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Inflammation–Immune Microenvironment In Carotid Atherosclerosis

Chronic Inflammation Intercellular Communication & Diseases Oxidative Stress Metabolic Diseases

Carotid atherosclerosis is an immune-vascular disease in which retained lipoproteins, disturbed flow, endothelial dysfunction, smooth-muscle remodeling, and innate and adaptive immunity generate plaques that may cause ischemic stroke. The plaque microenvironment contains macrophages, monocytes, T and B cells, neutrophils, endothelial cells, smooth-muscle-derived states, fibroblast-like cells, and extracellular matrix. These components differ between stable and symptomatic lesions and across regions of one plaque. Inflammation is therefore not adequately described by total leukocyte abundance or an M1/M2 ratio; specific cell states and their anatomical relationships influence lipid handling, necrotic-core growth, cap integrity, thrombosis, and embolization[1][2].

High-dimensional human studies reveal important heterogeneity. Single-cell analysis of carotid plaques identified plaque-specific activated and exhausted T-cell states, proinflammatory conversion-like features in regulatory T cells from symptomatic disease, monocyte subsets with opposing associations, and macrophage and endothelial states linked to cerebrovascular events. Computational fluid dynamics combined with mass cytometry suggests that low or oscillatory shear environments are associated with different neutrophil, macrophage, and T-cell patterns than favorable flow regions. Thus, hemodynamic forces act through endothelial and immune programs, coupling vessel geometry to local biology. Precision strategies could alter disease-specific leukocyte recruitment, stabilize pathogenic T-cell or macrophage programs, restore regulatory functions, or target vulnerable endothelial states while preserving systemic immunity. A large lipid core, thin fibrous cap, intraplaque hemorrhage, calcification pattern, neovascularization, and local stress can modify the consequence of an immune state[1][3][4][5].

Translation from mice requires caution. Mouse atherosclerosis atlases have defined diverse leukocyte clusters and cell-specific lipid, proliferation, and cytokine programs, but cross-species integration shows that human carotid plaques are particularly rich in activated and memory T-cell phenotypes that standard young mouse models reproduce poorly. Older mice may capture some features, yet anatomy, lesion rupture, therapy, and immune history remain different. Human endarterectomy samples also represent advanced disease and are influenced by symptoms, statins, antiplatelet treatment, surgery, and sampling location. Cell clusters should be validated by protein and spatial methods and tested functionally before being labeled causal therapeutic targets. Treatment studies must show fewer ischemic events, not merely a shifted cell signature. Integrating flow, spatial tissue biology, longitudinal imaging, and systemic risk provides the most coherent path toward mechanism-based prevention of carotid stroke. Combining high-resolution discovery with compact, reproducible assays may allow risk prediction without requiring single-cell sequencing for every patient[1][2][3][4][5].

Tissue-derived gene signatures and blood or imaging surrogates may help identify high-risk plaques, but retrospective risk models can overfit and require prospective external validation beyond patients already selected for surgery. Clinical utility should be compared with stenosis, plaque imaging, symptoms, and standard risk factors. Plaque composition should also be interpreted alongside morphology and mechanics. Endarterectomy tissue permits deep profiling but not repeated observation of an untreated lesion; less invasive imaging or blood biomarkers will need careful tissue anchoring. Sampling both plaque core and shoulder can reduce spatial bias. Studies should report time between neurologic event and surgery because acute events themselves alter immune programs. Prospective cohorts should determine whether these integrated features improve treatment decisions and outcomes beyond established clinical and imaging criteria. prospectively[1][3][4][5].

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Cat. No. Product Name Information Application Publication
HY-11109 Resatorvid
Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-α and IL-6 production with IC50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases.
Toll-like Receptor (TLR)   TNF Receptor   Interleukin Related   Autophagy  
Prostate Cancer   Pain   Digestive System Inflammation   Obesity   Lung Fibrosis   Rheumatoid Arthritis  
536
HY-12815A MCC950 sodium
MCC950 sodium (CP-456773 sodium; CRID3 sodium salt) is a potent, selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively.
NOD-like Receptor (NLR)  
Depression   Autoimmune Disease  
497
HY-12815 MCC950
MCC950 (CP-456773; CRID3) is a potent and selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively.
NOD-like Receptor (NLR)  
Depression   Autoimmune Disease  
497
HY-100381 Nigericin sodium salt
Nigericin sodium salt is an antibiotic derived from Streptomyces hygroscopicus that act as a K+/H+ ionophore, promoting K+/H+ exchange across mitochondrial membranes. Nigericin sodium salt is a NLRP3 activator. Nigericin sodium salt shows promising anti-cancer activities through decreasing intracellular pH (pHi), and inactivation of Wnt/β-catenin signals. Nigericin sodium salt induces pyroptosis through caspase 1/GSDMD in TNBC.

Source: Streptomyces hygroscopicus

Potassium Channel   NOD-like Receptor (NLR)   Bacterial   Antibiotic   Pyroptosis   Wnt   β-catenin  
Breast Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Ovarian Cancer   Bacterial Infection   Depression   Hypertension   Lung Fibrosis   Rheumatoid Arthritis  
258
HY-127019 Nigericin
Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K+/H+ ionophore, promoting K+/H+ exchange across mitochondrial membranes. Nigericin is a NLRP3 activator. Nigericin shows promising anti-cancer activities through decreasing intracellular pH (pHi), and inactivation of Wnt/β-catenin signals. Nigericin induces pyroptosis through caspase 1/GSDMD in TNBC.
Potassium Channel   NOD-like Receptor (NLR)   Bacterial   Antibiotic   Pyroptosis   Wnt   β-catenin  
Breast Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Ovarian Cancer   Bacterial Infection   Depression   Hypertension   Lung Fibrosis   Rheumatoid Arthritis  
258
HY-112879 Mito-TEMPO
Mito-TEMPO is a mitochondria-targeted antioxidant. Mito-TEMPO induces mitophagy by activating the PINK1/Parkin pathway, inhibits NLRP3 inflammasome activation, restores mitochondrial membrane potential, and improves renal function and podocyte injury. Mito-TEMPO regulates Ca2+ homeostasis, inhibits Bnip3 overexpression, shortens action potential duration, and exerts antiarrhythmic effects. Mito-TEMPO reverses premature senescence, reduces trabecular bone loss, and decreases cell apoptosis. Mito-TEMPO can be used in studies of chronic kidney disease, age-related cardiac dysfunction, postmenopausal osteoporosis, and ischemic stroke.
Calcium Channel   Apoptosis   Mitochondrial Metabolism   NOD-like Receptor (NLR)   PINK1/Parkin   Autophagy  
Ischemic Stroke   Osteoporosis   Chronic Kidney Disease  
186
HY-B2176 ATP
ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation. ATP can activate the NLRP3 inflammasome and induce IL-1β and chemokines secretion. ATP has anti-bacterial infection effects and can protect mice against bacterial infection in mice.

