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Psychedelics and Epigenetic Regulation

Intercellular Communication & Diseases Cellular Stress Neurodegeneration Proteostasis

Psychedelic compounds can produce lasting changes in perception, mood, and neural plasticity after brief exposure, prompting interest in durable transcriptional and epigenetic mechanisms. Direct evidence for stable, causal epigenetic editing by classic psychedelics remains limited; the strongest literature establishes receptor signaling, gene-expression responses, neurite growth, and persistent dendritic-spine remodeling. Epigenetic regulation is therefore a plausible downstream layer rather than a settled primary mechanism. This distinction matters because persistent morphology or behavior does not by itself demonstrate DNA methylation or a specific histone modification[1][2][3].

Classic psychedelics activate serotonin 5-HT2A receptors and downstream signaling that engages immediate-early transcription, cytoskeletal remodeling, and neurotrophic pathways. In cell and animal systems, compounds including psilocybin and LSD-related agents promote neuritogenesis or spinogenesis. Psilocybin produced rapid and persistent dendritic-spine growth in mouse frontal cortex, and intracellular 5-HT2A receptor signaling has been linked to neuroplastic effects. Activity-dependent transcription can recruit CREB, CREBBP, histone acetylation, and DNA-methylation machinery, but psychedelic-specific causal chains from receptor to chromatin mark to behavioral outcome require direct testing[1][2][3].

Applications focus on depression, trauma-related disorders, addiction, and mechanistic models of psychoplastogen action. Transcriptomic and chromatin profiling before and after exposure can nominate regulatory programs that accompany a therapeutic window, while receptor antagonists and pathway perturbations identify upstream dependence. Organoids, human induced neurons, and longitudinal animal imaging can connect molecular changes with synaptic remodeling. Epigenetic biomarkers in blood or saliva may report exposure or systemic response, but they cannot be assumed to mirror cortical cell types. Clinical benefit also includes psychotherapy and context, which molecular studies should not erase from interpretation[1][2][3].

Research gaps include dose equivalence, species translation, cell specificity, and separation of drug action from experience. Future studies should use single-nucleus multi-omics, defined behavioral context, receptor controls, and locus-specific perturbation to test whether a mark is necessary for persistent plasticity. Repeated or microdose exposure needs independent safety and mechanism studies rather than extrapolation from supervised single-dose protocols. Any epigenetic claim should specify tissue, cell type, time point, modification, and functional consequence. The field may reveal chromatin mechanisms that stabilize beneficial learning, but current evidence supports cautious mechanistic inquiry rather than broad claims of epigenetic reprogramming Clinical research should also separate pharmacology from expectancy, therapeutic alliance, and post-session learning. Randomized designs, active controls, blinded molecular analysis, and repeated sampling can determine which biological changes follow drug exposure and which track clinical experience. Brain-relevant inference from peripheral methylation requires validation against neural tissue or experimentally justified cross-tissue models. A persistent molecular signal should be evaluated alongside symptom trajectory, cognitive flexibility, sleep, and adverse events. Researchers should report prior psychedelic exposure, concomitant medication, and psychotherapy protocol because these factors can alter both response and transcription. These standards will keep epigenetic hypotheses connected to the complex intervention actually delivered to patients. Preclinical studies should include female and male animals, multiple ages, and clinically relevant routes of administration. Molecular changes after high repeated doses cannot be assumed to explain outcomes after one supervised human session. Replication with orthogonal chromatin assays is necessary because changes in cell composition can mimic differential methylation or accessibility[1][2][3].

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Cat. No. Product Name Information Application Publication
HY-10219 Rapamycin
Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin is a molecular glue that binds FKBP12 and mTOR proteins together, thereby inhibiting mTOR kinase activity. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.

