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Results for "

histone methylation

" in MedChemExpress (MCE) Product Catalog:

45

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4

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10

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4

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1

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Targets Recommended:
Cat. No. 상품명 Target 연구분야 Chemical Structure
  • HY-W015114
    L-2-Hydroxyglutaric acid disodium

    (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-B1018A
    Phenelzine sulfate
    5+ Cited Publications

    		 Monoamine Oxidase GABA Receptor Histone Demethylase Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Phenelzine sulfate, an antidepressant agent, is an irreversible and orally active monoamine oxidase (MAO-A and MAO-B) inhibitor. Phenelzine sulfate inhibits GABA transaminase and primary amine oxidase (PrAO), and sequester reactive aldehydes. Phenelzine sulfate also inhibits LSD1 (Ki: 5.6 μM) and suppresses oxidative stress and lipogenesis. Phenelzine sulfate elevates neurotransmitters (serotonin, norepinephrine, dopamine). Phenelzine sulfate is studied in neurological, metabolic and cancer diseases for depression and anxiety disorders, stroke, spinal cord injury, traumatic brain injury, multiple sclerosis, Parkinson’s disease, Alzheimer’s disease, inflammatory pain, obesity and prostate cancer .
    Phenelzine sulfate
  • 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-102047B
    KDOAM-25 citrate
    5+ Cited Publications

    		 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-113039
    L-2-Hydroxyglutaric acid

    (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-160924
    MS147

    		PROTACs BMI1 E1/E2/E3 Enzyme Histone Methyltransferase Cancer
    MS147 is a VHL-based PROTAC degrader of BMI1 and RING1B (polycomb repressive complex 1 core components). MS147 directly binds EED and VHL E3 ligase, recruiting the ligase to the EED-BMI1/RING1B complex to induce time-dependent, ubiquitination-mediated degradation of BMI1 and RING1B. MS147 reduces histone H2A Lys119 mono-ubiquitination without altering histone H3 Lys27 tri-methylation and inhibits cancer cells proliferation. MS147 can be used for the research of cancer, such as chronic myelogenous leukemia and b-cell lymphoma . (Pink: BMI1/RING1B ligand (HY-183634); Blue: VHL ligand (HY-125845); Black: linker)
    MS147
  • HY-N6625
    Chlorothalonil
    1 Publications Verification

    		 Environmental Pollutants Estrogen Receptor/ERR Fungal Infection
    Chlorothalonil is a broad-spectrum foliar fungicide with oral activity. Chlorothalonil can be used to combat fungal diseases in vegetable and crop leaves. Chlorothalonil can alter the microbial community in the soil. Chlorothalonil inhibits spermatogenesis. Chlorothalonil can cause intestinal epithelial barrier dysfunction and fetal toxicity .
    Chlorothalonil
  • HY-141539
    SETDB1-TTD-IN-1
    5 Publications Verification

    		 Histone Methyltransferase Akt Cancer
    SETDB1-TTD-IN-1 is a SETDB1 methyltransferase activator and SETDB1-TTD competitive inhibitor (Kd of 88 nM), and selectivity for SETDB1-TTD over other tudor and bromodomain proteins. SETDB1-TTD-IN-1 stimulates methyltransferase activity via increased catalytic activity, promotes Akt1 Lys64 methylation, Akt1 Thr308 phosphorylation and activation. SETDB1-TTD-IN-1 prevents SETDB1-TTD-histone H3 peptide association, induces global gene expression changes, exhibits cellular target engagement, and acts as a tool compound for SETDB1-TTD function exploration. SETDB1-TTD-IN-1 can be used for the research of breast cancer .
    SETDB1-TTD-IN-1
  • HY-122182
    OTS193320

    		Histone Methyltransferase Apoptosis Cancer
    OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX .
    OTS193320
  • HY-175802
    HBI-2375

