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GPCR Signaling Promotes Myelin Regeneration

Neurodegeneration Intercellular Communication & Diseases Calcium Homeostasis Cellular Degeneration

G protein-coupled receptor (GPCR) signaling has emerged as an important regulatory system for myelin regeneration because GPCRs are widely expressed in oligodendroglial cells, while adult oligodendrocyte precursor cells (OPCs) provide a cellular reservoir capable of supporting myelin repair after demyelination. Research has progressed from defining individual GPCR functions in oligodendrocyte development to identifying receptor-specific pharmacological strategies that alter OPC differentiation, myelination, and remyelination. In particular, screening of a GPCR-focused small-molecule library identified κ-opioid receptor (KOR) agonists as promoters of oligodendrocyte differentiation and myelination; the agonist (±) U-50488 accelerated remyelination after focal lysolecithin demyelination and enhanced differentiation of human induced pluripotent stem cell-derived OPCs. GPR30/GPER provides another positive regulatory route: the GPR30 agonist G1 enhanced oligodendrocyte maturation, neuronal ensheathment, and myelination in experimental systems. These findings place GPCR signaling at the intersection of oligodendrocyte biology, regenerative neuroscience, and drug discovery, although the functional consequences of many oligodendroglial GPCRs remain insufficiently characterized. GPCR-dependent myelin regeneration is not a single pathway but a receptor-specific network in which activation can either promote or restrain oligodendrocyte responses[1][2][3].

Microglia-derived transglutaminase-2, together with laminin, activates the adhesion GPCR ADGRG1/GPR56 on OPCs, promoting OPC proliferation and improving remyelination in two mouse demyelination models. By contrast, GPR17 functions as a differentiation brake. Activation of GPR17 engages Gαi/o signaling and reduces activity of the adenylyl cyclase-cAMP-PKA-CREB cascade and EPAC, decreasing myelin basic protein abundance and oligodendrocyte maturation. GPR17 can also engage Gαi, Gαs, Gαq and β-arrestin-associated signaling, with changes in cAMP, inositol phosphate, Ca2+ flux, and ERK1/2 phosphorylation. Following lysolecithin injury, Olig2 transcriptionally targets Gpr17; Gpr17 activation reduces intracellular cAMP and induces Xaf1, whereas Gpr17 inhibition increases Epac1, promotes oligodendrocyte differentiation, and advances remyelination. Thus, regenerative GPCR pharmacology may require receptor activation in some pathways and receptor inhibition in others[4][5][6][7].

These mechanisms create several experimentally supported therapeutic directions for demyelinating disease, particularly multiple sclerosis. GPR17 blockade with HAMI3379 enhanced maturation of primary rodent oligodendrocytes and favored differentiation of human iPSC-derived oligodendrocytes, supporting GPR17 antagonism as a regenerative drug-discovery strategy. CXCR2 antagonism likewise promoted OPC proliferation and differentiation, activated PI3K/AKT/mTOR signaling, and enhanced myelin repair in cuprizone-treated mice. Conversely, osteocalcin signaling through GPR37 restrains oligodendrocyte differentiation and CNS myelination, identifying another GPCR-linked pathway regulating the transition from OPCs to myelinating oligodendrocytes. Translation remains challenging because GPCR effects depend on receptor identity, cellular context, differentiation stage, ligand environment, and downstream signaling architecture; moreover, functional outcomes of oligodendroglial GPCR modulation remain incompletely explored. Future work therefore needs to define receptor-specific signaling in human oligodendroglia, distinguish developmental myelination from injury-induced remyelination, and establish which GPCR interventions produce durable myelin repair before these pathways can support disease-modifying remyelination therapies.[1][8][9][10].

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Cat. No. Product Name Information Application Publication
HY-13757 Tamoxifen Citrate
Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively. Tamoxifen Citrate activates autophagy and induces apoptosis. Tamoxifen Citrate can also be used to induce gene knockout in CreER transgenic mice.
Estrogen Receptor/ERR   HSP   Autophagy   Apoptosis  
Neurological, Eye or Ear Disease   Digestive System Disease   Prostate Cancer   Viral Infection   Digestive System Inflammation   Luminal Breast Cancer   Metastatic Breast Cancer   SARS-CoV-2 Infection   Lung Fibrosis  
273
HY-13757A Tamoxifen
Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively. Tamoxifen activates autophagy and induces apoptosis. Tamoxifen can also be dissolved in corn oil (HY-Y1888) for use in inducing gene knockout in CreER transgenic mice. Tamoxifen has better solubility in corn oil compared to Tamoxifen Citrate (HY-13757).
Estrogen Receptor/ERR   HSP   Autophagy   Apoptosis  
Neurological, Eye or Ear Disease   Metabolic or Endocrine Disease   Digestive System Disease   Prostate Cancer   Viral Infection   Digestive System Inflammation   Luminal Breast Cancer   Metastatic Breast Cancer   SARS-CoV-2 Infection   Lung Fibrosis  
273
HY-13636 Fulvestrant
Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
Estrogen Receptor/ERR   Autophagy   Apoptosis  
Prostate Cancer   Pancreatic Cancer   Ovarian Cancer   Digestive System Inflammation   Non-Small Cell Lung Cancer   Luminal Breast Cancer   HER-2 Positive Breast Cancer   Triple-Negative Breast Cancer   Metastatic Breast Cancer  
146
HY-B0141 Estradiol
Estradiol (β-Estradiol) is a steroid hormone and the major female sex hormone. Estradiol can up-regulate the expression of neural markers of human endometrial stem cells (hEnSCs) and promote their neural differentiation. Estradiol can be used for the research of cancers, neurodegenerative diseases and neural tissue engineering.
Estrogen Receptor/ERR   Endogenous Metabolite   Bacterial  
Metabolic or Endocrine Disease   Prostate Cancer   Viral Infection   Bacterial Infection   Neurodegenerative Disease   Cardiovascular Disease   Luminal Breast Cancer   Metastatic Breast Cancer   SARS-CoV-2 Infection  
141
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  
113
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  
113
HY-N0322 Cholesterol (from animal)
Cholesterol (from animal) is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol (from animal) plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol (from animal) is also an endogenous estrogen-related receptor α (ERRα) agonist.
Endogenous Metabolite   Liposome   Bacterial   Estrogen Receptor/ERR  
Breast Cancer   Viral Infection   Bacterial Infection   Pancreatic Ductal Adenocarcinoma   Hepatitis B Virus Infection   Alzheimer's Disease   Sepsis   Atherosclerosis   Type 2 Diabetes   Obesity   Hypercholesterolemia  
96
HY-L006 GPCR/G Protein Compound Library
GPCRs are a large family of cell surface receptors that respond to a variety of external signals. Binding of a signaling molecule to a GPCR results in G protein activation, which in turn triggers the production of any number of second messengers. GPCRs play an important role in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third to one-half of all approved drugs act by binding to GPCRs. GPCRs are a large group of drug targets in drug discovery. MCE provides a unique collection of 3,519 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.

Signaling Pathway Targeting Libraries

93
HY-L015 PI3K/Akt/mTOR Compound Library
The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials. MCE owns a unique collection of 1,149 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.

Signaling Pathway Targeting Libraries

90
HY-14590 Kaempferol
Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer.
Estrogen Receptor/ERR   Autophagy   Mitophagy   Apoptosis   HIV   Parasite   Endogenous Metabolite  
Digestive System Disease   Lung Cancer   Breast Cancer   Ovarian Cancer   Viral Infection   Parasitic Infection   Digestive System Inflammation   Glucose Metabolism  
85
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.

Signaling Pathway Targeting Libraries

84
HY-L070 Neuroprotective Compound Library
Neurodegenerative diseases are characterised by progressive dysfunction and death of neurons, such as Alzheimer’s disease, Parkinson’s disease, and multiple sclerosis (MS). Neuroprotection is an approach to preserve neurons so that neurons cannot be hurt by different pathological factors in neurodegenerative diseases. Neuroprotectors are some agonists and antagonists targeting some key targets in neuroprotactive signal pathways, such as calcium and sodium channel blockers, GABA receptor agonists, NMDA receptor Antagonists, etc. Current neuroprotectors cannot reverse existing damage, but they may protect against further nerve damage and slow down any degeneration of the central nervous system (CNS) and still play important roles in the treatment of neurodegenerative diseases. MCE offers a unique collection of 1,851 compounds with potential neuroprotective activities. These compounds mainly act on some key targets in neuroprotetive signal pathways, such as calcium channel, sodium channel, adenosine A1 receptor, etc. MCE Neuroprotective Compopund Library is a useful tool in neuroprotective drug discovery.

