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Molecular links between heart failure and disease

Heart failure is a syndrome in which impaired filling or ejection prevents the heart from meeting circulatory demands without elevated pressures. Its molecular links to other diseases are bidirectional: ischemia, obesity, diabetes, aging, kidney or lung disease, and systemic inflammation alter myocardial metabolism and microvascular function, while failing hearts reshape immune, metabolic, and hematopoietic systems. Heart failure with preserved ejection fraction is especially connected to cardiometabolic comorbidity. Obesity, diabetes, chronic obstructive pulmonary disease, and salt-sensitive hypertension can produce systemic inflammation, coronary microvascular endothelial dysfunction, and diastolic stiffening even when systolic ejection remains preserved Heart failure thus reflects a network disease in which comorbid organs continuously alter cardiac load, substrate availability, endothelial signaling, and immune-cell recruitment[1][2].

At the myocardial interface, inflammation and fibrosis communicate through defined cellular niches. Single-cell, spatial, and chromatin analyses of human hearts identify CCR2-positive macrophage IL-1β signaling as a driver of FAP- and POSTN-positive fibroblast states. BRD4-dependent enhancers regulate macrophage IL1B expression, and fibroblast RELA activates a profibrotic MEOX1 program. Disrupting IL-1 signaling in either compartment reduces fibroblast activation, fibrosis, and dysfunction in experimental models. In cardiometabolic HFpEF, reduced endothelial nitric oxide lowers cyclic GMP and protein kinase G activity, leaving titin hypophosphorylated, cardiomyocytes stiff, and interstitial fibrosis increased. These mechanisms connect systemic comorbidity to cell-specific cardiac remodeling The macrophage-fibroblast niche provides a tractable example of a systemic inflammatory signal becoming a spatially restricted profibrotic transcriptional program[1][2][3][4].

Immunometabolism broadens the link. Ischemic or metabolic stress recruits innate and adaptive immune cells whose glycolysis, oxidative phosphorylation, and substrate use determine inflammatory or reparative states. Those cells alter cardiomyocyte, fibroblast, and systemic metabolism, while bone-marrow and extramedullary myelopoiesis sustain nonresolving recruitment. Obesity adds adipose dysfunction, lipotoxicity, insulin resistance, mitochondrial calcium disturbance, oxidative stress, impaired autophagy, and microvascular disease. Therapeutic applications therefore include metabolic drugs, weight reduction, microvascular support, IL-1 pathway intervention, anti-fibrotic strategies, and restoration of cardiac fuel flexibility. Ketone bodies may provide mitochondrial substrate and signaling effects on inflammation, fibrosis, angiogenesis, and vasodilation, but their mechanisms and clinical value remain under study Metabolic therapies may improve both cardiomyocyte fuel supply and immune-cell phenotype, but these two mechanisms should be measured separately in clinical studies[3][4][5][6].

The key gap is heterogeneity. Broad anti-inflammatory treatment has not consistently improved HFpEF outcomes, indicating that inflammation is not a single target and may be protective during repair. Future trials should phenotype ventricular function, comorbidities, immune-cell state, fibrosis, microvascular dysfunction, and substrate metabolism before intervention. Biomarkers must identify the active macrophage-fibroblast or endothelial pathway and confirm target engagement. Human organ-level endpoints should include symptoms, exercise capacity, hospitalization, renal function, rhythm, and survival rather than fibrosis markers alone. Experimental models should reproduce the age and multimorbidity of patients. Molecularly informed treatment will require connecting a disease driver—such as obesity, ischemia, or clonal inflammation—to a defined cardiac cell circuit and testing whether interrupting that circuit improves both heart failure and its systemic context Phenotype-specific combinations could address load, metabolism, microvascular dysfunction, inflammation, and fibrosis, whereas undirected polypharmacy risks treating correlated markers without correcting the dominant driver[1][5][6][7].

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Cat. No. Product Name Information Application Publication
HY-18739 Phorbol 12-myristate 13-acetate
Phorbol 12-myristate 13-acetate (PMA; TPA; Phorbol myristate acetate), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator. Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells (Validated by MedChemExpress).
860
HY-10071 Y-27632
Y-27632 is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade.
602
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.
536
HY-13453 BAY 11-7082
BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
507
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.
309
HY-10227 Bortezomib
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM). Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs).
278
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

