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Epigenetic Regulation and the Tumor Immune Microenvironment

Tumor Microenvironment Cancer Immunotherapy Chronic Inflammation Intercellular Communication & Diseases

The tumor immune microenvironment is a spatial ecosystem of malignant, immune, stromal, endothelial, and extracellular-matrix components. Epigenetic regulation controls both tumor-intrinsic immunogenicity and the differentiation or persistence of T cells, macrophages, dendritic cells, myeloid-derived suppressor cells, and cancer-associated fibroblasts. DNA methylation, histone modifications, chromatin remodeling, and regulatory RNAs can convert inflammatory signals into durable states. This makes the epigenome a mechanism of immune escape and a potential route to sensitize tumors to immunotherapy[1][2][3].

Tumor methylation and Polycomb repression can reduce antigen presentation, interferon signaling, endogenous retroelement expression, and T-cell-attracting chemokines. In immune cells, DNMTs, TET enzymes, EZH2, HDACs, bromodomain proteins, and metabolic histone marks regulate exhaustion, memory, macrophage polarization, and suppressive myeloid function. Fibroblast and endothelial epigenomes control cytokines, adhesion, matrix, and immune-cell trafficking. Lactate, hypoxia, nutrient depletion, and cytokines reinforce these programs, linking tumor metabolism with chromatin across cell types[1][2][3].

Applications include combining DNMT, HDAC, EZH2, or BET inhibitors with immune-checkpoint blockade, adoptive-cell therapy, or cancer vaccines. Epigenetic treatment can induce viral-mimicry pathways, increase chemokines, or alter suppressive stromal and myeloid states. Single-cell and spatial multi-omics identify which compartment engages the drug and which immune population changes. Response biomarkers should measure tumor and host effects because the same agent can enhance antigen presentation yet impair effector-cell proliferation at another dose or schedule[1][2][3].

Clinical results remain context dependent. Broad epigenetic drugs can cause cytopenias, infection risk, and opposing immune effects, while pretreatment biopsies may miss spatial heterogeneity. Future trials should use pharmacodynamic biopsies, cell-type-resolved biomarkers, and schedules based on immune priming rather than maximum tolerated dose alone. Locus- or cell-selective delivery may widen therapeutic windows. Mechanistic combinations should show that chromatin modulation increases functional antitumor immunity and that checkpoint blockade is required for the added effect. Durable benefit will require preventing both tumor-cell escape and re-establishment of suppressive immune states A decisive preclinical combination study should include tumor-cell and immune-cell perturbations separately. If DNMT inhibition increases interferon genes in cancer cells, investigators should test whether tumor-intrinsic editing is sufficient, whether T cells are required, and whether the effect depends on antigen presentation. Conversely, editing T cells or myeloid cells can reveal host mechanisms masked by systemic drug exposure. Spatial analysis should show whether effector cells enter tumor nests and contact malignant cells, not simply increase in the surrounding stroma. Durable-response studies must assess memory after drug withdrawal and rechallenge. These experiments can identify the compartment that should receive an epigenetic agent and minimize opposing effects on antitumor and regulatory immune populations. Human trials should distinguish immune-cell redistribution from true expansion or activation and should monitor clonal T-cell responses. Cytokine induction without tumor recognition may add toxicity rather than efficacy. Comparative biopsies of responders and nonresponders can identify adaptive escape, including antigen loss, alternative checkpoints, myeloid recruitment, or fibroblast barriers. A successful regimen should produce a measurable sequence from chromatin change to immune-cell function to tumor regression and memory after complete treatment withdrawal and subsequent tumor rechallenge in clinically relevant models[1][2][3].

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Cat. No. Product Name Information Application Publication
HY-13818 Stattic
Stattic is a potent STAT3 inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727). Stattic inhibits the binding of a high affinity phosphopeptide for the SH2 domain of STAT3. Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice.
STAT   Apoptosis  
Lung Cancer   Breast Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Digestive System Inflammation   Obesity  
324
HY-10201 Sorafenib
Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.
Raf   VEGFR   FLT3   Autophagy   Apoptosis   STAT   Akt   MMP   Cadherin   p38 MAPK   ERK   MEK   PI3K   PARP   Bcl-2 Family   Ephrin Receptor   PDGFR  
Gastric Cancer   Liver Cancer   Ovarian Cancer   Digestive System Inflammation   Small Cell Lung Cancer   Non-Small Cell Lung Cancer   Metastatic Breast Cancer   Metastatic Colorectal Cancer   Metastatic Prostate Cancer   Multiple Myeloma   Metastatic Pancreatic Cancer   SARS-CoV-2 Infection   Alzheimer's Disease   Parkinson's Disease   Obesity   Lung Fibrosis  
317
HY-13030 (+)-JQ-1
(+)-JQ-1 (JQ1), a chemical probe, is a potent, specific, CNS-penetrant and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.
Epigenetic Reader Domain   Autophagy   Ligands for Target Protein for PROTAC   SWI/SNF Complex  
Neurological, Eye or Ear Disease   Leukemia/Lymphoma/Myeloma  
310
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  
262
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  
202
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  
184
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  
175
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  
142
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  
139
HY-B0069 Fludarabine
Fludarabine (NSC 118218) is a DNA synthesis inhibitor and a fluorinated purine analogue with antineoplastic activity in lymphoproliferative malignancies. Fludarabine inhibits the cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in normal resting or activated lymphocytes.
Nucleoside Antimetabolite/Analog   DNA/RNA Synthesis   STAT   Apoptosis  
Lung Cancer   Breast Cancer   Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Viral Infection   Digestive System Inflammation   SARS-CoV-2 Infection   Obesity   Lung Fibrosis  
120
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  
115
HY-13470 GSK126
GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM.
Histone Methyltransferase  
Colorectal Cancer   Leukemia/Lymphoma/Myeloma   Small Cell Lung Cancer  
105
HY-40354 Tofacitinib
Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.
JAK   STAT   NF-κB  
Depression   Pulmonary Disease   Systemic Lupus Erythematosus   Liver Injury   Rheumatoid Arthritis  
103
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 2,031 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  
99
HY-13803 Tazemetostat
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells.
Histone Methyltransferase   Apoptosis  
Pancreatic Cancer   Digestive System Inflammation   Castration-Resistant Prostate Cancer   Metastatic Prostate Cancer   Acute Myeloid Leukemia  
98
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  
95
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   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  
90
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 931 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 7,771 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 295 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-L041 Macrocyclic Compound Library
Macrocycles, molecules containing 12-membered or larger rings, are receiving increased attention in small-molecule drug discovery. The reasons are several, including providing access to novel chemical space, challenging new protein targets, showing favorable ADME- and PK-properties. Macrocycles have demonstrated repeated success when addressing targets that have proved to be highly challenging for standard small-molecule drug discovery, especially in modulating macromolecular processes such as protein–protein interactions (PPI). Otherwise, the size and complexity of macrocyclic compounds make possible to ensure numerous and spatially distributed binding interactions, thereby increasing both binding affinity and selectivity. MCE offers a unique collection of 468 macrocyclic compounds which can be used for drug discovery for high throughput screening (HTS) and high content screening (HCS). MCE Macrocyclic Compound Library is a useful tool for discovering new drugs, especially for “undruggable” targets and protein–protein interactions.

Structure Classified Libraries

83
HY-L170 Allosteric Modulators (AMs) Compound Library
An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands. MCE designs a unique collection of 258 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

Compound Characteristic Classified 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 351 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-L204 Lactic Acid Metabolic Compound Library
Lactic acid metabolism is one of the key metabolic pathways within living organisms. It plays a crucial role not only in cellular energy conversion but is also closely related to a variety of physiological and pathological processes. The production and clearance of lactic acid are important indicators of cellular metabolic balance, and its abnormal regulation may lead to conditions such as lactic acidosis, muscle fatigue, and hereditary metabolic diseases. Moreover, lactic acid is closely related to the malignancy of tumors and is considered a biomarker for malignant tumors and poor prognosis. Lactic acid can serve as a metabolic substrate to support the metabolic needs of tumor cells under hypoxic conditions, and it can also cause acidification of the tumor microenvironment, suppress immune cell function to promote immune evasion, and induce drug resistance in tumor cells. Currently, targeting lactic acid-lactylation and its related metabolic pathways has become a new research avenue for cancer treatment. In-depth exploration of the molecular mechanisms of lactic acid metabolism can help in screening lead compounds that regulate the lactic acid metabolism. MCE contains 582 small molecule compounds targeting enzymes involved in lactic acid metabolism. This library is of significant value for researching the role of lactate metabolism in the mechanisms of diseases.
83
HY-L213 Anti-Cancer Approved Drug Library
The anti-cancer drug library meticulously collects all drugs approved by FDA and other major national drug regulatory authorities for cancer treatment. These drugs cover a variety of cancer types, including but not limited to lung cancer, breast cancer, colorectal cancer, leukemia, and other common cancers. The library includes a wide range of drugs, from classic chemotherapeutic agents to cutting-edge targeted therapies and immunotherapies. It contains various types of drug compounds with different mechanisms of action. There are cytotoxic drugs that directly kill cancer cells, as well as drugs that work by modulating the tumor microenvironment, inhibiting tumor angiogenesis, and activating the immune system. This diversity provides researchers with a broad range of perspectives and options for intervention strategies. This library can be used for basic research on cancer treatment, exploring new targets and new mechanisms of drug action; Conducting drug reuse research to look for potential therapeutic effects of existing drugs on other cancer types or diseases; Or conducting research into combination drugs to optimize cancer treatment. MCE has collected 265 small-molecule compounds with cancer indications, which are good tools for drug repurposing.
83
HY-L215 Mass Spectrometry Human Metabolite Library
Metabolomics, positioned as the systemic characterization of small-molecule metabolites within biological systems, has emerged as an indispensable analytical platform in both fundamental research and translational applications across plant sciences, microbial biotechnology, and biomedical investigations. Functioning as a critical component in multi-omics integration, this discipline deciphers the intricate molecular networks operating downstream of genomic, transcriptomic, and proteomic regulation, thereby capturing the dynamic biochemical phenotype closest to organismal functionality. The metabolome, comprising endogenous compounds with molecular weights typically below 1500 Da, serves as the functional readout of cellular processes and environmental interactions, where perturbations in metabolic networks are frequently implicated in disease pathogenesis. Such unique attributes have propelled metabolomics into a pivotal role in pharmacological research, particularly in target deconvolution, pharmacodynamic assessment, and mechanistic elucidation of pathological processes. MCE can provide 6,077 mass spectrometry human metabolites that can be used for metabolite identification and quantification, functional cell detection and phenotypic screening of mass spectrometry.

Metabolism Focused Libraries

83
HY-L234 Nucleotide Metabolite Compound Library
Nucleotide metabolism is central to cancer aggressiveness, underpinning uncontrolled proliferation, chemotherapy resistance, immune evasion, and metastasis. It is transcriptionally regulated by oncogenes (e.g., MYC) and tumor suppressors (e.g., pRb). Nucleotide imbalance and nucleoside degradation further regulate cell state transitions, especially following replication stress. Additionally, secretion of nucleotides/nucleosides into the tumor microenvironment modulates immune responses and influences treatment efficacy. Therefore, nucleotide metabolites have roles in disease response and indication in cancer research, and can be utilized to develop cancer-related mechanisms and drugs. MCE can provide 83 metabolites produced by nucleotide metabolic pathways, which can be used for disease mechanism research and drug research.