Compound Characteristic Classified Libraries

84
HY-L101 Anti-Liver Cancer Compound Library
Liver cancer is one of the leading malignancies which occupies the second position in cancer deaths worldwide, becoming serious threat to human health. Hepatocellular carcinoma (HCC), also known as hepatoma is the most common type accounting for approximately 90% of all liver cancers. Current evidence indicates that during hepatocarcinogenesis, two main pathogenic mechanisms prevail: (1) cirrhosis associated with hepatic regeneration after tissue damage caused by hepatitis infection, toxins or metabolic influences, and (2) mutations occurring in single or multiple oncogenes or tumor suppressor genes. Both mechanisms have been linked with alterations in several important cellular signaling pathways. These include the RAF/MEK/ERK pathway, PI3K/AKT/mTOR pathway, WNT/b-catenin pathway, insulin-like growth factor pathway, c-MET/HGFR pathway , etc. MCE offers a unique collection of 3,003 compounds with identified and potential anti-liver cancer activity. MCE anti-liver cancer compound library is a useful tool for anti-liver cancer drugs screening and other related research.

Disease Focused Libraries

84
HY-L928 GPCR Targeted Diversity Library
G protein-coupled receptors (GPCRs) are membrane proteins in humans and one of the most important targets in drug discovery. Approximately 35% of launched drugs are targeted GPCRs, making them a crucial class of targets in drug discovery. The orthosteric site of a GPCR is its endogenous ligand’s (such as neurotransmitters or hormones) binding site. This site plays a central role in signal transduction. Small molecules binding to this site typically contain a protonatable amino group, enabling the formation of salt bridges or hydrogen bonds with acidic residues in the binding pocket. In contrast, the allosteric site does not directly initiate signaling but modulates the signal intensity of the GPCR by altering or stabilizing the conformation of the orthosteric site. Small molecules binding to the allosteric site often contain multiple aromatic rings to occupy hydrophobic pockets and achieve their functional effects. MCE has collected over 7,106 reported bioactive molecules targeting GPCRs, covering Class A, B, and C GPCRs. These small molecules were subjected to AI representation to extract 2D and 3D features. Subsequently, we do screening by AI score based on similarity to identify molecules in diversity library highly similar to the reported bioactive molecules in both 2D and 3D, with a threshold greater than 0.7. Further screening based on cLogP was applied to select molecules with good lipophilicity, which facilitates the binding of small molecules to GPCRs. This diversity library can be widely applied to the discovery of compounds targeting GPCR proteins.

Focused and target libraries

84
HY-L0122V Asinex CNS Macrocycles Library
Several CNS multi-parameter scoring approaches have been reported: CNS-MPO, CNS-MPO V.2, CNS-TEMPO, which suggesting an algorithm to predict CNS-ike properties of new chemical entities. We have applied these scoring algorithms to select macrocycles satisfying multiple cut-offs and structural desirability criteria. The resulting set consists of 1,122 macrocyclic compounds with CNS-MPO > 4, CNS-MPO.v2 > 4, and CNS-TEMPO < 4 for CNS-related drug discovery and research.
83
HY-L0124V Chemspace CNS-Focused Library
The basic requirements for the compounds that are supposed to penetrate the blood-brain barrier are somewhat different from those for the majority of drug discovery projects. Alongside the known problem with delivery of the large and non-polar compounds and their penetrability through the cell membrane, the other issue arises as well: small and polar compounds are not able to pass the Blood-Brain Barrier. Chemspace CNS-focused library comprises quite small, non-polar compounds that are also free from PAINS/toxic fragments and aggregators.
83
HY-L074 Anti-Breast Cancer Compound Library
Breast cancer is the most frequent cancer among women, impacting 2.1 million women each year, and also causes the greatest number of cancer-related deaths among women. Surgery is usually the first type of treatment for breast cancer, which is usually followed by chemotherapy or radiotherapy or, in some cases, hormone or targeted therapies, especially for metastatic breast cancer (MBC). Breast cancer is a heterogeneous disease, which is categorized into 3 major subtypes based on the presence or absence of molecular markers for estrogen or progesterone receptors and human epidermal growth factor 2 (ERBB2; formerly HER2): hormone receptor positive/ERBB2 negative (70% of patients), ERBB2 positive (15%-20%), and triple-negative (tumors lacking all 3 standard molecular markers; 15%). Different intrinsic subtypes exhibit different tumor behavior with different prognoses, and may require specific targeted therapies to maximize treatment effectiveness. Otherwise, some signaling pathways also play important roles in the development of breast cancer, such as NF-κB Signaling Pathway, TGF-beta Signaling Pathway, PI3K/AKT/mTOR signaling pathway and Notch Signaling Pathway. These signaling pathways offer ideal targets for development of new targeted therapies for breast cancer. MCE supplies a unique collection of 3,404 compounds with identified and potential anti-breast cancer activity. MCE Anti-Breast Cancer Compound Library is a useful tool for anti-breast cancer drugs screening.

Disease Focused Libraries

83
HY-L105 Peptide Library
Peptides are a group of biologically active substances that are involved in various cellular functions of organisms. Peptides are often used in functional analysis, vaccine research and especially in the field of drug research and development. At present, more than 80 peptide drugs have reached the market for a wide range of diseases, including diabetes, cancer, osteoporosis, multiple sclerosis, HIV infection and chronic pain. MedChemExpress (MCE) offers a comprehensive collection of 2,647 peptides, including bioactive peptides, amino acid derivatives, and blocking peptides. MCE Peptide Library can be used for peptide library screening, peptide drug discovery, vaccine development, target verification, structural activity research, etc.

Structure Classified Libraries

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.

Signaling Pathway Targeting Libraries

83
HY-L164 Serine/Threonine Kinase Inhibitor Library
Protein serine/threonine kinases (PSKs) are protein kinases that use ATP as a high-energy donor molecule to transfer phosphate groups to serine/threonine residues of target protein. As an important signal transduction regulator, serine/threonine kinases can affect the function of target proteins by disrupting enzyme activity or binding of target proteins to other proteins. Serine/threonine kinases are involved in the regulation of immune response, cell proliferation, differentiation, apoptosis and other physiological processes. Serine/threonine kinase inhibitors are an important class of compounds that have been widely studied in cancer, chronic inflammation, autoimmune diseases, aging and other diseases. MCE designs a unique collection of 2,276 serine/threonine kinase inhibitors, mainly targeting the receptor PKA, Akt, PKC, MAPK/ERK, etc, which is an effective tool for development and research of anti-cancer, anti-chronic inflammatory diseases, anti-autoimmune diseases and anti-aging compounds.

Signaling Pathway Targeting Libraries

83
HY-L165 Dopamine Receptor Compound Library
Dopamine receptor (DAR), widely distributed in the brain, plays a key role in regulating motor function, motivation, driving force and cognition. The role of DA is mediated by D1-type (D1, D5) and D2-type receptors (D2S, D2L, D3, D4), which are distributed in presynaptic, postsynaptic and extrasynaptic, projection neurons and interneurons. Each receptor has a different function. D1 and D5 receptors couple with G stimulation sites and activate Adenylyl cyclase. The activation of Adenylyl cyclase leads to the production of the second messenger cAMP, which leads to the production of protein kinase A (PKA), which leads to further transcription in the nucleus. D2 to D4 receptors are coupled to G inhibitory sites to inhibit adenylyl cyclase and activate potassium Ion channel. These receptors utilize phosphorylation cascades or direct membrane interactions to affect the functions of voltage-gated and neurotransmitter-gated channels, cytoplasmic enzymes, and transcription factors. Dopamine receptor plays an important role in daily life. MCE designs a unique collection of 282 small molecules related to dopamine receptor. It is a good tool for screening drugs from nervous system disease.