Source: bacterium Streptomyces hygroscopicus

mTOR   FKBP   Molecular Glues   Fungal   Autophagy   Endogenous Metabolite   Antibiotic   Bacterial  
Breast Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Viral Infection   Bacterial Infection   Fungal Infection   Pain   Non-Small Cell Lung Cancer   Lung Adenocarcinoma   SARS-CoV-2 Infection   Obesity   Lung Fibrosis  
1441
HY-10071 Y-27632
Y-27632 is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade.
ROCK   Reactive Oxygen Species (ROS)   Akt   Ras   mTOR   Apoptosis   PAK   NADPH Oxidase   NF-κB   Autophagy  
Cancer   Digestive System Disease   Digestive System Inflammation   Lung Fibrosis  
585
HY-10358 MK-2206 dihydrochloride
MK-2206 dihydrochloride (MK-2206 2HCl) is an orally active pan-AKT inhibitor, with IC50 values of 8 nM, 12 nM and 65 nM against AKT1, AKT2 and AKT3, respectively. MK-2206 dihydrochloride inhibits the Akt/mTOR signaling pathway and reduces the levels of downstream GSK3β and Mcl-1 via proteasomal degradation. MK-2206 dihydrochloride induces G1-phase cell cycle arrest, apoptosis, epithelial-mesenchymal transition, fibroblast activation and extracellular matrix deposition. MK-2206 dihydrochloride causes transient hyperglycemia and hyperinsulinemia in animals. MK-2206 dihydrochloride can be used in research related to solid tumors, renal fibrosis and hypercholesterolemia.
Bcl-2 Family   Akt   mTOR   Apoptosis   GSK-3  
Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Large Cell Lung Carcinoma   Metastatic Breast Cancer   Lung Fibrosis  
484
HY-A0281 4-Phenylbutyric acid
4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
HDAC   Virus Protease  
Lung Cancer   Breast Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Viral Infection   SARS-CoV-2 Infection  
259
HY-B0795 MHY1485
MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.
mTOR   Autophagy  
Breast Cancer   Pancreatic Cancer   Depression   Pain  
219
HY-17471A Metformin hydrochloride
Metformin (1,1-Dimethylbiguanide) hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride exerts central glucose-lowering effects by inhibiting Ras-related protein 1 (Rap1) in SF1 hypothalamic neurons. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, Metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo.
AMPK   Autophagy   Mitophagy   Apoptosis   mTOR  
Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Viral Infection   Digestive System Inflammation   Cardiovascular Disease   Glucose Metabolism   Non-Small Cell Lung Cancer   Lung Adenocarcinoma   Large Cell Lung Carcinoma   HER-2 Positive Breast Cancer   Triple-Negative Breast Cancer   Metastatic Breast Cancer   SARS-CoV-2 Infection   Parkinson's Disease   Chronic Pain   Obesity  
210
HY-B0627 Metformin
Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin exerts central glucose-lowering effects by inhibiting Ras-related protein 1 (Rap1) in SF1 hypothalamic neurons. Metformin also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, Metformin regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo.
AMPK   Autophagy   Mitophagy   Apoptosis   mTOR  
Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Viral Infection   Pain   Digestive System Inflammation   Cardiovascular Disease   Glucose Metabolism   Non-Small Cell Lung Cancer   Lung Adenocarcinoma   Large Cell Lung Carcinoma   HER-2 Positive Breast Cancer   Triple-Negative Breast Cancer   Metastatic Breast Cancer   Parkinson's Disease   Obesity   Lung Fibrosis  
210
HY-15144 Trichostatin A
Trichostatin A (TSA) is a potent and specific inhibitor of HDAC class I/II, with an IC50 value of 1.8 nM for HDAC.
Organoid   HDAC  
Breast Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer  
195
HY-A0004 Decitabine
Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell Apoptosis. Decitabine has potent anticancer activity.
DNA Methyltransferase   Apoptosis   Nucleoside Antimetabolite/Analog  
Pancreatic Cancer   Viral Infection   Digestive System Inflammation   Urogenital Cancer   Non-Small Cell Lung Cancer   Acute Myeloid Leukemia   SARS-CoV-2 Infection   Rheumatoid Arthritis  
177
HY-10221 Vorinostat
Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification.
HDAC   Autophagy   Mitophagy   Filovirus   Apoptosis   HPV  
Neurological, Eye or Ear Disease   Breast Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Viral Infection   Digestive System Inflammation   Lung Fibrosis  
171
HY-B0407A Chlorpromazine hydrochloride
Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis.
Dopamine Receptor   Autophagy   Cytochrome P450   5-HT Receptor  
Neurological, Eye or Ear Disease   Blood or Cardio-cerebrovascular Disease  
147
HY-12708 Chlorpromazine
Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis.
Dopamine Receptor   Cytochrome P450   Autophagy   5-HT Receptor  
Neurological, Eye or Ear Disease   Blood or Cardio-cerebrovascular Disease  
147
HY-B0075 Melatonin
Melatonin is a hormone made by the pineal gland that can activate melatonin receptor and inhibit PANoptosis. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress.
Melatonin Receptor   Autophagy   Mitophagy   Endogenous Metabolite   Apoptosis   PANoptosis   Ligands for Target Protein for PROTAC   Histone Acetyltransferase  
Lung Cancer   Breast Cancer   Prostate Cancer   Liver Cancer   Viral Infection   Neurodegenerative Disease   Digestive System Inflammation   SARS-CoV-2 Infection  
145
HY-13003 Torin 1
Torin 1 is a potent inhibitor of mTOR with an IC50 of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10 nM. Torin 1 is an effective inducer of autophagy.
mTOR   Autophagy  
Lung Cancer   Breast Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Pain   Obesity   Lung Fibrosis  
139
HY-10586 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.
Organoid   Nucleoside Antimetabolite/Analog   DNA Methyltransferase   Bacterial   Autophagy   Antibiotic  
Lung Cancer   Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Bacterial Infection   SARS-CoV-2 Infection   Rheumatoid Arthritis  
139
HY-N0005 Curcumin
Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
Histone Acetyltransferase   Epigenetic Reader Domain   Keap1-Nrf2   Autophagy   Mitophagy   Influenza Virus   Ferroptosis   Apoptosis  
Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Viral Infection   Pain   Digestive System Inflammation   Glucose Metabolism   Metastatic Breast Cancer   SARS-CoV-2 Infection   Obesity   Lung Fibrosis  
135
HY-10218 Everolimus
Everolimus (RAD001) is a Rapamycin (HY-10219) derivative and a potent, selective, orally active, blood-brain barrier-permeable mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities.
mTOR   FKBP   Autophagy   Apoptosis   Bacterial  
Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Bacterial Infection   Pain   Digestive System Inflammation   Non-Small Cell Lung Cancer   Luminal Breast Cancer   HER-2 Positive Breast Cancer   Triple-Negative Breast Cancer   Metastatic Breast Cancer   Cytomegalovirus Infection   SARS-CoV-2 Infection   Obesity   Lung Fibrosis  
119
HY-107455 A-485
A-485, a chemical probe, is a potent and selective catalytic inhibitor of p300/CBP with IC50s of 9.8 nM and 2.6 nM for p300 and CBP histone acetyltransferase (HAT), respectively.
Epigenetic Reader Domain   Histone Acetyltransferase  
Leukemia/Lymphoma/Myeloma   Lung Fibrosis  
110
HY-L005 Epigenetics Compound Library
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 2,010 epigenetics-related compounds that can be used in the research of the related diseases.