Source: widespread

Endogenous Metabolite   NOD-like Receptor (NLR)   Interleukin Related   Bacterial  
Infection   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
178
HY-B0240 Disulfiram
Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells. Disulfiram, a copper ion carrier, with Cu2+ increases intracellular ROS levels and induces cuproptosis.
Aldehyde Dehydrogenase (ALDH)   Interleukin Related   Pyroptosis   Apoptosis   Cuproptosis  
Metabolic or Endocrine Disease   Breast Cancer   Prostate Cancer   Pancreatic Cancer   Ovarian Cancer   Viral Infection   Depression   Pain   Autoimmune Disease   Digestive System Inflammation   SARS-CoV-2 Infection  
161
HY-100573 Necrosulfonamide
Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.
Mixed Lineage Kinase   Necroptosis   Pyroptosis   Caspase   NOD-like Receptor (NLR)   Keap1-Nrf2   TNF Receptor   Interleukin Related   NO Synthase   Heme Oxygenase (HO)  
Digestive System Disease   Prostate Cancer   Leukemia/Lymphoma/Myeloma   Depression   Digestive System Inflammation   Cardiovascular Disease   Parkinson's Disease   Obesity   Lung Fibrosis   Rheumatoid Arthritis  
147
HY-50912 Plerixafor octahydrochloride
Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC50 of 44 nM.
CXCR   HIV   Virus Protease  
Pancreatic Cancer   Viral Infection   Digestive System Inflammation   Glucose Metabolism   SARS-CoV-2 Infection   Lung Fibrosis   Rheumatoid Arthritis  
112
HY-10046 Plerixafor
Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM.
CXCR   HIV  
Pancreatic Cancer   Viral Infection   Digestive System Inflammation   Glucose Metabolism   SARS-CoV-2 Infection   Lung Fibrosis   Rheumatoid Arthritis  
112
HY-14519 Methotrexate
Methotrexate (Amethopterin; CL14377; WR19039) is an orally active antifolate (Antifolate). Methotrexate inhibits dihydrofolate reductase (DHFR), blocks tetrahydrofolate production, suppresses purine/pyrimidine synthesis and transmethylation, and causes intracellular accumulation of AICAR. Methotrexate promotes extracellular adenosine release, regulates the cytokine network, and inhibits the alarmin function of HMGB1. Methotrexate induces apoptosis and cytotoxicity, upregulates the expression of iNOS and COX-2, suppresses hippocampal neurogenesis, and induces pulmonary fibrosis. Methotrexate is used in the research of various immune and inflammation-related diseases such as arthritis, psoriasis, systemic lupus erythematosus, as well as pulmonary fibrosis and breast cancer.
Antifolate   Dihydrofolate reductase (DHFR)   NO Synthase   COX   Interleukin Related  
Breast Cancer   Arthritis   Systemic Lupus Erythematosus   Psoriasis   Lung Fibrosis  
87
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-L228 Lipid Metabolite Compound Library
Lipids are important energy storage substances in the human body. They are involved in the regulation of cell structure and function, as well as signaling pathways and gene expression. Abnormal lipid levels in tissues or their dysregulation can lead to various diseases. These include obesity, type 2 diabetes, non-alcoholic fatty liver disease, neurodegenerative diseases, infections, and cancer. Therefore, maintaining normal levels of lipid metabolism is critical to overall health. One of the key features of cancer is aberrant lipid metabolism. This includes alterations in lipid uptake, lipid desaturation, neolipogenesis, lipid droplets, and fatty acid oxidation in cancer cells. These changes all contribute to cellular survival in an ever-changing microenvironment. They do this by modulating feed-forward oncogenic signals and key oncogenic functions. Additionally, they affect oxidative stress, other types of stress, immune responses, and intercellular communication. Alterations in lipid metabolism have a strong impact on the properties of cancer stem cells. This includes aspects such as self-renewal, differentiation, invasion, metastasis, drug sensitivity, and resistance. Furthermore, these alterations also modulate T cell responses. MCE can offer 146 metabolites of lipid metabolism pathways, which can be used for drug screening in cancer, immune-based diseases, metabolic diseases, and other diseases.

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-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-16569 Colchicine
Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research.
Environmental Pollutants   Microtubule/Tubulin   Autophagy   Apoptosis   NOD-like Receptor (NLR)  
Digestive System Disease   Lung Cancer   Prostate Cancer   Viral Infection   Coronavirus Infection   Depression   Pain   Autoimmune Disease   Digestive System Inflammation   Alzheimer's Disease   Lung Fibrosis  
77
HY-107202 Polyinosinic-polycytidylic acid
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.
RIG-I-like receptor (RLR)   Toll-like Receptor (TLR)   PKD   HSP   Bcl-2 Family   Interleukin Related   Apoptosis  
Infection   Digestive System Disease   Prostate Cancer   Pain   Digestive System Inflammation   Lung Fibrosis   Rheumatoid Arthritis  
73
HY-13067 Celastrol
Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH.
Proteasome   Autophagy   Mitophagy   Apoptosis   Endogenous Metabolite   Antibiotic   Bacterial   Nuclear Hormone Receptor 4A/NR4A  
Cancer   Infection   Inflammation or Immune System Disease  
68
HY-16711 SB225002
SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits 125I-IL-8 binding to CXCR2 with an IC50 of 22 nM.
CXCR  
Metabolic or Endocrine Disease   Gastric Cancer   Digestive System Inflammation   Rheumatoid Arthritis  
66
HY-15251 Reparixin
Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
CXCR  
Metabolic or Endocrine Disease   Gastric Cancer   Pancreatic Cancer   Digestive System Inflammation   Rheumatoid Arthritis  
65
HY-108841 Raleukin
Raleukin (Kineret) is a recombinant, nonglycosylated human interleukin-1 receptor (IL-1R) antagonist. Raleukin significantly reduces neutrophil accumulation in blood vessels and brain infarct volume as well as improves motor coordination performance in ischemic stroke mice model. Anakinra can be used to study chronic inflammatory disorders like rheumatoid arthritis and cardiovascular recurrence post-myocardial infarction.