178
HY-13982 JSH-23
JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation.
162
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.
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.
147
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.
138
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.
114
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.
103
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.
98
HY-100487 TAK-243
TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
96
HY-B0673 Pirfenidone
Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities.
96
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.
87
HY-L020 Wnt/Hedgehog/Notch Compound Library
The developmental proteins Hedgehog, Notch and Wnt are key regulators of cell fate, proliferation, migration and differentiation in several tissues. Their related signaling pathways are frequently activated in tumors, and particularly in the rare subpopulation of cancer stem cells. The Wnt signaling pathway is a conserved pathway in animals. Deregulated Wnt signaling has catastrophic consequences for the developing embryo and it is now well appreciated that defective Wnt signaling is a causative factor for a number of pleiotropic human pathologies, including cancer. Hedgehog signaling pathway is linked to tumorigenesis and is aberrantly activated in a variety of cancers. The Notch signaling pathway is a highly conserved cell signaling system present in most animals. It plays an important role in cell-cell communication, and further regulates embryonic development. MCE designs a unique collection of 654 Wnt/Hedgehog/Notch signaling pathway-related small molecules. Wnt/Hedgehog/Notch Compound Library serves as a useful tool for stem cell research and anti-cancer drug screening.
86
HY-L013 Neuronal Signaling Compound Library
Neuronal Signaling is involved in the regulation of the mechanisms of the central nervous system (CNS) such as its structure, function, genetics and physiology as well as how this can be applied to understand diseases of the nervous system. Every information processing system in the CNS is composed of neurons and glia, neurons have evolved unique capabilities for intracellular signaling (communication within the cell) and intercellular signaling (communication between cells). G protein-coupled receptors (GPCRs), including 5-HT receptor, histamine receptor, opioid receptor, etc. are the largest class of sensory proteins and are important therapeutic targets in Neuronal Signaling. Besides, Notch signaling, such as β- and γ-secretase, also plays multiple roles in the development of the CNS including regulating neural stem cell (NSC) proliferation, survival, self-renewal and differentiation. GPCR dysfunction caused by receptor mutations and environmental challenges contributes to many neurological diseases. Notch signaling in neurons, glia, and NSCs is also involved in pathological changes that occur in disorders such as stroke, Alzheimer's disease and CNS tumors. Thus, targeting Neuronal Signaling, such as notch signaling and GPCRs, can be used as therapeutic interventions for several different CNS disorders. MCE designs a unique collection of 3,961 Neuronal Signaling-related compounds that act as a useful tool for the research of neuronal regulation and neuronal diseases.
84
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.
84
HY-L149 Membrane Protein-targeted Compound Library
A membrane protein is a protein molecule that is attached to or associated with the membrane of a cell or an organelle. Membrane proteins can be classified into two groups based on how the protein is associated with the membrane: integral membrane proteins and peripheral membrane proteins. In humans, about 30% genome encodes membrane proteins. Membrane proteins perform a variety of functions vital to the survival of organisms, for example, signal transduction, molecules or ion transportation, enzymatic catalysis, and intercellular communication. Membrane proteins also play important roles in drug discovery. As reported, more than 60% of current drug targets are membrane proteins. MCE supplies a unique collection of 7,999 compounds targeting a variety of membrane proteins. MCE Membrane Protein-targeted Compound Library can be used for membrane protein-focused screening and drug discovery.
84
HY-L087 Anti-Obesity Compound Library
Obesity is widely recognized as the largest and fastest growing public health problem and is associated with numerous chronic disorders including osteoarthritis, obstructive sleep apnea, gallstones, fatty liver disease, reproductive and gastrointestinal cancers, dyslipidemia, hypertension, type 2 diabetes, heart failure, coronary artery disease, stroke, etc. Although obesity has long been associated with serious health issues, it has only recently been regarded as a disease in the sense of being a specific target for medical therapy. Obesity may be viewed as the dysregulation of two physiological functions, appetite regulation and energy metabolism, which combine to create disordered energy balance. Consequently, developing obesity treatments that target novel pathways is a growing focus for both biopharmaceutical industries. MCE Anti-Obesity Compound Library owns a unique collection of 3,741 compounds, which mainly target signaling pathway of controlling appetite, fatty acid metabolism and energy expenditure, etc. This library is a useful tool for discovery anti-obesity drugs.
83
HY-L132 Chemokine Compound Library
Chemokines, or chemotactic cytokines, are small cytokines or signaling proteins secreted by cells. They are a component of intercellular communication, controlling the directional movement of immune cells especially leukocytes, as well as other cell types, for instance, endothelial and epithelial cells, which are essential to maintain human health and the function of the immune system. The biological effects of chemokines are achieved by binding to chemokine receptors, which are G protein-coupled receptors found on the surface of leukocytes. Some chemokine receptors are involved in directing tumor metastasis and over-expression by certain tumors. So inhibiting the interaction between chemokine and chemokine receptors on the surface of tumor cells may be a new possible therapeutic approach. Some chemokine receptors are coreceptors for HIV entry, and related inhibitors have been approved by the FDA to treat patients with HIV. Obviously, chemokines and chemokine receptors have become new targets for studying cancer, HIV, inflammation, and other diseases. MCE supplies a unique collection of 257 chemokine or chemokine receptor inhibitors and activators, all of which have the identified inhibitory or activated effect on chemokine or chemokine receptors. MCE Chemokine Library is a useful tool for drug research related to cancer, AIDS, and wound therapy.
83
HY-L150 Membrane Receptor-targeted Compound Library
Membrane receptors, also known cell surface receptors or transmembrane receptors, are transmembrane proteins embedded into the plasma membrane which play an essential role in maintaining communication between the internal processes within the cell and various types of extracellular signals. They act in cell signaling by receiving (binding to) extracellular molecules, which are also called ligands. These extracellular molecules include hormones, cytokines, growth factors, neurotransmitters, lipophilic signaling molecules such as prostaglandins, and cell recognition molecules. There are three kinds of membrane receptors: ion channel-linked receptors, enzyme-linked receptors and G-protein-linked receptors. They play important roles in keeping human normal physiologic processes. GPCRs and ion channels are important drug targets in drug discovery. MCE provides a unique collection of 7,133 compounds targeting a variety of membrane receptors. MCE Membrane reeptor-targeted Compound Library can be used for membrane receptor-focused screening and drug discovery.
83
HY-L168 Extracellular Vesicles (EVs) Compound Library
Extracellular vesicles (EVs) are small membrane binding structures that are released from cells into the surrounding environment and play a crucial role in mediating and regulating intercellular communication related to physiological and pathological processes. EVs are lipid membrane vesicles composed of proteins, lipids, and nucleic acids. EVs can be divided into several types based on their source, such as extracellular vesicles, microcapsules, and apoptotic vesicles. The size range of exosomes is 30-150nm, which are endocrine in multi vesicular endosomes (MVEs); microvesicles (50-1000nm) are secreted directly through extracellular interactions, thereby releasing plasma membrane vesicles. In contrast, apoptotic bodies are usually larger, ranging in size from 1 to 5 μ m. This is generated during programmed cell death. EV plays a crucial role in transmitting information between cells and influencing the behavior and function of receptor cells. MCE designs a unique collection of 707 small molecules related to extracellular vesicles (EVs). It is a good tool to be used for research on metabolize, cancer and other diseases.
83
HY-L185 Anti-Fibrosis Compound Library
Fibrosis is a kind of repair response to long-term tissue damage, which is mainly manifested by excessive deposition of extracellular matrix (ECM) and scar formation. Myofibroblasts are the main generating cells of extracellular matrix, and their activation process is related to various pathological mechanisms including Oxidative stress, chronic inflammation and cytokine secretion. Fibrosis can occur in many organs, such as kidneys, liver, heart, lungs, etc. Continuous fibrosis can lead to the destruction of the normal structure of tissues and organs, and if not controlled in time, may cause organ failure or even life-threatening. MCE contains 2,568 compounds targeting ant-fibrosis targets such as TGF-β, PI3K, Wnt, MMP, etc. These compounds have clear or potential anti-fibrosis activity and can be used for mechanism research and drug screening of fibrosis diseases.
83
HY-L227 Amino Acid Metabolite Compound Library
Amino acids are the fundamental components that sustain life activities, playing roles in ATP generation, promoting nucleotide synthesis, and maintaining cellular redox balance. Moreover, dysregulation of amino acid consumption is a significant potential regulatory mechanism leading to impaired anti-tumor immunity in immune cells. The normal functioning of immune cells relies on amino acid metabolic pathways to obtain energy and materials, and upon activation, they reprogram their metabolism to support growth, proliferation, and effector functions. Additionally, metabolic disorders of specific amino acids (such as branched-chain amino acids, glutamine, and arginine) can exacerbate mitochondrial dysfunction and oxidative stress, thereby promoting myocardial fibrosis and cardiac cell damage. Therefore, conducting research related to amino acid metabolism holds promise for discovering potential drugs for diseases related to cancer, immunity, and metabolism. MCE can provide 195 kinds of metabolites of amino acid metabolic pathways, which can be used for drug screening in various diseases such as cancer, immune disorders, metabolic diseases, mitochondrial-targeted diseases
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.
83
HY-L923 Ion Channel Lead-like Compound Library
Ion channels are key proteins on the cell membrane that regulate the flow of ions across membranes. They participate in nearly all physiological processes, including nerve conduction, muscle contraction, heart rhythm, and pain perception. Abnormalities in their function can lead to various serious diseases such as arrhythmia, epilepsy, hypertension, neuropathic pain, and cancer. Therefore, ion channels are highly valuable drug targets—over 15% of approved drugs target ion channels currently, demonstrating their irreplaceable therapeutic value in cardiovascular, neurological, and analgesic fields. MCE has collected a library of over 5,000 reported ion channel-related bioactive compounds targeting major sites such as Na+ channels, K+ channels, Ca2+ channels, GABA receptors, iGluRs, and others. Using AI models, these compounds are characterized through both 2D representations (molecular fingerprints, pharmacophores) and 3D representations (3D conformation) to screen for a collection of lead-like compounds highly similar to known active molecules. Additionally, an hERG channel prediction algorithm integrating XGB and ISE mapping strategy is employed to assess and exclude potential cardiotoxicity in the library.. This step significantly reduces safety risks in subsequent screenings, particularly for ion channel drug development related to cardiovascular systems (e.g., Nav1.5, Cav1.2), effectively minimizing failures due to hERG inhibition and serving as a valuable tool for ion channel drug screening.
83
HY-L926 Cysteine Protease Focused Covalent Library
Cysteine proteases (CPs), a key enzyme family regulating physiological metabolism and mediating pathological processes (e.g., abnormal bone resorption, tumour invasion, and pathogen infection), represent a core therapeutic target for disease intervention via the development of specific inhibitors. Currently reported CP covalent inhibitors encompass diverse structural types, including epoxides, aziridine, and activated double bonds (vinyl sulphones, α,β-unsaturated ketones), providing clear structural references for the development of novel CP covalent inhibitors. This compound library contains multiple warheads that specifically target cysteine proteases, serving as a powerful tool for the efficient discovery of novel covalent inhibitors against this enzyme family.
83
HY-32735 Triptolide
Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor.
76
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.
73
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

68
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.
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.
61
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.
61
HY-13004 Maraviroc
Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.
60
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