Signaling Pathway Targeting Libraries

102
HY-13823 C646
C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.
Histone Acetyltransferase   Autophagy   Epigenetic Reader Domain   Apoptosis  
Digestive System Disease   Leukemia/Lymphoma/Myeloma   Digestive System Inflammation   Glucose Metabolism  
97
HY-12163 Entinostat
Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively.
HDAC   Autophagy   Apoptosis  
91
HY-10224 Panobinostat
Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma.
HDAC   Autophagy   HIV   Apoptosis  
Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Viral Infection   Digestive System Inflammation   Small Cell Lung Cancer   Non-Small Cell Lung Cancer   HER-2 Positive Breast Cancer   Metastatic Breast Cancer   SARS-CoV-2 Infection   Lung Fibrosis  
89
HY-L024 Histone Modification Research Compound Library
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 924 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.

Signaling Pathway Targeting Libraries

85
HY-L034 Anti-Aging Compound Library
Aging is a complex biological process characterized by functional decline of tissues and organs, structural degeneration, and reduced adaptability and resistance, all of which contribute to an increase in morbidity and mortality caused by multiple chronic diseases, such as Alzheimer's disease, cancer, and diabetes. Many theories, which fall into two main categories: programmed and error theories, have been proposed to explain the process of aging, but neither of them appears to be fully satisfactory. The programmed theories imply that aging relies on specific gene regulation, and the error theories emphasize the internal and environmental damages accumulated to living organisms. The damage theories proposed the nine hallmarks that were generally considered to contribute to the aging process: genomic instability, telomere attrition, epigenetic alterations, loss of proteostasis, deregulated nutrient-sensing, mitochondrial dysfunction, cellular senescence, stem cell exhaustion, and altered intercellular communication. MCE Anti-Aging Compound Library contains 7,641 compounds, mainly targeting Sirtuin, mTOR, IGF-1R, AMPK, p53, Telomerase, Mitophagy, Mitochondrial Metabolism, COX, Cytochrome P450, Oxidase, etc. This library is a useful tool for anti-aging research.

Disease Focused Libraries

84
HY-L005M Epigenetics Compound Library Mini
Epigenetics involves heritable phenotypic changes that occur without alterations to the underlying DNA sequence. Key mechanisms include DNA methylation, histone modifications, and regulation by small non-coding RNAs such as microRNAs. By modifying DNA, histones, or RNA—while leaving their primary sequences intact—these processes influence molecular function and regulation, thereby playing critical roles in cellular differentiation, embryonic development, gene expression control, aging, and diseases such as cancer. MCE provide a unique collection of 296 epigenetics-related compounds. For each regulatory target and its subtype, 3 to 5 highly specific representative compounds have been retained, which can be used in epigenetic and related disease research.

Signaling Pathway Targeting Libraries

83
HY-L203 Methylation Compound Library
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 346 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.
83
HY-L249 Lactylation Compound Library
Protein lactylation, an emerging post-translational modification identified in recent years, plays a critical role in linking cellular metabolic reprogramming, epigenetic regulation, and signaling networks. Based on a systematic framework encompassing lactate metabolism, lactylation, and downstream signaling pathways, this compound library comprehensively targets multiple regulatory layers, including histone modification enzymes (such as p300 and HDACs), key glycolytic enzymes (such as PKM2, LDHA, and GAPDH), transcriptional regulators (such as STAT3, HMGB1, and p53), as well as central signaling pathway nodes including HIF-1α, NF-κB, and PI3K-AKT-mTOR. This integrated design enables a comprehensive representation of the regulatory roles of lactylation across the “metabolism–epigenetics–signaling” axis. MCE has assembled a collection of 6,092 known bioactive compounds and potential functional molecules, making this library suitable for a wide range of applications, including high-throughput drug screening, inhibitor identification, and mechanistic studies. It can be used to systematically evaluate the functional roles of lactylation in biological processes such as tumor metabolism, immune regulation, and inflammatory responses, and to efficiently identify small-molecule candidates with regulatory potential, thereby facilitating the development of innovative therapeutics targeting the interplay between metabolism and epigenetic regulation.

Signaling Pathway Targeting Libraries

83
HY-L250 Lactic Acid Metabolite Compound Library
In the progression of various diseases, metabolic reprogramming has emerged as a key hallmark. Lactate, as an important metabolic signaling molecule, is widely involved in tumorigenesis, immune regulation, and inflammatory responses. Particularly within the tumor microenvironment, the abnormal accumulation of lactate not only affects cellular energy metabolism but also promotes disease progression by modulating immune cell functions and mediating protein lactylation, thereby participating in epigenetic regulation and signaling networks. Therefore, systematic investigation of lactate metabolic pathways and their associated metabolites is of great significance for understanding disease mechanisms and developing novel therapeutic strategies. The MCE lactic acid metabolite compound library contains 61 compounds and is constructed around key metabolic pathways involving lactate production, transport, and utilization. This library systematically includes core intermediates from glycolysis, the tricarboxylic acid (TCA) cycle, and the lactate cycle. Focusing on disease-associated metabolic reprogramming, it is suitable for research in oncology, inflammation, and metabolic disorders. The library can be used to elucidate the roles of lactate in tumor microenvironment regulation, immune evasion, and epigenetic modifications (such as protein lactylation). In addition, it provides high-quality small-molecule resources for drug screening, facilitating the discovery of potential modulators targeting key enzymes (such as LDH) or transporters (such as MCTs) involved in lactate metabolism.

