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Methylation inhibitor

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95

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1

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6

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-Q36691

    Histone Methyltransferase Cancer
    PRMT5-IN-30 (compound 17) is a potent and selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.33 μM and a Kd of 0.987 μM. PRMT5-IN-30 exhibits a broad selectivity against a panel of other methyltransferases. PRMT5-IN-30 inhibits PRMT5 mediated SmD3 methylation .
    PRMT5-IN-30
  • HY-112080

    Histone Methyltransferase Cancer
    BAY-6035 is a potent, selective and substrate-competitive inhibitor of SMYD3. BAY-6035 inhibits methylation of MEKK2 peptide with an IC50 of 88 nM .
    BAY-6035
  • HY-100967

    Homodimaprit dihydrochloride

    Histone Methyltransferase Neurological Disease
    SKF 91488 (Homodimaprit) dihydrochloride is a potent and noncompetitive histamine N-methyltransferase inhibitor with a Ki value of 0.9 microM. SKF 91488 dihydrochloride inhibits the methylation of labeled histamine in mice .
    SKF 91488 dihydrochloride
  • HY-149730

    ICMT Cancer
    ICMT-IN-54 (compound 7c) is an adamantyl analogue and an ICMT inhibitor (IC50=12.4 μM), which can inhibit ICMT Methylation. ICMT-in-54 inhibits BFC (N-biotinyl-(6-aminohexanoic)-S-farnesyl-L-cysteine) methylation in saccharomyces cerevisiae expressing ICMT, which is an indirect effect of inhibiting ICMT methylation .
    ICMT-IN-54
  • HY-171132

    Histone Methyltransferase
    PRMT3-IN-5 (Compound 14) is an allosteric PRMT3 inhibitor (IC50: 291 nM). PRMT3-IN-5 can be used for investigating PRMT3's biological functions and disease associations .
    PRMT3-IN-5
  • HY-164144

    Histone Methyltransferase Cancer
    EPZ033294 is an inhibitor of SYMD2 (IC50 is 3.9 nM). SYMD2 itself has catalytic activity and can methylate the lysine residue of BTF3 to BTF3me1, which was experimentally demonstrated by detecting an IC50 of 2.9 nM for inhibition of BTF3ME1 by SYMD2, indicating an active inhibition of SYMD2 by EPZ033294. EPZ033294 (0-50 µM) has an inhibitory effect on SYMD2 and a concentration-dependent inhibitory effect in 293T .
    EPZ033294
  • HY-W013500

    alpha-Nitrostilbene; α-Nitrostilbene; NSC 385

    Histone Methyltransferase Others
    (1-Nitroethene-1,2-diyl)dibenzene (alpha-Nitrostilbene; α-Nitrostilbene) is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC50=11 μM in histone H4 methylation assay). It also inhibits histone H4 methylation by PRMT8, but not histone H3.1 methylation by CARM1 or Set7/9, at concentrations of 10 and 100 μM.
    (1-Nitroethene-1,2-diyl)dibenzene
  • HY-141677B

    Histone Demethylase Cancer
    INCB059872 tosylate is a potent, selective and orally active lysine-specific demethylase 1 inhibitor. INCB059872 binds to and inhibits LSD1, enhancing H3K4 methylation, thereby increasing the expression of tumor suppressor genes. INCB059872 inhibition also promotes H3K9 methylation, thereby reducing the transcription of tumor-promoting genes .
    INCB059872 tosylate
  • HY-154839

    c-Myc Cancer
    c-Myc inhibitor 10 (compound 17), a c-Myc inhibitor, exhibits increased cellular potency, consistent with an increase in permeability with methylation of the morpholine nitrogen .
    c-Myc inhibitor 10
  • HY-104009

    Histone Methyltransferase Cancer
    GSK2807 is a potent and selective SAM-competitive inhibitor of SMYD3, exhibiting a Ki value of 14 nM, and it may be useful for cancer treatment by preventing the methylation of MEKK2.
    GSK2807
  • HY-W242821

    Fungal Cancer
    Methyl 3,4-dimethoxycinnamate is an inhibitor of uredospore germination. Methyl 3,4-dimethoxycinnamate also inhibits global DNA methylation in in Hep3B cells .
    Methyl 3,4-dimethoxycinnamate
  • HY-118563

    Biochemical Assay Reagents Others
    S-Farnesyl thioacetic acid is an analog of S-farnesyl cysteine, which is a prenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase) competitive inhibitors. It also inhibits the methylation of farnesylated and geranylgeranylated substrates.
    Farnesylthioacetic acid
  • HY-103236
    NSC232003
    5 Publications Verification

    E1/E2/E3 Enzyme Cancer
    NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.
    NSC232003
  • HY-157719

    COMT Others
    S-Adenosylhomocysteine sulfoxide is an inhibitor of catechol-O-methyltransferase (COMT) with an IC50 value of 860 μM. S-Adenosylhomocysteine sulfoxide can be used in the research of methylation reaction modulators .
    S-Adenosylhomocysteine sulfoxide
  • HY-134828
    AZ506
    2 Publications Verification