Species: Human

Interleukin Related  
Metastatic Breast Cancer   SARS-CoV-2 Infection   Rheumatoid Arthritis  
57
HY-B1081A Oxidopamine hydrobromide
Oxidopamine (6-OHDA) hydrobromide is an antagonist of the neurotransmitter dopamine. Oxidopamine hydrobromide is a widely used neurotoxin and selectively destroys dopaminergic neurons. Oxidopamine hydrobromide promotes COX-2 activation, leading to PGE2 synthesis and pro-inflammatory cytokine IL-1β secretion. Oxidopamine hydrobromide can be used for the research of Parkinson’s disease (PD), attention-deficit hyperactivity disorder (ADHD), and Lesch-Nyhan syndrome.
Dopamine Receptor   Autophagy   Mitophagy   COX   PGE synthase   Interleukin Related   p38 MAPK   Apoptosis   Caspase  
Breast Cancer   Parkinson's Disease  
50
HY-12497 ANA-12
ANA-12 is a brain-penetrant, selective TrkB antagonist with IC50 values of 45.6 nM and 41.1 μM, and Kd values of 10 nM and 12 μM, for high- and low-affinity sites, respectively. ANA-12 specifically inhibits BDNF-induced TrkB receptor activation and its downstream signaling cascades by directly and non-competitively binding to the TrkB receptor, without affecting the functions of TrkA and TrkC. ANA-12 is used in research concerning neuropsychiatric disorders (such as depression and anxiety), acute and chronic pain, neuroimmune inflammation, and the mechanisms of learning and memory.
Trk Receptor   NOD-like Receptor (NLR)   AIM2   Caspase  
Depression   Anxiety or Fear-Related Disease   Pain   CNS Infection   Behavioral Addiction  
41
HY-15319 AMG 487
AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
CXCR  
Cancer   Metabolic or Endocrine Disease   Digestive System Disease   Digestive System Inflammation   Rheumatoid Arthritis  
40
HY-13624 Epirubicin
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
DNA/RNA Synthesis   Topoisomerase   Apoptosis   Antibiotic   FOXP  
Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Non-Small Cell Lung Cancer   HER-2 Positive Breast Cancer   Triple-Negative Breast Cancer   Metastatic Breast Cancer  
38
HY-13624A Epirubicin hydrochloride
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
DNA/RNA Synthesis   Topoisomerase   Apoptosis   Antibiotic   FOXP  
Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Non-Small Cell Lung Cancer   HER-2 Positive Breast Cancer   Triple-Negative Breast Cancer   Metastatic Breast Cancer  
38
HY-10198 Navarixin
Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.
CXCR  
Metabolic or Endocrine Disease   Prostate Cancer   Gastric Cancer   Digestive System Inflammation   SARS-CoV-2 Infection   Rheumatoid Arthritis  
32
HY-13848 Rugocrixan
AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively.
CX3CR1   CXCR  
Cancer   Metabolic or Endocrine Disease   Digestive System Disease   Digestive System Inflammation  
26
HY-N2148 Cytosporone B
Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77/NR4A1 agonist with an EC50 of 0.278 nM.

Source: fungus?Eupenicillium?sp. HJ002

Nuclear Hormone Receptor 4A/NR4A  
Neurological, Eye or Ear Disease   Lung Cancer   Glucose Metabolism  
18
HY-13406 TAK-779
TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
CCR   HIV   CXCR  
Cancer   Metabolic or Endocrine Disease   Digestive System Disease   Viral Infection   Digestive System Inflammation   Lung Fibrosis   Rheumatoid Arthritis  
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-B1322B Amodiaquine dihydrochloride
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
Nuclear Hormone Receptor 4A/NR4A   Parasite   Histone Methyltransferase  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Leukemia/Lymphoma/Myeloma   Viral Infection   Parasitic Infection  
12
HY-B1322 Amodiaquine dihydrochloride dihydrate
Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
Nuclear Hormone Receptor 4A/NR4A   Parasite   Histone Methyltransferase  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Leukemia/Lymphoma/Myeloma   Viral Infection   Parasitic Infection   SARS-CoV-2 Infection  
12
HY-B1322A Amodiaquine
Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
Nuclear Hormone Receptor 4A/NR4A   Parasite   Histone Methyltransferase  
Infection   Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
12
HY-19855 AZD-5069
AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.
CXCR  
Metabolic or Endocrine Disease   Prostate Cancer   Gastric Cancer   Pancreatic Cancer   Digestive System Inflammation   Rheumatoid Arthritis  
11
HY-100806 Kynurenic acid
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
iGluR   Endogenous Metabolite   Apoptosis   CXCR   GPR35  
Cancer   Metabolic or Endocrine Disease   Digestive System Disease   Depression   Digestive System Inflammation   Alzheimer's Disease   Parkinson's Disease  
11
HY-112055 DIM-C-pPhOH
DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively.
Nuclear Hormone Receptor 4A/NR4A   Apoptosis  
Cancer   Digestive System Disease   Digestive System Inflammation  
9
HY-P9926 Dupilumab
Dupilumab (REGN-668) is a fully human mAb to IL-4 receptor α (IL-4Rα) that inhibits both IL-4 and IL-13 signaling, markedly improved moderate-to-severe atopic dermatitis.

Species: Human

Interleukin Related  
Inflammation or Immune System Disease   Breast Cancer   Non-Small Cell Lung Cancer   Staphylococcus Aureus Infection  
9
HY-B1521 Aluminum Hydroxide
Aluminum Hydroxide is an orally active main form of aluminum used as adjuvant. Aluminum hydroxide-based adjuvant researches include the repository effect, pro-phagocytic effect, and activation of the pro-inflammatory NLRP3 pathway. Aluminum Hydroxide also acts as adjuvant to compensate low inherent immunogenicity of subunit vaccines.
Environmental Pollutants   NOD-like Receptor (NLR)  
Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
7
HY-W250978 Ovalbumins
Ovalbumins are the major proteins in egg white. Ovalbumins act as an allergen and inducer, and can be applied to mouse models of allergic diseases. Ovalbumins can induce allergic rhinitis in mice via sensitization and nasal challenge. Ovalbumins can be used to establish asthma models.
Ovalbumin, low endotoxin (HY-W250978A) is recommended for model establishment.
Interleukin Related   IFNAR  
Allergic Asthma   Allergic Rhinitis  
6
HY-N1910 4'-O-Methylbavachalcone
4'-O-Methylbavachalcone is an orally active prenylated flavonoid that inhibits the activity of SARS-CoV papain-like protease (PLpro), with an IC50 of 10.1 μM and a Ki of 4.6 μM. 4'-O-Methylbavachalcone inhibits poly (ADP-ribose) polymerase-mediated cell death (parthanatos), reduces cerebral infarct volume, binds to the orthosteric site of SUCNR1, blocks the interaction between succinate and SUCNR1, inhibits SUCNR1 activity, blocks the nuclear translocation of NFATc4, suppresses the activation of the ERK1/2 signaling pathway, inhibits cardiomyocyte hypertrophy and restores the expression of α-actinin. 4'-O-Methylbavachalcone can be used in studies related to ischemic stroke, SARS-CoV and cardiomyocyte hypertrophy.
SARS-CoV   Virus Protease   Succinate Receptor 1   ERK  
Neurological, Eye or Ear Disease   SARS-CoV-2 Infection  
4
HY-N0390S L-Glutamine-15N
L-Glutamine-15N is the 15N-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  
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-18555 TMPA
TMPA is a high-affinity Nur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. TMPA effectively lowers blood glucose and attenuates insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human T cells, can also be used in studies of cancer and T-cell apoptosis dysregulation.
Nuclear Hormone Receptor 4A/NR4A   AMPK  
Pancreatic Cancer   Pain   Digestive System Inflammation   Glucose Metabolism   Obesity  
3
HY-N0546 Ligustroflavone
Ligustroflavone is an orally active flavonoid compound. Ligustroflavone can be extracted from Ligustrum lucidum. Ligustroflavone antagonizes the calcium-sensing receptor (CaSR), inhibits the RIPK1/RIPK3/MLKL pathway, and downregulates TGF-β/Smad signaling. Ligustroflavone regulates calcium metabolism, protects bone tissue, reduces cerebral ischemic injury, and inhibits liver fibrosis. Ligustroflavone can be used in the study of diabetic osteoporosis, ischemic stroke, and liver fibrosis.
CaSR   RIP kinase   Mixed Lineage Kinase   TGF-beta/Smad  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Colorectal Cancer   Prostate Cancer   Cardiovascular Disease   Glucose Metabolism   Obesity   Lung Fibrosis  
2
HY-19808 C-DIM12
C-DIM12 is a potent, orally active Nurr1 modulator. C-DIM12 inhibits the tumor growth and autophagy, and induces the cell apoptosis. C-DIM12 has anti-inflammatory and neuroprotective effects, and can be used for cancer and neurological disease study.
Nuclear Hormone Receptor 4A/NR4A  
Cancer   Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
2
HY-N2484 Methylnissolin
Methylnissolin (Astrapterocarpan) is an osteoclast inhibitor with anti-inflammatory, neuroprotective and antioxidant activities. Methylnissolin downregulates the activation of the MAPK and PI3K/AKT pathways, inhibits the phosphorylation of MAPK1 and AKT1, and blocks PDGF-BB-induced phosphorylation of ERK1/2. Methylnissolin reduces the expression and secretion of proinflammatory mediators, decreases intracellular ROS levels, upregulates antioxidant enzymes, and downregulates osteoclastogenesis markers. Methylnissolin is applicable to research related to ischemic stroke, osteoporosis, cardiovascular diseases, skin aging, etc.
PDGFR   ERK  
Cellular Senescence   Ischemic Stroke   Osteoporosis  
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-P99644 ACT017
ACT017 is a Fab fragment of humanized anti-GPVI monoclonal antibody. ACT017 inhibits collagen-induced platelet aggregation. ACT017 has the potential for the research of acute ischemic stroke.

