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Pathways Recommended: Epigenetics
Results for "

Epigenetic Inhibitors

" in MedChemExpress (MCE) Product Catalog:

60

Inhibitors & Agonists

2

Screening-Bibliotheken

1

Biochemical Assay Reagents

2

Peptides

9

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Products

3

Isotope-Labeled Compounds

Art. -Nr. Produktname Target Forschungsgebiete Chemical Structure
  • HY-10586
    5-Azacytidine
    Maximum Cited Publications
    128 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-N0401A
    (Z)-Ligustilide
    5 Publications Verification

    Bacterial Estrogen Receptor/ERR FATP Infection Metabolic Disease Cancer
    (Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6 . (Z)-Ligustilide is orally active, it inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) . (Z)-Ligustilide is also able to reactivate ERα, has epigenetic regulation, and is used in the study of tamoxifen-resistant breast cancer .
    (Z)-Ligustilide
  • HY-16438
    RRx-001
    15+ Cited Publications

    Nibrozetone

    CD47 Apoptosis Parasite Infection Inflammation/Immunology Cancer
    RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes agent resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity . RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α . RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity .
    RRx-001
  • HY-103248
    Toyocamycin
    5+ Cited Publications

    Vengicide

    IRE1 Fungal Antibiotic Apoptosis CDK Infection Cancer
    Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC50 value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC50 value of 79 nM .
    Toyocamycin
  • HY-111558
    Bobcat339
    20+ 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-15273
    UNC0638
    10+ Cited Publications

    VSV Histone Methyltransferase Autophagy Influenza Virus Infection Cancer
    UNC0638, a chemical probe, selectively inhibits G9a and GLP histone methyltransferases with IC50 of 15 nM and 19 nM, respectively. UNC0638 inhibits TNBC cell invasion and migration in vitro. UNC0638 is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets .
    UNC0638
  • HY-111558A
    Bobcat339 hydrochloride
    20+ 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-103019
    Enitociclib
    2 Publications Verification

    (+)-BAY-1251152; (+)-VIP152; (S)-Enitociclib

    Drug Isomer CDK Apoptosis DNA/RNA Synthesis Inflammation/Immunology Cancer
    Enitociclib ((+)-BAY-1251152; (+)-VIP152) is a selective CDK9 inhibitor (IC50=3 nM) that inhibits transcriptional elongation by blocking Ser2/Ser5 phosphorylation of RNA polymerase II. Enitociclib specifically depletes key short-lived proteins such as c-MYC, MCL-1 and induces tumor cell apoptosis. Enitociclib also interferes with the production of enhancer RNAs (eRNA) and enhancer-promoter interactions, and downregulates oncogene expression at the epigenetic level. Enitociclib exerts synergistic effects with agents including Bortezomib (HY-10227), Lenalidomide (HY-A0003), Pomalidomide (HY-10984), Venetoclax (HY-15531) and Paclitaxel (HY-B0015), and even reverses paclitaxel resistance. Enitociclib serves as a vital research tool for various malignancies such as double-hit diffuse large B-cell lymphoma, multiple myeloma and pancreatic ductal adenocarcinoma .
    Enitociclib
  • 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-P5285

    Parasite Infection Inflammation/Immunology Cancer
    Lunasin is a bioactive peptide with antioxidant, anti-inflammatory, anticancer and anti-aging properties. Lunasin can be isolated from soybean. Lunasin also has an epigenetic mechanism of action associated with histone acetylation. Lunasin can be internalized into cells and inhibit Oncosphere formation in cancer cells .
    Lunasin
  • 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-162080
    METTL1-WDR4-IN-1
    1 Publications Verification

    DNA Methyltransferase Pyruvate Kinase Cancer
    METTL1-WDR4-IN-1 (Compound 1) is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50 = 144 μM). METTL1-WDR4-IN-1 inhibits the m 7G methyltransferase activity of the METTL1-WDR4 complex, blocking m 7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8 + T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy .
    METTL1-WDR4-IN-1
  • HY-19553

    Epigenetic Reader Domain Inflammation/Immunology
    LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells .
    LP99
  • HY-138830
    TAK-418
    2 Publications Verification

    Histone Demethylase Neurological Disease
    TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM. TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models .
    TAK-418
  • HY-126428
    ZL0580
    1 Publications Verification

