Search Result

Results for "

demethylases

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Histone Demethylase (126) AMPK (2) Anaplastic lymphoma kinase (ALK) (2) Antibiotic (5) Apoptosis (24) Autophagy (5) Bacterial (7) Biochemical Assay Reagents (2) CD38 (1) CFTR (2) Cholecystokinin Receptor (1) CMV (1) Cytochrome P450 (12) DNA/RNA Synthesis (3) Dopamine Receptor (3) Dopamine β-hydroxylase (1) Drug Intermediate (1) Drug Isomer (1) E1/E2/E3 Enzyme (1) Endogenous Metabolite (12) Estrogen Receptor/ERR (1) Fat Mass and Obesity-associated Protein (FTO) (7) Ferroportin (1) Fungal (24) HDAC (5) Hedgehog (4) HIF/HIF Prolyl-Hydroxylase (2) Histone Methyltransferase (5) HMG-CoA Reductase (HMGCR) (1) HSV (1) Isotope-Labeled Compounds (3) Ligands for Target Protein for PROTAC (1) MDM-2/p53 (1) Mitochondrial Metabolism (5) MMP (1) Monoamine Oxidase (13) PD-1/PD-L1 (1) Phytohormone (1) PROTACs (1) Reactive Oxygen Species (ROS) (2) Reference Standards (10) SOD (1) TGF-beta/Smad (1) TNF Receptor (1) Vasopressin Receptor (1) Virus Protease (1)
By Research Areas:	Cancer (139) Cardiovascular Disease (6) Endocrinology (1) Infection (31) Inflammation/Immunology (8) Metabolic Disease (5) Neurological Disease (11)

By Targets:

Histone Demethylase (126)

AMPK (2)

Anaplastic lymphoma kinase (ALK) (2)

Antibiotic (5)

Apoptosis (24)

Autophagy (5)

Bacterial (7)

Biochemical Assay Reagents (2)

CD38 (1)

CFTR (2)

Cholecystokinin Receptor (1)

CMV (1)

Cytochrome P450 (12)

DNA/RNA Synthesis (3)

Dopamine Receptor (3)

Dopamine β-hydroxylase (1)

Drug Intermediate (1)

Drug Isomer (1)

E1/E2/E3 Enzyme (1)

Endogenous Metabolite (12)

Estrogen Receptor/ERR (1)

Fat Mass and Obesity-associated Protein (FTO) (7)

Ferroportin (1)

Fungal (24)

HDAC (5)

Hedgehog (4)

HIF/HIF Prolyl-Hydroxylase (2)

Histone Methyltransferase (5)

HMG-CoA Reductase (HMGCR) (1)

HSV (1)

Isotope-Labeled Compounds (3)

Ligands for Target Protein for PROTAC (1)

MDM-2/p53 (1)

Mitochondrial Metabolism (5)

MMP (1)

Monoamine Oxidase (13)

PD-1/PD-L1 (1)

Phytohormone (1)

PROTACs (1)

Reactive Oxygen Species (ROS) (2)

Reference Standards (10)

SOD (1)

TGF-beta/Smad (1)

TNF Receptor (1)

Vasopressin Receptor (1)

Virus Protease (1)

By Research Areas:

Cancer (139)

Cardiovascular Disease (6)

Endocrinology (1)

Infection (31)

Inflammation/Immunology (8)

Metabolic Disease (5)

Neurological Disease (11)

195

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Histone Demethylase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-137187

FB23 1 Publications Verification	Fat Mass and Obesity-associated Protein (FTO)	Cancer
FB23 is a potent and selective FTO demethylase inhibitor with an IC₅₀ of 60 nM. FB23 directly binds to FTO and selectively inhibits FTO's mRNA N ⁶-methyladenosine (m6A) demethylase activity .

HY-141677

INCB059872	Histone Demethylase	Cancer
INCB059872 is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 can be used for the research of myeloid leukemia .

HY-141677A

INCB059872 dihydrochloride	Histone Demethylase	Cancer
INCB059872 dihydrochloride is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 dihydrochloride can be used for the research of myeloid leukemia .