Metabolism Focused Libraries

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 6,182 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-L252 Carbohydrate Metabolite Compound Library
Carbohydrate metabolism serves as a central hub for energy supply and biosynthesis in living organisms and plays a critical role in the onset and progression of various diseases. In recent years, studies have shown that tumor cells reprogram their energy metabolism through aerobic glycolysis (the Warburg effect) to support rapid proliferation. Immune cells also rely on specific carbohydrate metabolic pathways to regulate their activation and differentiation states, while disorders such as diabetes and metabolic syndrome arise directly from dysregulation of carbohydrate metabolism. In addition, enzymes and key metabolic nodes involved in carbohydrate metabolism have become important targets for drug discovery, and therapeutic strategies targeting glycolysis, the pentose phosphate pathway, and energy metabolism are continuously advancing the treatment of cancer and metabolic diseases. Therefore, systematic analysis of carbohydrate metabolic networks and their associated metabolites is of great significance for elucidating disease mechanisms and developing novel therapeutic approaches. The MCE Carbohydrate Metabolism Metabolite Library is constructed based on classical carbohydrate metabolic pathways and contains 76 metabolites. It systematically integrates key metabolic networks, including glycolysis, the pentose phosphate pathway, the tricarboxylic acid (TCA) cycle, monosaccharide metabolism, and sugar acid interconversions. The library comprehensively covers core metabolic nodes from glucose uptake and utilization to energy production and biosynthesis, while also incorporating important upstream and downstream intermediates. It enables accurate representation of intracellular metabolic flux dynamics and is well suited for applications such as metabolic flux analysis, target validation, and mechanistic studies. Furthermore, it provides robust support for multi-omics integration and the development of precision intervention strategies.
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 91 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-L257 Azide PROTAC Linker Library
Linkers, as key structural units in PROTAC molecules that connect the two functional ends, not only determine the overall molecular conformation and spatial compatibility but also directly influence the stability of the ternary complex, as well as cellular permeability and degradation efficiency. In recent years, with the widespread application of click chemistry in medicinal chemistry, the incorporation of bioorthogonal reactive groups such as azides (-N3) into PROTAC linker design has become an emerging research focus, providing an important tool for modular assembly and rapid structural optimization. The MCE Azide PROTAC Linker Library contains 0 linkers specifically designed for targeted protein degradation molecule design and optimization. These linkers serve as efficient “click handles,” enabling rapid and highly selective covalent coupling with alkyne reaction partners, thereby facilitating modular assembly and structural diversification of PROTAC molecules. In drug development, this design not only improves the efficiency of molecular construction but also significantly accelerates the screening and optimization of lead compounds. Meanwhile, by tuning linker properties such as length, flexibility, and polarity, the ability to form ternary complexes and degradation activity can be optimized.
83
HY-L259 Alkyne PROTAC Linker Library
In PROTAC drug development, linkers are often one of the key variables determining drug-likeness and degradation efficiency. Since PROTAC systems must simultaneously satisfy target protein binding, E3 ligase recruitment, and intracellular spatial conformational matching, their structural design is essentially a multi-parameter optimization problem. Differences in linker rigidity, flexibility, and spatial extension can significantly influence the formation pathway and stability of the ternary complex, leading to substantial variations in degradation activity. Therefore, the development of linker systems with modular tunability and high structural expandability has become an important direction in PROTAC optimization. The MCE Alkyne PROTAC Linker Library contains 0 linkers based on terminal and internal alkyne scaffolds, forming a highly derivatizable linker module system. These linkers serve as standardized building blocks for rapid assembly and iterative optimization of PROTAC molecules, and support efficient conjugation with azide-containing functional groups via click chemistry. In practical drug development, this type of structure not only facilitates the construction of diverse linker space libraries, accelerating lead compound screening, but also enables systematic tuning of molecular geometry and physicochemical properties, thereby improving ternary complex stability and targeted protein degradation efficiency.
83
HY-L944 MCE‑18 Novelty Focused Drug‑Like Library
MCE 18 stands for Medicinal Chemistry Evolution 2018. This metric was established based on structural data of 28,161 patented lead molecules, 1,370 marketed innovative drugs, and nearly 30,000 investigational candidates from preclinical to Phase III stages across 23 major global pharmaceutical companies from 1950 to 2018. After scaffold clustering analysis, a scoring model was constructed by integrating five three dimensional scaffold characteristics, including aromatic rings (AR), non aromatic heterocycles (NAR), chiral centers (CHIRAL), spirocycles (SPIRO), and the sp³ carbon ratio in cyclic and acyclic moieties, enabling quantitative assessment of molecular scaffold novelty and three dimensional complexity. According to the score distribution of patented molecules, the top 25% of the original patent dataset was defined as the high novelty region. MCE 18 high scoring compounds selected based on this criterion can effectively avoid scaffold patent conflicts and intellectual property risks from the source. Molecules in this range typically feature a high sp³ carbon ratio, abundant chiral centers, spirocycles, and fused heterocycles with prominent three dimensional conformations. Their spatial properties allow precise matching to complex non traditional undruggable target pockets such as PPI interfaces and allosteric sites, making them ideal structural types for early stage screening of First in class drugs. MCE‑18 Novelty Focused drug‑Like library strictly selects molecules from the aforementioned high scoring range, containing more than 10,000 premium drug like molecules with highly diverse scaffolds and rich 3D diversity. It can be used for high throughput screening of well established targets such as kinases, GPCRs, and proteases, and is especially suitable for hit identification in allosteric modulation, protein–protein interactions, and various undruggable orphan targets, fully supporting early stage drug discovery for cutting edge innovat

Distinctive Diversity 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  
79
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-16141 Cilengitide
Cilengitide (EMD 121974) is an integrin (integrin) inhibitor with blood-brain barrier permeability, with IC50 values against human targets as follows: 0.61 nM for αvβ3, 8.4 nM for αvβ5, 14.9 nM for α5β1, 5400 nM for αIIbβ3, 2050 nM for αvβ6, 2350 nM for αvβ8. Cilengitide inhibits the binding of integrins to vitronectin, fibronectin, fibrinogen and LAP (TGF-β), and serves as an internal standard for solid-phase integrin binding assays. Cilengitide inhibits tumor cell viability, induces apoptosis, reduces the phosphorylation levels of STAT3, AKT and mTOR, downregulates the expression of PD-L1, inhibits cell viability and angiogenesis, regulates anti-tumor immune responses and slows tumor growth. Cilengitide can be used in research related to glioblastoma, melanoma, advanced solid tumors and refractory brain tumors.
Integrin   TGF-β Receptor   Apoptosis   PD-1/PD-L1   STAT   Akt   mTOR  
Melanoma   Glioblastoma  
75
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  
70
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  
70
HY-18234A Leupeptin hemisulfate
Leupeptin hemisulfate is a broad-spectrum protease inhibitor. By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin hemisulfate significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin hemisulfate inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin hemisulfate can be used in research on chronic inflammatory diseases and skin tumorigenesis.

Source: Streptomyces roseus MB-26-AI

Ser/Thr Protease   Cathepsin   Autophagy   SARS-CoV   Atg8/LC3   NO Synthase   COX   p62   Arginase   PTEN   NF-κB   PI3K   Akt   p38 MAPK   ERK   Reactive Oxygen Species (ROS)  
Inflammation or Immune System Disease   Respiratory Disease   Coronavirus Infection   Skin Disease  
69
HY-101120 666-15
666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model.
Epigenetic Reader Domain  
Breast Cancer   Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pain   Obesity  
65
HY-50698 BI 2536
BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription.
Polo-like Kinase (PLK)   Epigenetic Reader Domain   Apoptosis  
Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Digestive System Inflammation  
62
HY-134653 5-Ph-IAA
5-Ph-IAA is a derivative of IAA. 5-Ph-IAA, a ligand, establishes the auxin-inducible degron 2 (AID2) system together with an OsTIR1 (F74G) mutant. AID2 induces rapid and efficient depletion of mAID-fused proteins to study protein function in living cells, causing tumor suppression.
Epigenetic Reader Domain  
Leukemia/Lymphoma/Myeloma  
61
HY-N0193 Artesunate
Artesunate is an inhibitor of both STAT-3 and exported protein 1 (EXP1).
STAT   Ferroptosis   Parasite   Virus Protease  
Inflammation or Immune System Disease   Lung Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Viral Infection   Parasitic Infection   Metastatic Breast Cancer   Obesity  
43
HY-P9904 Atezolizumab
Atezolizumab (MPDL3280A) is a selective humanized monoclonal IgG1 antibody against programmed death ligand 1 (PD-L1), used for cancer research.

Species: Human

PD-1/PD-L1   Apoptosis   Autophagy  
Colorectal Cancer   Liver Cancer   Non-Small Cell Lung Cancer   Triple-Negative Breast Cancer   Metastatic Breast Cancer  
42
HY-10442 3-Deazaneplanocin A
3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity.
Histone Methyltransferase   S-adenosylhomocysteine hydrolase (SAHH)   Orthopoxvirus  
Respiratory Disease   Leukemia/Lymphoma/Myeloma   Non-Small Cell Lung Cancer   Orthopoxvirus Infection  
37
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  
37
HY-14944 Homoharringtonine
Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.
STAT  
Inflammation or Immune System Disease   Lung Cancer   Breast Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Obesity  
37
HY-P9902 Pembrolizumab
Pembrolizumab (MK-3475) is a humanized IgG4 antibody inhibiting the programmed cell death 1 (PD-1) receptor, used in cancer immunotherapy.