Signaling Pathway Targeting Libraries

83
HY-L249 Lactylation Compound Library
Protein lactylation, an emerging post-translational modification identified in recent years, plays a critical role in linking cellular metabolic reprogramming, epigenetic regulation, and signaling networks. Based on a systematic framework encompassing lactate metabolism, lactylation, and downstream signaling pathways, this compound library comprehensively targets multiple regulatory layers, including histone modification enzymes (such as p300 and HDACs), key glycolytic enzymes (such as PKM2, LDHA, and GAPDH), transcriptional regulators (such as STAT3, HMGB1, and p53), as well as central signaling pathway nodes including HIF-1α, NF-κB, and PI3K-AKT-mTOR. This integrated design enables a comprehensive representation of the regulatory roles of lactylation across the “metabolism–epigenetics–signaling” axis. MCE has assembled a collection of 6,182 known bioactive compounds and potential functional molecules, making this library suitable for a wide range of applications, including high-throughput drug screening, inhibitor identification, and mechanistic studies. It can be used to systematically evaluate the functional roles of lactylation in biological processes such as tumor metabolism, immune regulation, and inflammatory responses, and to efficiently identify small-molecule candidates with regulatory potential, thereby facilitating the development of innovative therapeutics targeting the interplay between metabolism and epigenetic regulation.

Signaling Pathway Targeting Libraries

83
HY-L913 Tyrosine Focused Covalent Fragment Library
Recently, significant advancements in tyrosine-targeting electrophiles have primarily occurred in the field of protein-protein interactions (PPIs), where cysteine residues are often underrepresented and novel chemistries are needed to address these interfaces. In this context, tyrosines are frequently more accessible compared to more buried binding sites. Moreover, they are commonly found at "hot spots," which are functional epitopes of PPIs, with 12.3% of the residues consisting of tyrosines. This prevalence is likely due to the hydrophobic nature of tyrosine, its ability to participate in aromatic π-interactions, and its capacity for hydrogen bonding. Beyond PPIs, some progress has also been made in covalent tyrosine targeting in other areas where more commonly addressed side chains are lacking. Even though tyrosine has a slightly lower pKa value compared to the protonated lysine side chain (approximately 10 vs. 10.5 for the unprotected amino acid side chains), significantly less progress has been made in the development of tyrosine-targeted covalent ligands compared to lysine. This is likely due to the reduced flexibility of the tyrosine side chain and the greater steric hindrance of its hydroxy group, which makes it more challenging to adopt suitable reaction geometries. Through careful selection, we constructed a structural filter containing over 110 electrophilic groups. By analyzing the electrophilic fragments selected by the structural filter, we removed any molecules with trivial or undesirable structural features. Ultimately, we obtained 124 fragment molecules which can target tyrosine residue and can be used for fragment-based covalent drug discovery.

Functional Fragment Libraries

83
HY-L919 MCE CNS BBB Lead-like Library
With the aging population and increasing competitive pressures, neurodegenerative diseases of the central nervous system (CNS) have become a serious medical challenge in modern society, including Parkinson's disease, Alzheimer's disease, brain tumors, and multiple sclerosis. However, the success rate of CNS drug development remains remarkably low, primarily due to the blood-brain barrier (BBB). The blood-brain barrier (BBB) is a semipermeable barrier structure that surrounds the microvasculature of the CNS. In capillaries, the wedged endothelial cells are tightly packed and wedge-shaped, lining the interior of the vessels to form extensive tight junctions. Along with a range of receptors, transporters, efflux pumps, and other cellular components, this barrier regulates the entry and exit of molecules between the bloodstream and the brain. The intact BBB blocks the passage of most blood-borne substances into the brain, preventing nearly 100% of large-molecule drugs and over 98% of small-molecule drugs from entering. Compared to non-CNS drugs, physicochemical properties such as hydrogen bonds, lipophilicity, and molecular weight significantly influence a compound's ability to cross the BBB. Using artificial intelligence (AI) algorithms to predict BBB permeability, a predicted value greater than 0.75 indicates that the compound has strong potential to cross the BBB, providing a promising starting point for CNS drug discovery.

Focused and target libraries

83
HY-L920 CNS MPO Lead-like Library
With the aging population and increasing competitive pressures, neurodegenerative diseases of the central nervous system (CNS) have become a serious medical challenge in modern society, including Parkinson's disease, Alzheimer's disease, brain tumors, and multiple sclerosis. The CNS MPO (Multi-Parameter Optimization) score is a widely recognized algorithm in medicinal chemistry. Developed by Pfizer, this method is based on an analysis of approved CNS drugs and their interior CNS drug candidates, establishing the CNS MPO rules. It incorporates six key physicochemical properties (ClogP, ClogD, MW, TPSA, HBD, and pKa) to prospectively optimize CNS drug attributes—such as high blood-brain barrier (BBB) permeability, low P-gp efflux liability, low metabolic clearance, and high safety—thereby improving the clinical success rate of CNS drug candidates. The CNS MPO compound library is a collection of compounds with CNS MPO scores greater than 5, specifically designed for CNS drug discovery.

Focused and target libraries

83
HY-L950 7-Membered Ring Privileged Scaffold Lead-like Library
Seven-membered rings are privileged medium-sized scaffolds with distinct twist-chair conformations and greater 3D diversity than five- and six-membered rings. Their flexible conformations allow induced-fit protein binding and precise pharmacophore positioning. They also modulate Fsp³, pKa and logP to enhance solubility and permeability. Azepanes, oxepanes and benzodiazepines serve as bioisosteres for hit discovery against GPCRs, ion channels and kinases. Widely found in plant and microbial alkaloids, seven-membered heterocycles show excellent biocompatibility and target affinity. They underpin many approved drugs for CNS, cancer and infectious diseases, including diazepam, imipramine and carbamazepine. Clinical candidates further highlight their unique value. However, high transannular strain and synthetic difficulty limit their availability, leaving them rare in standard screening libraries. MCE 7 Membered Scaffold Library contains 2,792 structurally diverse, lead-like molecules covering azepanes, oxepanes, benzodiazepines and dibenzazepines. With varied substitutions, chiral centers and synthetic accessibility, it fills the shortage of medium-ring scaffolds. Ideal for HTS, virtual screening and SAR studies, these novel, patent-clear compounds offer a distinctive starting point for drug discovery in CNS disorders, oncology, antivirals and challenging targets such as PPIs.

According to Lead-like Structures

83
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-17363 Dimethyl fumarate
Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research.
Keap1-Nrf2   Reactive Oxygen Species (ROS)   HIV   Autophagy   Endogenous Metabolite  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Colorectal Cancer   Viral Infection   Obesity   Lung Fibrosis  
65
HY-16950 4-Hydroxytamoxifen
4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is an orally active, selective estrogen receptor modulator (SERM). 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is also the active metabolic form of Tamoxifen (HY-13757A) in vivo and can be used to induce gene knockout in transgenic mice expressing CreER.
Estrogen Receptor/ERR  
Breast Cancer  
59
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-13771A Ursodeoxycholic acid sodium
Ursodeoxycholic acid (Ursodeoxycholate) sodium is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid sodium can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active.