HY-13643

Daminozide 2 Publications Verification	Histone Demethylase	Cancer
Daminozide, a plant growth regulator, is a selective inhibitor of the human KDM2/7 histone demethylases, with IC₅₀s of 0.55, 1.5 and 2.1 μM for PHF8, KDM2A, and KIAA1718, respectively. Daminozide has >100-fold selectivity for KDM2/7 subfamily versus other demethylase subfamily members tested .

HY-116034

Arasertaconazole	Cytochrome P450 Bacterial Fungal	Infection
Arasertaconazole is a potent 14α-lanosterol demethylase inhibitor. Arasertaconazole has antifungal and antibacterial activity .

HY-122746

E67-2	Histone Methyltransferase	Cancer
E67-2, as the E67 derivative, is a low-toxicity, selective KIAA1718 Jumonji domain inhibitor with an IC₅₀ value of 3.4 µM. E67-2 selectively inhibits histone H3 lysine 9 (H3K9) Jumonji demethylase as well as histone H3 lysine 4 (H3K4) demethylase .

HY-105191

Azalanstat RS-21607	Cytochrome P450 Reactive Oxygen Species (ROS)	Infection Inflammation/Immunology
Azalanstat is an imidazole-dioxolane derivate that is a lanosterol 14-α demethylase inhibitor. Azalanstat is also a HO-1 (IC₅₀ = 5.5 µM) and HO-2 (IC₅₀ = 24.5 µM) inhibitor .

HY-160183

LSD1-IN-29	Histone Demethylase	Cancer
LSD1-IN-29 (compound 6) is a Lysine specific demethylase 1 (LSD1) inhibitor with the IC₅₀ of 19 nM .

HY-151194

LSD1/2-IN-4	Histone Demethylase	Cancer
LSD1/2-IN-4, a PCPA derivative, is an inhibitor of *lysine-specific demethylase* 1 (LSD1) and lysine-specific demethylase 2 (LSD2). LSD1/2-IN-4 inhibits LSD1 and LSD2 with K_i** values of 0.11 μM and 130 μM, respectively. LSD1/2-IN-4 can be used for the research of several cancers including T-cell acute lymphoblastic leukemia (TALL) .

HY-115747

Namoline	Histone Demethylase	Cancer
Namoline, a γ-pyrone, is a selective and reversible *Lysine-specific demethylase* 1 (LSD1)** inhibitor with an IC50 of 51 μM in a HRP-coupled enzymatic assay. Namoline impairs LSD1 demethylase activity and blocks cell proliferation. Namoline has the potential for androgen-dependent prostate cancer research .

HY-13643R

Daminozide (Standard)	Reference Standards Histone Demethylase	Cancer
Daminozide (Standard) is the analytical standard of Daminozide. This product is intended for research and analytical applications. Daminozide, a plant growth regulator, is a selective inhibitor of the human KDM2/7 histone demethylases, with IC50s of 0.55, 1.5 and 2.1 μM for PHF8, KDM2A, and KIAA1718, respectively. Daminozide has >100-fold selectivity for KDM2/7 subfamily versus other demethylase subfamily members tested .

HY-N2560

Senecionine Senecionan-11,16-dione, 12-hydroxy-; Aureine; Senecionin	Others	Metabolic Disease
Senecionine (Senecionan-11,16-dione, 12-hydroxy-) is a pyrrolizidine alkaloid could be isolated from Senecio vulgaris. Senecionine decreases the activities of glutathione S-transferase, aminopyrine demethylase and arylhydrocarbon hydroxylase (AHH) .

HY-117426

MO-I-500	Fat Mass and Obesity-associated Protein (FTO)	Cancer
MO-I-500 is a pharmacological of FTO inhibitor with an IC₅₀ of 8.7 μM for the inhibition of purified FTO demethylase catalyzing demethylation of an artificial small methylated substrate. MO-I-500 can be used for the research of rare panresistant triple-negative inflammatory breast cancer .

HY-W173146

ALKBH5-IN-4	DNA/RNA Synthesis	Cancer
ALKBH5-IN-4 (compound 3) is a RNA m6A demethylase ALKBH5 inhibitor with an IC₅₀ of 0.84 μM. ALKBH5-IN-4 shows inhibitory effect on leukemia cells_[1].