Species: Human

PD-1/PD-L1  
Non-Small Cell Lung Cancer   Lung Adenocarcinoma   HER-2 Positive Breast Cancer   Triple-Negative Breast Cancer   Metastatic Breast Cancer  
37
HY-117287 Deucravacitinib
Deucravacitinib (BMS-986165) is an orally active allosteric inhibitor of tyrosine kinase 2 (TYK2), with an IC50 of 0.2 nM and a Ki of 0.02 nM against the JH2 domain of TYK2, and it exhibits selectivity over other JAK subtypes and most of the kinome. Deucravacitinib blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation. Deucravacitinib can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus.
JAK   STAT   Interleukin Related   IFNAR  
Systemic Lupus Erythematosus   Psoriasis   Inflammatory Bowel Disease  
36
HY-19991 BMS-1
BMS-1 is an inhibitor of the PD-1/PD-L1 protein/protein interaction (IC50 between 6 and 100 nM).
PD-1/PD-L1   Apoptosis  
Lung Cancer   Breast Cancer   Colorectal Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Ovarian Cancer   Digestive System Inflammation  
34
HY-101563 Pemrametostat
GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma.
Histone Methyltransferase   SARS-CoV   MDM-2/p53   CDK   Apoptosis  
Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Viral Infection   HER-2 Positive Breast Cancer   SARS-CoV-2 Infection  
34
HY-13500 GSK343
GSK343, a chemical probe, is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
Histone Methyltransferase   Autophagy  
Leukemia/Lymphoma/Myeloma  
33
HY-15593 Pinometostat
Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.
Histone Methyltransferase  
Leukemia/Lymphoma/Myeloma   SARS-CoV-2 Infection  
33
HY-111558A Bobcat339 hydrochloride
Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
DNA Methyltransferase   TET Protein  
Leukemia/Lymphoma/Myeloma   Rheumatoid Arthritis  
29
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  
29
HY-B0350A Sodium butyrate
Sodium butyrate ((Butanoic acid; Butyric acid) sodium) is an orally active HDAC inhibitor. Sodium butyrate induces hyperacetylation of core histones and affects phosphorylation of H1/H2A, thereby altering chromatin structure and regulating gene expression. Sodium butyrate can be used in research related to various cancers, inflammatory bowel disease, and sickle cell anemia.
HDAC  
Cancer   Digestive System Disease   Digestive System Inflammation   Blood Disease  
28
HY-19745 BMS-202
BMS-202 is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC50 of 18 nM and a KD of 8 μM. BMS-202 binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 has antitumor activity.
PD-1/PD-L1   Apoptosis  
Neurological, Eye or Ear Disease   Lung Cancer   Breast Cancer   Colorectal Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Ovarian Cancer   Digestive System Inflammation  
27
HY-10587 BIX-01294
BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells.
Histone Methyltransferase   Autophagy  
Leukemia/Lymphoma/Myeloma  
27
HY-P99144 Anti-Mouse PD-1 Antibody (RMP1-14)
Anti-Mouse PD-1 Antibody (RMP1-14) is an anti-mouse PD-1 IgG2a antibody. Anti-Mouse PD-1 Antibody (RMP1-14) can be used for the study of colon carcinoma.

Species: Mouse

PD-1/PD-L1  
Cancer   Inflammation or Immune System Disease  
27
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-N0171 Beta-Sitosterol (purity>80%)
Beta-Sitosterol (purity≥80%) 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.
Apoptosis   Endogenous Metabolite  
Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease   Breast Cancer  
25
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  
25
HY-P9903 Nivolumab
Nivolumab is a programmed death receptor-1 (PD-1) blocking human IgG4 antibody to treat advanced (metastatic) non-small cell lung cancer.

Species: Human

PD-1/PD-L1  
Non-Small Cell Lung Cancer   Lung Adenocarcinoma   Triple-Negative Breast Cancer   Metastatic Breast Cancer   SARS-CoV-2 Infection  
23
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  
20
HY-P99145 Anti-Mouse PD-L1/B7-H1 Antibody (10F.9G2)
Anti-Mouse PD-L1/B7-H1 Antibody (10F.9G2) is an anti-mouse PD-L1/B7-H1 IgG2b antibody inhibitor derived from host rat. Anti-Mouse PD-L1/B7-H1 Antibody (10F.9G2) blocks PD-1 signaling. Anti-Mouse PD-L1/B7-H1 Antibody (10F.9G2) can be used for the research of cancer, such as colon cancer.

Species: Mouse

PD-1/PD-L1  
Colorectal Cancer  
20
HY-16900 Rolipram
Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis.
Bacterial   HIV   Phosphodiesterase (PDE)   Epigenetic Reader Domain   Amyloid-β  
Colorectal Cancer   Bacterial Infection   Depression   SARS-CoV-2 Infection   Alzheimer's Disease   Huntington's Disease   HIV-1 Infection  
19
HY-136175 Revumenib
Revumenib (SNDX-5613) is a potent and specific Menin-MLL inhibitor with a binding Ki of 0.149 nM and a cell based IC50 of 10-20 nM. Revumenib can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML).
Epigenetic Reader Domain  
Leukemia/Lymphoma/Myeloma  
17
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  
15
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-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  
14
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  
13
HY-N0390S1 L-Glutamine-13C5
L-Glutamine-13C5 is the 13C-labeled L-Glutamine (HY-N0390). L-Glutamine is an orally active nutritional agent and cellular metabolism regulator. L-Glutamine is taken up in a Na+-dependent manner and targets multiple key molecules including glutaminase, mTORC1, NF-κB, STAT-3 and HIF-1α. L-Glutamine enhances glutaminolytic catabolism, drives the conversion of glutamate to α-ketoglutarate, thereby regulating gene expression, integrating metabolic signals, mediating glutamine flux and maintaining redox homeostasis. L-Glutamine also promotes cell proliferation, osteogenic differentiation and fracture healing, exerts neuroprotective and cardioprotective effects, and inhibits osteoarthritis. L-Glutamine can be applied to research related to osteoporosis, osteoarthritis, ischemic stroke and acute cantharidin-induced cardiotoxicity.
Isotope-Labeled Compounds   mGluR   Ferroptosis   Environmental Pollutants   Endogenous Metabolite   HIF/HIF Prolyl-Hydroxylase   mTOR   STAT   NF-κB  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
13
HY-136328 EZM0414 TFA
EZM0414 (SETD2-IN-1) TFA is the TFA salt form of EZM0414 (HY-144858). EZM0414 TFA is a potent, selective, orally active inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 TFA can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma.
Histone Methyltransferase  
10
HY-107632 GYY4137
GY4137 is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GY4137 can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocking the STAT3 pathway, demonstrating potent anticancer activity.
Apoptosis   STAT   NF-κB   NO Synthase   COX   TNF Receptor   Interleukin Related  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
8
HY-W396714 Succinic acid sodium
Succinic acid sodium is a potent and orally active anxiolytic agent. Succinic acid sodium shows inhibitory effects on colonic epithelial cell proliferation in vivo. Succinic acid sodium can down-regulate the expression of KCNMB1 (potassium channel subunit β1) and TET1 (ten?eleven translocation 1). Succinic acid sodium can be used for gestational hypertension research.
Potassium Channel   TET Protein  
Neurological, Eye or Ear Disease   Blood or Cardio-cerebrovascular Disease  
7
HY-P9919 Durvalumab
Durvalumab (MEDI 4736) is an human anti-PD-L1 monoclonal antibody. Durvalumab (MEDI4736) completely blocks the binding of PD-L1 to both PD-1 and CD80, with IC50s of 0.1 and 0.04 nM, respectively.

Species: Human

PD-1/PD-L1  
Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Non-Small Cell Lung Cancer   Lung Adenocarcinoma   Triple-Negative Breast Cancer   Metastatic Breast Cancer  
7
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-109108 Valemetostat
Valemetostat (DS-3201), a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat can be used for the research of relapsed/refractory peripheral T-cell lymphoma.
Histone Methyltransferase  
Prostate Cancer   Leukemia/Lymphoma/Myeloma  
5
HY-113402A Gamma-glutamylcysteine TFA
Gamma-glutamylcysteine TFA (γ-Glu-Cys TFA) is an orally active, blood-brain barrier permeable dipeptide. Gamma-glutamylcysteine TFA activates AMPK, SIRT1, IL-4/STAT6, AC/cAMP/PI3K, IGF-1R/IRS1/PI3K, and Nrf2 signaling pathways; it inhibits NF-κB, JAK1/STAT1/3, MAPKs, cadmium-induced p38 MAPK, JNK, and PI3K/Akt signaling pathways. Gamma-glutamylcysteine TFA regulates macrophage polarization, modulates the trafficking of CD36 and GLUT4, induces glutathione synthesis, improves metabolic dysfunction, reduces lipid deposition, ameliorates glucose homeostasis, inhibits apoptosis (Apoptosis), stabilizes mitochondria, suppresses lipid peroxidation, iron accumulation and ferroptosis (Ferroptosis), reduces ds-HMGB1 levels, reverses mechanical hyperalgesia, and alleviates hepatic lipid droplet formation. Gamma-glutamylcysteine TFA is applicable to research related to inflammatory bowel disease, type 2 diabetes, cadmium-induced neurotoxicity, Alzheimer's disease, cerebral ischemia/reperfusion injury, neuropathy, and alcoholic liver disease.
Interleukin Related   TNF Receptor   Endogenous Metabolite   AMPK   Sirtuin   STAT   PI3K   NF-κB   JAK   p38 MAPK   JNK   Akt   Apoptosis   Ferroptosis  
Blood or Cardio-cerebrovascular Disease   Digestive System Disease   Digestive System Inflammation   Alzheimer's Disease   Inflammatory Bowel Disease  
4
HY-113402 Gamma-glutamylcysteine
Gamma-glutamylcysteine (γ-Glu-Cys) is an orally active, blood-brain barrier permeable dipeptide. Gamma-glutamylcysteine activates AMPK, SIRT1, IL-4/STAT6, AC/cAMP/PI3K, IGF-1R/IRS1/PI3K, and Nrf2 signaling pathways; it inhibits NF-κB, JAK1/STAT1/3, MAPKs, cadmium-induced p38 MAPK, JNK, and PI3K/Akt signaling pathways. Gamma-glutamylcysteine regulates macrophage polarization, modulates the trafficking of CD36 and GLUT4, induces glutathione synthesis, improves metabolic dysfunction, reduces lipid deposition, ameliorates glucose homeostasis, inhibits apoptosis (Apoptosis), stabilizes mitochondria, suppresses lipid peroxidation, iron accumulation and ferroptosis (Ferroptosis), reduces ds-HMGB1 levels, reverses mechanical hyperalgesia, and alleviates hepatic lipid droplet formation. Gamma-glutamylcysteine is applicable to research related to inflammatory bowel disease, type 2 diabetes, cadmium-induced neurotoxicity, Alzheimer's disease, cerebral ischemia/reperfusion injury, neuropathy, and alcoholic liver disease.
Endogenous Metabolite   Interleukin Related   TNF Receptor   AMPK   Sirtuin   STAT   PI3K   NF-κB   JAK   p38 MAPK   JNK   Akt   Apoptosis   Ferroptosis  
Blood or Cardio-cerebrovascular Disease   Digestive System Disease   Digestive System Inflammation   Alzheimer's Disease   Inflammatory Bowel Disease  
4
HY-139611 Navlimetostat
Navlimetostat is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study.
Histone Methyltransferase  
4
HY-B1180 Vinburnine
Vinburnine ((-)-Eburnamonine; (-)-Vincamone) is an orally active, blood-brain barrier permeable immunomodulator and apoptosis inducer. Vinburnine drives the secretion of IL-24 by activating the P38/MAPK/ATF3 signaling axis. Vinburnine induces reactive oxygen species production and DNA damage in cancer cells, thereby inhibiting cancer cell proliferation, activating the apoptotic cascade, and enhancing CD8+ T cell function to remodel the tumor immune microenvironment. Vinburnine can be used in the research of diseases such as melanoma.
Apoptosis   p38 MAPK  
Melanoma  
3
HY-N1939 Icariside I
Icariside I (GH01) is an orally active metabolite of icalin. Icariside I improves estrogen deficiency-induced osteoporosis by simultaneously regulating osteoblast and osteoclast differentiation. Icariside I promotes ATP (HY-B2176) or Nigericin (HY-127019)-induced mtROS production and NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Icariside I does not alter the activation of NLRC4 and AIM2 inflammasomes. Icariside I inhibits breast cancer proliferation, apoptosis, invasion, and metastasis by targeting the IL-6/STAT3 pathway. Icariside I is a kynurenine-AhR pathway inhibitor that alleviates cancer by blocking tumor immune escape.
Apoptosis   Reactive Oxygen Species (ROS)   NOD-like Receptor (NLR)   STAT   CDK   Bcl-2 Family   Aryl Hydrocarbon Receptor   JAK   Caspase   IFNAR   PD-1/PD-L1  
Metabolic or Endocrine Disease   Lung Cancer   Breast Cancer   Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Depression   Pain   Autoimmune Disease   Digestive System Inflammation  
3
HY-N6871 Abietic acid
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis.
Bacterial   IKK   Ferroptosis  
Inflammation or Immune System Disease   Lung Cancer   Prostate Cancer   Liver Cancer   Bacterial Infection   Obesity  
3
HY-W004260 Arachidic acid
Arachidic acid is an orally bioavailable membrane fluidity modulator and receptor/ion channel effector. Arachidic acid does not activate arachidonic acid-sensitive K+ channels in rat midbrain and hypothalamic neurons. Arachidic acid alleviates age-related spatial cognitive impairment. Arachidic acid is applicable for research related to age-related spatial cognitive impairment.