Species: Human

Glycoprotein VI  
Blood or Cardio-cerebrovascular Disease  
2
HY-P1624 Teduglutide
Teduglutide (ALX-0600) is an analog of human glucagon like peptide-2 (GLP-2). Teduglutide can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis.
Nuclear Hormone Receptor 4A/NR4A   FXR  
Inflammation or Immune System Disease  
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-N3307 (+)-Medioresinol
(+)-Medioresinol is a furofuran-type lignan with antifungal and antibacterial properties. (+)-Medioresinol synergizes with antibiotics to exert antimicrobial and antibiofilm effects. (+)-Medioresinol induces intracellular ROS accumulation and mitochondrial-mediated apoptosis in Candida albicans. (+)-Medioresinol inhibits LPS (HY-D1056)-stimulated IL-12p40 production. (+)-Medioresinol is a PGC-1α activator that protects against endothelial cell pyroptosis in ischemic stroke via the PPARα-GOT1 axis. (+)-Medioresinol can be used in research on fungal and bacterial infection, inflammation, and ischemic stroke.
Bacterial   Fungal   Reactive Oxygen Species (ROS)   Apoptosis   MMP   Interleukin Related   PI3K   Akt   mTOR   PPAR   PGC-1α   Pyroptosis  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
1
HY-N0390S5 L-Glutamine-1-13C
L-Glutamine-1-13C 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  
1
HY-124131 DS-437
DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3.
Histone Methyltransferase   FOXP  
Inflammation or Immune System Disease   Leukemia/Lymphoma/Myeloma  
1
HY-NP001 Cationic BSA Protein
Cationic BSA Protein (Cationic Bovine Serum Albumin) is a bovine serum albumin (BSA) modified with excess ethylenediamine, which has enhanced immunogenicity compared to native BSA. Positively charged primary amines block all negatively charged carboxyl groups, making Cationic BSA Protein a cationic protein. Cationic BSA Protein has remarkable neuroprotective effects on ischemic stroke when in combination with Tanshinone IIA (HY-N0135) .
Biochemical Assay Reagents  
Neurological, Eye or Ear Disease  
1
HY-P1684 Peptide P60
Peptide P60 is a FOXP3 inhibitor. Peptide P60 reduces the nuclear translocation of FOXP3 and impairs FOXP3-mediated inhibition of NF-κB and NFAT activity. Peptide P60 inhibits the immunosuppressive activity of regulatory T cells and restores the proliferation and activation of effector T cells. Peptide P60 induces lymphoproliferative autoimmune syndrome in neonatal ICR mice and reduces the number of CD4+CD25+Foxp3+ T cells in the spleen. Peptide P60 enhances the efficacy of AH1 (HY-P4193) peptide vaccine and recombinant adenovirus-based HCV NS3 vaccine in BALB/c mice, including protective effects against CT26 tumor implantation. Peptide P60 can be used in studies related to tumor immunity, viral infection and lymphoproliferative autoimmune syndrome.
FOXP   NF-κB   Nuclear Factor of activated T Cells (NFAT)  
Cancer   Infection   Inflammation or Immune System Disease  
1
HY-155659 4A7C-301
4A7C-301 is a blood-brain barrier-permeable Nurr1 agonist, with IC50 values of 48.22 nM and 107.71 nM for binding to Nurr1-LBD in the [3H]-CQ competition assay and TR-FRET assay, respectively. The EC50 of 4A7C-301 for activating Nurr1 transcriptional activity is 6.53 μM, and its EC50 in N27-A dopaminergic cells is approximately 0.2 μM. 4A7C-301 binds directly to Nurr1-LBD, enhances the transcriptional function of Nurr1, and restores the reduction of Nurr1 protein induced by MPP+ or αSyn. 4A7C-301 alleviates oxidative stress and mitochondrial dysfunction, protects midbrain dopaminergic neurons, inhibits microglial activation, and restores impaired autophagic flux. 4A7C-301 can be used in studies related to neuroprotection and Parkinson's disease.
Nuclear Hormone Receptor 4A/NR4A  
Parkinson's Disease  
1
HY-N0559 Kirenol
Kirenol is a diterpenoid compound, an orally active apoptosis inducer and signaling pathway regulator, with a Kd value of 5.47 μM against the target CK2. Kirenol promotes the cleavage of Bid into tBid, regulates the protein levels/phosphorylation of Bax, Bcl-2, p53 and p21, and induces caspase-independent apoptosis, S-phase cell cycle arrest, ROS accumulation and cytotoxicity in cancer cells. Kirenol activates the CK2/AKT and AMPK-mTOR-ULK1 pathways, inhibits the signaling of NF-κB, TGF-β/Smads and NLRP3 inflammasome, and regulates the GSK3β, BMP and Wnt/β-catenin pathways. Kirenol induces autophagy, mitophagy and osteoblast differentiation, promotes mitochondrial fusion, and exerts antioxidant, anti-inflammatory, antifibrotic, renoprotective, cardioprotective, neuroprotective and analgesic effects. Kirenol is applicable to research related to chronic myeloid leukemia, ischemic stroke, diabetic nephropathy, heart failure, acute lung injury and osteoporosis.
Casein Kinase   Apoptosis   AMPK   Akt   NF-κB   TGF-beta/Smad  
Neurological, Eye or Ear Disease   Acute Myeloid Leukemia   Acute Lung Injury   Heart Failure   Osteoporosis  
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-N0390S2 L-Glutamine-d5
L-Glutamine-d5 is the deuterium 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  
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-135556AS Norfluoxetine-d5
Norfluoxetine-d5 is the d5-labeled Norfluoxetine (HY-135556). Norfluoxetine is the active metabolite of the antidepressant Fluoxetine (HY-B0102); it is also a TREK-2 K2P potassium channel inhibitor. Norfluoxetine exhibits neuroimmunological activity, induces apoptosis in primary microglial cells, and inhibits the release of pro-inflammatory factors. Norfluoxetine inhibits high-threshold voltage-gated Ca2+ currents in neurons with an EC50 of 20.4 μM. Norfluoxetine can be used in research related to depression, ischemic stroke, and epilepsy.
Isotope-Labeled Compounds   Drug Metabolite   Potassium Channel   Calcium Channel   Apoptosis  
Depression   Epilepsy   Ischemic Stroke  
/
HY-P11289 Intermedin1-53 (Human)
Intermedin1-53 (Human) is a 53-aa human calcitonin family peptide that reduces the vulnerability of atherosclerotic plaques by inhibiting CHOP-mediated macrophage apoptosis and inflammasome.
Apoptosis  
Blood or Cardio-cerebrovascular Disease  
/
HY-151547S MRS4719-d3
MRS4719-d3 is the deuterium labeled MRS4719 (HY-151547). MRS4719 is a potent P2X4 receptor antagonist with an IC50 value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca2+]i influx in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke.
Isotope-Labeled Compounds   P2X Receptor  
Neurological, Eye or Ear Disease  
/
HY-P992368 HLX51
HLX51 is a regulatory T cell inhibitor and OX40/CD134/TNFRSF4 agonist with tumour growth inhibitory activity. HLX51 inhibits regulatory T cell differentiation and activity, relieves tumour microenvironment immunosuppression, enhances effector T cell function. HLX51 competitively binds OX40, activates OX40, promotes immune cell proliferation and T cell killing ability. HLX51 modulates immune cell function to inhibit tumour growth. HLX51 can be used for the research of advanced/metastatic solid tumours and lymphomas.