Source: intestinal bacteria

G protein-coupled Bile Acid Receptor 1   FXR   Endogenous Metabolite  
Cancer   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
32
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-13771 Ursodeoxycholic acid
Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection. Orally active.
G protein-coupled Bile Acid Receptor 1   FXR   Angiotensin-converting Enzyme (ACE)   Endogenous Metabolite  
Cancer   SARS-CoV-2 Infection  
32
HY-B1511A Cyclic AMP sodium
Cyclic AMP (Cyclic adenosine monophosphate) sodium, adenosine triphosphate derivative, is an intracellular signaling molecule responsible for directing cellular responses to extracellular signals. Cyclic AMP sodium is an important second messenger in many biological processes.
Biochemical Assay Reagents  
Cancer   Neurological, Eye or Ear Disease   Metabolic or Endocrine Disease  
30
HY-B1511 Cyclic AMP
Cyclic AMP (Cyclic adenosine monophosphate), adenosine triphosphate derivative, is an intracellular signaling molecule responsible for directing cellular responses to extracellular signals. Cyclic AMP is an important second messenger in many biological processes.
Endogenous Metabolite  
Cancer   Neurological, Eye or Ear Disease   Metabolic or Endocrine Disease  
30
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-15122A Sinomenine hydrochloride
Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.
NF-κB   Opioid Receptor   Autophagy   Apoptosis  
Breast Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Depression   Pain   Digestive System Inflammation   Obesity  
23
HY-15122 Sinomenine
Sinomenine, an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.
NF-κB   Opioid Receptor   Autophagy   Apoptosis  
Breast Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Depression   Pain   Digestive System Inflammation   Obesity  
23
HY-N0164 Matrine
Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI).
PINK1/Parkin   Opioid Receptor   Autophagy   Mitophagy   Ferroptosis   Apoptosis  
Lung Cancer   Liver Cancer   Depression   Pain   Digestive System Inflammation   Parkinson's Disease  
19
HY-N0143A Phlorizin dihydrate
Phlorizin (Floridzin) dihydrate is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC50 of 0.04 μM and a Ki of 39 nM against hSGLT2, and an IC50 of 0.17 μM and a Ki of 0.31 μM against hSGLT1. Phlorizin dihydrate promotes GLUT4 translocation, inhibits gluconeogenesis and promotes glycogen synthesis by activating the PI3K/Akt/mTOR pathway. Phlorizin dihydrate reduces DNA damage and apoptosis (apoptosis) by inhibiting the NF-κB inflammatory pathway. Phlorizin dihydrate induces apoptosis via activating the Caspase pathway by antagonizing the JAK/STAT3 and PCK pathways. Phlorizin dihydrate also exhibits antibacterial, anti-inflammatory and neuroprotective activities.
SGLT   PI3K   Akt   GLUT   NF-κB   JAK   STAT   Caspase   Apoptosis   DNA/RNA Synthesis   mTOR   Bacterial  
Cancer   Neurological, Eye or Ear Disease   Bacterial Infection   Type 2 Diabetes  
18
HY-P0210 DAMGO
DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR.
Opioid Receptor  
Cancer  
16
HY-13425 Deguelin
Deguelin, a naturally occurring rotenoid, acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis. Deguelin binding to Hsp90 leads to a decreased expression of numerous oncogenic proteins, including MEK1/2, Akt, HIF1α, COX-2, and NF-κB.
Akt   Autophagy   Apoptosis  
Lung Cancer   Breast Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Pain   Digestive System Inflammation   Obesity   Lung Fibrosis  
15
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-B0418A Loperamide hydrochloride
Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist. Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect.
Opioid Receptor   Autophagy  
Cancer   Metabolic or Endocrine Disease   Depression   Pain  
13
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  
12
HY-N0270 Ononin
Ononin is an orally active isoflavone. Ononin inhibits the ERK/JNK/p38 and PI3K/Akt/mTOR pathways. Ononin regulates Apoptosis. Ononin has anti-tumor effects on laryngeal cancer and lung cancer. Ononin has neuroprotective effects. Ononin alleviates endoplasmic reticulum stress and diabetic nephropathy.
ERK   JNK   p38 MAPK   PI3K   Akt   mTOR   Apoptosis  
Lung Cancer   Breast Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Depression   Pain   Digestive System Inflammation   Glucose Metabolism   Alzheimer's Disease   Parkinson's Disease   Obesity   Lung Fibrosis   Rheumatoid Arthritis  
11
HY-N0127 Yohimbine Hydrochloride
Yohimbine hydrochloride is an alpha-2 renal adenomatase receptor inhibitor, blocking pre- and post-contact alpha-2 renal adenomatase receptors, causing the release of renal adenoma and multiple sclerosis.
Adrenergic Receptor  
Depression   Glucose Metabolism   SARS-CoV-2 Infection   Alzheimer's Disease   Hypertension  
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  
Metabolic or Endocrine Disease   Colorectal Cancer   Depression   Digestive System Inflammation   Non-Small Cell Lung Cancer   Alzheimer's Disease   Parkinson's Disease  
11
HY-N2371 27-Hydroxycholesterol
27-Hydroxycholesterol (27-OHC) is a selective estrogen receptor modulator and an agonist of the liver X receptor.
Estrogen Receptor/ERR   LXR   Endogenous Metabolite  
Prostate Cancer  
10
HY-138642 Vepdegestrant
Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM.
PROTACs   Estrogen Receptor/ERR  
Luminal Breast Cancer  
9
HY-100903 Norbinaltorphimine dihydrochloride
Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain.
Opioid Receptor  
Pain  
8
HY-17417A Naloxone
Naloxone hydrochloride is an orally active opioid receptor antagonist. Naloxone hydrochloride attenuates spinal cord stimulation‑associated anti‑hyperalgesic effects, antagonizes physiologic effects of endogenous opioid peptides linked to central nervous system injury sequelae, functions as a pressor agent to induce modest elevations in mean arterial blood pressure, exerts neuroprotective effects to improve post‑traumatic neurologic motor function, blocks opioid receptor‑mediated amnesic pathways, enhances memory consolidation, reverses Adrenocorticotropic hormone (ACTH) (HY-106373)‑ and epinephrine‑induced amnesia, and potentiates the memory‑facilitatory effects of ACTH and epinephrine.
Opioid Receptor  
Neurological, Eye or Ear Disease  
8
HY-17417 Naloxone hydrochloride
Naloxone hydrochloride is an orally active opioid receptor antagonist. Naloxone hydrochloride attenuates spinal cord stimulation‑associated anti‑hyperalgesic effects, antagonizes physiologic effects of endogenous opioid peptides linked to central nervous system injury sequelae, functions as a pressor agent to induce modest elevations in mean arterial blood pressure, exerts neuroprotective effects to improve post‑traumatic neurologic motor function, blocks opioid receptor‑mediated amnesic pathways, enhances memory consolidation, reverses Adrenocorticotropic hormone (ACTH) (HY-106373)- and epinephrine‑induced amnesia, and potentiates the memory‑facilitatory effects of ACTH and epinephrine.
Opioid Receptor  
Neurological, Eye or Ear Disease  
8
HY-P1410C D-GsMTx4 TFA
D-GsMTx4 TFA is a spider peptide and the D enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 TFA inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 TFA inhibits [Ca2+]i elevation. D-GsMTx4 TFA inhibits mTOR and PI3K-Akt signaling pathways. D-GsMTx4 TFA inhibits mechanical allodynia and thermal hyperalgesia. D-GsMTx4 TFA can be used in researches of mechanical stress, chronic pain and idiopathic pulmonary fibrosis.
Piezo Channel   Calcium Channel   mTOR   PI3K   Akt  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
6
HY-N0787 Cryptochlorogenic acid
Cryptochlorogenic acid (4-Caffeoylquinic acid) is a naturally occurring phenolic acid compound with oral effectiveness, anti-inflammatory, antioxidant and anti-cardiac hypertrophy effects. Alleviating LPS (HY-D1056) and ISO (HY-B0468) by regulating proinflammatory factor expression, inhibiting NF-κB activity, promoting Nrf2 nuclear transfer, and regulating PI3Kα/Akt/ mTOR / HIF-1α signaling pathway Induced physiological stress response.
Endogenous Metabolite   NF-κB   Keap1-Nrf2   mTOR   HIF/HIF Prolyl-Hydroxylase  
Lung Cancer   Breast Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Depression   Pain   Digestive System Inflammation   Obesity   Lung Fibrosis  
6
HY-P1410B D-GsMTx4
D-GsMTx4 is a spider peptide and the D enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 inhibits [Ca2+]i elevation. D-GsMTx4 inhibits mTOR and PI3K-Akt signaling pathways. D-GsMTx4 inhibits mechanical allodynia and thermal hyperalgesia. D-GsMTx4 can be used in researches of mechanical stress, chronic pain and idiopathic pulmonary fibrosis.
Piezo Channel   Calcium Channel   mTOR   PI3K   Akt  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
6
HY-P1290 PKA Inhibitor Fragment (6-22) amide
PKA Inhibitor Fragment (6-22) amide is a highly potent and specific competitive inhibitor of PKA, with Ki values of 1.7 nM and 1.6 nM against human and bovine PKA catalytic subunits, respectively. The IC50 of PKA Inhibitor Fragment (6-22) amide targeting bovine PKA is 8.6 nM. PKA Inhibitor Fragment (6-22) amide effectively abolishes PKA activity in mouse brain and spinal cord, and exerts in vivo efficacy via intracerebroventricular administration. PKA Inhibitor Fragment (6-22) amide significantly reverses low-dose morphine analgesic tolerance in mice and blocks photoaffinity labeling of cAMP-dependent protein kinase. PKA Inhibitor Fragment (6-22) amide can be applied to research in fields related to the mechanism of morphine analgesic tolerance and skin wound healing.
PKA  
Pain  
5
HY-N0259 Epimedin B
Epimedin B (Epmedin B) is a flavonoid active component found in Epimedium, with oral activity, and exhibits anti-osteoporotic and neuroprotective effects. Epimedin B inhibits RANKL-induced osteoclast differentiation, F-actin ring formation, and mature osteoclast bone resorption, inhibits the phosphorylation of JNK, p38 MAPK, PI3K, and AKT, activates the AMPK-Nrf2 antioxidant pathway, and reduces cellular and mitochondrial ROS. Epimedin B acts on ESR1 and exerts its effects via GPER. Epimedin B alleviates bone loss and improves bone microstructure in vivo, and in Parkinson's models protects dopaminergic neurons and maintains striatal dopamine levels through anti-apoptotic and anti-endoplasmic reticulum stress effects. Epimedin B can be used for research related to osteoporosis, diabetic osteoporosis, and Parkinson's disease.
JNK   Estrogen Receptor/ERR   p38 MAPK   PI3K   Akt   AMPK   Keap1-Nrf2   Reactive Oxygen Species (ROS)   Apoptosis   Bcl-2 Family  
Glucose Metabolism   Parkinson's Disease   Osteoporosis  
5
HY-P1290A PKA Inhibitor Fragment (6-22) amide TFA
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse antinociceptive tolerance in mice.
PKA  
Neurological, Eye or Ear Disease  
5
HY-N0876 Arenobufagin
Arenobufagin is a natural bufadienolide that can be extracted from toad venom. Arenobufagin can induce apoptosis and autophagy in human hepatocellular carcinoma cells through inhibition of PI3K/Akt/mTOR pathway. Arenobufagin has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells. Arenobufagin can inhibit VEGF-mediated angiogenesis through suppression of VEGFR-2 signaling pathway.