Source: Bee Pollen

Endogenous Metabolite  
Neurodegenerative Disease  
3
HY-P2259 TAT-GluA2 3Y
TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction.
iGluR   HIV Integrase   Adenosine Receptor  
Neurological, Eye or Ear Disease   Blood or Cardio-cerebrovascular Disease  
2
HY-N0113 Hordenine
Hordenine (Ordenina; Peyocactine) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.
Bacterial   p38 MAPK   JNK   ERK   Akt   Interleukin Related   TNF Receptor   NO Synthase   COX   Reactive Oxygen Species (ROS)   Microphthalmia Associated Transcription Factor (MITF)   Wnt   β-catenin   Dopamine Receptor   Adrenergic Receptor   5-HT Receptor   Serotonin Transporter   Dopamine Transporter   α-synuclein  
Musculoskeletal and Skin Disease   Pseudomonas Aeruginosa Infection   Parkinson's Disease   Acute Lung Injury  
2
HY-N6985 Baccatin III
Baccatin III is an orally available, selective inhibitor of the TGF-β1 signaling pathway and myeloid-derived suppressor cell (MDSC) activation. Baccatin III targets the AKT/STAT6 and Smad2/3 pathways, blocking TGF-β1-induced fibroblast differentiation and MDSC-mediated immunosuppression. Baccatin III exerts anti-inflammatory and anti-fibrotic effects by inhibiting macrophage activation and extracellular matrix deposition, and shows potential in the treatment of pulmonary fibrosis and cancer in terms of regulating the tumor immune microenvironment.
Others  
Breast Cancer   Lung Fibrosis  
2
HY-D0175 3-Aminopropyltriethoxysilane
3-Aminopropyltriethoxysilane (APTES) acts as a strong glue to immobilize biomolecules such as antibodies and enzymes to silicon and silicon derivatives such as silicon nitride (Si3N4 )) on. 3-Aminopropyltriethoxysilane also acts as a spacer, providing biomolecules with more spatial freedom during immobilization for higher specific activity. 3-Aminopropyltriethoxysilane can form a more stable, sensitive, and highly biocompatible bioanalytical platform by immobilizing biomolecules onto some solid materials, electrode materials, nanomaterials, and nanocomposites.
Biochemical Assay Reagents  
2
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  
2
HY-P1181 Pam2CSK4
Pam2CSK4 is a TLR2 agonist. Pam2CSK4 induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis.
Toll-like Receptor (TLR)   NO Synthase   IKK   Akt   PKC   NF-κB   p38 MAPK   Interleukin Related  
Leukemia/Lymphoma/Myeloma   Cancer Immunology   Immunotherapy for Melanoma   Influenza Virus Infection   Atherosclerosis and Inflammation   Heart Failure  
1
HY-120395 UC-514321
UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.
STAT   Apoptosis   TET Protein  
Lung Cancer   Breast Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Digestive System Inflammation   Obesity  
1
HY-N6028 Darutoside
Darutoside is an orally effective diterpene compound with significant anti-inflammatory, analgesic, wound healing promotion, and immunomodulatory activities. Darutoside reduces edema and pain responses by inhibiting the expression of COX-2 and the migration of inflammatory cells. It regulates macrophage polarization towards the M2 type by inhibiting the NF-κB pathway, alleviating inflammation and promoting wound healing. Through multi-target regulation of metabolic networks, Darutoside significantly alleviates acute gouty arthritis.
COX   NF-κB   Interleukin Related   TNF Receptor  
Inflammation or Immune System Disease  
1
HY-160638 NSC-311068
NSC-311068 is TET1 inhibitor. NSC-311068 selectively suppress TET1 transcription and 5-hydroxymethylcytosine (5hmC) modification. NSC-311068 represses the level of TET1 expression and the global 5hmC level. NSC-311068 effectively inhibits cell viability in AML cells with high expression of TET1.
TET Protein  
Cancer  
1
HY-124344 Avenanthramide C
Avenanthramide C is an orally active polyphenolic compound that penetrates the blood-brain barrier. Avenanthramide C is derived from oats. Avenanthramide C inhibits NF-κB nuclear translocation and inhibits the phosphorylation of PI3K, PLCγ1, Lyn, Syk, and Akt. Avenanthramide C inhibits the expression and activity of MMP-9 and inhibits MAPK phosphorylation. Avenanthramide C scavenges DPPH radicals, reduces intracellular ROS, and inhibits pro-inflammatory cytokine release and adhesion molecule expression. Avenanthramide C inhibits cell degranulation. Avenanthramide C attenuates active systemic anaphylaxis and inhibits passive cutaneous anaphylaxis. Avenanthramide C ameliorates PHZ-induced blood stasis. Avenanthramide C inhibits neuroinflammation, restores long-term potentiation, and improves recognition and spatial memory in Alzheimer's disease models. Avenanthramide C can be used for research on allergic inflammation, thrombosis, atherosclerosis, and Alzheimer's disease.
NF-κB   PI3K   Phospholipase   Src   Syk   Akt   MMP   p38 MAPK   Free Radical Scavengers   Reactive Oxygen Species (ROS)  
Blood or Cardio-cerebrovascular Disease   Allergy   Alzheimer's Disease   Atherosclerosis and Inflammation  
1
HY-D1056F Biotin-Lipopolysaccharide, from E.coli O111:B4
Biotin-Lipopolysaccharide, from E.coli O111:B4 (Biotin-LPS, from Escherichia coli (O111:B4)) is a biotin-conjugated Lipopolysaccharide (LPS) (HY-D1056A1) that can be coupled with streptavidin protein. Biotin-Lipopolysaccharide, from E.coli O111:B4 can be used to identify Lipopolysaccharide ligands. Lipopolysaccharides, from E. coli O111:B4 (LPS, from Escherichia coli (O111:B4)) are endotoxins and TLR4 activators extracted from Escherichia coli (E. coli O111:B4) and are classified as S (smooth) type LPS. Lipopolysaccharides, from E. coli O111:B4 possess the typical three-part structure: O-antigen, R3-type core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O111:B4 activate TLR-4 in immune cells and can cause significant gastric diseases. Lipopolysaccharides, from E. coli O111:B4 can also induce M1-type polarization in mouse macrophages.
It is recommended to prepare a solution with concentration ≥2 mg/mL. Vortex thoroughly for more than 10 minutes. Due to the adsorption characteristics of LPS, silanized container or low adsorption centrifuge tubes should be used for aliquoting and storage, and mix thoroughly before use.
Biochemical Assay Reagents  
Inflammation or Immune System Disease  
1
HY-122258 NSC-370284
NSC-370284 is a selective inhibitor of ten-eleven translocation 1 (TET1) and 5-hydroxymethylcytosine (5hmC). NSC-370284 significantly inhibits the level of TET1 expression via targets STAT3/5.
STAT   TET Protein  
Lung Cancer   Breast Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Obesity  
1
HY-106373A Adrenocorticotropic hormone TFA
Adrenocorticotropic hormone (ACTH; Adrenocorticotrophic hormone) TFA is a polypeptide tropic hormone produced by the anterior pituitary gland. Adrenocorticotropic hormone TFA stimulates cortisol secretion from the adrenal cortex via the hypothalamic-pituitary-adrenal (HPA) axis. Adrenocorticotropic hormone TFA regulates cortisol and androgen production. Adrenocorticotropic hormone TFA can promote the development of spermatogenesis. Adrenocorticotropic hormone TFA can relieve acute inflammation in gout models by inhibiting the polarization of macrophages to M1 type, inhibiting ROS and proinflammatory factor production and protecting mitochondrial function. Adrenocorticotropic hormone TFA can be used for the researches of inflammation, endocrinology, metabolic disease, such as gout and nephrotic syndrome.
Androgen Receptor   Reactive Oxygen Species (ROS)   Mitochondrial Metabolism   Interleukin Related   TNF Receptor  
Inflammation or Immune System Disease   Gout  
1
HY-N3415 Kumatakenin
Kumatakenin is an orally active apoptosis inducer and autophagy inhibitor, with a Kd value of 2.94 μM for mouse ATG5. Kumatakenin increases the activities of caspase-3, caspase-8 and caspase-9, thereby inducing caspase-dependent apoptosis in ovarian cancer cells. Kumatakenin reduces the expression of chemokines and pro-oncogenic factors in ovarian cancer cells, and inhibits M2 macrophage polarization. Kumatakenin inactivates TRIM65 function, reduces the expression and stability of FASN, and thus inhibits the proliferation, migration, invasion and tumor progression of esophageal cancer cells. Kumatakenin interacts with ATG5 to reduce its protein level, decrease LC3 level, and reduce the number of autophagosomes in the hippocampus. Kumatakenin binds to Eno3 to upregulate its expression, reduce the stability and expression level of IRP1 mRNA, inhibit ferroptosis, alleviate intestinal inflammation, and restore epithelial barrier function. Kumatakenin enhances the efficacy of antibiotics against pathogenic bacteria, inhibits SARS-CoV-2 replication, and reduces cytokine production. Kumatakenin is applicable to research related to ovarian cancer, esophageal cancer, depression and colitis.
Apoptosis   Autophagy   Caspase   Ferroptosis   SARS-CoV  
Ovarian Cancer   Depression   Esophageal Cancer   Ulcerative Colitis  
1
HY-W105750 6-Hydroxyhexanoic acid
6-Hydroxyhexanoic acid (6-HHA) is a bacterial effector molecule with metabolic and immunomodulatory activities. 6-Hydroxyhexanoic acid activates the JAK1-STAT1 signaling pathway, promotes phenotypic conversion of M2 macrophages to M1 macrophages, and exerts anti-tumor effects by regulating macrophage polarization. 6-Hydroxyhexanoic acid inhibits lipolysis in adipocytes mediated by Gαi family GPCR, and reduces high-fat diet-induced weight gain and obesity. 6-Hydroxyhexanoic acid can be used in studies related to pancreatic ductal adenocarcinoma, obesity, and insulin resistance.
JAK   STAT   Adenylate Cyclase  
Pancreatic Ductal Adenocarcinoma   Insulin Resistance   Obesity  
1
HY-P1181A Pam2CSK4 TFA
Pam2CSK4 TFA is a TLR2 agonist. Pam2CSK4 TFA induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 TFA activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 TFA expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 TFA acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 TFA can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis.
Toll-like Receptor (TLR)   NO Synthase   IKK   Akt   PKC   NF-κB   p38 MAPK   Interleukin Related  
Leukemia/Lymphoma/Myeloma   Cancer Immunology   Immunotherapy for Melanoma   Influenza Virus Infection   Atherosclerosis and Inflammation   Heart Failure  
1
HY-12303 OAC1
OAC1 is a potent Oct4 activator. OAC1 activates Oct4 and Nanog promoters and enhances induced pluripotent stem cells (iPSC) formation. OAC1 activates OCT4 through upregulation of HOXB4 expression. OAC1 increases transcription of the Oct4-Nanog-Sox2 triad and TET1. OAC1 facilitates the reprogramming of cells by enhancing efficiency and shortening the reprogramming time.
Oct3/4   TET Protein  
Cancer  
1
HY-106373 Adrenocorticotropic hormone
Adrenocorticotropic hormone (ACTH; Adrenocorticotrophic hormone) is a polypeptide tropic hormone produced by the anterior pituitary gland. Adrenocorticotropic hormone stimulates cortisol secretion from the adrenal cortex via the hypothalamic-pituitary-adrenal (HPA) axis. Adrenocorticotropic hormone regulates cortisol and androgen production. Adrenocorticotropic hormone can promote the development of spermatogenesis. Adrenocorticotropic hormone can relieve acute inflammation in gout models by inhibiting the polarization of macrophages to M1 type, inhibiting ROS and proinflammatory factor production and protecting mitochondrial function. Adrenocorticotropic hormone can be used for the researches of inflammation, endocrinology, metabolic disease, such as gout and nephrotic syndrome.
Androgen Receptor   Reactive Oxygen Species (ROS)   Mitochondrial Metabolism   Interleukin Related   TNF Receptor  
Inflammation or Immune System Disease   Gout  
1
HY-143712 Allolithocholic acid
Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC50 = 2.7 μM) and RORγt inverse agonist (IC50 = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease.
Drug Metabolite   G protein-coupled Bile Acid Receptor 1   ROR  
Cancer   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
1
HY-P99117 Cadonilimab
Cadonilimab (AK104) is a humanized tetravalent IgG1 bispecific antibody targeting PD1/CTLA4. Cadonilimab blocks both PD-1 and CTLA-4 pathways, thereby relieving their corresponding immunosuppressive effects and reversing tumor specific T cell exhaustion. Cadonilimab significantly downregulates Fc-mediated effector functions, including antibody-dependent cell-mediated cytotoxicity (ADCC), antibody-dependent cellular phagocytosis (ADCP), complement dependent cytotoxicity (CDC). Cadonilimab can be used for research of metastatic cervical cancer, as well as other malignancies such as gastric cancer, GEJ adenocarcinoma and non-small cell lung cancer (NSCLC).