    HYBI-084

    		 WDR5 Potassium Channel Inflammation/Immunology Cancer
    HBI-2375 (HYBI-084) is a brain-penetrant WDR5 inhibitor with an IC50 of 4.48 nM. HBI-2375 binds to the WINR5 and disrupts MLL1-WDR5 protein-protein interactions. HBI-2375 inhibits cancer cells proliferation and shows anti-tumor activity in AML mouse models, and increases tumor CD8 + cytotoxic T lymphocyte infiltration. HBI-2375 inhibits hERG with an IC50 of 17 µM .
    HBI-2375
  • HY-121095
    Bizine

    		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-P2258
    Histone H3 (1-34)

    		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-P2254
    H3K27(Me3) (15-34)

    		Histone Methyltransferase Cancer
    H3K27(Me3) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) .
    H3K27(Me3) (15-34)
  • HY-102047
    KDOAM-25

    		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-W015114R
    L-2-Hydroxyglutaric acid disodium (Standard)

    (S)-2-Hydroxyglutaric acid disodium (Standard)

    		 Reference Standards Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite Cancer
    L-2-Hydroxyglutaric acid (disodium) (Standard) is the analytical standard of L-2-Hydroxyglutaric acid (disodium). This product is intended for research and analytical applications. 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 (Standard)
  • HY-175988
    DNMT/HDAC-IN-2

    		DNA Methyltransferase HDAC Cancer
    DNMT/HDAC-IN-2 (Compound Y7) is a DNMT and HDAC inhibitor with IC50 values for DNMT1, HDAC1, and HDAC6 of 365, 0.2, and 8.91 nM respectively. DNMT/HDAC-IN-2 inhibits the proliferation of breast cancer cells. DNMT/HDAC-IN-2 significantly reduces tumor growth in xenografts and transgenic breast cancer mouse models. DNMT/HDAC-IN-2 can be used for the study of breast cancer .
    DNMT/HDAC-IN-2
  • HY-W014004
    m-Carboxycinnamic acid bishydroxamide

    CBHA

    		 HDAC Apoptosis Others Cancer
    m-Carboxycinnamic acid bishydroxamide (CBHA) is a histone deacetylase inhibitor. m-Carboxycinnamic acid bishydroxamide modulates histone acetylation sites, alters DNA methylation and epigenetic status, increases global histone acetylation, alleviates transcription repression, and facilitates chromatin remodelling. m-Carboxycinnamic acid bishydroxamide can be used for the research of cloned embryo development and epigenetic regulation .
    m-Carboxycinnamic acid bishydroxamide
  • HY-103641C
    Octyl-α-hydroxyglutarate

    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-P2255
    H3K4(Me) (1-20)

    		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
    H3K4(Me3) (1-20)

    		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-P2556
    Histone H3 (21-44)

    		Biochemical Assay Reagents Others
    Histone H3 (21-44), derived from histone H3 21-44 amino acids, is usually used as a substrate (such as protein arginine methyltransferases) for methylation assays .
    Histone H3 (21-44)
  • HY-102047A
    KDOAM-25 trihydrochloride

    		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-116971
    DCG066

    		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-178114
    SKLB-0124

    		Histone Methyltransferase Apoptosis Cancer
    SKLB-0124 is a selective PRMT6 degrader with DC50s of 15.4 μM and a 16.4 μM in HCC827 and MDA-MB-435 cells. SKLB-0124 does not degrade PRMT1 or PRMT8. SKLB-0124 exhibits an IC50 on PRMT6 of 1.6 μM. SKLB-0124 induces proteasome dependent degradation of PRMT6 and significantly inhibits the proliferation. SKLB-0124 effectively induces apoptosis and cell cycle arrest. SKLB-0124 can be used for the studies of lung cancer and breast cancer .
    SKLB-0124
  • HY-W013500
    (1-Nitroethene-1,2-diyl)dibenzene

    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-10587A
    BIX-01294 hydrochloride hydrate

    		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-121095A
    Bizine dihydrochloride

    		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 dihydrochloride
  • HY-P2252
    H3K27(Me) (15-34)

