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methyltransferase activity

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Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-A0004
    Decitabine
    Maximum Cited Publications
    168 Publications Verification

    5-Aza-2'-deoxycytidine; 5-AZA-CdR; NSC 127716

    DNA Methyltransferase Apoptosis Nucleoside Antimetabolite/Analog Cancer
    Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity .
    Decitabine
  • HY-10442
    3-Deazaneplanocin A
    30+ Cited Publications

    DZNep; 3-Deazaneplanocin

    Histone Methyltransferase S-adenosylhomocysteine hydrolase (SAHH) Orthopoxvirus Infection Metabolic Disease Inflammation/Immunology Cancer
    3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor . 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity .
    3-Deazaneplanocin A
  • HY-101564
    Onametostat
    5+ Cited Publications

    JNJ-64619178

    Histone Methyltransferase Cancer
    Onametostat (JNJ-64619178) is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. Onametostat has potent activity in lung cancer .
    Onametostat
  • HY-12186

    DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride

    Histone Methyltransferase S-adenosylhomocysteine hydrolase (SAHH) Orthopoxvirus Infection Inflammation/Immunology Cancer
    3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor . 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor . 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities .
    3-Deazaneplanocin A hydrochloride
  • HY-B2194
    γ-Oryzanol
    5+ Cited Publications

    DNA Methyltransferase Metabolic Disease Cancer
    γ-Oryzanol is a potent DNA methyltransferases (DNMTs) inhibitor in the striatum of mice. γ-Oryzanol significantly inhibits the activities of DNMT1 (IC50=3.2 μM), DNMT3a (IC50=22.3 μM).
    γ-Oryzanol
  • HY-107777
    LLY-283
    5+ Cited Publications

    Histone Methyltransferase Cancer
    LLY-283, a chemical probe, 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 .
    LLY-283
  • HY-147525
    PROTAC EZH2 Degrader-1
    1 Publications Verification

    PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes .
    PROTAC EZH2 Degrader-1
  • HY-10930
    UNC0321
    2 Publications Verification

    Histone Methyltransferase GCGR Apoptosis Cancer
    UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 has anti-apoptotic activity and has potential application in diabetic vascular complications .
    UNC0321
  • HY-148458

    Histone Methyltransferase Cancer
    EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 .
    EZH2-IN-14
  • HY-118563

    ICMT Apoptosis Ras Cancer
    Farnesylthioacetic acid is a competitive, non-substrate inhibitor of Prenylcysteine α-carboxyl methyltransferase. It acts as a non-substrate competitive inhibitor of Arabidopsis thaliana Prenylcysteine α-carboxyl methyltransferase and blocks methyltransferase activity. Farnesylthioacetic acid does not inhibit protein farnesyltransferase activity in Arabidopsis. It induces Apoptosis. Farnesylthioacetic acid regulates the subcellular localization of Ras protein, reducing the proportion of cytoplasmic Ras protein without disrupting membrane binding. It enhances ABA-induced seed dormancy, delays seed germination, and promotes maximum stomatal closure at lower exogenous ABA concentrations. Farnesylthioacetic acid can be used in studies related to promyelocytic leukemia .
    Farnesylthioacetic acid
  • HY-15647
    BRD9539
    1 Publications Verification

    Histone Methyltransferase Cancer
    BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1 .
    BRD9539
  • HY-15228
    RX-3117
    2 Publications Verification

    TV-1360; Fluorocyclopentenylcytosine

    Nucleoside Antimetabolite/Analog Apoptosis Cancer
    RX-3117 (TV-1360) is a potent and orally active anticancer and antimetaboliteagent. RX-3117 inhibits DNA methyltransferase 1 (DNMT1). RX-3117 shows antiproliferative and anti-tumour activity. RX-3117 induces cell cycle arrest at S phase and apoptosis .
    RX-3117
  • HY-141429A
    AS-99 TFA
    2 Publications Verification

    Histone Methyltransferase Apoptosis Cancer
    AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
    AS-99 TFA
  • HY-A0004R

    5-Aza-2'-deoxycytidine (Standard); 5-AZA-CdR (Standard); NSC 127716 (Standard)

    Reference Standards DNA Methyltransferase Apoptosis Nucleoside Antimetabolite/Analog Cancer
    Decitabine (Standard) is the analytical standard of Decitabine. This product is intended for research and analytical applications. Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity .
    Decitabine (Standard)
  • HY-111213