Signaling Pathway Targeting Libraries

83
HY-L253 Fungal-Sourced Compound Library
For thousands of years, natural products have always been an important source for drug discovery. Fungi, due to their unique and diverse secondary metabolic capabilities, have become a valuable resource for natural active molecules. Since the discovery of penicillin, natural products derived from fungi have demonstrated significant application value in areas such as anti-infection, anti-tumor, immune regulation, and metabolic disease research. A large number of clinical drugs, such as antibiotics, immunosuppressants, and lipid-lowering drugs, are derived from fungal metabolites or their structurally optimized derivatives. MCE fungal-derived compound library contains 89 structurally diverse and bioactive fungal natural products and their derivatives. It can be widely applied in various research fields such as antibacterial, anti-tumor, anti-inflammatory, immune regulation, epigenetics, and cell signaling pathways, providing high-quality tools for natural product drug development and high-throughput screening.

Natural Product Screening Libraries

83
HY-13755 Sulforaphane
Sulforaphane is an orally active inducer of the Keap1/Nrf2/ARE pathway. Sulforaphane promotes the transcription of tumor-suppressing proteins and effectively inhibits the activity of HDACs. Through the activation of the Keap1/Nrf2/ARE pathway and further induction of HO-1 expression, Sulforaphane protects the heart. Sulforaphane suppresses high glucose-induced pancreatic cancer through AMPK-dependent signal transmission. Sulforaphane exhibits both anticancer and anti-inflammatory properties.
HDAC   Keap1-Nrf2   Apoptosis   Bcl-2 Family   Caspase   Reactive Oxygen Species (ROS)  
Inflammation or Immune System Disease  
77
HY-15149 Romidepsin
Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis.
HDAC   Apoptosis  
Lung Cancer   Triple-Negative Breast Cancer  
75
HY-66005 Acetaminophen
Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent.. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor. Acetaminophen induces ferroptosis and leads to acute liver injury in mice model.
Environmental Pollutants   Histone Acetyltransferase   Ferroptosis   COX   Bacterial   Endogenous Metabolite   Parasite  
Inflammation or Immune System Disease   Breast Cancer   Lung Adenocarcinoma  
73
HY-10585A Valproic acid sodium
Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.
Organoid   HDAC   Autophagy   Mitophagy   HIV   Notch   Apoptosis   Endogenous Metabolite  
Neurological, Eye or Ear Disease   Metabolic or Endocrine Disease  
69
HY-10585 Valproic acid
Valproic acid (VPA) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM. Valproic acid inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid is used in the epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.
Organoid   HDAC   Autophagy   Mitophagy   HIV   Notch   Apoptosis   Endogenous Metabolite  
Infection   Neurological, Eye or Ear Disease   Metabolic or Endocrine Disease   Respiratory Disease   Small Cell Lung Cancer  
69
HY-50876 Daporinad
Daporinad (FK866) is a non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a Ki value of 0.3 nM. Daporinad depletes NAD+ and ATP levels, inhibits mTORC1 and MAPK/ERK pathways, and activates TFEB to induce autophagy. Daporinad causes the depletion of the endoplasmic reticulum Ca²⁺ pool, ultimately weakening the mitogen-induced Ca²⁺ signal and the activation and function of T cells. Daporinad induces cell cycle arrest and apoptosis, and inhibits cell proliferation. Daporinad can be used for the study of myeloma, liver cancer, and immunosuppression.
NAMPT   Autophagy   Apoptosis   mTOR   p38 MAPK   ERK  
Cancer  
67
HY-B1473 Serotonin hydrochloride
Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist, with blood-brain barrier permeability. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
5-HT Receptor   COMT   Endogenous Metabolite  
Neurological, Eye or Ear Disease  
41
HY-B1473A Serotonin
Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
5-HT Receptor   COMT   Endogenous Metabolite  
Neurological, Eye or Ear Disease  
41
HY-12497 ANA-12
ANA-12 is a brain-penetrant, selective TrkB antagonist with IC50 values of 45.6 nM and 41.1 μM, and Kd values of 10 nM and 12 μM, for high- and low-affinity sites, respectively. ANA-12 specifically inhibits BDNF-induced TrkB receptor activation and its downstream signaling cascades by directly and non-competitively binding to the TrkB receptor, without affecting the functions of TrkA and TrkC. ANA-12 is used in research concerning neuropsychiatric disorders (such as depression and anxiety), acute and chronic pain, neuroimmune inflammation, and the mechanisms of learning and memory.
Trk Receptor   NOD-like Receptor (NLR)   AIM2   Caspase  
Depression   Anxiety or Fear-Related Disease   Pain   CNS Infection   Behavioral Addiction  
39
HY-112288 C188-9
C188-9 (TTI-101) is a STAT3 inhibitor with a Kd value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia.
STAT   Apoptosis   DNA Methyltransferase  
Lung Cancer   Breast Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Digestive System Inflammation   Obesity  
36
HY-19545A SCH-23390 hydrochloride
SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
Dopamine Receptor   5-HT Receptor   Potassium Channel  
Depression   Alzheimer's Disease   Obesity  
34
HY-N0145 Puerarin
Puerarin is an isoflavone extracted from Pueraria root and is a 5-HT2C receptor antagonist. Puerarin inhibits the dorsal motor nucleus of the vagus (DMV)-vagus nerve pathway, which in turn leads to decreased fat absorption.
5-HT Receptor  
Cancer   Inflammation or Immune System Disease   Cardiovascular Disease   Glucose Metabolism   SARS-CoV-2 Infection   Alzheimer's Disease   Parkinson's Disease  
32
HY-12678 Entrectinib
Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice.
ROS Kinase   Trk Receptor   Anaplastic lymphoma kinase (ALK)   Autophagy  
Lung Cancer   Prostate Cancer   Pancreatic Cancer   Pain   SARS-CoV-2 Infection  
31
HY-N0737 Harmine hydrochloride
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
Environmental Pollutants   5-HT Receptor   DYRK  
Cancer   Alzheimer's Disease   Parkinson's Disease   Obesity  
29
HY-N0737A Harmine
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
DYRK   5-HT Receptor  
Cancer   Inflammation or Immune System Disease   Alzheimer's Disease   Parkinson's Disease   Obesity  
29
HY-N6732 K-252a
K-252a, a staurosporine analog, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.