    HIV Epigenetic Reader Domain Infection Inflammation/Immunology
    ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter .
    ZL0580
  • HY-162683

    CDK E1/E2/E3 Enzyme Neurological Disease
    (S)-PHA533533 is a CDK2 and CDK5 inhibitor with blood-brain barrier permeability, with IC50 values of 37 nM and 55 nM, respectively. (S)-PHA533533 effectively restores UBE3A expression by downregulating UBE3A-ATS and relieving the epigenetic silencing of paternal UBE3A in mature neurons. (S)-PHA533533 can be used for the research of Angelman syndrome .
    (S)-PHA533533
  • HY-10586R

    Azacitidine (Standard); 5-AzaC (Standard); Ladakamycin (Standard)

    Organoid Reference Standards Nucleoside Antimetabolite/Analog DNA Methyltransferase Bacterial Autophagy Antibiotic Infection Cancer
    5-Azacytidine (Standard) is the analytical standard of 5-Azacytidine. This product is intended for research and analytical applications. 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 (Standard)
  • HY-43515

    Endogenous Metabolite Metabolic Disease
    ESI1 is a small molecule epigenetic silencing inhibitor. ESI1 can trigger the formation of nuclear condensates of key lipid metabolism regulators SREBP1/2, concentrating transcriptional co-activators to drive lipid/cholesterol biosynthesis. ESI1 can promote myelin regeneration in demyelinated animal models and facilitate de novo myelination on regenerating CNS axons, reversing age-related declines in cognitive abilities .
    ESI1
  • HY-19336
    BAZ2-ICR
    2 Publications Verification

    Epigenetic Reader Domain Cancer
    BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe .
    BAZ2-ICR
  • HY-114209
    MRK-740
    2 Publications Verification

    Histone Methyltransferase Cancer
    MRK-740, a chemical probe, is a potent, selective and substrate-competitive PRDM9 histone methyltransferase inhibitor with an IC50 of 80?nM. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 reduces PRDM9-dependent trimethylation of H3K4 (IC50?=?0.8?μM) .
    MRK-740
  • HY-W004924

    Endogenous Metabolite Others
    5-Hydroxymethyluracil is a product of oxidative DNA damage. 5-Hydroxymethyluracil can be used as a potential epigenetic mark enhancing or inhibiting transcription with bacterial RNA polymerase.
    5-Hydroxymethyluracil
  • HY-W015114R

    (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

    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-133083
    BAY-474
    1 Publications Verification

    c-Met/HGFR Cancer
    BAY-474 is a tyrosine-protein kinase c-Met inhibitor. BAY-474 acts as an epigenetics probe .
    BAY-474
  • HY-W014004

    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-116428

    Farnesyl Transferase Ras TGF-β Receptor Apoptosis Cancer
    L-744832 is a farnesyl transferase inhibitor. L-744832 effectively inhibits the farnesylation of H-Ras and N-Ras, but has little effect on K-Ras treatment. L-744832 not only directly targets the oncogenic pathway by inhibiting Ras farnesylation, but also enhances radiosensitivity by restoring TGF-β signaling through epigenetic reprogramming. L-744832 can induce cell cycle arrest and apoptosis. L-744832 can be used in combination therapy studies for Ras-driven tumors such as pancreatic cancer .
    L-744832
  • HY-179557

    Glutathione Peroxidase Reactive Oxygen Species (ROS) Apoptosis Ferroptosis PD-1/PD-L1 Cancer
    iMQT_020 is a selective allosteric SLC1A5_var inhibitor. iMQT_020 disrupts the trimeric assembly of SLC1A5_var, causing metabolic crisis in cancer cells and selectively suppressing their growth. iMQT_020 reduces glutamine anaplerosis and oxidative phosphorylation, resulting in a broad disruption of cancer metabolism. iMQT_020 reduces GSH levels and increases cellular ROS and mitochondrial ROS. iMQT_020 induces apoptosis and ferroptosis. iMQT_020 can epigenetically upregulate PD-L1 expression. iMQT_020 can be used for the study of pancreatic cancer, lung cancer, and colon cancer .
    iMQT_020
  • HY-179427