Species: Human

TNF Receptor  
Leukemia/Lymphoma/Myeloma  
/
HY-P10977 Tat-ASIC1a (1-20) (mouse, rat)
Tat-ASIC1a (1-20) (mouse, rat) is a competitive ASIC1a membrane-penetrating peptide. Tat-ASIC1a (1-20) (mouse, rat) has significantly neuroprotection effects, and reduces neuronal damage against acidotoxicity by targeting the ASIC1a-RIPK1 pathway and auto-inhibitory mechanism. Tat-ASIC1a (1-20) (mouse, rat) effectively protects brains from ischemic injury in ischemic stroke mice model. Tat-ASIC1a (1-20) (mouse, rat) can be used for neurodegenerative diseases research, such as Huntington disease and Parkinson’s disease.
Sodium Channel   RIP kinase  
Neurological, Eye or Ear Disease  
/
HY-N0390G L-Glutamine (GMP)
L-Glutamine GMP is L-Glutamine (HY-N0390) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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.
mTOR   NF-κB   STAT   HIF/HIF Prolyl-Hydroxylase  
Inflammation or Immune System Disease   Ischemic Stroke   Osteoporosis   Osteoarthritis  
/
HY-A0300 Cyclopeptide-5
Cyclopeptide-5 (EMD 270179) is an αvβ3 antagonist that can improve PAF-induced increased adhesion of sickle red blood cells, capillary post-obstruction, and enhance blood flow dynamics. Cyclopeptide-5 also has cytotoxic effects.
Integrin  
Blood or Cardio-cerebrovascular Disease  
/
HY-P10617 Salusin-β
Salusin-β is an endogenous bioactive peptide with significant hemodynamic and mitogenic activity. Salusin-β can stimulate the proliferation of quiescent vascular smooth muscle cells (VSMCs) and fibroblasts, leading to a rapid and significant decrease in blood pressure and heart rate. In addition, Salusin-β can stimulate the release of arginine vasopressin from the pituitary gland in rats. This makes Salusin-β have important application potential in cardiovascular disease research.
Endogenous Metabolite  
Blood or Cardio-cerebrovascular Disease  
/
HY-P11049 Stroke-homing peptide
Stroke-homing peptide is a homing peptide. Stroke-homing peptide can home to ischemic stroke brain tissue and detect the apoptotic neuronal cells. Stroke-homing peptide can be used for the research of molecular imaging and selective drug delivery to stroke tissue.
Others  
Neurological, Eye or Ear Disease  
/
HY-P11253 DOTA-Bn-CA-170
DOTA-Bn-CA-170 is a molecular probe targeting the VISTA protein, with a Kd value of 0.124 nM. DOTA-Bn-CA-170 is formed by covalently linking the p-SCN-Bn-DOTA ligand with CA-170 (HY-101093). DOTA-Bn-CA-170 labeled with [68Ga]Ga successfully achieves specific and high-contrast PET imaging of VISTA expression in various tumor-bearing mouse models. DOTA-Bn-CA-170 can be used for the study of VISTA-targeted immunotherapy.
VISTA  
Inflammation or Immune System Disease  
/
HY-P11048 Thrombin-cleavable peptide
Thrombin-cleavable peptide is a type of peptide that can be recognized and cleaved by thrombin. After cleavage, Thrombin-cleavable peptide releases thrombolytic peptides to initiate thrombolysis. Thrombin-cleavable peptide can be used in the research of diseases such as ischemic stroke.
Thrombin  
Neurological, Eye or Ear Disease   Blood or Cardio-cerebrovascular Disease  
/
HY-151546S MRS4596-d4
MRS4596-d4 is the deuterium labeled MRS4596 (HY-151546). MRS4596 is a potent and selective P2X4 receptor antagonist with an IC50 value of 1.38 μM for human P2X4 receptor. MRS4596 has neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4596 can be used in research of ischemic stroke.
Isotope-Labeled Compounds   P2X Receptor  
Neurological, Eye or Ear 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-76006R 3-Hydroxybenzaldehyde (Standard)
3-Hydroxybenzaldehyde (Standard) is the analytical standard of 3-Hydroxybenzaldehyde. This product is intended for research and analytical applications. 3-Hydroxybenzaldehyde (3-HBA) is a precursor compound for phenolic compounds like Protocatechuic aldehyde (PCA) (HY-N0295). 3-Hydroxybenzaldehyde, produced by 3-hydroxybenzyl-alcohol dehydrogenase, is a substrate of aldehyde dehydrogenase (ALDH) in rats and humans. 3-Hydroxybenzaldehyde has vasculoprotective effects in vitro and in vivo. 3-Hydroxybenzaldehyde is proming for research of atherosclerosis[1][2][3][4].
Reference Standards   Aldehyde Dehydrogenase (ALDH)   NF-κB   p38 MAPK  
Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
/
HY-N19029 Vernodalin
Vernodalin is an orally active, cytotoxic sesquiterpene lactone with a Kd value of 9.55 μM for p38 MAPK. Vernodalin downregulates the expression of phosphorylated ERK, JNK, AKT, PI3K, mTOR, p38MAPK, FAK, MMP-2, MMP-9, and uPA, while upregulates the expression of TIMP-1 and TIMP-2. Vernodalin increases ROS production, upregulates the expression of Bax and caspase 3, downregulates the expression of Bcl-2, and induces apoptosis (apoptosis), oxidative stress response and cell cycle arrest. Vernodalin inhibits the proliferation, adhesion and metastasis of cancer cells. Vernodalin enhances the activity of VEGF-B, AMPK and eNOS signaling pathways. Vernodalin alleviates myocardial injury and restores hemodynamic parameters. Vernodalin inhibits the growth of Trypanosoma brucei rhodesiense. Vernodalin can be used in research related to various cancers including gastric cancer, colorectal cancer and lung cancer, as well as African human trypanosomiasis and myocardial infarction.
p38 MAPK   PERK   JNK   Akt   PI3K   mTOR   FAK   MMP   PAI-1   Reactive Oxygen Species (ROS)   Caspase   Bcl-2 Family   Apoptosis   VEGFR   AMPK   Parasite  
Lung Cancer   Colorectal Cancer   Gastric Cancer   Trypanosome Infection   Myocardial Infarction  
/
HY-175824 PSD-95/nNOS PPI-IN-1
PSD-95/nNOS PPI-IN-1 is a inhibitor targeting the PSD-95/nNOS interaction with potential blood-brain barrier penetration. PSD-95/nNOS PPI-IN-1 binds to the PSD-95 PDZ2 domain with high affinity (Ki = 19.45 μM). PSD-95/nNOS PPI-IN-1 inhibits glutamate-induced excitotoxicity by reducing intracellular ROS levels and inhibiting apoptosis. PSD-95/nNOS PPI-IN-1 significantly reduces cerebral infarct volume in rat tMCAO models. PSD-95/nNOS PPI-IN-1 can be used for the study of acute ischemic stroke.
iGluR   NO Synthase   Apoptosis   Reactive Oxygen Species (ROS)  
Neurological, Eye or Ear Disease  
/
HY-P3765 Auriculin A
Auriculin A is a synthetic atrial natriuretic factor (ANF) with hemodynamic effect. Auriculin A antagonizes renal vasoconstriction in the dog, and influences on arterial baroreflex control of heart rate, systemic blood pressure, and perfusion pressure in the hind limb (perfused at constant flow) in rabbits.
Others  
Blood or Cardio-cerebrovascular Disease  
/
HY-N13251 Verbena Extract
Verbena Extract is a verbena extract. Verbena Extract is a potential anti-ischemic stroke agent, and its mechanism may be related to IL17A-mediated neuroinflammation regulation..
Others  
Neurological, Eye or Ear Disease  
/
HY-P991604 MLN2201
MLN2201 is a humanized monoclonal antibody inhibitor, targeting Integrin β2. MLN2201 inhibits the reperfusion injury after stroke and can be used for inflammatory diseases like ischemic stroke research.

