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histone methylation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Histone Demethylase (15) Histone Methyltransferase (12) Apoptosis (4) Autophagy (2) Endogenous Metabolite (6) Ferroptosis (1) GABA Receptor (1) Isotope-Labeled Compounds (1) MDM-2/p53 (1) Mitochondrial Metabolism (5) Monoamine Oxidase (1) Reference Standards (2)
By Research Areas:	Cancer (24) Cardiovascular Disease (1) Inflammation/Immunology (1) Metabolic Disease (2) Neurological Disease (3)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Histone Methyltransferase Histone Demethylase Histone Acetyltransferase HDAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 K_m and K_i 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 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 K_m and K_i of 2.52 mM and 11.13 mM, respectively .

HY-121095A

Bizine di(hydrochloride)	Histone Demethylase	Neurological Disease Cancer
Bizine dihydrochloride, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>K_i of 59 nM. Bizine dihydrochloride can modulate bulk histone methylation in cancer cells. Bizine dihydrochloride shows neuroprotective effects .

HY-121095

Bizine	Histone Demethylase	Neurological Disease Cancer
Bizine, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>K_i of 59 nM. Bizine can modulate bulk histone methylation in cancer cells. Bizine shows neuroprotective effects .

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.

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 .

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.

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 .

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 .

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) .

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 .

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 .

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) .

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) .

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 (K_d=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 .

HY-113039R

L-2-Hydroxyglutaric acid (Standard) (S)-2-Hydroxyglutaric acid (Standard)	Reference Standards Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite	Cancer
L-2-Hydroxyglutaric acid (Standard) is the analytical standard of L-2-Hydroxyglutaric acid. This product is intended for research and analytical applications. 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 K_m and K_i of 2.52 mM and 11.13 mM, respectively .

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 .

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 .

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 K_m and K_i of 2.52 mM and 11.13 mM, respectively .

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 .

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 .

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 .

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 .

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 .

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 .

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 .

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.

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 .

HY-B1018A

Phenelzine sulfate 5 Publications Verification	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 (K_i: 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 .

Cat. No.	Product Name

HY-L203

Methylation Compound Library	311 compounds
Methylation is an epigenetic modification mechanism that involves adding methyl groups to molecules such as DNA and histones, which can alter gene expression without changing the DNA sequence. This process is catalyzed by enzymes such as DNA methyltransferases (DNMTs) and histone methyltransferases (HMTs), and can be reversed by demethylases. The balance of methylation and demethylation is crucial for maintaining cellular function and genomic stability. Abnormal regulation of methylation may lead to a variety of diseases, including cancer, neurological disorders, and developmental abnormalities. A deep understanding of the molecular mechanisms of methylation metabolism is essential for developing therapeutic strategies for diseases associated with methylation dysregulation. MCE contains 311 compounds targeting methylation/demethylation enzymes, which is of significant value for studying the pathways of methylation metabolism and exploring their mechanisms of action in diseases.

Methylation Compound Library

311 compounds

Methylation is an epigenetic modification mechanism that involves adding methyl groups to molecules such as DNA and histones, which can alter gene expression without changing the DNA sequence. This process is catalyzed by enzymes such as DNA methyltransferases (DNMTs) and histone methyltransferases (HMTs), and can be reversed by demethylases. The balance of methylation and demethylation is crucial for maintaining cellular function and genomic stability. Abnormal regulation of methylation may lead to a variety of diseases, including cancer, neurological disorders, and developmental abnormalities. A deep understanding of the molecular mechanisms of methylation metabolism is essential for developing therapeutic strategies for diseases associated with methylation dysregulation.

MCE contains 311 compounds targeting methylation/demethylation enzymes, which is of significant value for studying the pathways of methylation metabolism and exploring their mechanisms of action in diseases.

HY-L024

Histone Modification Research Compound Library	814 compounds
A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases. MCE owns a unique collection of 814 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.

Histone Modification Research Compound Library

814 compounds

A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases.

MCE owns a unique collection of 814 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.

HY-L005

Epigenetics Compound Library	1,696 compounds
Epigenetics refers to changes in phenotype that are not rooted in DNA sequence. Many types of epigenetic processes have been identified, including DNA methylation, alteration in the structure of histone proteins and gene regulation by small noncoding microRNAs. Modification of DNA, protein, or RNA, resulting in changes to the function and/or regulation of these molecules, without altering their primary sequences, reveals the complexities of cellular differentiation, embryology, the regulation of gene expression, aging, cancer, and other diseases. MCE provide a unique collection of 1,696 epigenetics-related compounds that can be used in the research of the related diseases.

Epigenetics Compound Library

1,696 compounds

Epigenetics refers to changes in phenotype that are not rooted in DNA sequence. Many types of epigenetic processes have been identified, including DNA methylation, alteration in the structure of histone proteins and gene regulation by small noncoding microRNAs. Modification of DNA, protein, or RNA, resulting in changes to the function and/or regulation of these molecules, without altering their primary sequences, reveals the complexities of cellular differentiation, embryology, the regulation of gene expression, aging, cancer, and other diseases.

MCE provide a unique collection of 1,696 epigenetics-related compounds that can be used in the research of the related diseases.

Cat. No.	Product Name	Target	Research Area

HY-P2256

H3K4(Me2) (1-20) 1 Publications Verification	Peptides	Others
H3K4(Me2) (1-20) is a histone peptide. H3K4me2 regulates the recovery of protein biosynthesis and homeostasis following DNA damage .

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 .

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 .

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 .

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) .

HY-P2556

Histone H3 (21-44)	Peptides	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 .

HY-P2555

Histone H3 (23-34)	Peptides	Others
Histone H3 (23-34) is the histone H3 amino acid residues 23 to 34. Histone H3 (23-34) contains lysine residues at positions 23 and 27 that are subject to methylation and acetylation .

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) .

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) .

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 (K_d=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 .

L-2-Hydroxyglutaric acid (S)-2-Hydroxyglutaric acid	Structural Classification Microorganisms Classification of Application Fields Anti-aging Ketones, Aldehydes, Acids Source classification Endogenous metabolite Disease Research Fields Cancer	Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite
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 K_m and K_i of 2.52 mM and 11.13 mM, respectively .

Cat. No.	Product Name	Chemical Structure

HY-W744986

L-2-Hydroxyglutaric acid-d5 disodium

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 .

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histone methylation

Inhibitors & Agonists

Screening Libraries

Peptides

NaturalProducts

Isotope-Labeled Compounds

Natural
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