    Histone Methyltransferase Apoptosis Reactive Oxygen Species (ROS) Cancer
    NSD2/H3K36me2 modulator-1 is an orally active NSD2/H3K36me2 modulator. NSD2/H3K36me2 modulator-1 competitively binds to the SAM pocket of NSD2, potently inhibits NSD2 expression and suppresses H3K36me2 methylation. NSD2/H3K36me2 modulator-1 reverses epithelial-mesenchymal transition (EMT), inhibits cell migration, and induces G0/G1 phase arrest and apoptosis. NSD2/H3K36me2 modulator-1 induces decreased Mitochondrial membrane potential (MMP) and subsequent Reactive oxygen species (ROS) generation. NSD2/H3K36me2 modulator-1 can be used to research the NSD2-targeting epigenetic anticancer strategies for hepatocellular carcinoma (HCC) .
    NSD2/H3K36me2 modulator-1
  • HY-168088

    HDAC DNA Methyltransferase Cancer
    DNMT1/HDAC-IN-1 (compound (R)-23a) is a DNMT1/HDAC dual inhibitor (HDAC1:IC50=0.05 μM), HDAC1 is a major HDAC isoform that interacts with DNMT1 in multiple protein complexes for transcriptional silencing of TSGs. DNMT1/HDAC-IN-1 can reshape the tumor immune microenvironment and induce tumor regression, and effectively reverse cancer-specific epigenetic abnormalities .
    DNMT1/HDAC-IN-1
  • HY-178351

    HDAC Microtubule/Tubulin Apoptosis Caspase Bcl-2 Family Cancer
    HDAC6-IN-67 is a selective HDAC6 inhibitor (IC50 = 17.15 nM) that exhibits 19-fold selectivity over HDAC1. HDAC6-IN-67 selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by inducing the cleavage of caspases 9, 8, 3, and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. HDAC6-IN-67 effectively induces the acetylation of α-tubulin, without affecting histone H3 acetylation in MCF-7/ADR cells. HDAC6-IN-67 can be used for the study of breast cancer .
    HDAC6-IN-67
  • HY-W004924S

    Endogenous Metabolite Others
    5-Hydroxymethyluracil-d3 is the deuterium labeled 5-Hydroxymethyluracil . 5-Hydroxymethyluracil is a product of oxidative DNA damage. 5-Hydroxymethyluracil can be used as a potential epigenetic mark enhancing or inhibiting transcription with bacterial RNA polymerase .
    5-Hydroxymethyluracil-d3
  • HY-179446

    Histone Methyltransferase Cancer
    HP1-IN-2 (Compound (R)-18) is a HP1/H3K9me3 interaction inhibitor with an IC50 of 18.1 μM. HP1-IN-2 can be used for studying various cancers with overexpression of HP1 .
    HP1-IN-2
  • HY-123577

    Histone Demethylase Apoptosis Cancer
    TPC-144 is a LSD1/KDM1A inhibitor. TPC-144 inhibits LSD1, and leads to a decrease in the protein level of DNMT1, causing low methylation of the LINE-1 element. TPC-144 can also produce a synergistic effect with Decitabine (HY-A0004) (a DNMT inhibitor), jointly promoting DNA demethylation and thereby inducing differentiation and apoptosis of leukemia cells. TPC-144 has also demonstrated anti-tumor efficacy in acute myeloid leukemia (AML) models. TPC-144 can be used for the study of AML .
    TPC-144
  • HY-W653970

    Azacitidine-15N4; 5-AzaC-15N4; Ladakamycin-15N4

    Isotope-Labeled Compounds Antibiotic DNA Methyltransferase Organoid Autophagy Nucleoside Antimetabolite/Analog Bacterial Infection
    5-Azacytidine- 15N4 is 13C and 15N labeled 5-Azacytidine. 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-15N4
  • HY-78197

    Drug Intermediate Others
    3,5-Dimethylisoxazole-4-boronic acid pinacol ester is a drug intermediate that can be used for the synthesis of bromodomain inhibitors .
    3,5-Dimethylisoxazole-4-boronic acid pinacol ester
  • HY-176283