Source: Nocardiopsis sp.

Autophagy   Trk Receptor   PKC   PKA   CaMK  
Infection   Inflammation or Immune System Disease  
27
HY-111558 Bobcat339
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.
DNA Methyltransferase   TET Protein  
Leukemia/Lymphoma/Myeloma   Rheumatoid Arthritis  
26
HY-135146 GSK-3484862
GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma.
DNA Methyltransferase   Apoptosis  
Lung Cancer   Breast Cancer   Leukemia/Lymphoma/Myeloma  
26
HY-B0350A Sodium butyrate
Sodium Butyrate (sodium butanoate) is an inhibitor of HDAC, possessing anti-tumor activity.
HDAC   Autophagy   Apoptosis   Endogenous Metabolite  
Neurological, Eye or Ear Disease   Breast Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Digestive System Inflammation   SARS-CoV-2 Infection  
25
HY-15826 SGC-CBP30
SGC-CBP30, a chemical probe, 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.
Epigenetic Reader Domain   Histone Acetyltransferase  
Inflammation or Immune System Disease   Leukemia/Lymphoma/Myeloma   Depression   Lung Fibrosis  
24
HY-16706 Remodelin
Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model.
Histone Acetyltransferase  
Prostate Cancer   Liver Cancer   Non-Small Cell Lung Cancer  
23
HY-N0171A Beta-Sitosterol (purity>98%)
Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc.
Bacterial   Apoptosis   Reactive Oxygen Species (ROS)   MDM-2/p53   Caspase   PARP   MMP   Bcl-2 Family   HIF/HIF Prolyl-Hydroxylase   TNF Receptor   Interleukin Related   NF-κB   mTOR   Lactate Dehydrogenase   CDK   Glutathione Peroxidase   SOD  
Lung Cancer   Breast Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Bacterial Infection   Depression   Pain   Digestive System Inflammation   Cardiovascular Disease   Glucose Metabolism   Obesity   Lung Fibrosis   Rheumatoid Arthritis  
23
HY-W013372 7,8-Dihydroxyflavone
7,8-Dihydroxyflavone is a potent and selective TrkB agonist that mimics the physiological actions of Brain-derived neurotrophic factor (BDNF). Displays therapeutic efficacy toward various neurological diseases.
Trk Receptor   Apoptosis  
Neurological, Eye or Ear Disease  
21
HY-13962 SGI-1027
SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.
DNA Methyltransferase   Apoptosis  
Digestive System Disease   Leukemia/Lymphoma/Myeloma   Digestive System Inflammation   Rheumatoid Arthritis  
19
HY-12866 Larotrectinib
Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
Trk Receptor   Apoptosis  
Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Pain   Digestive System Inflammation   SARS-CoV-2 Infection  
17
HY-139664 GSK-3685032
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.
DNA Methyltransferase  
Leukemia/Lymphoma/Myeloma   Rheumatoid Arthritis  
15
HY-13642 RG108
RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.
DNA Methyltransferase  
Leukemia/Lymphoma/Myeloma   Rheumatoid Arthritis  
14
HY-14541 Olanzapine
Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic.
5-HT Receptor   Dopamine Receptor   mAChR   Adrenergic Receptor   Autophagy   Mitophagy   Apoptosis  
Cancer   Digestive System Disease   Depression   Digestive System Inflammation   SARS-CoV-2 Infection   Alzheimer's Disease   Parkinson's Disease   Hypertension  
14
HY-13765 6-Thioguanine
6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively.
SARS-CoV   Deubiquitinase   DNA Methyltransferase   Autophagy   Apoptosis   Endogenous Metabolite  
Digestive System Disease   Leukemia/Lymphoma/Myeloma   Viral Infection   Digestive System Inflammation   SARS-CoV-2 Infection   Rheumatoid Arthritis  
13
HY-14539 Clozapine
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
Dopamine Receptor   mAChR   Adrenergic Receptor   5-HT Receptor   Ligands for E3 Ligase  
Schizophrenia  
13
HY-111784 Inobrodib
Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression.
Ligands for Target Protein for PROTAC   Epigenetic Reader Domain   Histone Acetyltransferase  
Leukemia/Lymphoma/Myeloma   Non-Small Cell Lung Cancer   Metastatic Breast Cancer   Metastatic Prostate Cancer  
12
HY-18314 GW 441756
GW 441756 is a potent and specific nerve growth factor (NGF) receptor tyrosine kinases A (TrkA) inhibitor (IC50=2 nM), which eliminates the BmK NSPK-induced neurite outgrowth.
Trk Receptor   Apoptosis  
Cancer   Digestive System Disease   Pain   Digestive System Inflammation  
11
HY-134901 WM-3835
WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice.
Histone Acetyltransferase   Apoptosis  
Cancer   Digestive System Disease   Digestive System Inflammation  
11
HY-B0527 Amitriptyline
Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
Serotonin Transporter   5-HT Receptor   mAChR   Sodium Channel   Adrenergic Receptor   Trk Receptor   Histamine Receptor   Potassium Channel   Dopamine Transporter   Apoptosis  
Digestive System Disease   Depression   Pain   Digestive System Inflammation   SARS-CoV-2 Infection   Pseudomonas Aeruginosa Infection   Alzheimer's Disease   Parkinson's Disease   Hypertension   Obesity  
8
HY-103022 Repotrectinib
Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity.
ROS Kinase   Trk Receptor   Anaplastic lymphoma kinase (ALK)  
Lung Cancer   Pain   SARS-CoV-2 Infection  
8
HY-N0401A (Z)-Ligustilide
(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.
Bacterial   Estrogen Receptor/ERR   FATP  
Infection   Metabolic or Endocrine Disease   Breast Cancer  
5
HY-132283 PF-9363
PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer.
Histone Acetyltransferase  
Cancer  
5
HY-A0019 Paliperidone
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.
Drug Metabolite   Dopamine Receptor   5-HT Receptor   Adrenergic Receptor  
Depression   Alzheimer's Disease   Parkinson's Disease   Hypertension  
3
HY-107854 N-Acetyl-5-hydroxytryptamine
N-Acetyl-5-hydroxytryptamine is a Melatonin precursor, and that it can potently activate TrkB receptor.
Endogenous Metabolite   Trk Receptor  
Depression  
2
HY-N0122 5-Hydroxytryptophan
5-Hydroxytryptophan, a tryptophan metabolite, is a direct 5-hydroxytryptamine (5-HT) precursor and an L-aromatic amino acid decarboxylase substrate. .
Endogenous Metabolite   5-HT Receptor  
Glucose Metabolism   Alzheimer's Disease   Obesity  
2
HY-N0775 Isocorynoxeine
Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.
5-HT Receptor  
Alzheimer's Disease   Parkinson's Disease  
1
HY-P99221 Tanezumab
Tanezumab (RN-624) is a humanized anti-NGF mAb with high affinity and specificity. Tanezumab blocks NGF binding to its receptors, p75 and TrkA, in the peripheral nervous system. Tanezumab can be used in studies of acute and chronic pain such as osteoarthritis, knee and neuralgia, as well as post-herpetic neuralgia.

