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Pathways Recommended: Epigenetics
Targets Recommended: Epigenetic Reader Domain
Results for "

epigenetic

" in MCE Product Catalog:

47

Inhibitors & Agonists

6

Screening Libraries

4

Natural
Products

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-133083
    BAY-474

    c-Met/HGFR Cancer
    BAY-474 is a tyrosine-protein kinase c-Met inhibitor. BAY-474 acts as an epigenetics probe.
  • HY-136572
    CEM114

    Epigenetic Reader Domain CRISPR/Cas9 Cancer
    CEM114 is an effective chemical epigenetic modifier (CEM) that recruits endogenous chromatin machinery through CRISPR-Cas9 systems.
  • HY-111558
    Bobcat339

    DNA Methyltransferase 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.
  • HY-144188
    PRMT5-IN-17

    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.
  • HY-144187
    PRMT5-IN-16

    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.
  • HY-19553
    LP99

    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.
  • 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.
  • HY-W015114
    L-2-Hydroxyglutaric acid disodium

    (S)-2-Hydroxyglutaric acid disodium

    Histone Demethylase Mitochondrial Metabolism 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.
  • HY-109169
    Bomedemstat

    IMG-7289

    Histone Demethylase Cancer
    Bomedemstat (IMG-7289) is an orally active and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity.
  • HY-109169A
    Bomedemstat ditosylate

    IMG-7289 ditosylate

    Histone Demethylase Cancer
    Bomedemstat (IMG-7289) ditosylate is an oral and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity.
  • HY-19694
    BRD7552

    Others Endocrinology
    BRD7552, a potent PDX1 transcription factor inducer, upregulates PDX1 expression in both primary human islets and ductal cells, and induces epigenetic changes in the PDX1 promoter consistent with transcriptional activation. BRD7552 increases insulin expression. PDX1 is a key transcription factor involved in pancreas development and β cell function.
  • HY-19336
    BAZ2-ICR

    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.
  • HY-144501
    D18

    Toll-like Receptor (TLR) PD-1/PD-L1 Cancer Inflammation/Immunology
    D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC50=24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases PD-L1 expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2.
  • HY-I0626
    Cytosine

    Endogenous Metabolite Others
    Cytosine is one of the four main bases found in DNA and RNA. Cytosine modifications exhibit circadian oscillations that are involved in epigenetic diversity and aging.
  • HY-W004924
    5-Hydroxymethyluracil

    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.
  • HY-139576
    Larsucosterol

    DUR-928

    Endogenous Metabolite Metabolic Disease
    Larsucosterol (DUR-928) is a cholesterol metabolite from the nuclei of normal human liver tissues, epigenetically regulates the transcription of proteins and enzymes involved in lipid synthesis, inflammation, and apoptosis.
  • HY-139576A
    Larsucosterol sodium

    DUR-928 sodium

    Endogenous Metabolite Metabolic Disease
    Larsucosterol (DUR-928) sodium is a cholesterol metabolite from the nuclei of normal human liver tissues, epigenetically regulates the transcription of proteins and enzymes involved in lipid synthesis, inflammation, and apoptosis.
  • HY-107842
    (Z)-JIB-04

    NSC693627

    Others Cancer
    (Z)-JIB-04 (NSC693627) is the Z isomer of JIB-04 that has two forms, E (HY-13953) and Z isomers. (Z)-JIB-04 is inactive in epigenetic analysis.
  • HY-138830
    TAK-418

    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.
  • HY-139576AS
    Larsucosterol-d6 sodium

    DUR-928-d6 sodium

    Endogenous Metabolite Metabolic Disease
    Larsucosterol-d6 (DUR-928-d6) sodium is the deuterium labeled Larsucosterol sodium. Larsucosterol sodium is a cholesterol metabolite from the nuclei of normal human liver tissues, epigenetically regulates the transcription of proteins and enzymes involved in lipid synthesis, inflammation, and apoptosis.
  • HY-111558A
    Bobcat339 hydrochloride

    DNA Methyltransferase 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.
  • HY-10586
    5-Azacytidine

    Azacitidine; 5-AzaC; Ladakamycin

    Nucleoside Antimetabolite/Analog DNA Methyltransferase Bacterial Autophagy Antibiotic Cancer Infection
    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.
  • HY-126428
    ZL0580

    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.
  • HY-13803B
    Tazemetostat hydrochloride

    EPZ-6438 hydrochloride; E-7438 hydrochloride

    Histone Methyltransferase Cancer
    Tazemetostat (EPZ-6438) hydrochloride is a potent, selective and orally active EZH2 inhibitor with IC50 values of 11 and 16 nM for EZH2 peptide and nucleosome, respectively. Tazemetostat hydrochloride can be used for cancer research.
  • HY-13803C
    Tazemetostat hydrobromide