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.
50
HY-15027 5-Aminosalicylic Acid
5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
43
HY-15418 RS 504393
RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).
33
HY-128643 FAPI-4
FAPI-4 is a potent fibroblast activation protein (FAP) inhibitor for the targeting FAP. FAPI-4 can be used in cancer research. 68Ga-FAPI-4 PET/CT is a promising new diagnostic method for imaging various kinds of cancer, with good tumor-to-background contrast ratios.
FAP  
32
HY-50674 INCB3344
INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
30
HY-B0498 Bindarit
Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8, and no effect on other CC and CXC chemokines such as MIP-1α/CCL3, MIP-1β/CCL4, MIP-3/CCL23. Bindarit also has anti-inflammatory activity.
29
HY-12080 BX471
BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a Ki of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
29
HY-18611A Abaucin
RS102895 is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.
28
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.
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).
17
HY-N2329 Piperlongumine
Piperlongumine is a alkaloid, possesses ant-inflammatory, antibacterial, antiangiogenic, antioxidant, antitumor, and antidiabetic activities. Piperlongumine induces ROS, and induces apoptosis in cancer cell lines. Piperlongumine shows anti-cardiac fibrosis activity, suppresses myofibroblast transformation via suppression of the ERK1/2 signaling pathway. Piperlongumin could be used in the study of migrasome.
16
HY-113071 Mevalonic acid
Mevalonic acid (MVA) is a precursor substance of the mevalonate pathway, which is essential for cell growth and proliferation. Mevalonic acid is effective in inhibiting Simvastatin (HY-17502)-induced decrease in C2C12 cell viability in vitro. Mevalonic acid can be used in studies of myopathy and heart failure.
13
HY-17367 Atazanavir
Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.
13
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.
13
HY-113071A Mevalonic acid lithium salt
Mevalonic acid (MVA) lithium salt is a precursor substance of the mevalonate pathway, which is essential for cell growth and proliferation. Mevalonic acid lithium salt is effective in inhibiting Simvastatin (HY-17502)-induced decrease in C2C12 cell viability in vitro. Mevalonic acid lithium salt can be used in studies of myopathy and heart failure.
13
HY-111784 Inobrodib
Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression.
13
HY-108915 Trimethylamine N-oxide dihydrate
Trimethylamine N-oxide dihydrate is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide dihydrate induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide dihydrate also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.
12
HY-116084 Trimethylamine N-oxide
Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.

Source: Host intestinal bacteria

12
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

9
HY-D2295 Mito-FerroGreen
Mito-FerroGreen is a mitochondria-specific Fluorescent indicator used to detect mitochondrial Fe2+ levels (excitation: 488 nm; emission: 500-550 nm). Mito-FerroGreen can be applied to research related to colorectal cancer and chronic heart failure.
7
HY-147057 Rofapitide tetraxetan
Rofapitide tetraxetan (FAP-2286) is a potent and selective FAP-binding peptide with a mean IC50 value of 2.7 nM for binding to FAP. Rofapitide tetraxetan can be labeled with radionuclides for diagnostic applications. Rofapitide tetraxetan has antitumor activity.
FAP  
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.
6
HY-101801 Ac-Gly-BoroPro
Ac-Gly-BoroPro is a selective FAP inhibitor with a Ki of 23 nM.
FAP  
Cancer  
5
HY-D0098 Fluorescein-5-maleimide
Fluorescein-5-maleimide (N-(5-Fluoresceinyl)maleimide) is a fluorescent dye. Fluorescein-5-maleimide can be used to detect the redox state of thiols in eukaryotic cells. Fluorescein-5-maleimide can label peptides and is used to detect negatively charged nanoparticles. Fluorescein-5-maleimide can also label actin to explore its interaction with cardiac myosin-binding protein C (cMyBP-C), which helps in developing small molecule modulators for heart failure. Fluorescein-5-maleimide can screen mutant proteins that contain cysteine residues. The excitation wavelength of Fluorescein-5-maleimide is 494 nm, and the emission wavelength is 519 nm.
5
HY-N0617 Sanggenon C
Sanggenon C, a flavonoid, exerts protective effects against cardiac hypertrophy and fibrosis via suppression of the calcineurin/NFAT2 pathway. Sanggenon C inhibits mitochondrial fission to induce apoptosis by blocking the ERK signaling pathway. Sanggenon C inhibits inducible nitric oxide synthase expression in RAW264.7 cells, and TNF-α-stimulated cell adhesion and VCAM-1 expression, by suppressing NF-κB activity. Sanggenon C possesses antioxidant, anti-inflammatory and antitumor activities.
4
HY-151435 CCR6 antagonist 1
CCR6 antagonist 1 is a CCR6 antagonist that inhibits the CCL20/CCR6 axis. CCR6 antagonist 1 can be used in the research of autoimmune-mediated inflammatory diseases, such as inflammatory bowel diseases (IBDs).
4
HY-112537A D-Glucose 6-phosphate dipotassium
D-Glucose 6-phosphate dipotassium is a key central node metabolite in glucose metabolism. It serves as the initiating metabolite for glycolysis and the pentose phosphate pathway, as well as a substrate for glycogen synthesis. D-Glucose 6-phosphate dipotassium acts as a metabolic stress signal, which activates the mTOR pathway to promote protein synthesis, especially when phosphoglucose isomerase (PGI) is inhibited, thereby participating in cardiac remodeling processes. D-Glucose 6-phosphate dipotassium can be used in research related to non-insulin-dependent diabetes mellitus and heart failure.
3
HY-P2141A TRV-120027 TFA
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling. TRV120027?TFA induces?acute?catecholamine?secretion?through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the?acute decompensated heart failure (ADHF) treatment.
3
HY-P2141 TRV-120027
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages β-arrestins while blocking G-protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R-β-arrestin-1-TRPC3-PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II-mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment.
3
HY-137331 Linofapib bentoxetan
FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted tracer. Use radioactivity FAPI-46 labeled with 68Ga or 177Lu can be used for tumor imaging in a variety of cancers and has higher tumor uptake rates and longer tumor accumulation.
3
HY-112197 PKG drug G1
PKG agent G1 targets C42 of PKG. PKG agent G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.
2
HY-P1292 PKG inhibitor peptide
PKG inhibitor peptide is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM.
PKG  
Cancer  
2
HY-N6884 Bixin
Bixin is an orally active carotenoid found in the seeds of Bixa orellana. Bixin induces apoptosis in cancer cells. Bixin possessing anti-inflammatory, anti-tumor and anti-oxidant activities. Bixin treatment ameliorated cardiac dysfunction through inhibiting fibrosis, inflammation and reactive oxygen species (ROS) generation.
2
HY-P2692B DT-2 acetate
DT-2 is a potent and selective inhibitor of the cGMP-dependent protein kinase (PKG). DT-2 inhibits PKG catalyzed phosphorylation (Ki: 12.5 nM).
PKG  
Cancer  
2
HY-Y0248A Farnesol
Farnesol is a sesquiterpene alcohol that modulates cell-to-cell communication in Candida albicans, and has the activity in inhibiting bacteria.
2
HY-100684 UAMC-1110
UAMC-1110 is a highly potent and selective inhibitor of fibroblast activation protein (FAP) with an IC50 of 3.2 nM. UAMC-1110 also inhibits prolyl oligopeptidase (PREP) with an IC50 of 1.8 μM.
2
HY-P72153 CCN2/CTGF Protein, Human (His)
CCN2/CTGF Protein, secreted by vascular endothelial cells, crucially promotes chondrocyte proliferation and differentiation, and mediates heparin- and divalent cation-dependent cell adhesion in diverse cell types. Additionally, it enhances fibroblast growth factor-induced DNA synthesis while existing as a monomer and interacting with TSKU. CCN2/CTGF Protein, Human (His) is the recombinant human-derived CCN2/CTGF protein, expressed by E. coli , with N-6*His labeled tag.

Species: Human; Source: E. coli

2
HY-P72154 CCN2/CTGF Protein, Mouse (GST)
CCN2/CTGF protein is a major connective tissue mitochondrial attractant secreted by vascular endothelial cells and promotes chondrocyte proliferation and differentiation. It mediates heparin- and divalent cation-dependent cell adhesion in various cell types, including fibroblasts, myofibroblasts, endothelial cells, and epithelial cells. CCN2/CTGF Protein, Mouse (GST) is the recombinant mouse-derived CCN2/CTGF protein, expressed by E. coli , with N-GST labeled tag.