Species: Human

Trk Receptor  
Inflammation or Immune System Disease   Pain  
1
HY-158301 MY-1B
MY-1B is a covalent inhibitor of the RNA Methyltransferase NSUN2 (IC50: 1.3 μM). MY-1B stereoselectively ligands active-site cysteine residues (C271) of NSUN2. MY-1B can stereoselectively and covalently bind to PSME1, disrupting the proteasome regulatory complex and downregulating the presentation of specific MHC-I subtypes.
DNA Methyltransferase   Ligands for E3 Ligase   RNA MTase  
Prostate Cancer  
1
HY-11018S2 Risperidone-d6
Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
5-HT Receptor   Dopamine Receptor   P-glycoprotein  
Neurological, Eye or Ear Disease  
/
HY-N20747 Norpsilocin
Norpsilocin (4-hydroxy-N-methyltrypt amine; 4-HO-NMT) is a natural tryptamine alkaloid isolated from the hallucinogenic mushroom Psilocybe cubensis. Norpsilocin activates human 5-HT2 receptors (5-HT2A: EC50 = 8.4 nM; 5-HT2B = 12.8 nM; 5-HT2C = 39.6 nM) and displays binding affinity toward 5-HT1 receptors (5-HT1B: Ki = 212 nM; 5-HT1D = 48.9 nM; 5-HT1E = 81.7 nM). Norpsilocin induces β-arrestin recruitment at the 5-HT1B receptor. Norpsilocin fails to produce psychedelic-like effects in mice, whereas high doses can induce hypothermia in vivo. Norpsilocin acts as an important research tool for exploring the structure–activity relationship of tryptamine hallucinogens and the pharmacology of serotonin receptors.

