhibitor with an IC50 value of 5 nM in TR-FRET assay. | ||
| S8702 | EBI-2511 | EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G). | ||
| S9659 | UNC6852 | UNC6852 is a selective degrader that targets polycomb repressive complex 2 (PRC2) with IC50 of 247 nM for EED. UNC6852 is based on PROTAC and contains an EED226-derived ligand and a ligand for VHL. | ||
| E1967New | ORIC-944 | ORIC-944 is a potent and selective allosteric inhibitor of the polycomb repressive complex 2 (PRC2) via the embryonic ectoderm development (EED) subunit. It exhibits anti-tumor activity in vivo prostate cancer models. | ||
| S7833 | OICR-9429 | OICR-9429 is a potent antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3 and reduces viability of acute myeloid leukemia cells in vitro. It binds to WDR5 with high affinity (KD = 93 ± 28 nM. |
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| S2184 | WDR5-0103 | WDR5-0103 (WD-Repeat Protein 5-0103) is a small-molecule antagonist of WDR5 (WD40 repeat protein 5) with Kd of 450 nM. | ||
| S8359 | UNC3866 | UNC3866 is a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. UNC3866 binds the chromodomains of CBX4 and CBX7 most potently, with a K(d) of ∼100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains. | ||
| E1163New | MS177 | MS177 is an EZH2-targeting PRTOAC degrader and a potent inhibitor of enzymatic EZH2, that effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukemia cell growth inhibition, apoptosis, and cell cycle progression arrest. | ||
| E1728New | STC-15 | STC-15 is an oral, small-molecule inhibitor of RNA methyltransferase METTL3. It inhibits tumor growth through the activation of anti-cancer immune responses associated with increased interferon signaling and synergizes with T-cell checkpoint blockade. | ||
| E1967New | ORIC-944 | ORIC-944 is a potent and selective allosteric inhibitor of the polycomb repressive complex 2 (PRC2) via the embryonic ectoderm development (EED) subunit. It exhibits anti-tumor activity in vivo prostate cancer models. |
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Tags: Histone Methyltransferase inhibitor|Histone Methyltransferase agonist|Histone Methyltransferase activator|Histone Methyltransferase inducer|Histone Methyltransferase antagonist|Histone Methyltransferase signaling pathway|Histone Methyltransferase assay kit
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