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methylations

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143

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3

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2

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2

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25

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16

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8

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-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-111130

    Histamine Receptor mAChR Neurological Disease Cancer
    Methapyrilene is a histamine antagonist, a pyridine chemical with anticholinergic activity. Methapyrilene can cause target organ-specific epigenetic alterations, such as a decrease in DNA methylation levels. Methapyrilene induces hepatocellular carcinoma in rats .
    Methapyrilene
  • 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-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-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-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-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-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-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-W125425

    HIV METTL3 Infection
    Methyl piperazine-2-carboxylate (compound 4) is a potent METTL3/METTL14/WTAP activator. Methyl piperazine-2-carboxylate increases HIV-1 p24 virion production. Methyl piperazine-2-carboxylate increases the N6-adenosine methylation level in the viral RNA genome .
    Methyl piperazine-2-carboxylate
  • HY-161334

    Histone Methyltransferase Apoptosis Cancer
    CARM1-IN-4 (compound 11f) is a potent CARM1 inhibitor with IC50s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity .
    CARM1-IN-4
  • HY-D1603

    Fluorescent Dye Others
    BODIPY FL-EDA is a widely used fluorescent dye for quantitative analysis of nucleotides. BODIPY FL-EDA is an aliphatic amine analog that can react with aldehydes and ketones. BODIPY FL-EDA can be used to detect both modified and unmodified deoxynucleotides and to determine DNA damage and genomic DNA methylation through capillary electrophoresis with laser-induced fluorescence (CE-LIF). Additionally, it can be used for quantifying intracellular ATP levels. The excitation wavelength is 500 nm, and the emission wavelength is 510 nm .
    BODIPY FL-EDA
  • HY-W025074

    Sirtuin Histone Methyltransferase Cancer
    BML-278 is a SIRT1 activator (EC150: 1 μM). BML-278 increases H3K9 methylation and inhibits H3K9 acetylation in both the paternal and maternal pronucleus. BML-278 improves early embryonic development. BML-278 arrests the cell cycle at the G1/S phase, and reduces senescence in primary human mesenchymal cells. BML-278 reduces tubulin acetylation in U937 cells. BML-278 also increases mitochondrial density in murine C2C12 myoblasts .
    BML-278
  • HY-102047

    Histone Demethylase Cancer
    KDOAM-25 is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells .
    KDOAM-25
  • HY-102047A

    Histone Demethylase Cancer
    KDOAM-25 trihydrochloride is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells .
    KDOAM-25 trihydrochloride
  • HY-102047B
    KDOAM-25 citrate
    5 Publications Verification

    Histone Demethylase Cancer
    KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells .
    KDOAM-25 citrate
  • 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-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-16513
    VAL-083
    1 Publications Verification

    Dianhydrodulcitol; Dianhydrogalactitol

    DNA Alkylator/Crosslinker Cancer
    VAL-083 is an alkylating agent that creates N7 methylation on DNA, with antitumor activity.
    VAL-083
  • HY-153421

    Histone Methyltransferase Cancer
    PRMT5-IN-28 (compound 36) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) enzyme. Protein arginine methylation is a common post-translational modification involved in gene transcription, mRNA splicing, DNA repair, protein cellular localization, cell fate determination and signal transduction, etc. Abnormal PRMT5 can promote cancer cell proliferation, resist apoptosis, enhance invasion and metastasis, and affect immune escape .
    PRMT5-IN-28
  • 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-N0739
    Betaine chloride
    3 Publications Verification

    Endogenous Metabolite Others
    Betaine hydrochloride is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns.
    Betaine chloride
  • HY-22385A

    Monoamine Oxidase Neurological Disease
    Salsolidine hydrochloride, a tetrahydroisoquinoline alkaloid, acts as a stereoselective competitive MAO A (monoamine oxidase A) inhibitor.
    Salsolidine hydrochloride
  • HY-P10828

    Virus Protease Infection Inflammation/Immunology
    MAPI is a polypeptide irreversible 3C cysteine protease (SV3CP) inhibitor. MAPI inhibits SV3CP by covalently binding its C-terminal Michael-acceptor extension to the active site thiol of SV3CP Cys 139. MAPI is promising for research of noroviruses infection .
    MAPI
  • HY-113352