    		Histone Methyltransferase Cancer
    H3K27(Me) (15-34), a histone peptide, is a repressive chromatin markderived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) .
    H3K27(Me) (15-34)
  • HY-P2253
    H3K27(Me2) (15-34)

    		Histone Demethylase Cancer
    H3K27(Me2) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) .
    H3K27(Me2) (15-34)
  • HY-163592
    PRMT5-IN-43

    		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-163593
    PRMT5-IN-44

    		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-P10570
    [Nle20] H4 peptide (16−23)

    		Histone Methyltransferase Cancer
    [Nle20] H4 peptide (16−23) is a peptide with strong inhibitory activity against histone methyltransferase SETD8 (Kd=0.14 μM), which inhibits SETD8's methylation of histone H4 by competing with SETD8's substrate binding site. [Nle20] H4 peptide (16−23) can be used as a lead compound for anticancer therapy .
    [Nle20] H4 peptide (16−23)
  • HY-W744986
    L-2-Hydroxyglutaric acid-d5 disodium

    (2S)-2-Hydroxyglutaric acid-d5 disodium

    		 Isotope-Labeled Compounds Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite Cancer
    L-2-Hydroxyglutaric acid-d5 disodium ((2S)-2-Hydroxyglutaric acid-d5 disodium) is the deuterium labeled L-2-Hydroxyglutaric acid disodium (HY-W015114). 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-d5 disodium
  • HY-117540
    ZLD10A

    		Histone Methyltransferase Cancer
    ZLD10A is a highly potent and selective EZH2 inhibitor with the activity of inhibiting H3K27 methylation. ZLD10A can inhibit wild-type and mutant EZH2 with nanomolar potency and has more than 1000-fold selectivity for the other 10 histone methyltransferases. ZLD10A inhibited cell proliferation of DLBCL cell lines in a concentration- and time-dependent manner, showing a potential antiproliferative effect. ZLD10A can be used in the study of EZH2 mutant lymphomas .
    ZLD10A
  • HY-15313B
    CBB1007 hydrochloride

    		Histone Demethylase Metabolic Disease Cancer
    CBB1007 hydrochloride is a reversible and selective LSD1 inhibitor with an IC50 of 5.27 µM for human LSD1. CBB1007 hydrochloride significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 hydrochloride shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 hydrochloride is studied in  non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma .
    CBB1007 hydrochloride
  • HY-185051
    OTX-2002

    		mRNA Cancer
    OTX-2002 is an mRNA encoding two bifunctional fusion proteins (ZFBD-MQ1 and ZFBD-KRAB). OTX-2002 targets regulatory elements located within the MYC protection gene domain (IGD) and induces the methylation of DNA and histone, leading to the downregulation of MYC expression.
    OTX-2002
  • HY-182486
    LEM-06

    		Histone Methyltransferase Cancer
    LEM-06 is an NSD2 inhibitor with a human IC50 of 890 μM and 0.8 mM. LEM-06 binds to the histone-tail binding groove of NSD2-SET, inhibiting NSD2-mediated H3K36 histone methyltransferase activity and H3K36 mono-methylation. LEM-06 serves as a hit molecule for further optimization or derivation to explore NSD2 biology. LEM-06 can be used for the research of multiple myeloma .
    LEM-06
  • HY-12970B
    EPZ020411 dihydrochloride

    		Histone Methyltransferase Reactive Oxygen Species (ROS) Apoptosis Neurological Disease Cancer
    EPZ020411 dihydrochloride is a selective, blood-brain barrier-permeable PRMT6 inhibitor with an IC50 of 0.010 μM. EPZ020411 dihydrochloride blocks PRMT6-mediated histone H3R2 methylation, reduces ROS production, and inhibits Apoptosis. EPZ020411 dihydrochloride is applicable to research related to neuropathic pain, colorectal cancer, ototoxicity, hearing loss and glioblastoma .
    EPZ020411 dihydrochloride
  • HY-133567
    SET7-IN-DC21