Species: Human

Integrin  
Inflammation or Immune System Disease  
/
HY-P10616 Salusin-α
Salusin-α is an endogenous bioactive peptide with hemodynamic and cell proliferation activities. Salusin-α can stimulate the proliferation of quiescent vascular smooth muscle cells (VSMCs) and fibroblasts, leading to a rapid and significant decrease in blood pressure and heart rate, but its effect is weaker than that of Salusin-β (HY-P10617). Salusin-α has potential application value in cardiovascular disease research.
Endogenous Metabolite  
Blood or Cardio-cerebrovascular 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-N0361S Dihydrocapsaicin-d3
Dihydrocapsaicin-d3 is the deuterium labeled Dihydrocapsaicin (HY-N0361). Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat.
Isotope-Labeled Compounds   Reactive Oxygen Species (ROS)   PI3K   Bcl-2 Family   Caspase   Apoptosis   TRP Channel   Akt  
/
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-W015777R 4-Methoxybenzyl alcohol (Standard)
4-Methoxybenzyl alcohol (Standard) (P-Methoxy-benzyl alcoho (Standard); (4-Methoxyphenyl)methanol (Standard)) is the analytical standard of 4-Methoxybenzyl alcohol (HY-W015777). This product is intended for research and analytical applications. 4-Methoxybenzyl alcohol (P-Methoxy-benzyl alcoho; (4-Methoxyphenyl) methanol) is a naturally derived volatile aromatic compound. 4-Methoxybenzyl alcohol upregulates the phosphorylation level of PI3K/Akt pathway proteins, downregulates the expression of pro-inflammatory factors, increases the content of tight junction proteins occludin and claudin-5, and alleviates structural damage to the blood-brain barrier. 4-Methoxybenzyl alcohol improves the decrease in viability and NO level of cerebral microvascular endothelial cells induced by oxygen-glucose deprivation/reperfusion, and reduces the release of lactate dehydrogenase. 4-Methoxybenzyl alcohol serves as a substrate in the two-phase persulfate-mediated electro-oxidation system, where it is directionally oxidized to p-anisaldehyde. 4-Methoxybenzyl alcohol acts as a substrate for wild-type fungal aryl alcohol oxidase. 4-Methoxybenzyl alcohol can be used in studies related to ischemic stroke, as well as in research across various fields such as chemical synthesis, including the synthesis of fragrances and flavorings.
Reference Standards   Drug Intermediate   Interleukin Related   TNF Receptor   Claudin   Akt   NO Synthase  
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HY-76520S Sitaxsentan-13C6
Sitaxsentan-13C6 (IPI 1040-13C6) is 13C labeled Sitaxsentan (HY-76520). Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension.
Isotope-Labeled Compounds   Endothelin Receptor   TGF-β Receptor  
Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
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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  
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HY-P11117 TAT-EE3
TAT-EE3 is a neuroprotective peptide which can uncouple TRPM2-NMDARs interaction. TAT-EE3 inhibits TRPM2-induced enhancement of NMDAR surface expression and current amplitude.TAT-EE3 protects neurons against ischemic injury in vitro and in vivo. TAT-EE3can be used for the study of ischemic stroke.
TRP Channel   iGluR   Calcium Channel  
Neurological, Eye or Ear Disease  
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HY-P5117 TAT-CIRP
TAT-CIRP is a a small peptide, refers to Trans-trans-activating (Tat)-cold-inducible RNA binding protein. TAT-CIRP is an inhibitor of myeloid differentiation protein 2 (MD2). TAT-CIRP exhibits robust neuroprotection against ischemic and hemorrhagic stroke in mice.
Toll-like Receptor (TLR)  
Neurological, Eye or Ear Disease  
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HY-W011235S Norfluoxetine-d5 hydrochloride
Norfluoxetine-d5 hydrochloride is the d5-labeled Norfluoxetine hydrochloride (HY-W011235). Norfluoxetine hydrochloride is the active metabolite of the antidepressant Fluoxetine (HY-B0102); it is also a TREK-2 K2P potassium channel inhibitor. Norfluoxetine hydrochloride exhibits neuroimmunological activity, induces apoptosis in primary microglial cells, and inhibits the release of pro-inflammatory factors. Norfluoxetine hydrochloride inhibits high-threshold voltage-gated Ca2+ currents in neurons with an EC50 of 20.4 μM. Norfluoxetine hydrochloride can be used in research related to depression, ischemic stroke, and epilepsy.
Isotope-Labeled Compounds   Drug Metabolite   Potassium Channel   Calcium Channel   Apoptosis  
Depression   Epilepsy   Ischemic Stroke  
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HY-113248R 3-Nitro-L-tyrosine (Standard)
3-Nitro-L-tyrosine (Standard) is the analytical standard of 3-Nitro-L-tyrosine (HY-113248). This product is intended for research and analytical applications. 3-Nitro-L-tyrosine serves as a biomarker of oxidative stress. 3-Nitro-L-tyrosine attenuates the pressor and vasoconstrictive effects of angiotensin II by inhibiting the α1-adrenergic receptor-mediated signaling pathway, and participates in hemodynamic regulation under pathological conditions such as inflammation and ischemia. 3-Nitro-L-tyrosine can be used in studies related to atherosclerosis, ischemia-reperfusion and sepsis.
Reference Standards   Reactive Oxygen Species (ROS)   Endogenous Metabolite   Adrenergic Receptor  
Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
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HY-13624AR Epirubicin hydrochloride (Standard)
Epirubicin (hydrochloride) (Standard) is the analytical standard of Epirubicin (hydrochloride). This product is intended for research and analytical applications. Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
Reference Standards   DNA/RNA Synthesis   Topoisomerase   Apoptosis   Antibiotic   FOXP  
Cancer  