    Microtubule/Tubulin Histone Demethylase Apoptosis Wee1 Bcl-2 Family Caspase Cancer
    Tubulin/LSD1-IN-1 is an effective dual inhibitor of Tubulin polymerization and LSD1 (IC50 = 1.72 μM). Tubulin/LSD1-IN-1 has broad-spectrum antiproliferative activity against cancer cell lines. Tubulin/LSD1-IN-1 inhibits tubulin polymerization by targeting colchicine binding sites, thereby disrupting the microtubule network in gastric cancer cells. Tubulin/LSD1-IN-1 increases the methylation levels of H3K4me1/2 and H3K9me2/3, thereby achieving epigenetic regulation. Tubulin/LSD1-IN-1 induces G2/M arrest, promotes apoptosis, and effectively inhibits colony formation of gastric cancer cells .
    Tubulin/LSD1-IN-1
  • HY-176535

    BBC0115

    Epigenetic Reader Domain Interleukin Related STAT Inflammation/Immunology
    KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with Kd values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model.
    KB-0118
  • 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
  • HY-156489

    Sirtuin Cancer
    Epigenetic factor-IN-1 (40569Z) is a epigenetic factor inhibitor. Epigenetic factor-IN-1 has strong binding effect on SIRT7. Epigenetic factor-IN-1 can be used for liver cancer research .
    Epigenetic factor-IN-1
  • HY-120106

    HDAC Others
    BG14 is a chemical optical modulation of epigenetic regulation of transcription (COMET) probe. BG14 enables high-resolution optical control of epigenetic mechanisms using visible light and can photochromically inhibit human histone deacetylases (HDACs). BG14 can be used to study the dynamic regulation of the human genome .
    BG14
  • HY-163698

    Sirtuin Cancer
    SIRT-IN-4 is an inhibitor of the NAD+-dependent lysine deacetylase Sirtuin2 (Sirt2) (IC50=0.35 μM). SIRT-IN-4 is a potent Sirt2 deacetylase inhibitor that reduces cell survival and inhibits the migration of prostate cancer cells. SIRT-IN-4 can be used to study Sirt2 in cell cycle regulation, gene expression regulation, etc .
    SIRT-IN-4
  • HY-W004924R

    Reference Standards Endogenous Metabolite Others
    5-Hydroxymethyluracil is a product of oxidative DNA damage. 5-Hydroxymethyluracil can be used as a potential epigenetic mark enhancing or inhibiting transcription with bacterial RNA polymerase.
    5-Hydroxymethyluracil (Standard)
  • HY-157408

    Histone Demethylase Others
    KDM4D-IN-3 (compound 1) is a small-molecule epigenetic inhibitor target at KDM4D with an IC50 value of 4.8 μM .
    KDM4D-IN-3
  • HY-110093

    VSV Histone Methyltransferase Autophagy Influenza Virus Infection Cancer
    UNC0638 hydrate selectively inhibits G9a and GLP histone methyltransferases with IC50 of 15 nM and 19 nM, respectively. UNC0638 hydrate inhibits TNBC cell invasion and migration in vitro. UNC0638 hydrate is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 hydrate has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets .
    UNC0638 hydrate
  • HY-162003

    Histone Methyltransferase Cancer
    DCPT1061 potently inhibits PRMT1, PRMT6 and PRMT8 in vitro with less inhibitory effect on PRMT3, PRMT4, and PRMT5 or other epigenetic enzymes. DCPT1061 has antitumor effect .
    DCPT1061
  • HY-P3822

    Histone Methyltransferase Cancer
    PRMT5-IN-23 (compound 50) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) 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-23
  • HY-155237

    MicroRNA Cancer
    LIN28-IN-1 (compound 5) is an inhibitor of the RNA-binding and regulatory protein LIN28 and binds to the LIN28 cold shock domain (CSD). LIN28-IN-1 effectively inhibits the interaction between LIN28 and let-7 miRNA (IC50: 5.4 μM), blocking the negative impact of LIN28 on epigenetic gene regulation. LIN28-IN-1 significantly inhibits the proliferation of JAR cancer cells expressing LIN28 (IC50: 6.4 μM) .
    LIN28-IN-1
  • HY-W744986

    (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-162080A
    METTL1-WDR4-IN-1 TFA
    1 Publications Verification

    DNA Methyltransferase Pyruvate Kinase Cancer
    METTL1-WDR4-IN-1 (Compound 1) TFA is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50=144 μM). METTL1-WDR4-IN-1 TFA inhibits the m 7G methyltransferase activity of the METTL1-WDR4 complex, blocking the m 7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 TFA can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8 + T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 TFA can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy .
    METTL1-WDR4-IN-1 TFA

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