Source: toad

Apoptosis   Autophagy   PI3K   Akt   mTOR   PARP   Caspase   Atg8/LC3  
Liver Cancer   Pancreatic Cancer   Pain   Digestive System Inflammation  
4
HY-N2187 Deoxyshikonin
Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF. Deoxyshikonin inhibited colorectal cancer (CRC) through the PI3K/Akt/mTOR pathway. Deoxyshikonin has proangiogenesis effect and antitumor activity. Deoxyshikonin is an antibacterial agent against methicillin-resistant S. aureus (MRSA) and S. pneumonia (MIC=17 μg/mL).
Bacterial   HIF/HIF Prolyl-Hydroxylase   PI3K   Apoptosis  
Lung Cancer   Breast Cancer   Colorectal Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Bacterial Infection   Pain   Digestive System Inflammation   Cardiovascular Disease   Obesity   Lung Fibrosis   Rheumatoid Arthritis  
4
HY-P0073 Tyr-Gly-Gly-Phe-Met-OH
Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor.
Opioid Receptor  
Cancer   Depression   Pain  
4
HY-W013935 Bisphenol B
Bisphenol B is a close structural analog of Bisphenol A (BPA) (HY-18260). Bisphenol B is a potent, orally active endocrine disruptor (ED). Bisphenol B binds to G protein-coupled estrogen receptor (GPER) (IC50 = 3.3 μM) with higher affinity and agonistic activity than BPA. Bisphenol B promotes GPER mediated cell migration. Bisphenol B exerts estrogenic effects via GPER pathway at nanomolar concentration. Bisphenol B is used in the manufacture of polycarbonate resin with ED properties.
Endogenous Metabolite   Estrogen Receptor/ERR   Reactive Oxygen Species (ROS)  
Metabolic or Endocrine Disease  
3
HY-15922A Luminol sodium salt
Luminol sodium salt is a chemical that exhibits chemiluminescence with pKa values of 6.74 and 15.1. Luminol sodium salt exhibits chemiluminescence (CL) at 425 nm λmax. Luminol sodium salt is commonly used in forensics as a diagnostic tool for the detection of blood stains.
Fluorescent Dye  
3
HY-101407 Nicotinamide N-oxide
Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.
Oxidative Phosphorylation   CXCR   Drug Metabolite   Endogenous Metabolite  
Metabolic or Endocrine Disease   Gastric Cancer   Digestive System Inflammation   Rheumatoid Arthritis  
3
HY-W004284 Heptadecanoic acid
Heptadecanoic acid is an odd-chain saturated fatty acid (OCS-FA) with oral activity. Heptadecanoic acid can inhibit cell proliferation and induce Apoptosis. Heptadecanoic acid has antitumor activity. Heptadecanoic acid is associated with a number of diseases, including coronary heart disease, pre-diabetes and type 2 diabetes, and multiple sclerosis.
Apoptosis   Akt   PI3K  
Pancreatic Cancer   Cardiovascular Disease   Glucose Metabolism   Multiple Sclerosis  
3
HY-P1291 PKI 14-22 amide,myristoylated
PKI 14-22 amide, myristoylated is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated can prevent the development of morphine analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated can be used in research fields such as opioid tolerance mechanisms and antiviral drugs.
PKA   Flavivirus   Epigenetic Reader Domain  
Infection   Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pain   Obesity  
3
HY-15922 Luminol
Luminol is a chemical that exhibits chemiluminescence with pKa values of 6.74 and 15.1. Luminol exhibits chemiluminescence (CL) at 425 nm λmax. Luminol is commonly used in forensics as a diagnostic tool for the detection of blood stains.
Fluorescent Dye  
3
HY-16950A (E/Z)-4-Hydroxytamoxifen
(E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is a selective estrogen receptor modulator with mixed estrogenic and antiestrogenic activity, which is also an active metabolite of Tamoxifen (HY-13757A). (E/Z)-4-Hydroxytamoxifen is an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100-1000 nM). (E/Z)-4-Hydroxytamoxifen is promising for research of cyclical mastalgia, such as breast pain, tenderness, and nodularity.
Estrogen Receptor/ERR   Adhesion G Protein-coupled Receptors (AGPCRs)   Drug Metabolite  
Cancer   Metabolic or Endocrine Disease  
3
HY-N1414A 3′,6-Disinapoylsucrose
3′,6-Disinapoylsucrose is a type of oligosaccharide that's effective when taken orally, and it has antidepressant, anti-anxiety, and antioxidant properties. 3′,6-Disinapoylsucrose inhibits neuronal apoptosis by lowering the ratio of Bax to Bcl-2 in hippocampal neurons, and it enhances cognitive function in APP/PS1 transgenic mice by activating the CREB/BDNF signaling pathway.
Bcl-2 Family   Apoptosis  
Digestive System Disease   Prostate Cancer   Leukemia/Lymphoma/Myeloma   Ovarian Cancer   Depression   Pain   Digestive System Inflammation   Obesity  
2
HY-P3609 CR 665
CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain.
Opioid Receptor  
Depression   Pain  
2
HY-P4846 Ac-Pro-Gly-Pro-OH
Ac-Pro-Gly-Pro-OH is an endogenous degradation product of extracellular collagen and acts as a CXCR2 agonist. Ac-Pro-Gly-Pro-OH exerts bactericidal activity by generating hydrogen peroxide, inhibits pulmonary inflammation, and reduces immune cell apoptosis (apoptosis). Ac-Pro-Gly-Pro-OH promotes the production of IFN-γ and inhibits the production of TNF-α and IL-6 in leukocytes. Ac-Pro-Gly-Pro-OH increases the survival rate of mice in sepsis models, enhances the bactericidal activity of neutrophils, acts as a neutrophil chemoattractant, induces neutrophil polarization, and regulates inflammatory and repair processes. Ac-Pro-Gly-Pro-OH induces chronic inflammation and tissue remodeling through sustained action. Ac-Pro-Gly-Pro-OH is released via alkaline hydrolysis of corneal proteins in alkali-injured eyes, thereby driving the early infiltration of neutrophils into the cornea. Ac-Pro-Gly-Pro-OH is applicable to research related to sepsis, chronic obstructive pulmonary disease, cystic fibrosis, bronchiolitis obliterans syndrome, severe asthma, idiopathic pulmonary fibrosis, and corneal ulcer.
CXCR   Apoptosis   IFNAR   TNF Receptor   Interleukin Related  
Infection   Allergy  
2
HY-N2447 Amarogentin
Amarogentin is a secoiridoid glycoside that is mainly extracted from Swertia and Gentiana roots. Amarogentin exhibits many biological effects, including anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin exerts hepatoprotective and immunomodulatory effects. Amarogentin promotes apoptosis, arrests G2/M cell cycle and downregulates of PI3K/Akt/mTOR signalling pathways. Amarogentin exerts beneficial vasculo-metabolic effect by activating AMPK.
AMPK   Apoptosis  
Liver Cancer   Glucose Metabolism  
2
HY-N2312 Mogrol
Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.
ERK   STAT  
Inflammation or Immune System Disease   Lung Cancer   Breast Cancer   Colorectal Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Pain   Obesity   Lung Fibrosis  
2
HY-N6950 Hederacolchiside A1
Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro.
PI3K   Akt   mTOR   Parasite   Apoptosis  
Breast Cancer   Pancreatic Cancer   Parasitic Infection   Pain   Digestive System Inflammation  
2
HY-P1333 Dynorphin A
Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease.
Opioid Receptor   Apoptosis   Caspase   Endogenous Metabolite  
Neurological, Eye or Ear Disease  
2
HY-N9481 Lipoteichoic acid
Lipoteichoic acid is an orally effect anti-inflammatory and antitumor agent. Lipoteichoic acid is a crucial immune molecule in Gram-positive bacteria that activates the complement system by inducing C3 and inhibiting CD55. Lipoteichoic acid regulates macrophage autophagy through the PI3K/Akt/mTOR pathway. Lipoteichoic acid induces lung damage in mice. Lipoteichoic acid inhibits the production of melanin.