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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  
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HY-162946 Alkyne-P60
Alkyne-P60 is a potent 15-mer peptide inhibitor of Foxp3. Alkyne-P60 can bind with Foxp3, hinder its nuclear translocation, and diminish Foxp3-mediated inhibition of NFKB and NFAT functions. Alkyne-P60 is a ligand for target protein for PROTAC (HY-162943).
Ligands for Target Protein for PROTAC   FOXP  
Cancer  
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HY-113248S 3-Nitro-L-tyrosine-d3
3-Nitro-L-tyrosine-d3 is the deuterium labeled 3-Nitro-L-tyrosine (HY-113248). 3-Nitro-L-tyrosine serves as a biomarker of oxidative stress. 3-Nitro-L-tyrosine attenuates the pressor and vasoconstrictive effects of angiotensin II by inhibiting the α1-adrenergic receptor-mediated signaling pathway, and participates in hemodynamic regulation under pathological conditions such as inflammation and ischemia. 3-Nitro-L-tyrosine can be used in studies related to atherosclerosis, ischemia-reperfusion and sepsis.
Endogenous Metabolite  
Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
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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  
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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  
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HY-P11315 MG1 peptide
MG1 peptide is an M1 microglia-targeting peptide with blood-brain barrier permeability. MG1 peptide can be used in studies related to ischemic stroke and cerebral ischemia-reperfusion injury.
Biochemical Assay Reagents  
Neurological, Eye or Ear Disease   Blood or Cardio-cerebrovascular Disease  
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HY-113248S1 3-Nitro-L-tyrosine-13C6
3-Nitro-L-tyrosine-13C6 is the 13C labeled 3-Nitro-L-tyrosine (HY-113248). 3-Nitro-L-tyrosine serves as a biomarker of oxidative stress. 3-Nitro-L-tyrosine attenuates the pressor and vasoconstrictive effects of angiotensin II by inhibiting the α1-adrenergic receptor-mediated signaling pathway, and participates in hemodynamic regulation under pathological conditions such as inflammation and ischemia. 3-Nitro-L-tyrosine can be used in studies related to atherosclerosis, ischemia-reperfusion and sepsis.
Endogenous Metabolite  
Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
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HY-Y1783 2-(Methylamino)ethanol
2-(Methylamino) ethanol (N-Methylethanolamine) is an orally active Phospholipase D inhibitor and analog of Ethanolamine (HY-Y0524). 2-(Methylamino) ethanol reduces the mRNA levels of ACE, ppET-1 and ECE-1, and inhibits MMP-2 activity. 2-(Methylamino) ethanol inhibits Collagen synthesis. 2-(Methylamino) ethanol attenuates ventricular hypertrophy, prevents increased myocardial stiffness and hemodynamic deterioration. 2-(Methylamino) ethanol can capture industrial acid gases and react with carbon dioxide to form carbamates and bicarbonates. 2-(Methylamino) ethanol can be used in studies related to hypertensive heart failure (diastolic heart failure).
Phospholipase   Drug Derivative   Angiotensin-converting Enzyme (ACE)   Endothelin Receptor   MMP   Collagen   Biochemical Assay Reagents  
Hypertension   Heart Failure  
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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  
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HY-N0390S4 L-Glutamine-5-13C
L-Glutamine-5-13C 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  
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HY-P1453A CMD178 TFA
CMD178 TFA is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling and inhibits Treg cell development.
Interleukin Related   STAT   FOXP  
Lung Cancer   Breast Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Obesity  
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HY-159692 AZD8701
AZD8701 (IONIS-1063734) is an antisense oligonucleotide targeting FOXP3 in regulatory T cells (Tregs), with a human IC50 of 65.2 nM. AZD8701 binds to intronic sites of all FOXP3 pre-mRNA isoforms and mediates dose-dependent FOXP3 knockdown via free uptake. AZD8701 can be used in cancer-related research.
FOXP  
Cancer  
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HY-P10275 Tat-NTS peptide
Tat-NTS peptide is a cell-penetrating peptide with neuroprotective effects. Tat-NTS peptide can specifically inhibit the nuclear translocation of ANXA1 and reduce neuronal apoptosis in ischemic areas. Moreover, Tat-NTS peptide can reduce the volume of cerebral ischemic infarction and can be used in the research of ischemic stroke.
Apoptosis  
Neurological, Eye or Ear Disease  
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HY-P5883 TAT-M2NX
TAT-M2NX (tatM2NX) is a selective inhibitor targeting human TRPM2 channels and exerts inhibitory effects on ischemic stroke. TAT-M2NX reduces H2O2-induced calcium influx via TRPM2 channels. After traumatic brain injury in mice, TAT-M2NX preserves hippocampal long-term potentiation, improves memory function, and reduces infarct volume after middle cerebral artery occlusion, but it shows no effect on female mice. TAT-M2NX can be used in studies related to traumatic brain injury and ischemic stroke.
TRP Channel  
Ischemic Stroke  
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HY-135556 Norfluoxetine
Norfluoxetine is the active metabolite of the antidepressant Fluoxetine (HY-B0102); it is also a TREK-2 K2P potassium channel inhibitor. Norfluoxetine exhibits neuroimmunological activity, induces apoptosis in primary microglial cells, and inhibits the release of pro-inflammatory factors. Norfluoxetine inhibits high-threshold voltage-gated Ca2+ currents in neurons with an EC50 of 20.4 μM. Norfluoxetine can be used in research related to depression, ischemic stroke, and epilepsy.