HY-139348

PFI-90	Histone Demethylase Apoptosis	Cancer
PFI-90 is a selective inhibitor of histone demethylase (KDM3B) that inhibits PAX3-FOXO1 action. PFI-90 induces apoptosis and myogenic differentiation, resulting in the cell death increased. PFI-90 has the potential for the antitumor activity. (patent WO2021101929A1).

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-151106

FTO-IN-8	Fat Mass and Obesity-associated Protein (FTO)	Cancer
FTO-IN-8 (FTO-43) is a N6-methyladenosine demethylase (FTO) (fat mass- and obesity-associated protein) inhibitor with the IC₅₀ value of 5.5 μM. FTO-IN-8 has anti-cancer cell proliferative activity .

HY-147697

LSD1-IN-21	Histone Demethylase TNF Receptor	Inflammation/Immunology Cancer
LSD1-IN-21 (compound 5a) is a potent and BBB-penetrated LSD1 (Lysine specific demethylase-1) inhibitor, with an IC₅₀ of 0.956 µM. LSD1-IN-21 significantly reduces the pro-inflammatory cytokine TNF-α. LSD1-IN-21 shows good anticancer and anti-inflammatory activity .

HY-W017132

2,4-PDCA	Histone Demethylase	Cancer
2,4-PDCA (2,4 pyridine dicarboxylic acid) is a broad-spectrum inhibitor of 2OG oxygenase, including *JmjC domain-containing family of histone demethylases* (JHDMs)**. 2,4-PDCA is a target chemical in the field of bio-based plastics .

HY-15648F

GSK-J4 hydrochloride Maximum Cited Publications 46 Publications Verification	Histone Demethylase	Cancer
GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC₅₀s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC₅₀ of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1 .

HY-N2560R

Senecionine (Standard) Senecionan-11,16-dione, 12-hydroxy- (Standard); Aureine (Standard); Senecionin (Standard)	Reference Standards Others	Metabolic Disease
Senecionine (Standard) is the analytical standard of Senecionine. This product is intended for research and analytical applications. Senecionine (Senecionan-11,16-dione, 12-hydroxy-) is a pyrrolizidine alkaloid could be isolated from Senecio vulgaris. Senecionine decreases the activities of glutathione S-transferase, aminopyrine demethylase and arylhydrocarbon hydroxylase (AHH) .

HY-127103

FB23-2 15+ Cited Publications	Apoptosis	Cancer
FB23-2 is a potent and selective inhibitor of mRNA N ⁶-methyladenosine (m ⁶A) demethylase FTO, with an IC₅₀ of 2.6 μM. FB23-2 has anti-proliferation activity. FB23-2 can be used for the research of acute myeloid leukemia (AML) .

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-141677B

INCB059872 tosylate	Histone Demethylase	Cancer
INCB059872 tosylate is a potent, selective and orally active lysine-specific demethylase 1 inhibitor. INCB059872 binds to and inhibits LSD1, enhancing H3K4 methylation, thereby increasing the expression of tumor suppressor genes. INCB059872 inhibition also promotes H3K9 methylation, thereby reducing the transcription of tumor-promoting genes .

HY-146670

KDM5B-IN-3	Histone Demethylase	Cancer
KDM5B-IN-3 (Compound 5) is a histone lysine specific demethylase 5B (KDM5B/JARID1B) inhibitor with an IC₅₀ of 9.32 μM. KDM5B-IN-3 can be used for the research of gastric cancer .

HY-15648B

GSK-J4 Maximum Cited Publications 46 Publications Verification	Histone Demethylase Apoptosis	Cancer
GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC₅₀s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC₅₀ of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1 . GSK-J4 induces endoplasmic reticulum stress-related apoptosis .

HY-15648FR

GSK-J4 hydrochloride (Standard)	Histone Demethylase	Cancer
GSK-J4 (hydrochloride) (Standard) is the analytical standard of GSK-J4 (hydrochloride). This product is intended for research and analytical applications. GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1 .