Source: Staphylococcus aureus

Complement System   Autophagy   mTOR   Akt   PI3K   ERK   Interleukin Related  
Infection   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
2
HY-P0288 [Leu5]-Enkephalin
[Leu5]-Enkephalin is a pentapeptide with morphine like properties. [Leu5]-Enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.
Opioid Receptor   Endogenous Metabolite  
Depression   Pain  
2
HY-W040074 Glycylglycine hydrochloride hydrate
Glycylglycine hydrochloride hydrate is a non-selective Glycylglycine hydrochloride hydrate dipeptidase substrate and iNOS inhibitor. Glycylglycine hydrochloride hydrate can cross the cell membrane by passive diffusion and is hydrolyzed to glycine in the cell, participating in energy metabolism and antioxidant processes. Glycylglycine hydrochloride hydrate promotes spermatogonial stem cells (SSCs) proliferation, inhibits astrocyte overactivation and reduces nitric oxide (NO) release, while upregulating the expression of neurotrophic factors (such as PDGFA, FGF2, CNTF) to support nerve myelin repair. Glycylglycine hydrochloride hydrate can be used to study male reproductive biology (such as SSCs proliferation regulation) and neurodegenerative diseases (such as neuroprotective mechanisms in multiple sclerosis).
Biochemical Assay Reagents  
Metabolic or Endocrine Disease  
1
HY-B0298AS Clemastine-d5 fumarate
Clemastine (HS-592; Meclastine)-d5 fumarate is the deuterium labeled Clemastine fumarate. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
Isotope-Labeled Compounds   mAChR   p62   IKK   Apoptosis   Keap1-Nrf2   mTOR   Histamine Receptor   Pyroptosis   Autophagy  
Neurological, Eye or Ear Disease   Metabolic or Endocrine Disease  
1
HY-P1342A Prosaptide Tx14(A) TFA
Prosaptide Tx14(A) TFA, a prosaposin-derived peptide, is a potent GPR37L1 and GPR37 agonist with EC50s of 5 and 7 nM, respectively. Prosaptide Tx14(A) TFA increases both ERK1 and ERK2 phosphorylation in Schwann cells.
ERK  
Neurological, Eye or Ear Disease  
1
HY-P1597 Malantide
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.
PKA   PKC  
Cancer  
1
HY-P2261 STAD 2
STAD 2 is a potent and selective disruptor of PKA-RII, with a Kd of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism.
PKA  
Infection  
1
HY-P99891 Rovelizumab
Rovelizumab is a humanized monoclonal leukointegrin antibody. Rovelizumab is a monoclonal antibody directed against the CD11/CD18 cell adhesion proteins. Rovelizumab can be used for research of multiple sclerosis (MS), hemorrhagic shock, myocardial infarction (MI) and stroke.

Species: Human

Integrin  
Blood or Cardio-cerebrovascular Disease  
1
HY-N2411 Geissoschizine methyl ether
Geissoschizine methyl ether is an orally active, blood-brain barrier permeable alkaloid, and a partial agonist of the 5-HT1A receptor. It can be isolated from Uncaria hook. Geissoschizine methyl ether potently inhibits the binding of [3H]8-OH-DPAT to the 5-HT1A receptor in a concentration-dependent manner, with an IC50 of 0.904 μM. It ameliorates isolation-induced increased aggression and reduced sociability in mice. Geissoschizine methyl ether promotes oligodendrocyte differentiation and remyelination in the medial prefrontal cortex of adult mice.
5-HT Receptor  
Neurological, Eye or Ear Disease  
1
HY-P99524 Vatelizumab
Vatelizumab (GBR500) is a monoclonal antibody that targets the α2 subunit (CD49b) of very late antigen 2 (VLA-2). Vatelizumab can be used for research on multiple sclerosis.

Species: Human

Integrin  
Multiple Sclerosis  
1
HY-P5982 PTPσ Inhibitor, ISP
PTPσ Inhibitor, ISP is a PTPσ intracellular wedge domain mimetic peptide containing a TAT cell-penetrating domain, which acts as a PTPσ inhibitor. PTPσ Inhibitor, ISP binds to and inhibits PTPσ, thereby relieving CSPG-mediated axonal growth inhibition. PTPσ Inhibitor, ISP enhances CSPG degradation by promoting the secretion of Cathepsin B or MMP-2, and promotes DRG axonal growth, OPC migration and remyelination. PTPσ Inhibitor, ISP promotes nerve regeneration and improves sensory, motor and urinary functions in animal models of spinal cord injury, dorsal root injury and multiple sclerosis. PTPσ Inhibitor, ISP also increases the phosphorylation of ERK and AKT in colorectal cancer cells. PTPσ Inhibitor, ISP can be used in studies related to PTPσ/CSPG signaling, nerve regeneration, demyelinating diseases and RAS/ERK signaling.
Phosphatase   Transmembrane Glycoprotein   MMP   ERK   Akt   Cathepsin  
Neurological, Eye or Ear Disease   Colorectal Cancer  
1
HY-P1422A Spadin TFA
Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC50 value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research.
Potassium Channel   5-HT Receptor  
Neurological, Eye or Ear Disease  
1
HY-N10574A Queuine dihydrochloride
Queuine dihydrochloride is a selective substrate for tRNA guanine transglycosylase (TGT) and can be incorporated into eukaryotic tRNA. Queuine dihydrochloride promotes tRNA modification, affecting mitochondrial function and Warburg metabolic phenotype. If Queuine dihydrochloride is deficient, aerobic glycolysis can be enhanced, oxidative phosphorylation can be inhibited, and Warburg metabolism can be promoted, accompanied by increased ammonia and lactate production and increased lactate dehydrogenase activity. Queuine dihydrochloride can be used for autoimmune diseases (such as experimental models of multiple sclerosis) and cancer metabolic regulation, and its deficiency is associated with low tRNA modification in tumor cells.