Species: Human

PD-1/PD-L1   CTLA-4  
Inflammation or Immune System Disease   Gastric Cancer   Non-Small Cell Lung Cancer   Triple-Negative Breast Cancer  
1
HY-P99144A Anti-Mouse PD-1 Antibody (S-5001)
Anti-Mouse PD-1 Antibody (S-5001) is a selective inhibitor targeting PD-1, blocking the PD-1/PD-L1 immune checkpoint axis through competitive binding to PD-1. Anti-Mouse PD-1 Antibody (S-5001) works by reversing the tumor immunosuppressive microenvironment and reactivating the anti-tumor activity of cytotoxic T lymphocytes. It can be used in research on tumors such as melanoma and HPV-positive oropharyngeal squamous cell carcinoma. Anti-Mouse PD-1 Antibody (S-5001) is often combined with photothermal therapy, chemotherapy, etc., to enhance efficacy.

Species: Mouse

PD-1/PD-L1  
Cancer Immunology   Immunotherapy for Melanoma   Squamous Cell Carcinoma  
1
HY-D1056B3 Lipopolysaccharides, from Klebsiella pneumoniae
Lipopolysaccharides, from Klebsiella pneumoniae (LPS, from bacterial (Klebsiella pneumoniae)) are lipopolysaccharide endotoxins and TLR4 activators derived from Klebsiella pneumoniae, and are classified as S-type LPS. Lipopolysaccharides, from Klebsiella pneumoniae exhibit a typical three-part structure: O-antigen, core oligosaccharide, and lipid A. Lipopolysaccharides, from Klebsiella pneumoniae may participate in bacterial immune evasion by inhibiting complement-mediated killing and suppressing the host's secretion of antimicrobial peptides, thereby allowing the bacteria to escape immune defenses. Lipopolysaccharides, from Klebsiella pneumoniae possess high viscosity and resistance to serum-mediated killing, which may lead to sepsis. Lipopolysaccharides, from Klebsiella pneumoniae can be used to construct Acute Lung Injury Model.
It is recommended to prepare a solution with concentration ≥2 mg/mL. Vortex thoroughly for more than 10 minutes. Due to the adsorption characteristics of LPS, silanized container or low adsorption centrifuge tubes should be used for aliquoting and storage, and mix thoroughly before use.
Toll-like Receptor (TLR)  
Inflammation or Immune System Disease  
1
HY-402410 TETi76
TETi76 is an orally active TET family inhibitor with IC50 values ??of 1.5, 9.4 and 8.8 μM for TET1, TET2 and TET3, respectively. TETi76 competitively binds to the active site of TET enzymes, reduces cytosine hydroxymethylation and restricts clonal growth of TET2 mutants in vitro and in vivo, but does not affect the growth of normal hematopoietic precursor cells. TETi76 can be used for leukemia research.
TET Protein  
1
HY-P99675 Ivonescimab
Ivonescimab (AK112) is a PD-1/VEGF bispecific antibody. Ivonescimab competitively inhibiting PD-1/PD-L1 interaction, reversing the immunosuppression mediated by it, and blocks the binding of VEGF-A to VEGFR2, inhibiting tumour angiogenesis in the tumour microenvironment. Ivonescimab also has significantly anticancer activity against EGFR-mutated locally advanced or metastatic non-squamous non-small cell lung cancer (NSCL).

Species: Human

PD-1/PD-L1   VEGFR  
Respiratory Disease   Non-Small Cell Lung Cancer   Triple-Negative Breast Cancer  
1
HY-144026S 9-PAHSA-d9
9-PAHSA-d9 is the deuterium labeled 9-PAHSA (HY-120657). 9-PAHSA is an orally active endogenous GPR120 agonist (EC50=18 μM). 9-PAHSA significantly inhibits LPS-induced inflammatory responses by blocking the NF-κB pathway. 9-PAHSA induces adipocyte browning, enhances glucose uptake and reduces lipid accumulation, while improving mitochondrial function and the survival rate of steatotic hepatocytes. In terms of neuroprotection, 9-PAHSA regulates the expression of REST and BDNF in the prefrontal cortex of diabetic mice, and effectively prevents spatial working memory deficits and abnormal social behaviors. 9-PAHSA does not directly regulate insulin secretion or improve systemic insulin sensitivity, and possesses specific anti-inflammatory, metabolic regulatory and neuroprotective properties. 9-PAHSA can be used in the research of diabetes-related cognitive impairment, obesity and non-alcoholic fatty liver disease.
CGRP Receptor   NF-κB  
Inflammation or Immune System Disease  
/
HY-P2004 FFAGLDD
FFAGLDD is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release.
MMP  
Cancer  
/
HY-187155 Cyclo(Gly-{Tyr(PO3H2)}-Val-Pro-Met-Leu)
Cyclo (Gly-{Tyr (PO3H2)-Val-Pro-Met-Leu) is a binding peptide for the PI3K SH2 domain, as well as an inhibitory peptide for the mitogenic signal transduction-mediating domain. Cyclo (Gly-{Tyr (PO3H2)}-Val-Pro-Met-Leu) binds to the SH2 domain of the phosphorylated PI3K p85 subunit, and the spatial arrangement of its phosphotyrosine residue and methionine residue is associated with this interaction.
PI3K  
/
HY-P1835 CEF8, Influenza Virus NP (383-391)
CEF8, Influenza Virus NP (383-391), an influenza A virus nucleoprotein containing residues 383 to 391, is the most important HLA-B*2705-restricted epitope in the nucleoprotein of influenza A viruses and is associated with escape from cytotoxic T lymphocytes-mediated immunity.
Influenza Virus  
Inflammation or Immune System Disease  
/
HY-120657R 9-PAHSA (Standard)
Flumethrin (Standard) is the analytical standard of Flumethrin. This product is intended for research and analytical applications. 9-PAHSA is an orally active endogenous GPR120 agonist (EC50=18 μM). 9-PAHSA significantly inhibits LPS-induced inflammatory responses by blocking the NF-κB pathway. 9-PAHSA induces adipocyte browning, enhances glucose uptake and reduces lipid accumulation, while improving mitochondrial function and the survival rate of steatotic hepatocytes. In terms of neuroprotection, 9-PAHSA regulates the expression of REST and BDNF in the prefrontal cortex of diabetic mice, and effectively prevents spatial working memory deficits and abnormal social behaviors. 9-PAHSA does not directly regulate insulin secretion or improve systemic insulin sensitivity, and possesses specific anti-inflammatory, metabolic regulatory and neuroprotective properties. 9-PAHSA can be used in the research of diabetes-related cognitive impairment, obesity and non-alcoholic fatty liver disease.
Reference Standards   CGRP Receptor   NF-κB  
Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular 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-142140S 3-epi-25-Hydroxy Vitamin D3-d6
3-epi-25-Hydroxy Vitamin D3-d6 is the deuterium labeled 3-epi-25-Hydroxy Vitamin D3 (HY-142140). 3-epi-25-Hydroxy Vitamin D3 is the vitamin D metabolite, while vitamin D metabolism highly dependent on macrophage polarization. The C3-epimerase pathway for vitamin D is active in macrophages.
Isotope-Labeled Compounds  
/
HY-P992000 F8-IL-4
F8-IL-4 is an immune cytokine targeting IL-4. F8-IL-4 specifically delivers IL-4 to inflammatory sites via binding to targets expressed on neovascular vessels. F8-IL-4 alleviates collagen-induced arthritis in mice by regulating T cell subsets and macrophage polarization. When combined with Dexamethasone (HY-14648), F8-IL-4 produces a synergistic and long-lasting therapeutic effect, and prevents arthritis recurrence after drug withdrawal by maintaining anti-inflammatory cell phenotypes and cytokine profiles. F8-IL-4 can be used in the research of collagen-induced arthritis.