Species: Mouse; Source: E. coli

2
HY-E70182 Hyaluronidase 2
Hyaluronidase 2 (EC:3.2.1.35; HYAL2) is a hyaluronidase. Hyaluronidase 2 cleaves high-molecular-weight hyaluronan into intermediate, ~20 kDa, and tetrasaccharide fragments. Hyaluronidase 2 directly interacts with CD44 and ERM proteins, reduces CD44 hyaluronan binding capacity and ERM activation. Hyaluronidase 2 can be used for the research of gliomas, inflammatory bowel disease, congenital heart defects, heart failure.
1
HY-P990247 Anti-Mouse E-selectin/CD62E Antibody (9A9)
Anti-Mouse E-selectin/CD62E Antibody (9A9) is an anti-mouse E-selectin/CD62E IgG2b monoclonal antibody. Anti-Mouse E-selectin/CD62E Antibody (9A9) has an inhibitory effect on cancer cell colonization. Anti-Mouse E-selectin/CD62E Antibody (9A9) can be used for researches on inflammation conditions and cancer such as acute microvascular inflammation and breast cancer.

Species: Mouse

1
HY-P99177 Enibarcimab
Enibarcimab is a humanized, non-neutralizing monoclonal antibody targeting adrenomedullin (ADM). Enibarcimab binds to the N-terminus of ADM, retains ADM in the circulation, and mobilizes interstitial ADM to increase the level of active bio-ADM, ultimately stabilizing blood vessels. Enibarcimab can be used in research related to septic shock and acute heart failure.

Species: Human

1
HY-N2263 Skimmin
Skimmin (Umbelliferone glucoside) is a major pharmacologically active and orally active molecule present in Hydrangea paniculata, a medical herb used in traditional Chinese medicine as an anti-inflammatory agent. Skimmin has renal protective activity. Skimmin can improve creatinine clearance, and reduce plasma creatinine, and kidney injuries. Skimmin has good anti-amoebic activity against the HM1:IMMS strain of Entamoeba histolytica. Skimmin has anti-cancer and neuroprotective activities. Skimmin reduces cardiac fibrosis as well as decreasing TNF-α, IL-6, IL1β, and TGFβ1 in cardiac tissues. Skimmin can be studied in research for diabetes and diabetes-related diseases.
1
HY-N0657 Pinoresinol Diglucoside
Pinoresinol Diglucoside is an orally active lignan with multifunctional bioactivity. Pinoresinol Diglucoside interacts with targets including ALB, HIF1A, GSK3B, BCL2, MARK3, IL6, NF-κB p65, Nrf2, HO-1, and TLR4, and modulates pathways including PI3K-Akt, estrogen, MAPK, Rap1, AKT/mTOR/NF-κB, and TGF-β1/Smads. Pinoresinol Diglucoside regulates osteogenesis, bone resorption, oxidative stress, inflammation, apoptosis, ferroptosis, ferritinophagy, cardiac fibrosis, and vasorelaxation. Pinoresinol Diglucoside can be used for the research of osteoporosis, ischemia/reperfusion-induced brain injury, Alzheimer’s disease, myocardial ischemia-reperfusion injury, chondrodysplasia, diabetic cardiomyopathy, cardiac hypertrophy, hypertension, cisplatin-induced hearing loss, atherosclerotic cardiovascular diseases, and disuse osteoporosis.
1
HY-116084S Trimethylamine N-oxide-d9
Trimethylamine N-oxide-d9 is the deuterium labeled Trimethylamine N-oxide. Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.
1
HY-113168 Butyrylcarnitine
Butyrylcarnitine is an endogenous metabolite found in plasma. Elevated levels of Butyrylcarnitine are closely associated with abnormalities in lipid and energy metabolism. Butyrylcarnitine can serve as a diagnostic and prognostic indicator for certain diseases, such as heart failure and head and neck cancer.
1
HY-145983 Suc-Gly-Pro-AMC
Suc-Gly-Pro-AMC is a fluorescent substrate. Suc-Gly-Pro-AMC is a fibroblast activation protein (FAP) specific substrate. Suc-Gly-Pro-AMC reacts with recombinant porcine prolyl oligopeptidase. Suc-Gly-Pro-AMC can be used to study the activity of FAP, prolyl endopeptidase (PREP). Suc-Gly-Pro-AMC is used in glioma research.
1
HY-P99269 Sibrotuzumab
Sibrotuzumab (BIBH 1) is a humanized IgG1 monoclonal antibody targets fibroblast activation protein (FAP). Sibrotuzumab can be used for the research of colorectal cancer and non-small cell lung cancer (NSCLC).

Species: Human

1
HY-P3719 MOG(35-55) amide, mouse, rat
MOG (35-55) amide, mouse, rat the terminal amidation form of the 35-55 fragment of the myelin oligodendrocyte glycoprotein (MOG) immunogenic peptide (MOG (35-55) (HY-P1240)). MOG(35-55) amide, mouse, rat can be used for experimental autoimmune encephalomyelitis (EAE) modeling.
1
HY-P70106 CCN2/CTGF Protein, Human (HEK293)
CCN2/CTGF (Connective Tissue Growth Factor) is a protein produced primarily by endothelial cells in blood vessels. It plays an important role in various cellular processes. CCN2/CTGF Protein, Human (HEK293) is the recombinant human-derived CCN2/CTGF protein, expressed by HEK293 , with tag free.

Species: Human; Source: HEK293

1
HY-P70602 CCN2/CTGF Protein, Human (HEK293, Fc)
CCN2/CTGF (Connective Tissue Growth Factor) is a protein produced primarily by endothelial cells in blood vessels. It plays an important role in various cellular processes. CCN2/CTGF Protein, Human (HEK293, Fc) is the recombinant human-derived CCN2/CTGF protein, expressed by HEK293 , with C-hFc labeled tag.

Species: Human; Source: HEK293

1
HY-P78104 CCN2/CTGF Protein, Human (Biotinylated, HEK293, His-Avi)
CCN2/CTGF (Connective Tissue Growth Factor) is a protein produced primarily by endothelial cells in blood vessels. It plays an important role in various cellular processes. CCN2/CTGF Protein, Human (Biotinylated, HEK293, His-Avi) is the recombinant human-derived CCN2/CTGF protein, expressed by HEK293 , with C-Avi, C-His labeled tag.