Source: eubacteria

Others  
Metabolic or Endocrine Disease  
1
HY-N6983 Licoricesaponin G2
Licoricesaponin G2 is an orally active component found in Licorice. Licoricesaponin G2 significantly ameliorates Bleomycin (HY-108345)-induced pulmonary fibrosis by inhibiting the TNF-α signaling pathway, reducing epithelial-mesenchymal transition, and decreasing extracellular matrix deposition. Licoricesaponin G2 inhibits cancer cells proliferation, migration, inhibits PI3K/AKT/mTOR signaling pathway and increases ROS production. Licoricesaponin G2 can be used for the research of lung cancer and pulmonary fibrosis.
TNF Receptor   PI3K   Akt   mTOR   Reactive Oxygen Species (ROS)  
Lung Cancer   Pulmonary Disease  
1
HY-W011927S 4,4'-Sulfonyldiphenol-d8
4,4'-Sulfonyldiphenol-d8 (Bisphenol S (4,4'-Sulfonyldiphenol)-d8) is the deuterium labeled 4,4'-Sulfonyldiphenol (HY-W011927).4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone), a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC50 values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.
Isotope-Labeled Compounds   Estrogen Receptor/ERR   Histone Methyltransferase   Thyroid Hormone Receptor   PI3K   Akt   mTOR   Androgen Receptor  
Cancer   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
1
HY-113478S Ursodeoxycholic acid-d4
Ursodeoxycholic acid-2,2,4,4-d4 is the deuterium labeled Ursodeoxycholic acid (HY-13771). Ursodeoxycholic acid is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection.
Isotope-Labeled Compounds  
Metabolic or Endocrine Disease  
1
HY-N1420A Rhamnose monohydrate
Rhamnose monohydrate (L-Rhamnose monohydrate) is an orally active deoxysugar. Rhamnose monohydrate can inhibit levels of pro-inflammatory interleukin and matrix metalloproteinases (MMPs) in skin aging models. Rhamnose can promote the phosphorylation levels of PKA substrates and HSL in SVF-derived adipocytes, stimulating PKA signaling. Rhamnose monohydrate can act against obesity in mice by stimulating fat dopamine receptors and inducing thermogenesis. Rhamnose monohydrate shows anti-aging effects. Rhamnose monohydrate can be used in the study of Ehrlich’s solid tumors and sarcomas.

Source: Widespread

Endogenous Metabolite   MMP   Interleukin Related   PKA  
Infection   Metabolic or Endocrine Disease   Pancreatic Cancer   Pain   Digestive System Inflammation   Lung Fibrosis  
1
HY-P1422 Spadin
Spadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC50 value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research.
Potassium Channel   5-HT Receptor  
Neurological, Eye or Ear Disease  
1
HY-P0248 Kemptide
Kemptide is a synthetic heptapeptide that acts as a specific substrate for cAMP-dependent protein kinase (PKA).
PKA  
Metabolic or Endocrine Disease  
1
HY-128700 Nicotinic acid mononucleotide
Nicotinic acid mononucleotide acts as a SARM1 inhibitor and a NAD+ biosynthesis intermediate, with an IC50 value of 93.3 μM against SARM1. Nicotinic acid mononucleotide exerts axon-protective effects, delays axonal degeneration, elevates NAD+ levels, enhances Sirt1 activity, improves myocardial capillary density and alleviates myocardial fibrosis. Nicotinic acid mononucleotide reverses diabetic cardiomyopathy in diabetic mice by increasing myocardial NAD+ levels. Nicotinic acid mononucleotide is applicable to research related to cancer, multiple sclerosis, diabetic cardiomyopathy, neurodegenerative diseases and Huntington's disease.
Endogenous Metabolite   Sirtuin  
Cancer   Huntington's Disease   Multiple Sclerosis  
1
HY-W105750 6-Hydroxyhexanoic acid
6-Hydroxyhexanoic acid (6-HHA) is a bacterial effector molecule with metabolic and immunomodulatory activities. 6-Hydroxyhexanoic acid activates the JAK1-STAT1 signaling pathway, promotes phenotypic conversion of M2 macrophages to M1 macrophages, and exerts anti-tumor effects by regulating macrophage polarization. 6-Hydroxyhexanoic acid inhibits lipolysis in adipocytes mediated by Gαi family GPCR, and reduces high-fat diet-induced weight gain and obesity. 6-Hydroxyhexanoic acid can be used in studies related to pancreatic ductal adenocarcinoma, obesity, and insulin resistance.
JAK   STAT   Adenylate Cyclase  
Pancreatic Ductal Adenocarcinoma   Insulin Resistance   Obesity  
1
HY-P1023 VIP(6-28)(human, rat, porcine, bovine)
VIP(6-28)(human, rat, porcine, bovine) is an effective antagonist of the actions of exogenous vasoactive intestinal peptide (VIP) on cAMP.
GCGR  
Metabolic or Endocrine Disease  
1
HY-12664 AF64394
AF64394 is a GPR3 inverse agonist, with a pIC50 of 7.3.
Orphan GPCR  
1
HY-B0188A Mianserin hydrochloride
Mianserin hydrochloride (Org GB 94) is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy.
Histamine Receptor   Opioid Receptor   ERK   p38 MAPK  
Metabolic or Endocrine Disease   Depression   Parkinson's Disease  
1
HY-D0889 Glycylglycine
Glycylglycine is a non-selective glycylglycine dipeptidase substrate and iNOS inhibitor. Glycylglycine can cross the cell membrane by passive diffusion and is hydrolyzed to glycine in the cell, participating in energy metabolism and antioxidant processes. Glycylglycine promotes spermatogonial stem cells (SSCs) proliferation, inhibits astrocyte overactivation and reduces nitric oxide (NO) release, while upregulating the expression of neurotrophic factors (such as PDGFA, FGF2, CNTF) to support nerve myelin repair. Glycylglycine can be used to study male reproductive biology (such as SSCs proliferation regulation) and neurodegenerative diseases (such as neuroprotective mechanisms in multiple sclerosis).
Endogenous Metabolite  
Neurodegenerative Disease   Male Reproductive System Disease  
1
HY-P1342 Prosaptide Tx14(A)
Prosaptide Tx14(A), a prosaposin-derived peptide, is a potent GPR37L1 and GPR37 agonist with EC50s of 5 and 7 nM, respectively. Prosaptide Tx14(A) increases both ERK1 and ERK2 phosphorylation in Schwann cells.
Neurological, Eye or Ear Disease  
1
HY-160187 AAA
AAA is an orally active 20-HETE receptor antagonist. AAA exerts antihypertensive and organoprotective effects. AAA blocks 20-HETE prohypertensive actions, suppresses intrarenal and circulating angiotensin II levels, and interferes with renin-angiotensin system interactions. AAA attenuates development of, and reverses established, ANG II (HY-13948)-dependent malignant hypertension. AAA reduces albuminuria, glomerulosclerosis, and cardiac hypertrophy linked to malignant hypertension. AAA can be used for the research of malignant hypertension.
Orphan GPCR   Angiotensin Receptor  
Hypertension  
1
HY-N10574 Queuine
Queuine is a selective substrate for tRNA guanine transglycosylase (TGT) and can be incorporated into eukaryotic tRNA. Queuine promotes tRNA modification, affecting mitochondrial function and Warburg metabolic phenotype. If Queuine is deficient, aerobic glycolysis can be enhanced, oxidative phosphorylation can be inhibited, and Warburg metabolism can be promoted, accompanied by increased ammonia and lactate production and increased lactate dehydrogenase activity. Queuine can be used for autoimmune diseases (such as experimental models of multiple sclerosis) and cancer metabolic regulation, and its deficiency is associated with low tRNA modification in tumor cells.

Source: eubacteria

Bacterial  
Metabolic or Endocrine Disease  
1
HY-N1420 Rhamnose
Rhamnose (L-Rhamnose ) is an orally active deoxysugar. Rhamnose can inhibit levels of pro-inflammatory interleukin and matrix metalloproteinases (MMPs) in skin aging models. Rhamnose can promote the phosphorylation levels of PKA substrates and HSL in SVF-derived adipocytes, stimulating PKA signaling. Rhamnose can act against obesity in mice by stimulating fat dopamine receptors and inducing thermogenesis. Rhamnose shows anti-aging effects. Rhamnose monohydrate can be used in the study of Ehrlich’s solid tumors and sarcomas.

Source: Widespread

Endogenous Metabolite   Interleukin Related   MMP   PKA  
Pancreatic Cancer   Bacterial Infection   Digestive System Inflammation   Obesity  
1
HY-W012980 Isovaleric acid
Isovaleric acid is an oral active short-chain fatty acid that inhibits osteoclast differentiation by stimulating AMPK phosphorylation and promotes colonic smooth muscle relaxation by activating the cAMP/PKA pathway. Isovaleric acid can be used in research on skeletal diseases (such as osteoporosis) and intestinal disorders.
Endogenous Metabolite   AMPK   PKA  
Pancreatic Cancer   Osteoporosis  
1
HY-P99113 Inebilizumab
Inebilizumab is an anti-CD19 monoclonal antibody (mAb) with enhanced antibody-dependent cell-mediated cytotoxicity against B cells. Inebilizumab can be used for multiple sclerosis and neuromyelitis optica research.