Species: Human

Interleukin Related  
Autoimmune Disease  
/
HY-P992518 Pumitamig (Mouse IgG2a)
Pumitamig (Mouse IgG2a) is the Mouse IgG2a control antibody for Pumitamig (HY-P991097). Pumitamig (PM-8002, BNT-327) is a bispecific antibody targeting PD-L1 and VEGF-A, with immune activation and anti-angiogenic activities. By binding to PD-L1, Pumitamig restores the function of effector T cells, while neutralizing VEGF-A in the tumor microenvironment to reverse its inhibition on the infiltration and activation of immune cells and normalize tumor blood vessels. Pumitamig can also be combined with various ADCs targeting TROP2, B7H3, HER2, HER3 for the research of advanced/metastatic solid tumors, including non-small cell lung cancer, ovarian cancer, triple-negative breast cancer, cervical cancer, etc. Pumitamig also exhibits potential efficacy in "cold" tumors with low PD-L1 expression that are insensitive to immunotherapy.
VEGFR   PD-1/PD-L1  
Ovarian Cancer   Non-Small Cell Lung Cancer   Triple-Negative Breast Cancer   Metastatic Breast Cancer  
/
HY-P990038 Eurestobart
Eurestobart (ES002023) is a recombinant human IgG1 antibody against CD39. Eurestobart restores antitumor immunity by stabilizing the pro-inflammatory extracellular ATP (eATP) and interfering with synthesis of the immunosuppressive adenosine within the tumor microenvironment (TME). Eurestobart is used in the research of locally advanced and metastatic solid tumors.

Species: Human

NTPDase  
Neurological, Eye or Ear Disease  
/
HY-P2004A FFAGLDD TFA
FFAGLDD TFA is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release.
MMP  
Cancer  
/
HY-W142432S Perfluoroundecanoic acid-13C7
Perfluoroundecanoic acid-13C7 is the 13C-labeled Perfluoroundecanoic acid (HY-W142432). Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation.
Autophagy   Isotope-Labeled Compounds   Arginase   Akt   p62   Wnt   mTOR   Atg8/LC3   β-catenin   TGF-beta/Smad   ERK  
/
HY-143712S1 Allolithocholic Acid-d4
Allolithocholic Acid-d4 (3α-hydoxy-5α-Cholaoic Acid-d4, allo-LCA-d4) is deuterium labeled Allolithocholic acid (HY-143712). Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC50 = 2.7 μM) and RORγt inverse agonist (IC50 = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease.
Isotope-Labeled Compounds   Drug Metabolite   G protein-coupled Bile Acid Receptor 1   ROR  
Cancer   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-P10947 MACTIDE-V
MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. MACTIDE-V delivers Verteporfin (HY-B0146) to CD206+ tumor-associated macrophages (TAM) to inhibit the YAP/TAZ signaling pathway, prompting YAP exclusion from the nucleus, inducing TAM polarization toward an anti-tumoral phenotype with enhanced phagocytosis and antigen presentation, and boosting T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models.
Epigenetic Reader Domain   YAP  
/
HY-135525 Agroclavine
Agroclavine acts as an agonist of the D1-dopamine receptor and α1-adrenergic receptor. Agroclavine enhances the sensitivity of the brain to magnetic fields; it impairs spatial memory without affecting hippocampal long-term potentiation (LTP). Agroclavine exerts bidirectional regulatory effects on immune activity: it enhances NK cell activity with low toxicity under normal conditions, while it inhibits NK cell activity and exhibits significant cardiac and hepatic toxicity under stress conditions. Agroclavine can be used for research on neuroelectrophysiology, learning and memory, and immunoregulation.

Source: Saccharomyces cerevisiae

Dopamine Receptor   Adrenergic Receptor  
Neurodegenerative Disease   Immunomodulation  
/
HY-136611S ω-Hydroxy-DEET-d10
ω-Hydroxy-DEET-d10 is the deuterium labeled ω-Hydroxy-DEET (HY-136611). ω-Hydroxy-DEET is a major metabolite of insect repellent N-N-diethyl-meta-toluamide (DEET). ω-Hydroxy-DEET has anti-proliferative effects. DEET is a spatial repellent and an irritant that commonly used to prevent contact with mosquitoes.
Isotope-Labeled Compounds   Drug Metabolite  
Infection  
/
HY-P10435 KEMPFPKYPVEP
KEMPFPKYPVEP is a 12-amino acids neuropeptide, which upregulates levels of dopamine (DA) and norepinephrine (NE) in the prefrontal cortex, exhibits spatial and object recognition memory promoting ability in Scopolamine (HY-N0296)-induced amnesia mouse model.
Dopamine Receptor  
Neurological, Eye or Ear Disease  
/
HY-P991403 BC011
BC011 is a human monoclonal antibody (mAb) targeting TNFRSF1B. BC011 promotes CD8+T cell proliferation and depletes Treg cells, thereby increasing the proportion of effector T cells in the tumor microenvironment. BC011 can be used in tumor Immunity research.

Species: Human

TNF Receptor  
Cancer  
/
HY-W041470R 4-Methyl-1-phenyl-2-pentanone (Standard)
Chlorpromazine (hydrochloride) (Standard) is the analytical standard of Chlorpromazine (hydrochloride). This product is intended for research and analytical applications. 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.
Reference Standards   Endogenous Metabolite  
Metabolic or Endocrine Disease  
/
HY-P11629 KBP-336
KBP-336 is a dual amylin and calcitonin receptor agonist (DACRA). KBP-336 exhibits antidiabetic and insulin-sensitizing properties, improves glucose levels, spatial learning, and memory in diabetic rats, and reduces blood glucose. KBP-336 also alleviates pain-like symptoms in osteoarthritis rats. KBP-336 also promotes weight and fat reduction. KBP-336 is useful for research on diabetes, obesity, and arthritis.
Amylin Receptor   CGRP Receptor  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-169232 PCC16 chloride
PCC16 chloride is a dual PROTAC degrader targeting DHHC3 and PD-L1, with a DC50 of 0.103 μM for PD-L1 degradation. PCC16 chloride induces DHHC3 degradation via the ubiquitin-proteasome pathway by recruiting the CRBN E3 ubiquitin ligase (E3 ubiquitin ligase). By targeting DHHC3-which is essential for PD-L1 palmitoylation and membrane stability-PCC16 chloride reduces PD-L1 levels, decreases PD-L1 membrane retention time, and impairs its immunosuppressive function. PCC16 chloride enhances anti-tumor immunity by disrupting PD-L1-mediated immunosuppression. PCC16 chloride can be used in the research of immune checkpoint blockade-resistant cancers.
PROTACs   PD-1/PD-L1  
Cancer  
/
HY-P991309 ZM-008
ZM-008 is an anti-LLT1 monoclonal antibody. ZM-008 blocks the interaction between LLT1 and CD161 on the surface of NK cells and T cells. ZM-008 restores anti-tumor immune activity, shifts the tumor microenvironment to an immune-responsive state, and recovers NK cell-mediated cytotoxicity against tumor cells, thereby reversing immunosuppression in immune-resistant "cold" tumors. ZM-008 is applicable to the research of immune-resistant solid tumors.