Species: Human; Source: HEK293

1
HY-116084S1 Trimethylamine-N-oxide-13C3
Trimethylamine-N-oxide-13C3 is the 13C-labeled Trimethylamine N-oxide. Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.
/
HY-B0592S Trandolapril-d5
Trandolapril-d5 is a deuterium labeled Trandolapril (RU44570). Trandolapril is an orally active angiotensin converting enzyme (ACE) inhibitor for hypertension and congestive heart failure (CHF).
/
HY-12879G IWP-4 (GMP)
IWP-4 (GMP) is the GMP-grade form of IWP-4 (HY-12879). IWP-4 is a Wnt inhibitor with an IC50 of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC50 of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC50 = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure.
/
HY-W016773S 1,10-Decanediol-d20
1,10-Decanediol-d20 is the deuterium labeled 1,10-Decanediol. 1,10-Decanediol is a diol compound that can react with α-ketoglutarate (aKG) to generate polymeric microparticles (termed paKG MPs) for the sustained release of aKG, thereby promoting immunosuppressive regulation. Additionally, paKG MPs can bind to dendritic cells (DCs), reducing their glycolysis and mitochondrial respiration in vitro. These metabolic changes lead to the modulation of MHC-II and CD86 expression in DCs and alter the frequency of regulatory T cells (Tregs) as well as T-helper type 1/2/17 cells in vitro. 1,10-Decanediol can be used in research within the field of immunometabolism. can be used as a surfactant/stabilizer in the synthesis of nanomaterials.
/
HY-145581S Mitiperstat-d3
Mitiperstat-d3 (AZD4831-d3) is the deuterated -labeled Mitiperstat (HY-145581).Mitiperstat (AZD4831) is an effective oral inhibitor of myeloperoxidase (MPO). Mitiperstat inhibits MPO and thyroid peroxidase (TPO) with IC50s of 1.5 nM and 0.69 μM. Mitiperstat exhibits a weak inhibitory activity against CYP3A4 with an IC50 of 6 μM. Mitiperstat can reduce inflammation and improve microvascular function, and it can be used in studies related to heart failure, preserved or mildly reduced ejection fraction, non-alcoholic fatty liver disease, and chronic obstructive pulmonary disease.
/
HY-15407S3 Sacubitril-13C4
Sacubitril-13C4 (AHU-377-13C4) is a 13C-labeled version of Sacubitril (HY-15407). Sacubitril is an orally active inhibitor of neprilysin NEP (IC50=5 nM). Sacubitril is used in research on heart failure, hypertension and COVID-19.
/
HY-P2687 Ularitide
Ularitide (Urodilatin), natriuretic peptide, is a vasodilator. Ularitide binds to and activates renal receptors. Ularitide also regulates renal dopamine metabolism Ularitide can be used in the research of heart failure.
/
HY-120521 Urodilatin
Urodilatin is an analogue of ANF-(99-126). Urodilatin is a diuretic-natriuretic regulatory peptide. Urodilatin can be used for research of acute renal failure, congestive heart failure, and bronchial asthma, etc.
/
HY-N15743 Anti-Heart Failure Agent 2
Anti-Heart Failure Agent 2 (Compound 1) is an anti-heart failure agent with anti-inflammatory activity found in processed Cornus officinalis. Anti-Heart Failure Agent 2 inhibits NO release in LPS-induced RAW264.7 cells. Anti-Heart Failure Agent 2 alleviates myocardial ischemia-reperfusion injury, reduces myocardial infarction size, and improves myocardial histopathological changes. Anti-Heart Failure Agent 2 is promising for research of heart failure.
/
HY-N7764 Tellimagrandin I
Tellimagrandin I is a gap junction protein 43 (Cx43) activator, which is a hydrolyzable ellagitannin (ellagitannin) secondary metabolite extractable from various plants. Tellimagrandin I mainly restores gap junction intercellular communication (GJIC) and induces S-phase arrest in tumor cells by upregulating Cx43; activates inflammatory cells to release TNF-α and VEGF to promote angiogenesis in vivo; and protects DNA from damage via antioxidant and metal chelating effects. Tellimagrandin I can be used in research related to human cervical cancer.
/
HY-P11197 ACT1
ACT1 is a peptide that targets endogenous Cx43 by stabilizing its activity at gap junctions. ACT1 stabilizes gap junction intercellular communication in breast cancer cells. ACT1 enhances the activity of Tamoxifen (HY-13757A) and Lapatinib (HY-50898) in breast cancer. ACT1 can be used for breast cancer research.
/
HY-D1777 Pyrromethene 605
Pyrromethene 605 (PM605) is a green-fluorescent polar tracer dye. It is used for investigations of membrane fusion, lysis, and gap-junctional communication and to detect volume changes in cells or liposomes.
/
HY-N15744 Anti-Heart Failure Agent 3
Anti-Heart Failure Agent 3 (Compound 2) is an anti-heart failure agent with anti-inflammatory activity found in processed Cornus officinalis. Anti-Heart Failure Agent 3 inhibits NO release in LPS-induced RAW264.7 cells. Anti-Heart Failure Agent 3 alleviates myocardial ischemia-reperfusion injury, reduces myocardial infarction size, and improves myocardial histopathological changes. Anti-Heart Failure Agent 3 is promising for research of heart failure.
/
HY-B0252S3 Hydrochlorothiazide-15N2,13C,d2
Hydrochlorothiazide-15N2,13C,d2 is 15N and deuterated labeled Hydrochlorothiazide (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.
/
HY-N15745 Anti-Heart Failure Agent 4
Anti-Heart Failure Agent 4 (Compound 3) is an anti-heart failure agent with anti-inflammatory activity found in processed Cornus officinalis. Anti-Heart Failure Agent 4 inhibits NO release in LPS-induced RAW264.7 cells. Anti-Heart Failure Agent 4 alleviates myocardial ischemia-reperfusion injury, reduces myocardial infarction size, and improves myocardial histopathological changes. Anti-Heart Failure Agent 4 is promising for research of heart failure.
/
HY-W722562 Trimethylamine oxide-15N
Trimethylamine oxide-15N is the deuterium labeled Trimethylamine N-oxide (HY-116084). Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.
/
HY-P11041 VS-IP1
VS-IP1 is an interfering peptide that blocks viperin-mediated STAT1 degradation, thereby preventing coxsackievirus B3 (CVB3)-induced acute heart failure (AHF).
/
HY-B0209S Metolazone-d7
Metolazone-d7 is deuterium labeled Metolazone. Metolazone (SR-720-22) is primarily used to treat congestive heart failure and high blood pressure.
/
HY-184830 Isosilychristin
Isosilychristin is a P-glycoprotein inhibitor with an IC50 of 25.9 μM. Isosilychristin downregulates the expression of transmembrane efflux pumps, exerts intracellular antioxidant effects, and inhibits NO production in macrophages. Isosilychristin regulates cell cycle progression, and exerts weak antiproliferative and colony formation inhibitory effects in prostate cancer cells. Isosilychristin reduces bacterial intercellular communication and reverses the drug resistance of Staphylococcus aureus. Isosilychristin can be used in studies related to prostate cancer, inflammation and bacterial infections.
/
HY-113071AR Mevalonic acid lithium salt (Standard)
Mevalonic acid lithium salt (Standard) is the analytical standard of Mevalonic acid lithium salt. This product is intended for research and analytical applications. Mevalonic acid (MVA) lithium salt is a precursor substance of the mevalonate pathway, which is essential for cell growth and proliferation. Mevalonic acid lithium salt is effective in inhibiting Simvastatin (HY-17502)-induced decrease in C2C12 cell viability in vitro. Mevalonic acid lithium salt can be used in studies of myopathy and heart failure.
/
HY-A0115S2 Ramiprilat-d4 hydrochloride
Ramiprilat-d4 hydrochloride is deuterated labeled Ramiprilat (HY-A0115). Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research.
/
HY-A0154R Deslanoside (Standard)
Deslanoside (Standard) is the analytical standard of Deslanoside. This product is intended for research and analytical applications. Deslanoside (Desacetyllanatoside C) is a rapidly acting cardiac glycoside used to treat congestive heart failure and supraventricular arrhythmias due to reentry mechanisms, and to control ventricular rate in the treatment of chronic atrial fibrillation. Deslanoside inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular sodium and calcium concentrations .
/
HY-P991848 Anti-CD64 Antibody (10.1)
Anti-CD64 Antibody (10.1) recognizes an epitope on human CD64 (Fc_RI). Fc gamma receptors (Fc_Rs) are membrane-bound proteins which control and mediate communication of IgG antibodies within the immune system. Recommend Isotype Controls: Mouse IgG1 kappa, Isotype Control (HY-P99977).

Species: Human

/
HY-B0202S3 Irbesartan-d7
Irbesartan-d7 is deuterated labeled Irbesartan (HY-B0202). Irbesartan (SR-47436) is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan can be used for the research of high blood pressure, heart failure, and diabetic kidney disease.
/
HY-18206S1 (S)-Lisinopril-d5 sodium
(S)-Lisinopril-d5 (sodium) (MK-521-d5 (sodium)) is deuterium labeled Lisinopril. Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
/
HY-W130074R α-Pinene oxide (Standard)
α-Pinene oxide (Standard) is the analytical standard of α-Pinene oxide (HY-W130074). This product is intended for research and analytical applications. α-Pinene oxide is a type of monoterpene epoxidation intermediate. α-Pinene oxide is produced via the cytochrome P-450-mediated oxidation pathway in Dendroctonus terebrans body microsomes and rat liver microsomes, and can be further converted into alcohols, ketones and insect pheromone derivatives. α-Pinene oxide can generate the perfume intermediate myrtenal. α-Pinene oxide is used in studies related to terpenoid metabolism and perfume synthesis.
/
HY-P992108 Efadirelaxin alfa
Efadirelaxin alfa (RELAX10) is a highly selective agonist of relaxin/insulin-like family peptide receptor RXFP1. After subcutaneous administration in animal experiments, Efadirelaxin alfa exhibits a significantly prolonged terminal half-life (7 days in mice, 3.75 days in rats), and shows no activity against related receptors such as RXFP2 and RXFP3. Efadirelaxin alfa has significant anti-cardiac hypertrophy and anti-fibrotic effects. Efadirelaxin alfa effectively attenuates and reverses cardiac hypertrophy and collagen deposition by regulating the TGF-β1/Smad2 and AKT/eNOS signaling pathways. Efadirelaxin alfa improves cardiac systolic function without causing fluctuations in blood pressure or heart rate, demonstrating favorable safety. Efadirelaxin alfa is currently mainly used in studies related to heart failure.