HY-152032

LSD1-IN-23	Histone Demethylase	Cancer
LSD1-IN-23 is a competitive/non-competitive mixed inhibitor of *lysine specific demethylase* 1 (LSD1). LSD1-IN-23 has LSD1 inhibitory activity with an IC₅₀** value of 0.58 μM. LSD1-IN-23 can be used for the research of neuroblastoma (NB) .

HY-15648BR

GSK-J4 (Standard)	Histone Demethylase Apoptosis	Cancer
GSK-J4 (Standard) is the analytical standard of GSK-J4. This product is intended for research and analytical applications. GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1 . GSK-J4 induces endoplasmic reticulum stress-related apoptosis .

HY-109169B

Bomedemstat hydrochloride 3 Publications Verification IMG-7289 hydrochloride	Histone Demethylase Apoptosis	Cancer
Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible *lysine-specific demethylase* 1 (LSD1**) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .

HY-109169C

Bomedemstat dihydrochloride IMG-7289 dihydrochloride	Histone Demethylase Apoptosis	Cancer
Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible *lysine-specific demethylase* 1 (LSD1**) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .

HY-109169

Bomedemstat 3 Publications Verification IMG-7289	Histone Demethylase Apoptosis	Cancer
Bomedemstat (IMG-7289) is an orally active and irreversible *lysine-specific demethylase* 1 (LSD1**) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .

HY-B0735A

Fenoldopam mesylate 4 Publications Verification Fenoldopam methanesulfonate; SKF-82526 mesylate	Dopamine Receptor Apoptosis	Cardiovascular Disease Cancer
Fenoldopam mesylate (SKF-82526) is a D₁ receptor agonist and a novel *lysine-specific demethylase* 1 (LSD1) inhibitor (IC₅₀**=0.8974 μM). Fenoldopam mesylate shows anti-hypertensive effects, anti-cancer cell proliferation activity and can induce cells apoptosis .

HY-109169A

Bomedemstat ditosylate 3 Publications Verification IMG-7289 ditosylate	Histone Demethylase Apoptosis	Cancer
Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible *lysine-specific demethylase* 1 (LSD1**) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .

HY-131970

LSD1/HDAC6-IN-1	Histone Demethylase HDAC	Cancer
LSD1/HDAC6-IN-1 is an orally active dual inhibitor of *lysine specific demethylase* 1(LSD1)/Histone deacetylase 6 (HDAC6)**, with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM) .

HY-147777

*14α-Demethylase/DNA Gyrase-IN-2*	Bacterial DNA/RNA Synthesis	Infection
14α-Demethylase/DNA Gyrase-IN-2 (Compound 6a) is a potent inhibitor of *14α-Demethylase/DNA* Gyrase. 14α-Demethylase/DNA Gyrase-IN-2 has antimicrobial activities .

HY-147778

*14α-Demethylase/DNA Gyrase-IN-1*	Bacterial DNA/RNA Synthesis	Infection
14α-Demethylase/DNA Gyrase-IN-1 (Compound 7c) is a potent inhibitor of *14α-Demethylase/DNA* Gyrase. 14α-Demethylase/DNA Gyrase-IN-1 has antimicrobial activities .

HY-B0735AR

Fenoldopam mesylate (Standard) Fenoldopam methanesulfonate (Standard); SKF-82526 mesylate (Standard)	Reference Standards Dopamine Receptor Apoptosis	Cardiovascular Disease Cancer
Fenoldopam (mesylate) (Standard) is the analytical standard of Fenoldopam (mesylate). This product is intended for research and analytical applications. Fenoldopam mesylate (SKF-82526) is a D1 receptor agonist and a novel lysine-specific demethylase 1 (LSD1) inhibitor (IC50=0.8974 μM). Fenoldopam mesylate shows anti-hypertensive effects, anti-cancer cell proliferation activity and can induce cells apoptosis .

HY-156405

FTO-IN-10	Fat Mass and Obesity-associated Protein (FTO) Autophagy	Metabolic Disease
FTO-IN-10 (compound 7) is a potent human demethylase FTO (the fat mass and obesity-associated protein) inhibitor with an IC₅₀ of 4.5 μM. FTO-IN-10 enters the FTO’s structural domain II binding pocket through hydrophobic and hydrogen bonding interactions. FTO-IN-10 induces DNA damage and autophagic cell death in A549 cells .