    		Histone Methyltransferase Infection Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
    SET7-IN-DC21 is a selective, potent SET7 inhibitor (IC50 = 15.93 μM; KD = 18.00 μM). SET7-IN-DC21 has good selectivity for several other epigenetic targets, such as SUV39H1, G9a, NSD1, DOT1L and MOF. SET7-IN-DC21 can be used for the researches of cancer, infection, inflammation, metabolic and cardiovascular disease, such as breast cancer .
    SET7-IN-DC21
  • HY-124660A
    A-395N

    		Endogenous Metabolite Others
    A-395N serves as a control probe for A-395, a highly potent and selective chemical probe targeting the polycomb protein EED, a key player in Polycomb repressive complex 2 (PRC2) responsible for transcriptional repression via histone H3K27 methylation. While A-395N bears structural similarities to A-395, it demonstrates no pharmacological activity in biochemical or cellular assays, making it an ideal control compound.
    A-395N
  • HY-114510
    PRMT/HKMT-IN-1

    		Discoidin Domain Receptor Histone Acetyltransferase Sirtuin Fungal Apoptosis Infection Cancer
    PRMT/HKMT-IN-1 is an epigenetic multi-target protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) inhibitor. PRMT/HKMT-IN-1 inhibits Aspergillus nidulans RmtA with an IC50 of 29 μM. PRMT/HKMT-IN-1 inhibits human PRMT1, p300/CBP HAT, CARM1, SET7, SIRT1 and SIRT2. PRMT/HKMT-IN-1 inhibits methylation of histone H3K4, H4R3, and H3R17 residues. CBP/p300-IN-23 induces apoptosis, arrests cell cycle in S phase, and triggers granulocytic differentiation in leukemia cells. PRMT/HKMT-IN-1 can be used for the research of leukemia .
    PRMT/HKMT-IN-1
  • HY-181781
    LSD1-IN-48

    		Histone Demethylase CD44 Apoptosis Cancer
    LSD1-IN-48 is a tranylcypromine-pyrimidine derivative and selective LSD1 inhibitor with a human IC50 of 7.87 nM. LSD1-IN-48 increases H3K4me1/2 histone methylation levels. LSD1-IN-48 induces apoptosis, upregulates CD86, downregulates SOX2 and CD44, inhibits proliferation in cancer cells. LSD1-IN-48 can be used for the research of acute myeloid leukemia .
    LSD1-IN-48
  • HY-179650
    NSD2-PWWP1-IN-5

    		Histone Methyltransferase Apoptosis Cancer
    NSD2-PWWP1-IN-5 (Compound 13) is an effective NSD2-PWWP1 inhibitor with a Kd value of 78 nM. NSD2-PWWP1-IN-5 competitively blocks the recognition of H3K36me2 and DNA by NSD2-PWWP1, thereby weakening its binding ability to nucleosomes. NSD2-PWWP1-IN-5 inhibits the proliferation of U2OS osteosarcoma cells and induces cell cycle arrest and apoptosis. NSD2-PWWP1-IN-5 can be used for the study of osteosarcoma .
    NSD2-PWWP1-IN-5
  • HY-115619
    EPZ004777 formate

    		Histone Methyltransferase Apoptosis Cancer
    EPZ004777 formate is an effective and selective DOT1L inhibitor, with IC50 being 0.4 nM. EPZ004777 formate reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 formate selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 formate can be used for the study of leukemia .
    EPZ004777 formate
  • HY-N18236
    3β-Acetoxyl-atractylenolide I

    		Histone Demethylase Cancer
    3β-Acetoxyl-atractylenolide I is a LSD1 inhibitor with an IC50 of 57 μM. 3β-Acetoxyl-atractylenolide I blocks tumor growth, metastasis and invasion. 3β-Acetoxyl-atractylenolide I is used in the research of various cancers including prostate cancer, breast cancer, neuroblastoma, gastric cancer, colon cancer, bladder cancer, esophageal cancer, acute myeloid leukemia and retinoblastoma .
    3β-Acetoxyl-atractylenolide I

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