Species: Human

/
HY-B0202AS Irbesartan-d7 hydrochloride
Irbesartan-d7 hydrochloride is deuterated labeled Irbesartan hydrochloride (HY-B0202A). Irbesartan (SR-47436) hydrochloride is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan hydrochloride can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan hydrochloride can be used for the research of high blood pressure, heart failure, and diabetic kidney disease.
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HY-17367S5 Atazanavir-d24
Atazanavir-d24 (BMS-232632-d24) is deuterium labeled Atazanavir. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.
/
HY-18204S Valsartan-d9
Valsartan-d9 is deuterium labeled valsartan. Valsartan is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research.
/
HY-P3429 SAMβA
SAMβA is conjugated to the cell permeable peptide TAT47-57. SAMβA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats.
/
HY-P3557A Mibenratide TFA
Mibenratide TFA, a small cyclic peptide, is an adrenergic β1 receptor antagonist. Mibenratide TFA can be used for heart failure research.
/
HY-DY1088 Fluorescein-5-maleimide (solution)
Fluorescein-5-maleimide (solution) (N-(5-Fluoresceinyl)maleimide (solution)) is a fluorescent dye. Fluorescein-5-maleimide can be used to detect the redox state of thiols in eukaryotic cells. Fluorescein-5-maleimide can label peptides and is used to detect negatively charged nanoparticles. Fluorescein-5-maleimide can also label actin to explore its interaction with cardiac myosin-binding protein C (cMyBP-C), which helps in developing small molecule modulators for heart failure. Fluorescein-5-maleimide can screen mutant proteins that contain cysteine residues. The excitation wavelength of Fluorescein-5-maleimide is 494 nm, and the emission wavelength is 519 nm.

Solvent and concentration: DMSO: 10 mM
/
HY-P10504 C-Terminally encoded peptide 1
C-Terminally encoded peptide 1 (CEP1) is a small secreted peptide hormone. C-Terminally encoded peptide 1 is involved in regulating plant growth and abiotic stresses through cellular communication. C-Terminally encoded peptide 1 can be used in the study of plant growth and development.
Others  
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HY-P11797 EP9
EP9 is a peptide targeting CD63. EP9 binds specifically to the extracellular region of CD63, including a groove in the large extracellular loop (EC2) or the extracellular end of CD63’s central cavity, triggering endocytosis of decorated nanoemulsions/liposomes into cells. EP9 promotes cellular uptake of decorated nanoemulsions/liposomes into activated cardiac fibroblasts and epicardial stromal cells via caveolae and/or clathrin-coated pits. EP9 can be used for the research of myocardial infarction, cardiac fibrosis.
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HY-B0252S1 Hydrochlorothiazid-13C,d2
Hydrochlorothiazid-13C,d2 is the 13C- and deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.
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HY-133685S N-Hexanoyl-L-Homoserine lactone-d3
N-Hexanoyl-L-Homoserine lactone-d3 (C6-HSL-d3) is deuterium labeled N-Hexanoyl-L-homoserine lactone. N-Hexanoyl-L-homoserine lactone is a short-chained N-acyl homoserine lactone (AHL). Diatoms are frequently found in association with Proteobacteria, many members of which employ cell-to-cell communication via AHLs in aquatic habitats.
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HY-18206S Lisinopril-d5
Lisinopril-d5 is the deuterium labeled Lisinopril. Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
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HY-P11553B DOTA-ECL1i
DOTA-ECL1i is a conjugate of the CCR2 inhibitor ECL1i (HY-P11553) and DOTA. When radiolabeled with 68Ga, DOTA-ECL1i serves as a PET tracer that targets CCR2 expression. DOTA-ECL1i can be used in research related to pulmonary fibrosis, cardiac injury, abdominal aortic aneurysm inflammation, atherosclerosis, head and neck cancer, and pancreatic cancer.
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HY-P3557 Mibenratide
Mibenratide, a small cyclic peptide, is an adrenergic β1 receptor antagonist. Mibenratide can be used for heart failure research.
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HY-P3678 Neuropeptide Y (18-36) (porcine)
Neuropeptide Y (18-36) (porcine) is a competitive neuropeptide Y (NPY) cardiac receptor antagonist. Neuropeptide Y (18-36) (porcine) inhibits the binding of I-NPY to cardiac ventricular membranes in a concentration-dependent manner with an IC50 value of 158 nM and an Ki value of 140 nM. Neuropeptide Y (18-36) (porcine) can be used for the research of congestive heart failure.
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HY-P5389 Connexin mimetic peptide 40GAP27
Connexin mimetic peptide 40GAP27 is a biological active peptide. (This peptide corresponds to the GAP27 domain of the second extracellular loop of dominant vascular connexin (Cx40), designated as 40Gap 27. It was used to investigate mechanisms through which oxidant stress impairs communication via gap junctions. When administered, 40Gap27attenuates endothelium-dependent subintimal smooth muscle hyperpolarization.)
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HY-Y0248AR Farnesol (Standard)
Farnesol (Standard) is the analytical standard of Farnesol. This product is intended for research and analytical applications. Farnesol is a sesquiterpene alcohol that modulates cell-to-cell communication in Candida albicans, and has the activity in inhibiting bacteria.
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HY-W248583 Pyrromethene 650
Pyrromethene 650 (PM650) is a green-fluorescent polar tracer dye. It is used for investigations of membrane fusion, lysis, and gap-junctional communication and to detect volume changes in cells or liposomes.
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HY-W130074 α-Pinene oxide
α-Pinene oxide is a type of monoterpene epoxidation intermediate. α-Pinene oxide is produced via the cytochrome P-450-mediated oxidation pathway in Dendroctonus terebrans body microsomes and rat liver microsomes, and can be further converted into alcohols, ketones and insect pheromone derivatives. α-Pinene oxide can generate the perfume intermediate myrtenal. α-Pinene oxide is used in studies related to terpenoid metabolism and perfume synthesis.
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HY-174134 PI4Kβ/PKG-IN-2
PI4Kβ/PKG-IN-2 (Compound 20) is an orally active dual inhibitor of Plasmodium phosphatidylinositol 4-kinase beta (PI4Kβ) and cGMP-dependent protein kinase (PKG). PI4Kβ/PKG-IN-2 has potent inhibitory effects on Plasmodium. PI4Kβ/PKG-IN-2 is promising for research of malaria.
PI4K   PKG   Parasite  
Infection  
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HY-P99645 Goflikicept
Goflikicept (RPH 104) is a fusion protein that selectively binds and inactivates both circulating IL-1β and IL-1α. Goflikicept has the potential for the research of ST-segment elevation myocardial infarction (STEMI).
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HY-155106 SMA4
SMA4 is a selective PKG1α activator with basal EC50 value of 29 μM. SMA4 facilitates phosphorylation of the known PKG1 substrate, vasodilator-stimulated phosphoprotein (VASP), and inhibits human pulmonary arterial smooth muscle cells (hPASMC) proliferation. SMA4 can be used for cardiovascular disease research.
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HY-108548 Rp-8-Br-PET-cGMPS sodium
Rp-8-Br-PET-cGMPS sodium (Rp-8-Bromo-PET-cGMPS) is an analog of cyclic GMP (cGMP). It is a cell permeable, competitive, and reversible inhibitor of cGMP-dependent protein kinases (cGKs) that blocks activation of cGKI and cGKII by cGMP (Kis=35 and 30 nM). It less potently inhibits protein kinase A (Ki=11 μM) and cGMP-induced activation of cyclic nucleotide-gated channels (IC50=25 μM). In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (Ki=1 μM). Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11.
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HY-112465 H-8 dihydrochloride
H-8 dihydrochloride is a selective Cyclic nucleotide-dependent protein kinase inhibitor. H-8 dihydrochloride potently inhibits cGMP- and cAMP-dependent protein phosphorylation. H-8 dihydrochloride enhances the vasodilatory effect induced by 8-bromo-cAMP (HY-12306A). H-8 dihydrochloride fails to attenuate the vasodilatory effects induced by 8-bromo-cGMP (HY-101379A), atrial natriuretic peptide II, or Sodium nitroprusside (HY-B0564) in rat aorta.
PKA   PKC   PKG  
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HY-136409R N-Decanoyl-L-homoserine lactone (Standard)
Formoterol (hemifumarate hydrate) (Standard) is the analytical standard of Formoterol (hemifumarate hydrate). This product is intended for research and analytical applications. Formoterol hemifumarate hydrate is a selective, long-acting beta 2-adrenoceptor agonist. Formoterol is a bronchodilator used for the research of the asthma and chronic obstructive pulmonary disease (COPD). Formoterol hemifumarate hydrate induces mitochondrial biogenesis and promotes cognitive recovery after traumatic brain injury.
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HY-P3429A SAMβA TFA
SAMβA TFA is a rationally designed selective antagonist of Mfn1-βIIPKC association and can bind to TAT (HY-P0281). SAMβA TFA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats.
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HY-B0252S Hydrochlorothiazid-d2
Hydrochlorothiazid-d2 is the deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.
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HY-B0252S2 Hydrochlorothiazide-13C6
Hydrochlorothiazide-13C6 is the 13C labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.
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HY-P0142A DT-3 acetate
DT-3 acetate is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling.
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HY-N3431 Kaempferol-7-O-rhamnoside
Kaempferol-7-O-rhamnoside is a PD-1/PD-L1 inhibitor and farnesoid X receptor (FXR) agonist. Kaempferol-7-O-rhamnoside demonstrates cardioprotective potential targeting the AMPKα1 signaling pathway. Kaempferol-7-O-rhamnoside significantly upregulates the mRNA expression of AMPKα1 in H9c2 cardiomyocytes. Kaempferol-7-O-rhamnoside reverses APAP-induced reduction of glutathione (GSH) content and increase of ROS production in L02 cells. Kaempferol-7-O-rhamnoside has the potential for heart failure.
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HY-N7055 Trierucin
Trierucin (Trierucoylglycerol) is a triester formed by glycerol and erucic acid, which serves as an occlusive skin conditioning agent and non-aqueous thickener in cosmetics. Long-term feeding of Trierucin to rats induces chronic toxicities such as cardiac lipid deposition and fibrosis.
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HY-114294A DL-3-Hydroxy-3-methylglutaryl coenzyme A disodium hydrate
DL-3-Hydroxy-3-methylglutaryl coenzyme A disodium hydrate is a disodium salt compound of HMG-CoA, is a intermediate of terpenes and ketone bodies. DL-3-Hydroxy-3-methylglutaryl coenzyme A disodium also involves in ester metabolism in vivo, as a precursor for cholesterol synthesis, and regulates cholesterol synthesis by coupling LDL receptor.
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HY-D0830 Calcein (tetraethyl ester)
Calcein tetraethyl ester is a tetraethylated derivative of calcein, with its core function serving as a live cell-specific fluorescent tracer. Calcein tetraethyl ester can diffuse between human periodontal ligament cells via gap junctions, thus enabling the evaluation of gap junction intercellular communication function, and its diffusion is enhanced under hydrogen peroxide induction. Calcein tetraethyl ester can be applied in the fields of cell biology and fluorescent labeling.
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HY-131900 Protein kinase inhibitor H-7
Protein kinase inhibitor H-7 is a selective inhibitor of PKC and cyclic nucleotide-dependent protein kinases, with a Ki value of 6.0 μM for rabbit protein kinase C, a Ki value of 3.0 μM for rabbit cAMP-dependent protein kinase, and a Ki value of 5.8 μM for porcine cGMP-dependent protein kinase. Protein kinase inhibitor H-7 has no effect on Ca2+-calmodulin-dependent enzymes. Protein kinase inhibitor H-7 regulates the Actin cytoskeleton, inhibits contractility, disrupts stress fibers, induces protrusive activity, stabilizes intercellular junctions, and triggers rapid and reversible cytoskeletal reorganization. Protein kinase inhibitor H-7 serves as a research tool for elucidating the functions of protein kinase C-mediated signaling systems.
PKC   PKA   PKG   Arp2/3 Complex  
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HY-100983 Protein kinase inhibitor H-7 dihydrochloride
Protein kinase inhibitor H-7 dihydrochloride is a potent PKC (protein kinase C) inhibitor. At 100 μM, Protein kinase inhibitor H-7 dihydrochloride completely inhibits both TPA (skin tumour promoter, 12-O-tetradecanoylphorbol-13-acetate) and phospholipase C-induced ODC (ornithine decarboxylase).
PKC   PKA   PKG   Arp2/3 Complex  
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HY-P990951 Vixticibart
Vixticibart (REGN-5381) is a fully human IgG4 monoclonal antibody and NPR1 agonist that targets NPR1. Vixticibart stabilizes the receptor in an activated conformation by binding to the N-terminal domain of NPR1, and enhances the activity of endogenous ligands ANP and BNP without blocking ligand binding when these ligands are present. Vixticibart exerts vasodilatory and hypotensive effects by inducing cGMP production, preferentially dilating venous vessels to reduce systolic and venous pressure, but does not induce diuresis and may trigger a compensatory increase in heart rate. Vixticibart produces a synergistic hypotensive effect when combined with angiotensin-converting enzyme inhibitors or angiotensin receptor blockers, and is currently mainly used in research related to heart failure and hypertension.