    Histone Methyltransferase Cancer
    AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal .
    AZ506
  • HY-121095A

    Histone Demethylase Neurological Disease Cancer
    Bizine dihydrochloride, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>Ki of 59 nM. Bizine dihydrochloride can modulate bulk histone methylation in cancer cells. Bizine dihydrochloride shows neuroprotective effects .
    Bizine di(hydrochloride)
  • HY-106689A

    DHAC acetate; NSC 264880 acetate

    Nucleoside Antimetabolite/Analog DNA Methyltransferase Cancer
    Dihydro-5-azacytidine acetate (DHAC), the nucleoside analog, is incorporated into DNA and inhibits DNA methylation. Dihydro-5-azacytidine acetate has an antitumor activity .
    Dihydro-5-azacytidine acetate
  • HY-121095

    Histone Demethylase Neurological Disease Cancer
    Bizine, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>Ki of 59 nM. Bizine can modulate bulk histone methylation in cancer cells. Bizine shows neuroprotective effects .
    Bizine
  • HY-106689

    DHAC; NSC 264880

    Nucleoside Antimetabolite/Analog DNA Methyltransferase Cancer
    Dihydro-5-azacytidine (DHAC), the nucleoside analog, is incorporated into DNA and inhibits DNA methylation. Dihydro-5-azacytidine has an antitumor activity .
    Dihydro-5-azacytidine
  • HY-112080A

    Histone Methyltransferase Others
    (R)-BAY-6035 is a novel inhibitor that selectively targets the methylation of MAP3K2 by SMYD3, demonstrating nanomolar potency and specificity against kinases and other protein lysine methyltransferases.
    (R)-BAY-6035
  • HY-19980A
    PRIMA-1
    2 Publications Verification

    NSC-281668

    Autophagy MDM-2/p53 Ferroptosis Apoptosis Cancer
    PRIMA-1 (NSC-281668) is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.
    PRIMA-1
  • HY-101938
    Sinefungin
    5 Publications Verification

    Adenosyl-Ornithine; A-9145; Antibiotic 32232RP

    Histone Methyltransferase Fungal Antibiotic Parasite Infection Inflammation/Immunology
    Sinefungin is a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication . Sinefungin, a SET7/9 inhibitor, ameliorates renal fibrosis by inhibiting H3K4 methylation .
    Sinefungin
  • HY-111589

    Histone Methyltransferase Cancer
    EPZ-4777 is a selective DOT1L inhibitor which inhibits H3K79 methylation in cancer cells, blocks the expression of leukemogenic genes, and selectively kills cells that contain the translocation. EPZ-4777 can be used for cancer research .
    EPZ-4777
  • HY-12759
    CARM1-IN-1
    3 Publications Verification

    Histone Methyltransferase Cancer
    CARM1-IN-1 (compound 7g) is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity .
    CARM1-IN-1
  • HY-12759A
    CARM1-IN-1 hydrochloride
    3 Publications Verification

    Histone Methyltransferase Cancer
    CARM1-IN-1 (compound 7g) hydrochloride is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 hydrochloride inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 hydrochloride also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity .
    CARM1-IN-1 hydrochloride
  • HY-168143

    Histone Methyltransferase Cancer
    YD1342 is a prodrug of YD1130, which exhibits potent inhibitory effects on cellular substrate methylation, breast cancer cell clonogenicity, and tumor growth in animal models, exceeding or matching known PRMT4-specific inhibitors. .
    YD1342
  • HY-30008
    Cycloleucine
    5+ Cited Publications

    iGluR Infection Neurological Disease Metabolic Disease Cancer
    Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine has anxiolytic and cytostatic effects .
    Cycloleucine
  • HY-111086

    GSK1733953A

    Bacterial Infection
    DG70 (GSK1733953A), a biphenyl amide, is a respiration inhibitor in Mycobacterium tuberculosis, inhibits MenG activity with an IC50 value of 2.6 ± 0.6 μM. DG70 inhibits the catalytic methylation of Mycobacterium tuberculosis demethylmenaquinone methyltransferase enzymes. DG70 can be used for Tuberculosis (TB) research .
    DG70
  • HY-P10028

    Fluorescent Dye Cancer
    HCT116 is a peptidomimetic inhibitor of N-terminal methyltransferase 1/2 (NTMT1/2) with an IC50 of 54 nM. HCT116 can inhibit the N-terminal methylation level of NTMT1/2 substrates in HCT116 cells, and is used for the study of NTMT1/2 probes.
    DC432
  • HY-10587A

    Histone Methyltransferase Apoptosis Autophagy Cancer
    BIX-01294 hydrochloride hydrate is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC50 of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells .
    BIX-01294 hydrochloride hydrate
  • HY-122635A