HY-119730

Tripartin	Histone Demethylase	Cancer
Tripartin is an inhibitor of histone demethylase. Tripartin inhibits the histone H3 lysine 9 demethylase KDM4 in HeLa cells .

HY-125796

U-14624	Dopamine β-hydroxylase	Neurological Disease
U-14624 is a potent and orally active dopamine beta-hydroxylase inhibitor. U-14624 suppresses the activities of aminopyrine N-demethylase, aniline hydroxylase and p-nitroanisole O-demethylase enzymes .

HY-112308

NCGC00247743 1 Publications Verification	Histone Demethylase	Cancer
NCGC00247743 is a histone lysine demethylase KDM4 inhibitor.

HY-169165

*14α-Demethylase-IN-1*	Fungal	Infection
14α-Demethylase-IN-1 (compound 2e) is a *14α-demethylase* inhibitor and can be used as an antifungal agent. 14α-Demethylase-IN-1 (48 h) exhibits MIC50 values of 2.47 μM, 1.23 μM, 19.70 μM, and 19.70 μM for C. albicans, C. parapsilosis, C. krusei, and C. glabrata, respectively .

HY-116232

2-(3-Pyridyl)-benzimidazole	Cytochrome P450
2-(3-Pyridyl)-benzimidazole is an Aminopyrine N-Demethylase inhibitor .

HY-122635A

T-448	Histone Demethylase	Neurological Disease
T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC₅₀ of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons .

HY-15774A

CBB1003 hydrochloride	Histone Demethylase	Cancer
CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.

HY-15774

CBB1003	Histone Demethylase	Cancer
CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.

HY-136522

S2116	Histone Demethylase Apoptosis	Cancer
S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent *lysine-specific demethylase* 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis** in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice .

HY-122635

T-448 free base	Histone Demethylase	Neurological Disease
T-448 free base is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC₅₀ of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons .

HY-12635

SP2509 5+ Cited Publications	Histone Demethylase Apoptosis	Cancer
SP2509 is a potent and selective antagonist of *lysine specific demethylase* 1 (LSD1) with an IC₅₀** of 13 nM .

Cat. No.	Product Name

HY-L024

Histone Modification Research Compound Library

786 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 786 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-L203

Methylation Compound Library

304 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 304 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-L005

Epigenetics Compound Library

1,630 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 1,630 epigenetics-related compounds that can be used in the research of the related diseases.

Cat. No.	Product Name	Target	Research Area

HY-P2509

Histone H2A (1-20)	Peptides	Others
Histone H2A (1-20), a 35-residue a peptide of histone H2A, is a substrate for methyltransferase/demethylase enzymes .

HY-P1108

Astressin 2B	CFTR	Others
Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC₅₀ values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying .

HY-P1108A

Astressin 2B TFA	CFTR	Others
Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC₅₀ values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying .

HY-P3066

SKF 100398 d(CH2)5Tyr(Et)VAVP	Vasopressin Receptor	Metabolic Disease
SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP .

HY-P10828

MAPI	Virus Protease	Infection Inflammation/Immunology
MAPI is a polypeptide irreversible 3C cysteine protease (SV3CP) inhibitor. MAPI inhibits SV3CP by covalently binding its C-terminal Michael-acceptor extension to the active site thiol of SV3CP Cys 139. MAPI is promising for research of noroviruses infection .

HY-P4756

*N-(2-Carbamoyl-ethyl)-Val-Leu-anilide*	Peptides	Others
N-(2-Carbamoyl-ethyl)-Val-Leu-anilide is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .

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-P2592

Ro 23-7014	Cholecystokinin Receptor	Others
Ro 23-7014 is an appetite suppressant. Ro 23-7014 is an analog of cholecystokinin (CCK-7) .

HY-P4521

*Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt*	MMP	Others
Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt is a MMP12 substrate, and can be used to detect MMP12 enzyme activity .

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-125628

Kahalalide A	Endogenous Metabolite	Infection
Kahalalide A is an anti-mycobacterial compound with antimicrobial activity. Kahalalide A is derived from the marine mollusk Elysia rufescens. Kahalalide A has attracted extensive attention in natural product research due to its potential medicinal value .