Species: Human

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HY-P1940 Maculosin
Maculosin (Cyclo (Tyr-Pro)) is a host-specific phytotoxin for spotted knapweed from Alternaria alternata. Maculosin is a quorum-sensing molecule involved in cell-cell communication. Maculosin also acts as a signaling molecule regulating virulence gene expression. Maculosin shows antimicrobial, antifungal, antioxidant and anti-cancer properties.Maculosin (Cyclo (Tyr-Pro)) is a host-specific phytotoxin for spotted knapweed from Alternaria alternata. Maculosin is a quorum-sensing molecule involved in cell-cell communication. Maculosin also acts as a signaling molecule regulating virulence gene expression. Maculosin shows antimicrobial, antifungal, antioxidant and anti-cancer properties.

Source: Streptomyces sp. KTM18

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HY-P990294 Anti-Mouse CD106/VCAM-1 Antibody (M/K-2.7)
Anti-Mouse CD106/VCAM-1 Antibody (M/K-2.7) is an anti-mouse CD106/VCAM-1 IgG1 monoclonal antibody. Anti-Mouse CD106/VCAM-1 Antibody (M/K-2.7) reduces inflammatory response and oxidative stress by lowering p-STAT3 and reactive oxygen species (ROS) levels. Anti-Mouse CD106/VCAM-1 Antibody (M/K-2.7) can alleviate cardiac inflammation and fibrosis by reducing the expression of collagen I and collagen III. Anti-Mouse CD106/VCAM-1 Antibody (M/K-2.7) can be used for research on cardiovascular conditions such as hypertensive heart condition and subretinal fibrosis.

Species: Mouse

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HY-P3136 TRV055
TRV055 (TRV120055) is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV120055 induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. TRV055 activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. TRV055 induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. TRV055 can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses[1]
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HY-P990245 Anti-Mouse FAP Antibody (73.3)
Anti-Mouse FAP Antibody (73.3) is an anti-mouse FAP IgG1 monoclonal antibody. Anti-Mouse FAP Antibody (73.3) can be used to accurately detect the expression and localization of FAP protein in mice. Anti-Mouse FAP Antibody (73.3) can be used for research on cancer.