    Histone Demethylase Neurological Disease
    T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons .
    T-448
  • HY-139664
    GSK-3685032
    5+ Cited Publications

    DNA Methyltransferase Cancer
    GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
    GSK-3685032
  • HY-109169B
    Bomedemstat hydrochloride
    3 Publications Verification

    IMG-7289 hydrochloride

    Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
    Bomedemstat hydrochloride
  • HY-170523

    SARS-CoV DNA Methyltransferase Infection
    RU-0415529 is an orally active inhibitor for SARS-CoV-2 nonstructural protein 14 (NSP14) with an IC50 of 356 nM. RU-0415529 binds to the SAH-stabilized cap binding pocket, inhibits viral RNA methylation and the viral replication. RU-0415529 exhibits anti-infectious activity in mouse models .
    RU-0415529
  • HY-109169C

    IMG-7289 dihydrochloride

    Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
    Bomedemstat dihydrochloride
  • HY-109169
    Bomedemstat
    3 Publications Verification

    IMG-7289

    Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
    Bomedemstat
  • HY-10586
    5-Azacytidine
    Maximum Cited Publications
    102 Publications Verification

    Azacitidine; 5-AzaC; Ladakamycin

    Organoid Nucleoside Antimetabolite/Analog DNA Methyltransferase Bacterial Autophagy Antibiotic Infection Cancer
    5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes . 5-Azacytidine induces cell autophagy .
    5-Azacytidine
  • HY-111558
    Bobcat339
    15+ Cited Publications

    DNA Methyltransferase TET Protein Cancer
    Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription .
    Bobcat339
  • HY-111558A
    Bobcat339 hydrochloride
    15+ Cited Publications

    DNA Methyltransferase TET Protein Cancer
    Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription .
    Bobcat339 hydrochloride
  • HY-13599
    Cladribine
    5+ Cited Publications

    2-Chloro-2′-deoxyadenosine; CldAdo; 2CdA

    Adenosine Deaminase Apoptosis Cardiovascular Disease Cancer
    Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis .
    Cladribine
  • HY-113039

    (S)-2-Hydroxyglutaric acid

    Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite Cancer
    L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively .
    L-2-Hydroxyglutaric acid
  • HY-109169A
    Bomedemstat ditosylate
    3 Publications Verification

    IMG-7289 ditosylate

    Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
    Bomedemstat ditosylate
  • HY-13642
    RG108
    5+ Cited Publications

    N-Phthalyl-L-tryptophan

    DNA Methyltransferase Cancer
    RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences .
    RG108
  • HY-122635

    Histone Demethylase Neurological Disease
    T-448 free base is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons .
    T-448 free base
  • HY-W015114

    (S)-2-Hydroxyglutaric acid disodium

    Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite Cancer
    L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively .
    L-2-Hydroxyglutaric acid disodium
  • HY-18684

    5'-Isobutylthioadenosine; 5'-Deoxy-5'-isobutylthioadenosine

    Nucleoside Antimetabolite/Analog HSV Parasite Infection Metabolic Disease Cancer
    SIBA (5'-Isobutylthioadenosine) is a transmethylation inhibitor (SAH (HY-19528) analogue), with potent anti-proliferative activity. SIBA reversibly inhibits the production of HSV-1 by blocking methylation, specifically by blocking the 5' end-capping of viral mRNA. SIBA also inhibits the growth of tumour cells in vitro and metastatic spread in vivo. SIBA can be used in cancer, HSV-1 infection and anti-malaria studies .
    SIBA
  • HY-139664A

    DNA Methyltransferase Cancer
    (R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
    (R)-GSK-3685032
  • HY-13599R

    2-Chloro-2′-deoxyadenosine (Standard); CldAdo (Standard); 2CdA (Standard)

    Reference Standards Adenosine Deaminase Apoptosis Cardiovascular Disease Cancer
    Cladribine (Standard) is the analytical standard of Cladribine. This product is intended for research and analytical applications. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis .
    Cladribine (Standard)
  • HY-116971

    Histone Methyltransferase Apoptosis Cancer
    DCG066 is an inhibitor of lysine methyltransferase G9a. DCG066 can bind directly to G9a and inhibit methyltransferase activity in vitro. DCG066 decreases di-methylation levels of histone H3 lysine 9 (H3K9Me2), inhibits cell proliferation and induces cell apoptosis. DCG066 displays low cytotoxicity in leukemia cell lines with high levels of G9a expression, including K562 .
    DCG066
  • HY-W004883

    5A-DMP

    E1/E2/E3 Enzyme DNA/RNA Synthesis Cancer
    3-Amino-4,6-dimethylpyridine (5A-DMP) is a UHRF1 inhibitor that targets the Arg-binding cavity site within the UHRF1 TTD domain. 3-Amino-4,6-dimethylpyridine disrupts the interaction between UHRF1 and LIG1, interfering with DNA methylation, and can be utilized in cancer research .
    3-Amino-4,6-dimethylpyridine

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