    Histone Methyltransferase Cancer
    PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity .
    PRMT5-IN-20
  • HY-100757

    Histone Methyltransferase Cancer
    CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity .
    CPUY074020
  • 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-N11722

    Apoptosis NF-κB Keap1-Nrf2 AMPK Autophagy SARS-CoV DNA Methyltransferase Infection Inflammation/Immunology Endocrinology
    Panduratin A is an orally active natural compound with multiple pharmacological activities. By specifically inhibiting the NF-κB signaling pathway, Panduratin A exerts potent anti-inflammatory and antioxidant effects in intestinal and vascular inflammation models. Panduratin A exerts a definite protective effect against Colistin (HY-113678)-induced nephrotoxicity by alleviating oxidative stress, improving mitochondrial dysfunction and inhibiting cell apoptosis. Panduratin A activates autophagy via an AMPK-dependent pathway and exhibits anti-tuberculosis activity. Panduratin A exerts antiviral effects by inhibiting the methyltransferase (DNA Methyltransferase) of SARS-CoV-2 .
    Panduratin A
  • HY-156048
    Trifluoromethyl-tubercidin
    2 Publications Verification

    TFMT

    Influenza Virus Infection
    Trifluoromethyl-tubercidin (TFMT) is an inhibitor of 2'-O-ribose methyltransferase 1 (MTr1). Trifluoromethyl-tubercidin can inhibit the replication of influenza A and B viruses by interfering with the cap-snatching process of the influenza virus. Trifluoromethyl-tubercidin has antiviral activity and low toxicity .
    Trifluoromethyl-tubercidin
  • 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-121093

    Histone Methyltransferase Cancer
    DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC50 value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity .
    DC-S239
  • HY-W578275

    Nucleoside Antimetabolite/Analog Cancer
    3′-O-Methylcytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities .
    3′-O-Methylcytidine
  • HY-W115186

    Nucleoside Antimetabolite/Analog Phosphoramidites Cancer
    DMT-2'-OMe-Bz-C is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities .
    DMT-2'-OMe-Bz-C
  • HY-W130466

    Nucleoside Antimetabolite/Analog Others Cancer
    N4-Methylcytidine (Nsc518744) is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities .
    N4-Methylcytidine
  • HY-141430

    Histone Methyltransferase Cancer
    AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC50=0.6 μM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the Kd value of 0.78 μM .
    AS-85
  • HY-W114787

    Nucleoside Antimetabolite/Analog Cancer
    N4-Benzoyl-2’-O-methylcytidine is a natural cytidine nucleoside analog. Cytidine analogs have the mechanism of inhibiting DNA methyltransferase (such as Zebularine (HY-13420)) and have potential antimetabolite and antitumor activities .
    N4-Benzoyl-2’-O-methylcytidine
  • HY-154414

    Nucleoside Antimetabolite/Analog Phosphoramidites Cancer
    2’-Fluoro-2’-deoxy-ara-C(Bz)-3’-phosphoramidite is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities .
    2’-Fluoro-2’-deoxy-ara-C(Bz)-3’-phosphoramidite
  • HY-128579

    Histone Methyltransferase Cancer
    DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity .
    DW14800
  • HY-111367

    Amine N-methyltransferase Neurological Disease Metabolic Disease Cancer
    MS2734 is a inhibitor of nicotinamide N-methyltransferase (NNMT). MS2734 potently inhibits the methyltransferase activity of human NNMT (hNNMT) with an IC50 value of 14 μM. MS2734 can be used for the study of obesity, diabetes, Parkinson's disease, and various cancers with high NNMT expression .
    MS2734
  • HY-104039

    Nucleoside Antimetabolite/Analog Phosphoramidites Cancer
    2'-Deoxy-5'-O-DMT-5-methylcytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities .
    2'-Deoxy-5'-O-DMT-5-methylcytidine
  • HY-172614