Source: human plasma

Drug Metabolite   Potassium Channel   Calcium Channel   Apoptosis  
Depression   Epilepsy   Ischemic Stroke  
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HY-162943 P60-L3-VHL
P60-L3-VHL is a PROTAC degrader targeting Foxp3. P60-L3-VHL triggers the ubiquitination modification of Foxp3 by conjugating the Foxp3-targeting peptide P60 with the VHL E3 ubiquitin ligase ligand via a long linker, and mediates protein degradation through the proteasome pathway. P60-L3-VHL blocks the nuclear translocation of Foxp3, relieves the transcriptional inhibition of IL2 and IFN-γ, and inhibits the differentiation of iTreg cells. P60-L3-VHL is applicable to cancer-related research.
PROTACs   FOXP   Interleukin Related   IFNAR  
Cancer  
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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  
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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  
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HY-113248 3-Nitro-L-tyrosine
3-Nitro-L-tyrosine serves as a biomarker of oxidative stress. 3-Nitro-L-tyrosine attenuates the pressor and vasoconstrictive effects of angiotensin II by inhibiting the α1-adrenergic receptor-mediated signaling pathway, and participates in hemodynamic regulation under pathological conditions such as inflammation and ischemia. 3-Nitro-L-tyrosine can be used in studies related to atherosclerosis, ischemia-reperfusion and sepsis.
Endogenous Metabolite   Adrenergic Receptor   Reactive Oxygen Species (ROS)  
Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
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HY-P2159 Dynorphin A (1-8)
Dynorphin A (1-8) is a ligand with preference for the κ-opioid receptor, and its IC50 value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke.
Opioid Receptor   Endogenous Metabolite  
Neurological, Eye or Ear Disease  
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HY-76006 3-Hydroxybenzaldehyde
3-Hydroxybenzaldehyde (3-HBA) is a precursor compound for phenolic compounds like Protocatechuic aldehyde (PCA) (HY-N0295). 3-Hydroxybenzaldehyde, produced by 3-hydroxybenzyl-alcohol dehydrogenase, is a substrate of aldehyde dehydrogenase (ALDH) in rats and humans. 3-Hydroxybenzaldehyde has vasculoprotective effects in vitro and in vivo. 3-Hydroxybenzaldehyde is proming for research of atherosclerosis.
Aldehyde Dehydrogenase (ALDH)   NF-κB   p38 MAPK  
Inflammation or Immune System Disease   Atherosclerosis  
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HY-W015777 4-Methoxybenzyl alcohol
4-Methoxybenzyl alcohol (P-Methoxy-benzyl alcoho; (4-Methoxyphenyl) methanol) is a naturally derived volatile aromatic compound. 4-Methoxybenzyl alcohol upregulates the phosphorylation level of PI3K/Akt pathway proteins, downregulates the expression of pro-inflammatory factors, increases the content of tight junction proteins occludin and claudin-5, and alleviates structural damage to the blood-brain barrier. 4-Methoxybenzyl alcohol improves the decrease in viability and NO level of cerebral microvascular endothelial cells induced by oxygen-glucose deprivation/reperfusion, and reduces the release of lactate dehydrogenase. 4-Methoxybenzyl alcohol serves as a substrate in the two-phase persulfate-mediated electro-oxidation system, where it is directionally oxidized to p-anisaldehyde. 4-Methoxybenzyl alcohol acts as a substrate for wild-type fungal aryl alcohol oxidase. 4-Methoxybenzyl alcohol can be used in studies related to ischemic stroke, as well as in research across various fields such as chemical synthesis, including the synthesis of fragrances and flavorings.
Drug Intermediate   Interleukin Related   TNF Receptor   Claudin   Akt   NO Synthase  
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HY-N2125 Parishin C
Parishin C is a brain-penetrant major bioactive component found in Gastrodia elata Blume. Parishin C is a 5-HT1A receptor agonist with an EC50 of 34 nM. Parishin C has antipsychotic and neuroprotective effects. Parishin C protects against Aβ-induced long-term potentiation damage and NMDA receptor current impairment. Parishin C reduces oxidative stress, pro-inflammatory cytokine levels, caspase activity, brain water content, and cerebral infarct volume; increases antioxidant enzyme activity and BDNF levels; improves nerve function and histopathological brain damage. Parishin C attenuates phencyclidine-induced immobility time increases, sociability deficits, and visual recognition memory impairment. Parishin C can be used for the research of ischemic stroke, Alzheimer's disease, and schizophrenia-like psychosis.
5-HT Receptor   iGluR   Caspase   Interleukin Related   TNF Receptor   SOD   NF-κB  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
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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  
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HY-111485 Ertabresib
Ertabresib (INCB-057643) is an orally active BET protein inhibitor. Ertabresib blocks gene transcription by targeting the BET protein family, induces cell cycle arrest and apoptosis by downregulating proto-oncogenes such as c-MYC, and additionally reduces the expression of FOXP3 and PD-L1 to improve the immune microenvironment. It also exerts synergistic effects and overcomes drug resistance when combined with chemotherapy and XPO1 inhibitors. Ertabresib can be used in research related to high-grade B-cell lymphoma with MYC and BCL2 rearrangements, pancreatic cancer, pancreatitis, and metastatic castration-resistant prostate cancer.
Epigenetic Reader Domain   Apoptosis   c-Myc   FOXP   PD-1/PD-L1  
Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer  
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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-110281 Dehydroascorbic acid
Dehydroascorbic acid is an oxidized form of vitamin C that can cross the blood-brain barrier (BBB). Dehydroascorbic acid clears cytotoxic reactive oxygen species (ROS) produced after ischemic stroke by converting to ascorbic acid (AA), thereby reducing neuronal and glial cell damage and stabilizing cerebral microvascular NO signaling to maintain perfusion in the ischemic area. Dehydroascorbic acid can be used in research on ischemic stroke.
Endogenous Metabolite  
Ischemic Stroke  
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Keywords

carotid atherosclerosis | immune microenvironment | single-cell transcriptomics | plaque vulnerability | hemodynamics | ischemic stroke