Species: Human

C-type Lectin-like Receptors (CTLRs)  
Cancer  
/
HY-124329AS BS3 Crosslinker-d4 disodium
BS3 Crosslinker-d4 disodium is the deuterated-labeled BS3 Crosslinker disodium (HY-124329A). BS3 Crosslinker disodium is a cell-impermeable NHS ester crosslinker. BS3 Crosslinker disodium "covalently locks" two spatially adjacent proteins on the surface of living cells into a covalent complex, and the dimerization/oligomerization status is determined by observing molecular weight shifts via Western blot. BS3 Crosslinker disodium can crosslink EGFR and c-MET to assist in detecting and evaluating their dimerization status. It can be used in research related to oral cancer and glioblastoma.
Isotope-Labeled Compounds   Biochemical Assay Reagents  
Cancer  
/
HY-N1939R Icariside I (Standard)
Icariside I (Standard) is the analytical standard of Icariside I (HY-N1939). This product is intended for research and analytical applications. Icariside I (GH01) is an orally active metabolite of icalin. Icariside I improves estrogen deficiency-induced osteoporosis by simultaneously regulating osteoblast and osteoclast differentiation. Icariside I promotes ATP (HY-B2176) or Nigericin (HY-127019)-induced mtROS production and NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Icariside I does not alter the activation of NLRC4 and AIM2 inflammasomes. Icariside I inhibits breast cancer proliferation, apoptosis, invasion, and metastasis by targeting the IL-6/STAT3 pathway. Icariside I is a kynurenine-AhR pathway inhibitor that alleviates cancer by blocking tumor immune escape.
Reference Standards   Apoptosis   Reactive Oxygen Species (ROS)   NOD-like Receptor (NLR)   STAT   CDK   Bcl-2 Family   Aryl Hydrocarbon Receptor   JAK   Caspase   IFNAR   PD-1/PD-L1  
Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-120657S 9-PAHSA-d4
9-PAHSA-d4 is the deuterium labeled 9-PAHSA. 9-PAHSA is an orally active endogenous GPR120 agonist (EC50=18 μM). 9-PAHSA significantly inhibits LPS-induced inflammatory responses by blocking the NF-κB pathway. 9-PAHSA induces adipocyte browning, enhances glucose uptake and reduces lipid accumulation, while improving mitochondrial function and the survival rate of steatotic hepatocytes. In terms of neuroprotection, 9-PAHSA regulates the expression of REST and BDNF in the prefrontal cortex of diabetic mice, and effectively prevents spatial working memory deficits and abnormal social behaviors. 9-PAHSA does not directly regulate insulin secretion or improve systemic insulin sensitivity, and possesses specific anti-inflammatory, metabolic regulatory and neuroprotective properties. 9-PAHSA can be used in the research of diabetes-related cognitive impairment, obesity and non-alcoholic fatty liver disease.
Isotope-Labeled Compounds   CGRP Receptor   NF-κB  
/
HY-120657S1 9-PAHSA-d31
9-PAHSA-d31 is the deuterium labeled 9-PAHSA. 9-PAHSA is an orally active endogenous GPR120 agonist (EC50=18 μM). 9-PAHSA significantly inhibits LPS-induced inflammatory responses by blocking the NF-κB pathway. 9-PAHSA induces adipocyte browning, enhances glucose uptake and reduces lipid accumulation, while improving mitochondrial function and the survival rate of steatotic hepatocytes. In terms of neuroprotection, 9-PAHSA regulates the expression of REST and BDNF in the prefrontal cortex of diabetic mice, and effectively prevents spatial working memory deficits and abnormal social behaviors. 9-PAHSA does not directly regulate insulin secretion or improve systemic insulin sensitivity, and possesses specific anti-inflammatory, metabolic regulatory and neuroprotective properties. 9-PAHSA can be used in the research of diabetes-related cognitive impairment, obesity and non-alcoholic fatty liver disease.
Isotope-Labeled Compounds   CGRP Receptor   NF-κB  
/
HY-141432G NX-1607 (GMP)
NX-1607 (Cbl-b-IN-3) (GMP) is a GMP-grade NX-1607 (HY-141432). GMP-grade small molecules can be used as adjuvant agents in cell therapy. NX-1607 (GMP) enhances antigen recall, reduces T cell exhaustion and increases cytokine production. NX-1607 is an inhibitor of Cbl-b (an E3 enzyme).
E1/E2/E3 Enzyme  
Cancer   Inflammation or Immune System Disease  
/
HY-184849 Glu-Arg
Glu-Arg is a dipeptide linked by L-glutamic acid and L-arginine. Glu-Arg contributes to the construction of the hydrophobic network and maintenance of stability of mouse cAMP-dependent protein kinase; it acts as a core hub connecting the activation segment and the GHI subdomain in eukaryotic protein kinases, and promotes signal transmission between elements and within enzymes. As a salt bridge, Glu-Arg regulates the formation and unfolding rates of α-helices, and its optimized spatial conformation is conducive to the stability and folding rate of α-helices. Glu-Arg induces concentration-dependent intracellular calcium changes in cultured human fungiform taste bud cells.
Amino Acid Derivatives  
/
HY-B1180R Vinburnine (Standard)
Vinburnine ((-)-Eburnamonine; (-)-Vincamone) (Standard) is the analytical standard of Vinburnine (HY-B1180). This product is intended for research and analytical applications. Vinburnine ((-)-Eburnamonine; (-)-Vincamone) phosphate is an orally active, blood-brain barrier permeable immunomodulator and apoptosis inducer. Vinburnine drives the secretion of IL-24 by activating the P38/MAPK/ATF3 signaling axis. Vinburnine induces reactive oxygen species production and DNA damage in cancer cells, thereby inhibiting cancer cell proliferation, activating the apoptotic cascade, and enhancing CD8+ T cell function to remodel the tumor immune microenvironment. Vinburnine can be used in the research of diseases such as melanoma.
Reference Standards   Apoptosis   p38 MAPK  
Melanoma  
/
HY-P11094 Tet1-Cys peptide
Tet1-Cys peptide is a peptide with the sequence HLNILSTLWKYRC. Tet1 (HLNILSTLWKYR) (HY-P10998) can specifically bind to the neuronal ganglioside receptor GT1b, possessing neuronal targeting capabilities. The Tet1-Cys peptide sequence has an added Cys, which can be used for drug conjugation for research on drug delivery.
TET Protein  
Neurological, Eye or Ear Disease  
/
HY-P10998 Tet1 peptide
Tet1 peptide is a peptide that specifically binds to neurons. Tet1 peptide binds to GT1B ganglioside and trisialoganglioside clostridial toxin receptor on the surface of neuronal cells, and can be used in peptide conjugation and drug delivery research.
TET Protein  
Neurological, Eye or Ear Disease  
/
HY-W770410 9-PAHSA-13C4
9-PAHSA-13C4 is 13C-labeled 9-PAHSA. 9-PAHSAis an orally active endogenous GPR120 agonist (EC50=18 μM). 9-PAHSAsignificantly inhibits LPS-induced inflammatory responses by blocking the NF-κB pathway. 9-PAHSAinduces adipocyte browning, enhances glucose uptake and reduces lipid accumulation, while improving mitochondrial function and the survival rate of steatotic hepatocytes. In terms of neuroprotection, 9-PAHSAregulates the expression of REST and BDNF in the prefrontal cortex of diabetic mice, and effectively prevents spatial working memory deficits and abnormal social behaviors. 9-PAHSAdoes not directly regulate insulin secretion or improve systemic insulin sensitivity, and possesses specific anti-inflammatory, metabolic regulatory and neuroprotective properties. 9-PAHSAcan be used in the research of diabetes-related cognitive impairment, obesity and non-alcoholic fatty liver disease.
Isotope-Labeled Compounds   CGRP Receptor   NF-κB  
/
HY-123115 Leucrose
Leucrose (5-O-α-D-Glucopyranosyl-D-fructose) is an orally active Sucrose (HY-B1779) isomer naturally found in pollen and honey. Leucrose promotes phosphorylation of JAK1 and STAT6, reduces pro-inflammatory mediators and cytokinesas (TNFα, and IL-1β), increases M2 macrophage polarization and suppresses DSS (HY-116282C)-induced colitis. Leucrose suppresses hepatic triglyceride accumulation, improves fasting blood glucose levels, and regulates hepatic lipogenesis and fatty acid β-oxidation in high-fat diet-induced obese mice. Leucrose is slowly hydrolyzed into glucose and fructose by α-glucosidase and acts as as a sugar substitute in diet.
JAK   STAT   TNF Receptor   Interleukin Related  
Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-P6292 KS-133
KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer.
PACAP Receptor   PKA   ERK   PI3K   Akt   GSK-3  
Breast Cancer   Colorectal Cancer   Neurodegenerative Disease   Schizophrenia  
/
HY-N1414 (E)-3',6-Disinapoylsucrose
(E)-3',6-Disinapoylsucrose is an orally active, blood-brain barrier permeable neuroprotective agent that inhibits Aβ protein aggregation. (E)-3',6-Disinapoylsucrose exerts anxiolytic, anti-inflammatory and cognitive-enhancing effects. (E)-3',6-Disinapoylsucrose regulates the TrkB/BDNF signaling pathway, inhibits the expression of NF-κB p65, reduces pro-inflammatory cytokine levels, and alleviates neuronal damage. (E)-3',6-Disinapoylsucrose also enhances the functions of central 5-HT and noradrenergic systems, thereby improving spatial learning and memory abilities and reducing anxiety-like behaviors. (E)-3',6-Disinapoylsucrose can be used for the research of related diseases such as Alzheimer's disease, depression, memory impairment and anxiety disorder.
Trk Receptor   NF-κB   Amyloid-β  
Depression  
/
HY-176785S MCB-294
MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRASG12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer.
Ras   Apoptosis   p38 MAPK   Caspase   TNF Receptor  
/
HY-P99027 Ieramilimab
Ieramilimab (LAG525; IMP701) is a humanized IgG4 monoclonal antibody that binds to LAG-3, resulting in inhibition of LAG-3 interaction with MHC-II molecules. Ieramilimab restores T-cell and NK-cell-mediated antileukemic immunity by reducing exhaustion and augmenting cytokine output and cytotoxicity. Ieramilimab increases the infiltration of cytotoxic T lymphocytes and reduces baseline densities of regulatory T cells (Tregs) and ADAM10-expressing tumor cells. Ieramilimab can be used for the study of various malignancies including melanoma, RCC, and advanced solid tumors.

Species: Human

LAG-3  
Triple-Negative Breast Cancer  
/
HY-N14001 Naamidine J
Naamidine J is an imidazole-type alkaloids discovered in a sponge. Naamidine J inhibits inflammation by binding to the protein CSE1L (KD = 5.41 μM). Namidine J significantly inhibits the expression of pro-inflammatory factors such as TNF-α, IL-1β, and IL-6, and upregulates anti-inflammatory factors such as CD206 and Arg-1. Namidine J inhibits PD-L1 and shows antitumor activity. Namidine J significantly reduces pulmonary tissue edema, inflammatory cell infiltration and cytokine storm in mice. Namidine J can be used for the research on the immune microenvironment of acute lung injury and tumors.

Source: Pericharax heteroraphis

TNF Receptor   Interleukin Related   Arginase   PD-1/PD-L1  
Cancer   Inflammation or Immune System Disease  
/
HY-P990704 Rilvegostomig
Rilvegostomig (AZD-2936) is a bispecific humanized IgG1 antibody targeting PD-1 and TIGIT. Rilvegostomig induces tumor growth inhibition and modulates the tumor immune microenvironment. Rilvegostomig exhibits anti-tumor activity in metastatic non-small cell lung cancer (without prior immune checkpoint inhibitor treatment). Rilvegostomig can be used in research related to metastatic non-small cell lung cancer and endometrial cancer.

Species: Human

PD-1/PD-L1   Transmembrane Glycoprotein  
Non-Small Cell Lung Cancer   Endometrial Cancer  
/
HY-P10449 M2 Peptide
M2 Peptide is a peptide targeting M2-like tumor-associated macrophages (TAMs). M2 Peptide is used to carry drugs or small interfering RNA (siRNA) to promote the repolarization of M2-like macrophages to M1-like macrophages, thereby altering the immunosuppressive state in the tumor microenvironment and enhancing the anti-tumor immune response. M2 Peptide can be used to study the effect of macrophage polarization and how this polarization change affects tumor growth and metastasis.
Others  
Cancer   Inflammation or Immune System Disease  
/
HY-P990120 Anti-Rat Kappa Immunoglobulin Light Chain Antibody (MAR 18.5)
Anti-Rat Kappa Immunoglobulin Light Chain Antibody (MAR 18.5) is an anti-rat Kappa Immunoglobulin Light Chain IgG2a monoclonal antibody. Anti-Rat Kappa Immunoglobulin Light Chain Antibody (MAR 18.5) can enhance B cell depletion. Anti-Rat Kappa Immunoglobulin Light Chain Antibody (MAR 18.5) can enhance T cell exhaustion after the injection of CD4 mAb (HY-P990792) and CD8 mAb (HY-P99129). Anti-Rat Kappa Immunoglobulin Light Chain Antibody (MAR 18.5) can be used for research on immunology.

Species: Rat

Others  
Inflammation or Immune System Disease  
/
HY-P10424 OPBP-1
OPBP-1 is a D-peptide obtained by phage display screening, molecular docking and molecular dynamics simulation. OPBP-1 has high stability and strong antitumor and oral activity. OPBP-1 can selectively bind PD-L1 protein, significantly block the interaction between PD-1 and PD-L1, and this blocking effect helps to restore and improve the function of T lymphocytes and reduce the proportion of bone marrow derived suppressor cells (MDSCs) to combat tumor-induced immune escape. OPBP-1 can be used in cancer immunotherapy research.
PD-1/PD-L1  
Lung Cancer   Breast Cancer   Colorectal Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Ovarian Cancer  
/
HY-P10420 RS17
RS17 is an anti-tumor peptide designed to bind specifically to the CD47 molecule and block the interaction between CD47 and its ligand, SIRPα, on the surface membrane of macrophages. The main regulatory mechanism of RS17 is to prevent CD47 from transmitting selective phagocytosis signals to SIRPα by binding to CD47, so that macrophages do not recognize tumor cells as their own tissue, but phagocytose them as foreign substances, thereby inhibiting immune escape of tumor cells. RS17 can be used to study the mechanism of anti-tumor response and immune escape.
CD47   Interleukin Related  
Cancer  
/
HY-P991490 ISB2001
ISB2001 is a trispecific antibody targeting CD38, CD3 and BCMA. ISB2001 effectively counteracts tumor immune escape mechanisms caused by antigen downregulation, antigen loss, soluble factor competition and other factors. ISB2001 is applicable to relevant research on multiple myeloma and relapsed/refractory multiple myeloma.