HY-P10272

Rusfertide PTG-300	Ferroportin	Others
Rusfertide is a peptide mimetic of natural hepcidin, which targets and degrades ferroportin, reduces serum iron and transferrin-saturation, and thus regulates the production of red blood cells. Rusfertide ameliorates the polycythemia vera, β-thalassemia and hereditary hemochromatosis .

HY-A0248A

Polymyxin B1 1 Publications Verification	Bacterial	Infection
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

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-P10819

S9-CMC1 TFA	Histone Demethylase Apoptosis	Cancer
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC₅₀ value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .

HY-P10563

Noraramtide BHV-1100	CD38	Cancer
Noraramtide (BHV-1100) is an antibody recruitment molecule. Noraramtide can specifically bind to CD38 molecules to recruit natural killer (NK) cells. Noraramtide enhances the ability of NK cells to kill tumor cells through antibody-dependent cellular cytotoxicity (ADCC). This mechanism allows NK cells to more effectively recognize and eliminate tumor cells while avoiding mutual killing between NK cells. Noraramtide can be used for the study of autologous cancer immunity .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-13643

Daminozide 2 Publications Verification	Classification of Application Fields Ketones, Aldehydes, Acids Source classification Dendranthema morifolium (Ramat.) Tzvel. Plants Compositae Disease Research Fields Biological Pesticide Research Cancer Agricultural Research	Histone Demethylase
Daminozide, a plant growth regulator, is a selective inhibitor of the human KDM2/7 histone demethylases, with IC₅₀s of 0.55, 1.5 and 2.1 μM for PHF8, KDM2A, and KIAA1718, respectively. Daminozide has >100-fold selectivity for KDM2/7 subfamily versus other demethylase subfamily members tested .

HY-N2560

Senecionine Senecionan-11,16-dione, 12-hydroxy-; Aureine; Senecionin	Pterogyne nitens Tul. Alkaloids Pyrrole Alkaloids Classification of Application Fields Erinacea anthyllis Link Source classification Metabolic Disease Plants Compositae Disease Research Fields	Others
Senecionine (Senecionan-11,16-dione, 12-hydroxy-) is a pyrrolizidine alkaloid could be isolated from Senecio vulgaris. Senecionine decreases the activities of glutathione S-transferase, aminopyrine demethylase and arylhydrocarbon hydroxylase (AHH) .

HY-113039

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 .

HY-W015114

L-2-Hydroxyglutaric acid disodium (S)-2-Hydroxyglutaric acid disodium	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Source classification Endogenous metabolite Disease Research Fields Cancer	Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite
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-113038B

α-Hydroxyglutaric acid 2-Hydroxyglutarate; 2-Hydroxyglutaric acid; 2-Hydroxypentanedioic acid	Structural Classification Immune System Disorder Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Source classification Disease markers Endocrine diseases Nervous System Disorder Endogenous metabolite Disease Research Fields Cancer	Histone Demethylase Endogenous Metabolite
α-Hydroxyglutaric acid (2-Hydroxyglutarate) is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .

HY-113038A

α-Hydroxyglutaric acid disodium 2-Hydroxyglutarate disodium; 2-Hydroxyglutaric acid disodium; 2-Hydroxypentanedioic acid disodium	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Source classification Endogenous metabolite Disease Research Fields Cancer	Histone Demethylase Endogenous Metabolite
α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .

HY-17514

Itraconazole Maximum Cited Publications 19 Publications Verification R51211	Microorganisms Source classification	Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Bacterial
Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC₅₀ of ~800 nM. Itraconazole potently inhibits lanosterol *14α-demethylase* (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor .

HY-13643R

Daminozide (Standard)	Ketones, Aldehydes, Acids Source classification Dendranthema morifolium (Ramat.) Tzvel. Plants Compositae	Reference Standards Histone Demethylase
Daminozide (Standard) is the analytical standard of Daminozide. This product is intended for research and analytical applications. Daminozide, a plant growth regulator, is a selective inhibitor of the human KDM2/7 histone demethylases, with IC50s of 0.55, 1.5 and 2.1 μM for PHF8, KDM2A, and KIAA1718, respectively. Daminozide has >100-fold selectivity for KDM2/7 subfamily versus other demethylase subfamily members tested .