    Endogenous Metabolite Others
    7-Methylguanine is a metabolite of DNA methylation. It can be generated by methylating agents, and used as a probe of protein–DNA interactions and a key component of DNA sequencing method.
    7-Methylguanine
  • HY-W012078
    5-Methyl-2'-deoxycytidine
    2 Publications Verification

    5-Methyldeoxycytidine

    DNA Methyltransferase Endogenous Metabolite Others
    5-Methyl-2'-deoxycytidine in single-stranded DNA can act in cis to signal de novo DNA methylation .
    5-Methyl-2'-deoxycytidine
  • 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-W850994

    Tridecyl beta-D-maltopyranoside

    Biochemical Assay Reagents Others
    Tridecyl β-D-maltopyranoside is a synthetic sugar, modified by fluorination and methylation. Carbohydrates can be used for the synthesis of glycosylated proteins (biosynth: W-204093).
    Tridecyl β-D-maltopyranoside
  • 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-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-103641C

    Octyl-2-HG

    Histone Methyltransferase Cancer
    Octyl-α-hydroxyglutarate (octyl-2-HG) increases histone methylation and enhances viability of LMP1-negative NPC cells .
    Octyl-α-hydroxyglutarate
  • HY-133605

    Bacterial Others
    Tetrachloroveratrole is one of the biodegradation products of bacterial O-methylation of Tri- and Tetra chloroguaiacols. The Tri- and Tetra chloroguaiacols are formed during bleaching of wood pulp in the paper manufacturing industry .
    Tetrachloroveratrole
  • 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-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-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-147101

    PARP Cancer
    SK-575-NEG (compound 28), a methylation counterpart of SK-575, is synthesized by methylation of the amino group of piperidine-2,6-dione in SK-575 as an control compound. SK-575-NEG is strongly bound to PARP1, with an IC50 of 2.64 nM. SK-575-NEG was completely ineffective in inducing PARP1 degradation in MDA-MB-436 and Capan-1 cells at concentrations up to 1 μM .
    SK-575-NEG
  • HY-163593

    Histone Methyltransferase Cancer
    PRMT5-IN-44 (compound 12) is a PRMT5 inhibitor. PRMT5-IN-44 can be used in cancer research .
    PRMT5-IN-44
  • HY-163592

    Histone Methyltransferase Cancer
    PRMT5-IN-43 (compound 4A) is a PRMT5 inhibitor. PRMT5-IN-43 can be used in cancer research .
    PRMT5-IN-43
  • HY-P2255

    Histone Demethylase Others
    H3K4(Me) (1-20), a histone peptide. H3K4me is an intricately regulated posttranslational modification, which is broadly associated with enhancers and promoters of actively transcribed genomic loci .
    H3K4(Me) (1-20)
  • HY-P2257

    Histone Demethylase Others
    H3K4(Me3) (1-20) is a histone peptide. Trimethylation of histone H3 on lysine 4 (H3K4 me3) is found in active euchromatin but not in silent heterochromatin .
    H3K4(Me3) (1-20)
  • HY-P2258

    Histone Methyltransferase Others
    Histone H3 (1-34) is a peptide derived from human histone isotype 3.1. Histones are the main protein components of eukaryotic chromatin. Histone variants and histone modifications modulate chromatin structure, ensuring the precise operation of cellular processes associated with genomic DNA .
    Histone H3 (1-34)
  • 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-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-103236
    NSC232003
    3 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-Y0678

    TRIMETHYL PHLOROGLUCINOL

    Endogenous Metabolite Neurological Disease
    1,3,5-Trimethoxybenzene is a key component of the Chinese rose odor. 1,3,5-Trimethoxybenzene is synthesized in three successive methylation steps from phloroglucinol, the initial precursor .
    1,3,5-Trimethoxybenzene
  • 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-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-133604

    Drug Intermediate Others
    3,4,5-Trichloroveratrole is one of the biodegradation products of bacterial O-methylation of Tri- and Tetra chloroguaiacols. The Tri- and Tetra chloroguaiacols are formed during bleaching of wood pulp in the paper manufacturing industry .
    3,4,5-Trichloroveratrole
  • 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

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