Species: Human

CD38   CD3   TNF Receptor  
Cancer  
/
HY-N0600 Ginsenoside F3
Ginsenoside F3 is a saponin extracted from the leaves of Panax ginseng with immunoenhancing and antitumor immunostimulatory activities. Ginsenoside F3 upregulates RIPOR2 with a Kd value of 3.77 μM. Ginsenoside F3 enhances NF‑κB activation, upregulates T‑bet and downregulates GATA‑3, increases the production of IL‑2 and IFN‑γ, decreases the production of IL‑4 and IL‑10, reverses CD8⁺ T‑cell exhaustion, restores cytokine secretion, and enhances antitumor immunity in a mouse non‑small cell lung cancer model. Ginsenoside F3 can be used for the research of non-small cell lung cancer.
Interleukin Related   IFNAR   NF-κB  
Digestive System Disease   Cancer Immunology   Digestive System Inflammation  
/
HY-P990061 Polzastobart
Polzastobart (JTX-8064) is a humanized IgG4 monoclonal antibody and LILRB2 (ILT4) antagonist. Polzastobart specifically binds to and antagonizes LILRB2, relieves ILT4-mediated myeloid immunosuppression, and promotes the polarization of macrophages from an M2-like phenotype to an M1-like phenotype. Polzastobart induces macrophage polarization, IFNγ signaling, and T cell inflammation-related pharmacodynamic responses in ex vivo human renal cancer, lung cancer, and head and neck cancer tissues. Polzastobart can be used in studies related to tumor-associated macrophages and tumor immunity. For the isotype control of Polzastobart, refer to: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).

Species: Human

Transmembrane Glycoprotein   LILRB  
Cancer   Inflammation or Immune System Disease  
/
HY-P991449 LY3415244
LY3415244 is a bispecific antibody that targets and inhibits TIM-3 and PD-L1. LY3415244 blocks the interaction between TIM-3 on immune cells and PD-L1 on the surface of tumor cells, establishes intercellular connections between TIM-3-positive immune cells and PD-L1-positive tumor cells, and blocks dual immunosuppressive signals. LY3415244 alleviates T cell exhaustion and restores T cell proliferation. LY3415244 induces broad-spectrum anti-drug antibodies, which impairs the binding capacity to soluble TIM-3 targets. LY3415244 can be used in research related to various advanced solid tumors.

Species: Human

PD-1/PD-L1   Tim3  
Cancer  
/
HY-N10889 Sominone
Sominone is the active metabolite of Withanoside IV (HY-N8693). Sominone enhances neuronal morphological plasticity by activating the RET pathway. Sominone can also induce axon/dendrite regeneration and synaptic reconstruction, thereby improving spatial memory. Sominone can be used in the research of neurodegenerative diseases such as Alzheimer's disease.
Drug Metabolite   RET  
Neurological, Eye or Ear Disease  
/
HY-P991316 KD014
KD014 (DX-2400) is a human monoclonal antibody that selectively targets MMP‑14. KD014 inhibits collagen degradation and regulates the polarization of macrophages toward an anti-inflammatory/anti-tumor phenotype. KD014 alleviates joint damage in rheumatoid arthritis and suppresses tumor growth and invasion. KD014 can be used in studies related to breast cancer and rheumatoid arthritis.

Species: Human

MMP   NO Synthase  
Inflammation or Immune System Disease   Breast Cancer  
/
HY-P990651 PY314
PY314 is a humanized antibody targeting TREM2. PY314 binds TREM2 on tumor-associated macrophages, depletes TREM2-high tumor-associated macrophages, reduces pro-tumorigenic M2 macrophage infiltration, increases CD8+ T cell, NK cell, and M1 macrophage infiltration, creates a proinflammatory tumor microenvironment, and promotes antitumor immune responseS. PY314 can be used for the research of platinum-resistant ovarian cancer, advanced solid tumors, breast cancer, and advanced refractory solid tumors.

Species: Human

TREM receptor  
Ovarian Cancer   Lung Adenocarcinoma   Triple-Negative Breast Cancer  
/
HY-P990961 Palverafusp alfa
Palverafusp alfa (IMM-2510; SYN-2510) is a PD-L1/VEGF-targeting IgG1κ type humanized antibody. Palverafusp alfa blocks PD-1/PD-L1 binding, relieves immune suppression, mediates PD-L1-directed antibody-dependent cellular cytotoxicity (ADCC). Palverafusp alfa blocks VEGF/VEGFR binding, inhibits angiogenic signaling, relieves VEGF-induced immune suppression. Palverafusp alfa reduces endothelial cell proliferation, enhances ADCC and antibody-dependent cellular phagocytosis (ADCP), inhibits tumor growth, reverses T cell immune suppression. Palverafusp alfa exhibits immune stimulatory, antiangiogenic, and anti-tumor activity in the tumor microenvironment. Palverafusp alfa can be used for the research of cancer, such as solid tumors, non-small cell lung cancer.

Species: Human

VEGFR   PD-1/PD-L1  
Cancer   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
/
HY-P1341 OXA(17-33)
OXA (17-33) (Orexin A (17-33) (human, mouse, rat, bovine)) is the shortest active orexin peptide that selectively targets OX1 (EC50=8.29 nM), with 23-fold selectivity for the OX1 receptor over the OX2 receptor. The activity of OXA (17-33) depends on the Tyr17, Leu20, Asn25, His26 residues and the spatial conformation of the α-helix. OXA (17-33) activates signaling pathways involving inositol-1,4,5-trisphosphate receptor (IP3R), phospholipase D (PL-D) and choline-Sigma-1R, thereby increasing the cytoplasmic Ca2+ level in nucleus accumbens neurons, an effect that is blocked by Sigma-1R antagonists. OXA (17-33) serves as an important biological probe for investigating the function of the OX1 receptor. OXA (17-33) can be modified via incorporation of mixed disulfide bonds of homocysteine and cysteamine, and is widely used in studies related to insomnia and narcolepsy.
Orexin Receptor (OX Receptor)   Sigma Receptor   Phospholipase  
Neurological, Eye or Ear Disease  
/
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  
/
HY-107202GL Polyinosinic-polycytidylic acid (GMP Like)
Polyinosinic-polycytidylic acid (Poly(I:C)) (GMP Like) is the GMP Like class Polyinosinic-polycytidylic acid (HY-107202), and can be used as pharmaceutical excipients. Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid can directly trigger cancer cells to undergo apoptosis.
Toll-like Receptor (TLR)   PKD   HSP   Bcl-2 Family   Interleukin Related   Apoptosis  
Infection   Inflammation or Immune System Disease  
/
HY-120657 9-PAHSA
9-PAHSA is an orally active endogenous GPR120 agonist (EC50=18 μM). 9-PAHSA significantly inhibits LPS-induced inflammatory responses by blocking the NF-κB pathway. 9-PAHSA induces adipocyte browning, enhances glucose uptake and reduces lipid accumulation, while improving mitochondrial function and the survival rate of steatotic hepatocytes. In terms of neuroprotection, 9-PAHSA regulates the expression of REST and BDNF in the prefrontal cortex of diabetic mice, and effectively prevents spatial working memory deficits and abnormal social behaviors. 9-PAHSA does not directly regulate insulin secretion or improve systemic insulin sensitivity, and possesses specific anti-inflammatory, metabolic regulatory and neuroprotective properties. 9-PAHSA can be used in the research of diabetes-related cognitive impairment, obesity and non-alcoholic fatty liver disease.
CGRP Receptor   NF-κB  
Neurological, Eye or Ear Disease   Digestive System Disease   Digestive System Inflammation   Glucose Metabolism   Obesity  
/
HY-P99139 Anti-Mouse IL-1b Antibody (B122)
Anti-Mouse IL-1b Antibody (B122) is an anti-mouse IL-1b IgG monoclonal antibody. Anti-Mouse IL-1b Antibody (B122) enhances ferroptosis and increases levels of reactive oxygen species (ROS) combined with Sulfasalazine (SAS) (HY-14655). Anti-Mouse IL-1b Antibody (B122) can reduce monocyte infiltration and alleviate T cell exhaustion by blocking IL-1β signaling. Anti-Mouse IL-1b Antibody (B122) can be used for researches on cancer and cardiovascular conditions such as oral squamous cell carcinoma (OSCC), glioblastoma (GBM) and heart failure.

Species: Mouse

Interleukin Related   Reactive Oxygen Species (ROS)   Ferroptosis  
Blood or Cardio-cerebrovascular Disease   Glioma  
/
HY-NP0204 MSA Protein
MSA Protein (Mouse Serum Albumin) is most abundant protein in plasma, which leaks into the brain parenchyma when the blood-brain barrier (BBB) is impaired. Mouse Serum Albumin induces astrocytes to A1 phenotype to remarkably increase levels of Elovl1. Mouse Serum Albumin promotes VLSFAs secretion and causes neuronal lippoapoptosis through endoplasmic reticulum stress response pathway. MSA-activated microglia triggeres remarkable tau phosphorylation at multiple sites (Ser202/Thr205) through NLRP3 inflammasome pathway. Mouse Serum Albumin decreases the spatial learning and memory abilities in mice. Mouse Serum Albumin can be used for the study of neurodegenerative diseases like Alzheimer’s disease (AD) and frontotemporal dementia (FTD).
ELOVL   Apoptosis   NOD-like Receptor (NLR)   Caspase   Tau Protein  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
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HY-P6292A KS-133 TFA
KS-133 TFA is a highly selective and potent antagonist of the vascular active enteropeptide receptor 2 (VIPR2) with IC50 values for Ca influx measurement and cAMP measurement of 24.8 nM and 500 nM, respectively. KS-133 TFA reverses the tumor-promoting M2 phenotype of tumor-associated macrophages to the anti-tumor M1 phenotype, alters the tumor immune microenvironment, and inhibits tumor growth. KS-133 TFA can be used for research on schizophrenia and cancer immune regulation.
PACAP Receptor  
Cancer   Neurological, Eye or Ear Disease   Immunomodulation  
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HY-P991097 Pumitamig
Pumitamig (PM-8002, BNT-327) is a bispecific antibody targeting PD-L1 and VEGF-A, with immune activation and anti-angiogenic activities. By binding to PD-L1, Pumitamig restores the function of effector T cells, while neutralizing VEGF-A in the tumor microenvironment to reverse its inhibition on the infiltration and activation of immune cells and normalize tumor blood vessels. Pumitamig can also be combined with various ADCs targeting TROP2, B7H3, HER2, HER3 for the research of advanced/metastatic solid tumors, including non-small cell lung cancer, ovarian cancer, triple-negative breast cancer, cervical cancer, etc. Pumitamig also exhibits potential efficacy in "cold" tumors with low PD-L1 expression that are insensitive to immunotherapy.

Species: Human

VEGFR   PD-1/PD-L1  
Ovarian Cancer   Non-Small Cell Lung Cancer   Triple-Negative Breast Cancer   Metastatic Breast Cancer  
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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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Keywords

tumor immune microenvironment | epigenetic regulation | immune escape | T-cell exhaustion | macrophage polarization | viral mimicry | checkpoint blockade | spatial multi-omics