HY-N2560R

Senecionine (Standard) Senecionan-11,16-dione, 12-hydroxy- (Standard); Aureine (Standard); Senecionin (Standard)	Pterogyne nitens Tul. Alkaloids Structural Classification Pyrrole Alkaloids Erinacea anthyllis Link Source classification Plants Compositae	Reference Standards Others
Senecionine (Standard) is the analytical standard of Senecionine. This product is intended for research and analytical applications. Senecionine (Senecionan-11,16-dione, 12-hydroxy-) is a pyrrolizidine alkaloid could be isolated from Senecio vulgaris. Senecionine decreases the activities of glutathione S-transferase, aminopyrine demethylase and arylhydrocarbon hydroxylase (AHH) .

HY-N10340

Clausine E Clauszoline I	Structural Classification Alkaloids Classification of Application Fields Source classification Rutaceae Plants Disease Research Fields Clausena harmandiana (Pierre) Guillaumin Cancer	Others
Clausine E, is a alkaloid which can be isolated from Clausena excavata, is a inhibitor of fat mass and obesity-associated protein (FTO) demethylase. Clausine E shows inhibitory activities against proliferation of synoviocytes and cancer cells.

HY-17514R

Itraconazole (Standard) R51211 (Standard)	Microorganisms Source classification	Reference Standards Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Bacterial
Itraconazole (Standard) is the analytical standard of Itraconazole. This product is intended for research and analytical applications. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor .

HY-113039R

L-2-Hydroxyglutaric acid (Standard) (S)-2-Hydroxyglutaric acid (Standard)	Structural Classification Microorganisms Ketones, Aldehydes, Acids Endogenous metabolite	Reference Standards Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite
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-W015114R

L-2-Hydroxyglutaric acid disodium (Standard) (S)-2-Hydroxyglutaric acid disodium (Standard)	Structural Classification Ketones, Aldehydes, Acids Source classification Endogenous metabolite	Reference Standards Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite
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-A0248A

Polymyxin B1 1 Publications Verification	Infection Structural Classification Microorganisms Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Disease Research Fields Other Antibiotics	Bacterial
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .

Cat. No.	Product Name	Chemical Structure

HY-113038AS

α-Hydroxyglutaric acid-13C5 disodium
α-Hydroxyglutaric acid- ¹³C₅ (sodium) is the ¹³C labeled α-Hydroxyglutaric acid sodium . α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .

HY-17514S

Itraconazole-d5

Itraconazole-d₅ is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC₅₀ of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects .

HY-113038AS1

α-Hydroxyglutaric acid-d4 disodium

α-Hydroxyglutaric acid-d₄ (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium . α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .

HY-17514S2

Itraconazole-d9

Itraconazole-d₉ is the deuterium labeled Itraconazole . Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC₅₀ of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor .

HY-17447SA

Tranylcypromine-d5 hydrochloride

Tranylcypromine-d₅ (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis .

HY-W706180

(±)-Triadimefon-d4

(±)-Triadimefon-d₄ is deuterium labeled Triadimefon. Triadimefon is a triazole fungicide used to control powdery mildew, rusts, and other fungal pests on grains, fruit and vegetable crops, turf, shrubs, and trees. Triadimefon inhibits lanosterol 14α-demethylase, interfering with oxidative demethylation reactions in the ergosterol biosynthesis pathway of fungi, and also blocks gibberellin biosynthesis .

HY-W704805

Sodium 2-hydroxypentanedioate-2,3,3-d3

Sodium 2-hydroxypentanedioate-2,3,3-d₃ is the deuterium labeled α-Hydroxyglutaric acid disodium (HY-113038A). α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .

HY-17447AS

(1S,2R)-Tranylcypromine-d5 hydrochloride

(1S,2R)-Tranylcypromine-d₅ (hydrochloride) is the deuterium labeled Tranylcypromine hydrochloride . Tranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110) and monoamine oxidase (MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B with IC₅₀s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression .

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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