    EPZ-6438 hydrobromide; E-7438 hydrobromide

    Histone Methyltransferase Cancer
    Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits Rat EZH2 with an IC50 of 4 nM. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM.
  • HY-13803
    Tazemetostat

    EPZ-6438; E-7438

    Histone Methyltransferase Cancer
    Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat (EPZ-6438) inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat (EPZ-6438) inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.
  • HY-13803A
    Tazemetostat trihydrochloride

    EPZ-6438 trihydrochloride; E-7438 trihydrochloride

    Histone Methyltransferase Cancer
    Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat trihydrochloride inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki of 2.5 nM. Tazemetostat trihydrochloride inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat trihydrochloride inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.
  • HY-A0067
    Oxybenzone

    Benzophenone 3

    RAR/RXR Autophagy Apoptosis Neurological Disease
    Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.
  • HY-I0626S
    Cytosine-2,4-13C2-1,3-15N2

    Endogenous Metabolite Others
    Cytosine-2,4-13C2-1,3-15N2 is the 13C-labeled and 15N-labeled Cytosine. Cytosine is one of the four main bases found in DNA and RNA. Cytosine modifications exhibit circadian oscillations that are involved in epigenetic diversity and aging.
  • HY-114209
    MRK-740

    Histone Methyltransferase Cancer
    MRK-740 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).
  • HY-100729A
    GSK9311 hydrochloride

    Epigenetic Reader Domain Cancer
    GSK9311 hydrochloride, a less active analogue of GSK6853, can be used as a negative control. GSK9311 hydrochloride inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.
  • HY-18665
    GSK-5959

    Epigenetic Reader Domain Cancer
    GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with an IC50 of ~ 80 nM.
  • HY-100729
    GSK9311

    Epigenetic Reader Domain Cancer
    GSK9311, a less active analogue of GSK6853, can be used as a negative control. GSK9311 inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.
  • HY-16438
    RRx-001

    Apoptosis Parasite Cancer Infection Inflammation/Immunology
    RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes drug 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.
  • HY-135146
    GSK-3484862

    DNA Methyltransferase Cancer
    GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity.
  • HY-19313
    LLY-507

    Histone Methyltransferase Cancer
    LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2. LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC50 <15 nM. LLY-507 serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes.
  • HY-134828
    AZ506

    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.
  • HY-143339
    CBP/p300-IN-15

    Epigenetic Reader Domain Histone Acetyltransferase Cancer
    CBP/p300-IN-15 (compound 13a) is a potent p300/CBP inhibitor, with IC50 values of 2.50 and 28.0 nM, respectively. CBP/p300-IN-15 shows good activity against OVCAR-3 and A2780 cell line, with EC50 values of 0.865 and 2.71 μM, respectively. CBP/p300-IN-15 can be used for ovarian cancer research.
  • HY-12583
    A-366

    Histone Methyltransferase Epigenetic Reader Domain Cancer
    A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families.
  • HY-100360
    MS049

    Histone Methyltransferase Cancer
    MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells.
  • HY-100360A
    MS049 dihydrochloride

    Histone Methyltransferase Cancer
    MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells.
  • HY-15826
    SGC-CBP30

    Epigenetic Reader Domain Histone Acetyltransferase Cancer Inflammation/Immunology
    SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects.
  • HY-101925
    CM-272

    Histone Methyltransferase DNA Methyltransferase Apoptosis Cancer
    CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death.
  • HY-N2150
    Psammaplin A

    HDAC DNA Methyltransferase DNA/RNA Synthesis Bacterial Cancer Infection
    Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective DAC1 inhibitor with an IC50 of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity.
  • HY-130853
    Thalidomide-NH-PEG2-C2-NH-Boc

    E3 Ligase Ligand-Linker Conjugates Cancer
    Thalidomide-NH-PEG2-C2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a PEG linker used for dBRD9 (compound 6) synthesis. dBRD9 is a selective BRD9 probe PROTAC degrader for the study of BAF complex biology.
  • HY-144755
    MC2652

    Histone Demethylase Cancer
    MC2652 (compound 1a) is a potent LSD1 inhibitor. MC2652 displays high inhibiting effects in MV4-11 and NB4 leukaemia cells. MC2652 shows antiproliferative activity against prostate cancer LNCaP cells.
  • HY-144725
    HDAC1/6-IN-1

    HDAC Apoptosis Cancer
    HDAC1/6-IN-1 (compound D7) is a potent multitarget inhibitor of GLP, HDAC6 and HDAC1, with IC50 values of 1.3, 13, and 89 nM, respectively. HDAC1/6-IN-1 can inhibit the methylation and deacetylation of H3K9 on protein level. HDAC1/6-IN-1 induces cancer cell apoptosis, G0/G1 cell cycle arrest, and blocks migration and invasion.