Source: Psilocybe cubensis

5-HT Receptor  
/
HY-N0775R Isocorynoxeine (Standard)
Isocorynoxeine (Standard) is the analytical standard of Isocorynoxeine. This product is intended for research and analytical applications. Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.
Reference Standards   5-HT Receptor  
Neurological, Eye or Ear Disease  
/
HY-175483S TrkB activator-1
TrkB activator-1 is a specific, orally active and brain-penetrant tropomyosin receptor kinase B (TrkB) activator. TrkB activator-1 shows potent antidepressant effects through activation of the activates the BDNF (brainderived neurotrophic factor)-Tropomyosin-related kinase B (TrkB)-CREB (cAMP response element binding protein) signaling aixs. TrkB activator-1 increaes neuroplasticity. TrkB activator-1 can be used for the research of neurological disease, such as depression.
Trk Receptor   Isotope-Labeled Compounds  
Neurological, Eye or Ear Disease  
/
HY-P3035 Corazonin
Corazonin is a highly conserved neuropeptide hormone of wide-spread occurrence in insects, serves a central regulator of caste identity and behavior in social insects. Corazonin is also preferentially expressed in workers and/or foragers from other social insect species.
G Protein-coupled Receptor Kinase (GRK)  
Neurological, Eye or Ear Disease  
/
HY-B0781S1 Promethazine-d3 hydrochloride
Promethazine-d3 (hydrochloride) is deuterium labeled Promethazine (hydrochloride). Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors.
Isotope-Labeled Compounds   Histamine Receptor   Adrenergic Receptor   mAChR  
Neurological, Eye or Ear Disease   Metabolic or Endocrine Disease  
/
HY-W783478 Calebin A
Calebin A is a PI3K/Akt/mTOR, MAPK, and NF-κB inhibitor with oral effectiveness. Calebin A can block the autophagy-repressive, inhibiting apoptosis. Calebin A has anti-tumor activity by epigenetic regulation. Calebin A suppresses adipogenesis, modulates thermogenesis, and enriches gut probiotics. Calebin A can be used in research on osteoarthritis, Alzheimer's disease, type 2 diabetes, malignant peripheral nerve sheath tumors, and colorectal cancer.
PI3K   Akt   mTOR   p38 MAPK   NF-κB  
Inflammation or Immune System Disease   Colorectal Cancer   Alzheimer's Disease   Type 2 Diabetes   Osteoarthritis  
/
HY-P992426 NS101
NS101 is an anti-FAM19A5 antibody with an IC50 of 0.2 nM and a Kd of 111 pM, as well as blood-brain barrier permeability. NS101 binds to key amino acid residues of FAM19A5, thereby blocking the interaction of LRRC4B and disrupting the FAM19A5-LRRC4B complex. NS101 increases the dendritic spine density in hippocampal neurons and the prefrontal cortex, normalizes the dendritic spine elimination rate, elevates the frequencies of mEPSC and fEPSP, and promotes the transport of brain-derived FAM19A5 into the peripheral circulation. NS101 improves cognitive function in mouse models of Alzheimer's disease. NS101 can be used for research on Alzheimer's disease. The recommended isotype control is human IgG1 kappa (HY-P99001).

Species: Human

Tau Protein  
Alzheimer's Disease  
/
HY-11018S1 Risperidone-d4-1
Risperidone-d4-1 (R 64 766-d4-1) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
Isotope-Labeled Compounds   Dopamine Receptor   P-glycoprotein   5-HT Receptor  
Neurological, Eye or Ear Disease  
/
HY-A0019AS Paliperidone palmitate-d4
Paliperidone palmitate-d4 (9-Hydroxyrisperidone palmitate-d4) is the deuterium labeled Paliperidone palmitate (HY-A0019A). Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia.
Isotope-Labeled Compounds   5-HT Receptor   Dopamine Receptor  
Neurological, Eye or Ear Disease  
/
HY-19733S1 Lumateperone-d4 tosylate
Lumateperone-d4 tosylate (ITI-007-d4 tosylate) is the deuterium labeled Lumateperone tosylate (HY-19733). Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.
Isotope-Labeled Compounds   5-HT Receptor   Dopamine Receptor  
Cancer   Neurological, Eye or Ear Disease  
/
HY-G0002S Lurasidone metabolite 14326-d8
Lurasidone metabolite 14326-d8 is a deuterium-labeled form of Lurasidone metabolite 14326 (HY-G0002). Lurasidone metabolite 14326 is a minor active metabolite of Lurasidone (HY-B0032A) generated via metabolism by CYP3A4. Lurasidone metabolite 14326 shares similar receptor-binding properties with Lurasidone, acting as an antagonist of the dopamine D2 receptor (dopamine D2 receptor), an antagonist of the serotonin 5-HT2A and 5-HT7 receptors (5-HT2A and 5-HT7 receptor), and a partial agonist of the serotonin 5-HT1A receptor. Lurasidone metabolite 14326 can be used in the research of schizophrenia and bipolar depression.
Isotope-Labeled Compounds   Drug Metabolite   Dopamine Receptor   5-HT Receptor  
Schizophrenia   Depression  
/
HY-N15448 Dihydrosamidin
Dihydrosamidin is a coumarin component isolated from the fruits of ammi visnaga. Dihydrosamidin promotes neuroplasticity, modulates glycolysis and oxidative phosphorylation and enhances antioxidant defences. Dihydrosamidin inhibits triacylglycerol accumulation in 3T3-L1 preadipocytes. Dihydrosamidin can be used for neuroprotective, anti-obesity study.
Endogenous Metabolite  
Neurological, Eye or Ear Disease   Metabolic or Endocrine Disease  
/
HY-A0019R Paliperidone (Standard)
Paliperidone (Standard) is the analytical standard of Paliperidone. This product is intended for research and analytical applications. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.
Drug Metabolite   Reference Standards   Dopamine Receptor   5-HT Receptor   Adrenergic Receptor  
Neurological, Eye or Ear Disease  
/
HY-17637S2 Lumateperone-d4
Lumateperone-d4 (ITI-007-d4) is deuterium labeled Lumateperone. Lumateperone (ITI-007) is an orally active 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used for the study of schizophrenia and bipolar depression.
Isotope-Labeled Compounds   5-HT Receptor   Dopamine Receptor  
Cancer   Neurological, Eye or Ear Disease  
/
HY-N0737R Harmine hydrochloride (Standard)
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
Reference Standards   DYRK   5-HT Receptor  
Cancer   Neurological, Eye or Ear Disease  
/
HY-110232 Risperidone-d4
Risperidone-d4 is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
5-HT Receptor   Dopamine Receptor   P-glycoprotein  
Neurological, Eye or Ear Disease  
/
HY-N12613 Sydowimide A
Sydowimide A is a potent inhibitor of Src homology region 2 domain-containing phosphatase-1 (SHP1), T-cell protein tyrosine phosphatase (TCPTP) and leukocyte common antigen (CD45), with IC50 values of 1.5, 2.4 and 18.83 μM, respectively.