Species: Mouse

FAP  
Cancer  
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HY-159069 Zymosan (ZM), 95%
Zymosan (ZM), 95% is a yeast cell wall-derived carbohydrate-rich preparation and immunomodulator. Zymosan (ZM), 95% binds to and activates TLR-2, TLR-4, and Dectin-1 receptor to trigger downstream signaling pathways. Zymosan (ZM), 95% upregulates TLR-2, TLR-4, and TNF-α mRNA expression, increases serum TNF-α levels, and stimulates splenocyte number and viability in mice. Zymosan (ZM), 95% attenuates melanoma growth progression, modulates macrophage marker gene expression, and mediates phagocytosis, ROS generation, and cytokine production. Zymosan (ZM), 95% reduces Connexin 43 protein and mRNA levels, inhibits gap junctional intercellular communication, and induces proinflammatory factor production in human corneal cells. Zymosan (ZM), 95% induces peritoneal inflammation in mice, functions as a drug carrier, and supports fibroblast cell attachment in hydrogel formulations. Zymosan (ZM), 95% can be used for the research of melanoma, tumors, fungal keratitis, ocular surface inflammatory disorders, and peritoneal inflammation.
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HY-136409 N-Decanoyl-L-homoserine lactone
N-decanoyl-L-homoserine lactone (C10-HSL) is a N-acyl-homoserine lactone (AHL) N-decanoyl-L-homoserine lactone can inhibit primary root growth in Arabidopsis. N-decanoyl-L-homoserine lactone triggers a transient and immediate increase in the concentrations of cytosolic free Ca2+ and reactive oxygen species (ROS), increases the activity of mitogen-activated protein kinase 6 (MPK6), and induces nitric oxide (NO) production in Arabidopsis roots.

Source: Agrobacterium tumefaciens

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HY-153552A NH2-UAMC1110 TFA
NH2-UAMC1110 TFA is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110 (HY-100684), and is a precursor compound for the synthesis of FAP inhibitor probes, not directly used in bioactivity experiments. For example, NH2-UAMC1110 TFA is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose effect, and has been used in tumor diagnosis. NH2-UAMC1110 TFA structurally incorporates an active amino group, allowing it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.) to synthesize molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 TFA specifically binds to the FAP active site, inhibiting its proline-selective serine protease activity (including dipeptidyl peptidase and endopeptidase activity), blocking FAP-mediated tissue remodeling-related processes. Its key activity is high targeting and high affinity, and its core function is to act as a targeting module coupled with bifunctional chelators (such as DOTA, DATA5m). NH2-UAMC1110 TFA can be applied to diagnostic imaging studies of tumors expressing FAP (such as colorectal cancer, pancreatic cancer, etc.), and also provides molecular tools for targeted research of FAP-related diseases with high FAP expression, such as fibrosis and arthritis.
FAP  
Cancer  
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HY-P991219 Anti-IL11RA Antibody (X209)
Anti-IL11RA Antibody (X209) (EnX209) is a human-derived IgG4, κ-type antibody inhibitor targeting IL11RA, with a KD of 6 nM. Anti-IL11RA Antibody (X209) blocks the IL11RA signaling pathway, inhibits ERK-dependent activation, and reduces the activation level of ERK1/2. Anti-IL11RA Antibody (X209) exerts a protective effect against fibrosis. Anti-IL11RA Antibody (X209) is applicable to studies related to liver fibrosis, cardiac fibrosis and other related conditions. Recommended isotype control: Human IgG4 kappa, Isotype Control (HY-P99003).

Species: Human

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HY-P99047 Simtuzumab
Simtuzumab (AB 0024; GS 6624) is a monoclonal antibody directed against Lysyl oxidase like-2 (LOXL2). Simtuzumab non-competitively blocks collagen cross-linking, reduces LOXL2 protein expression and attenuates extracellular matrix changes. Simtuzumab reduces myocardial fibrosis and prevents cardiac dysfunction. Simtuzumab lowers Myh7 and Nppa gene expression, reduces contraction heterogeneity, and cuts COL1A1 deposition. Simtuzumab can be used for the research of LMNA mutation-induced dilated cardiomyopathy, idiopathic pulmonary fibrosis, and primary sclerosing cholangitis.

Species: Human

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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

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HY-128483 Fusaric acid
Fusaric acid is an orally active multi-pathway inhibitor with the activity of inducing oxidative stress and apoptosis. Fusaric acid can chelate divalent metal cations, damage mitochondrial membrane structure, and activate apoptosis-related proteases such as Caspase-3/7, -8, and -9. Fusaric acid also regulates Bax/Bcl-2 protein, inhibits fibrosis-related signaling pathways such as NF-κB, TGF-β1/SMADs, and PI3K/AKT/mTOR, and reduces collagen deposition. Fusaric acid is also a dopamine β-hydroxylase inhibitor, which reduces endogenous levels of norepinephrine and epinephrine in the brain, heart, spleen, and adrenal glands. Fusaric acid can play a role in myocardial fibrosis and improve cardiac hypertrophy in heart disease, and can also be used in the study of esophageal cancer and liver cancer.

Source: Fusarium spp.

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HY-147173 FAPI-74
FAPI-74 is a PET (positron emission tomography) tracer targeting the fibroblast activation protein (FAP). FAPI-74 can be used for FAP-positive tumor research.
FAP  
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HY-A0154 Deslanoside
Deslanoside (Desacetyllanatoside C) is a rapidly acting cardiac glycoside used to treat congestive heart failure and supraventricular arrhythmias due to reentry mechanisms, and to control ventricular rate in the treatment of chronic atrial fibrillation. Deslanoside inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular sodium and calcium concentrations .
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HY-P700701 CCN2/CTGF Protein, Human (HEK293, His)
CCN2/CTGF (Connective Tissue Growth Factor) is a protein produced primarily by endothelial cells in blood vessels. It plays an important role in various cellular processes. CCN2/CTGF Protein, Human (HEK293, His) is the recombinant human-derived CCN2/CTGF protein, expressed by HEK293 , with C-His labeled tag.

Species: Human; Source: HEK293

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HY-P79369 CCN2/CTGF Protein, Rat (HEK293)
The CCN2/CTGF protein is a major connective tissue mitochondrial attractant secreted by vascular endothelial cells and critical for chondrocyte proliferation and differentiation. Additionally, it mediates heparin- and divalent cation-dependent cell adhesion in various cell types, including fibroblasts, myofibroblasts, endothelial cells, and epithelial cells. CCN2/CTGF Protein, Rat (HEK293) is the recombinant rat-derived CCN2/CTGF protein, expressed by HEK293 , with tag free.

Species: Rat; Source: HEK293

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HY-P704517 CCN5 Protein, Human (His)
CCN5 Protein, Human (His) is the recombinant human-derived CCN5 protein, expressed by E. coli, with C-10*His tag.

Species: Human; Source: E. coli

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HY-P78713 CCN2/CTGF Protein, Rhesus macaque (HEK293, His)
CCN2 is a mitogen secreted by vascular endothelial cells and a mechanosensor of mesenchymal cell differentiation that secretes stromal cell proteins. CCN2 can sense appropriate mechanical stress and downregulate its expression accordingly. CCN2 is a classic epithelial-to-mesenchymal transition (EMT) and fibrosis marker. CCN2/CTGF Protein, Rhesus macaque (HEK293, His) is the recombinant Rhesus Macaque-derived CCN2/CTGF protein, expressed by HEK293 , with C-His labeled tag.

Species: Rhesus Macaque; Source: HEK293

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HY-P704310 CCN2/CTGF Protein, Mouse (HEK293, His)
CCN2/CTGF protein is a major connective tissue mitochondrial attractant secreted by vascular endothelial cells and promotes chondrocyte proliferation and differentiation. It mediates heparin- and divalent cation-dependent cell adhesion in various cell types, including fibroblasts, myofibroblasts, endothelial cells, and epithelial cells. CCN2/CTGF Protein, Mouse (HEK293, His) is the recombinant mouse-derived CCN2/CTGF protein, expressed by HEK293, with C-His labeled tag.

Species: Mouse; Source: HEK293

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Keywords

heart failure | HFpEF | immune-fibroblast communication | cardiac fibrosis | immunometabolism | microvascular inflammation | obesity cardiomyopathy | ketone metabolism