    RK-552

    Histone Methyltransferase Apoptosis Cancer
    RK-0080552 (RK-552) is a NSD2 inhibitor with an IC50 of 0.11 μM, and it exhibits selectivity over histone methyltransferases G9a (IC50: 1.2 μM) and SET7/9 (IC50: >50 μM). RK-0080552 functionally inhibits NSD2 histone methyltransferase activity, reduces the dimethylation level of histone H3 lysine 36, suppresses IRF4 transcription, induces apoptosis and triggers cell death. RK-0080552 inhibits the growth of xenograft tumors and prolongs host survival. RK-0080552 is available for the research of multiple myeloma .
    RK-0080552
  • HY-100869

    WDR5 Cancer
    MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM .
    MM-589
  • HY-141429
    AS-99 free base
    2 Publications Verification

    Histone Methyltransferase Apoptosis Cancer
    AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
    AS-99 free base
  • HY-122936

    Histone Methyltransferase Keap1-Nrf2 Sirtuin Cardiovascular Disease Cancer
    Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .
    Tanshindiol C
  • HY-122427

    Nucleoside Antimetabolite/Analog Cancer
    Xylocytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities .
    Xylocytidine
  • HY-154150

    Nucleoside Antimetabolite/Analog Cancer
    N-(1-Oxopropyl)cytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities .
    N-(1-Oxopropyl)cytidine
  • HY-101904

    Nucleoside Antimetabolite/Analog Others
    2-Chloro-2'-deoxycytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities .
    2-Chloro-2'-deoxycytidine
  • HY-152822

    Nucleoside Antimetabolite/Analog Others
    5-Iodo-2’-O-methylcytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities .
    5-Iodo-2’-O-methylcytidine
  • HY-152483

    Nucleoside Antimetabolite/Analog Others
    N4,N4-Dimethylarabinocytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities .
    N4,N4-Dimethylarabinocytidine
  • HY-W128788A

    Nucleoside Antimetabolite/Analog Others
    2’-Deoxy-2’-fluoro-b-D-arabinocytidine(hydrochloride) is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities .
    2’-Deoxy-2’-fluoro-b-D-arabinocytidine hydrochloride
  • HY-152763

    Nucleoside Antimetabolite/Analog Others
    2’-Deoxy-2’-fluoro-5-methylcytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities .
    2’-Deoxy-2’-fluoro-5-methylcytidine
  • HY-136809

    Histone Methyltransferase Cancer
    PRMT6-IN-2 (compound 2) is a dual inhibitor of protein arginine methyltransferase PRMT6 and CARM1 with an IC50 of 30 nM. PRMT6 is abnormally expressed in many cancer cells, and PRMT6-IN-2-based derivatives have potential anticancer activity.
    PRMT6-IN-2
  • 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-152714

    Nucleoside Antimetabolite/Analog Others
    5-Formyl-2’-O-methylcytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities .
    5-Formyl-2’-O-methylcytidine
  • HY-177963

    DNA Methyltransferase Inflammation/Immunology
    NV914 is an inhibitor of FTSJ1 (tryptophan tRNA-specific 2'-O-methyltransferase) that inhibits the methyltransferase activity of FTSJ1, induces translational readthrough of premature termination codons, and enables genes carrying nonsense mutations to synthesize full-length proteins. NV914 belongs to translational readthrough-inducing compounds (TRIDs). NV914 exhibits translational readthrough activity against nonsense mutations in in vitro systems, does not induce readthrough of natural termination codons, and restores CFTR protein expression. NV914 shows favorable acute oral tolerance in mice, with low health risks and good safety profiles. NV914 is applicable to research related to cystic fibrosis and Shwachman-Diamond syndrome .
    NV914
  • HY-100869A

    WDR5 Cancer
    MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM .
    MM-589 TFA
  • HY-141429C

    Histone Methyltransferase Apoptosis Cancer
    AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
    AS-99
  • HY-176534

    Histone Methyltransferase Cancer
    PRMT5-IN-52 (Compound 17) is a non-nucleoside Protein Arginine Methyltransferase 5 (PRMT5) inhibitor with inhibitory rates of 20.2% at 10 μM. PRMT5-IN-52 has potent antitumor activity, promising for research of cancers, including lung, prostate cancer, and colorectal carcinoma .
    PRMT5-IN-52
  • HY-144188

    Histone Methyltransferase Cancer
    PRMT5-IN-17 (Compound 6) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .
    PRMT5-IN-17
  • HY-144187

    Histone Methyltransferase Cancer
    PRMT5-IN-16 (Compound 20) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .
    PRMT5-IN-16

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