Source: Aspergillus sydowii DL1045

SHP1   Phosphatase  
Inflammation or Immune System Disease  
/
HY-B0781S Promethazine-d4 hydrochloride
Promethazine-d4 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.
Histamine Receptor  
Neurological, Eye or Ear Disease   Metabolic or Endocrine Disease  
/
HY-N18343 Ebelin lactone
Ebelin lactone is an acetylcholinesterase (AChE) inhibitor, with a Ki of 0.45 μM against human M1 muscarinic acetylcholine receptor (mAChR) and a Ki of 4.21 μM against human 5-HT2A serotonin receptor. Ebelin lactone binds to the allosteric cavity above the orthosteric site of M1 via nonpolar interactions with subtype-selective residues. Ebelin lactone binds to the cavity between transmembrane helices 4 and 5 of 5-HT2A through nonpolar interactions with orthosteric site residues. Ebelin lactone exhibits free radical scavenging activity, inhibits cancer cell proliferation, and regulates memory and cognitive processes by interacting with M1 and 5-HT2A receptors. Ebelin lactone can be used in studies related to Alzheimer's disease, breast cancer and colorectal cancer.
Drug Derivative   Cholinesterase (ChE)   mAChR   5-HT Receptor  
Breast Cancer   Colorectal Cancer   Alzheimer's Disease  
/
HY-N0737AR Harmine (Standard)
Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
Reference Standards   DYRK   5-HT Receptor  
Cancer   Neurological, Eye or Ear Disease  
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HY-113008AS cis-Urocanic acid-13C3
cis-Urocanic acid-13C3 is the 13C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.
Isotope-Labeled Compounds   5-HT Receptor  
Inflammation or Immune System Disease  
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HY-N0737AG Harmine (GMP)
Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
DYRK   5-HT Receptor  
Cancer   Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
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HY-N12614 Diorcinol
Diorcinol is a potent SHP1 inhibitor with an IC50 value of 0.96 μM. Diorcinol can be isolated from Aspergillus sydowii. Diorcinol has good blood-brain barrier penetration and can be used for diabetes research.

Source: A. sydowii DL1045

SHP1   Phosphatase  
Glucose Metabolism  
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HY-P10506 CMX-8933
CMX-8933 is an octapeptide fragment of the goldfish brain neurotrophic factor ependymin. CMX-8933 increases the enzymatic activity of c-Jun N-terminal kinase (JNK), increases the phosphorylation of JNK and c-Jun proteins, and increases the cellular levels of c-Jun and c-Fos mRNA. CMX-8933 can be used to study the role of ependymin in neuroplasticity, learning, memory formation, and neural regeneration.
JNK  
Pain  
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HY-P1958 Histone H4 (2-21)
Histone H4 (2-21) is a substrate peptide derived from the N-terminal region of histone H4, which serves as an acyl acceptor for lysine acetyltransferases of the MYST family (KAT). Histone H4 (2-21) participates in enzymatic reactions together with acyl-coenzyme A (acyl-CoA, and undergoes lysine acetylation and propionylation modifications catalyzed by KATs such as MOF. The apparent Km of Histone H4 (2-21) for MOF is 788.8 μM, while in the picNuA4 catalytic system, the Km and Kd values of the H4 peptide are 192 μM and 251 μM, respectively. Histone H4 (2-21) can be used in studies related to histone post-translational modifications, epigenetic regulation, and lysine acylation.
Histone Acetyltransferase  
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HY-113491 3-Phosphoglyceric acid
3-Phosphoglyceric acid is a metabolic intermediate in both glycolysis and the Calvin cycle. 3-Phosphoglyceric acid is involved in alveolar macrophage epigenetic regulation.
Endogenous Metabolite  
Glycolysis  
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HY-P703149 5HT2A Protein, Human (S162K, M164W, sf9, Flag, His)
5HT2A Protein, Human (S162K, M164W, sf9, Flag, His) is the recombinant human-derived 5HT2A, expressed by sf9 insect cells, with His, Flag labeled tag.,

Species: Human; Source: Sf9 insect cells

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HY-P703150 5HT2A Protein, Human (L247A, L371A, sf9, Flag, His)
5HT2A Protein, Human (L247A, L371A, sf9, Flag, His) is the recombinant human-derived 5HT2A, expressed by sf9 insect cells, with His, Flag labeled tag.,

Species: Human; Source: Sf9 insect cells

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HY-P810892 Human IgG1 Antibody
Human IgG1 Antibody is a Rabbit-derived and non-conjugated IgG Polyclonal antibody, targeting to Human IgG1.

Host: Rabbit; Reactivity: Human

Polyclonal Antibodies Primary Antibodies

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HY-P810890 5-HT2A Antibody
5-HT2A Antibody is a Rabbit-derived and non-conjugated IgG Polyclonal antibody, targeting to 5-HT2A.

Host: Rabbit; Reactivity: Human, Mouse, Rat, Monkey, Pig, Bovine

Polyclonal Antibodies Primary Antibodies

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HY-P89684 5HT2A Receptor Antibody (YA9028)
5HT2A Receptor Antibody (YA9028) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to 5HT2A Receptor.

Host: Mouse; Reactivity: human, mouse, rat

Monoclonal Antibodies Primary Antibodies

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Keywords

psychedelics | psilocybin | neuroplasticity | epigenetic regulation | 5-HT2A receptor | dendritic spines | activity-dependent transcription | psychoplastogens