Species: Human

ADC Antibodies   CD19  
Myasthenia gravis   Multiple Sclerosis  
1
HY-P80120 Epac1 Antibody (YA459)
Epac1 Antibody (YA459) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Epac1.

Host: Rabbit; Reactivity: Human, Mouse

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

1
HY-15371G Forskolin (GMP)
Forskolin (Coleonol) (GMP) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin (GMP) is also an inducer of intracellular cAMP formation. Forskolin (GMP) induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin (GMP) exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin (GMP) also induces autophagy.
Adenylate Cyclase   FXR   Autophagy   PKC  
Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-B1203S Fludrocortisone-d5
Fludrocortisone-d5 (9α-Fludrocortisone-d5) is the deuterium labeled Fludrocortisone (HY-B1203). Fludrocortisone is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency.
Isotope-Labeled Compounds   Mineralocorticoid Receptor   Glucocorticoid Receptor   Apoptosis  
Cancer   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-184075S Nomelcitinib
Nomelcitinib is a TYK2 inhibitor that modulates the IL23 signaling pathway. Nomelcitinib is used for research on multiple sclerosis, rheumatoid arthritis, inflammatory bowel disease, systemic lupus erythematosus, psoriasis, psoriatic arthritis, Crohn's disease, Sjögren's syndrome, and scleroderma.
JAK   Interleukin Related  
Digestive System Disease   Digestive System Inflammation   Systemic Lupus Erythematosus   Multiple Sclerosis   Crohn's Disease   Psoriasis   Rheumatoid Arthritis  
/
HY-139521S Doxepin-d3
Doxepin-d3 is the deuterated-labeled Doxepin (HY-B0725A). Doxepin is an orally active, blood-brain barrier penetrant tricyclic antidepressant with multiple activities including hypnosis, sedation, analgesia and vasodilation. Doxepin enhances the expression of PSD-95 and synapsin 1 via the PI3K/AKT/mTOR signaling pathway, and is metabolized to Desmethyldoxepin in vivo. Doxepin can be used in research related to various diseases such as depression, anxiety, obesity and atopic dermatitis.
Isotope-Labeled Compounds   Akt   mTOR   Drug Intermediate  
Depression   Atopic Dermatitis   Obesity  
/
HY-B1139S Tolperisone-d10 hydrochloride
Tolperisone-d10 (hydrochloride) is the deuterium labeled Tolperisone hydrochloride. Tolperisone hydrochloride is a centrally acting muscle relaxant, is indicated for use in the treatment of pathologically increased tone of the cross-striated muscle caused by neurological diseases (damage of the pyramidal tract, multiple sclerosis, myelopathy, encephalomyelitis) and of spastic paralysis and other encephalopathies manifested with muscular dystonia.
Isotope-Labeled Compounds  
Neurological, Eye or Ear Disease  
/
HY-N19702 Calphostin B
Calphostin B is a protein kinase C (PKC) inhibitor with an IC50 of 1.04 μM in rats and an IC50 of 22.9 μM for bovine cyclic adenosine monophosphate-dependent protein kinase (PKA). Calphostin B bears aromatic structures at positions C-14 and C-17, which accounts for its higher selectivity for PKC over PKA. Calphostin B can be used in studies related to human cervical cancer and human breast cancer.

Source: Cladosporium cladosporioides

PKC   PKA  
Breast Cancer   Cervical Cancer  
/
HY-P991351 RTX-002
RTX-002 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. RTX-002 can be used to study autoimmune diseases such as systemic lupus erythematosus and multiple sclerosis.

Species: Human

PD-1/PD-L1  
Inflammation or Immune System Disease  
/
HY-B1511G Cyclic AMP (GMP)
Cyclic AMP (GMP) (Cyclic adenosine monophosphate (GMP)) is Cyclic AMP (HY-B1511) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Cyclic AMP (Cyclic adenosine monophosphate), adenosine triphosphate derivative, is an intracellular signaling molecule responsible for directing cellular responses to extracellular signals. Cyclic AMP is an important second messenger in many biological processes.
Endogenous Metabolite  
Cancer   Neurological, Eye or Ear Disease   Metabolic or Endocrine Disease  
/
HY-P990248 Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1)
Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) is an anti-mouse E-Cadherin/CD324 IgG1 monoclonal antibody. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can downregulate the HER signaling axis and PI3K/Akt/mTOR signaling pathway. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can inhibit the proliferation of tumor cells and induce their apoptosis. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can be used for researches on cancer and inflammation conditions such as breast cancer, chronic compression injury (CCI) and asthma.

Species: Mouse

Cadherin   EGFR   PERK   Akt   mTOR  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Breast Cancer  
/
HY-D1187 2-Aza-ε-cAMP
2-Aza-ε-cAMP is a multifunctional dye. Dyes are important tools in biological experiments. They can help researchers observe and analyze cell structures, track biomolecules, evaluate cell functions, distinguish cell types, detect biomolecules, study tissue pathology and monitor microorganisms. Their applications range from basic scientific research to clinical A wide range of diagnostics. Dyes are also widely used in traditional fields such as textile dyeing, as well as in emerging fields such as functional textile processing, food pigments and dye-sensitized solar cells.
Fluorescent Dye  
/
HY-P1052 Myelin Basic Protein(87-99)
Myelin Basic Protein(87-99) is an encephalitogenic peptide that induces basic protein-specific T cell proliferation. Myelin Basic Protein(87-99) causes a Th1 polarization in peripheral blood mononuclear cells with is implicated of multiple sclerosis (MS).
Others  
Inflammation or Immune System Disease  
/
HY-P10833 C-VGB3
C-VGB3 is a selective vascular endothelial growth factor receptor 2 (VEGFR2) antagonist, which inhibits VEGFR2-mediated PI3K/AKT/mTOR and PLCγ/ERK1/2 signaling pathways. C-VGB3 binds to the extracellular domain of VEGFR2, blocking ligand-receptor interaction and inducing apoptosis in endothelial and tumor cells through both intrinsic (involving Bcl2 family and caspases) and extrinsic (death receptor-mediated) pathways. C-VGB3 is promising for research of angiogenesis-related cancers, such as breast cancer.
VEGFR   PI3K   Akt   mTOR   ERK   Apoptosis  
Blood or Cardio-cerebrovascular Disease  
/
HY-14153S Tegaserod-d11
Tegaserod-d11 is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research.
5-HT Receptor   Apoptosis   Isotope-Labeled Compounds  
Metabolic or Endocrine Disease  
/
HY-13599S4 Cladribine-13C,15N2
Cladribine-13C,15N2 (2-Chloro-2′-deoxyadenosine-13C,15N2) is the 13C- and 15N-labeled Cladribine (HY-13599). Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active?adenosine deaminase?inhibitor. Cladribine functions as an inhibitor of?DNA synthesis?to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.
Isotope-Labeled Compounds   Adenosine Deaminase   Apoptosis  
Cancer   Blood or Cardio-cerebrovascular Disease  
/
HY-N0378AGL D-Mannitol, M200 (GMP Like)
D-Mannitol, M200 (GMP Like) (Mannitol, M200 (GMP Like)) is the GMP Like class D-Mannitol that can be used as pharmaceutical excipients. D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells.
Endogenous Metabolite   PGC-1α   Adrenergic Receptor   Apoptosis   PKA  
Cancer   Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
/
HY-12355S Siponimod-d11
Siponimod-d11 (BAF-312-d11) is deuterium labeled Siponimod (HY-12355). Siponimod is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis.
Isotope-Labeled Compounds   Potassium Channel   LPL Receptor  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
/
HY-106605S Flumezapine-d8 hydrochloride
Flumezapine-d8 (LY 120363-d8) hydrochloride is deuterated labeled Flumezapine hydrochloride. Flumezapine hydrochloride is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine hydrochloride does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine hydrochloride inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine hydrochloride can be used in antipsychotic research.
Isotope-Labeled Compounds   Dopamine Receptor   5-HT Receptor  
/
HY-P10992 YVPGP
YVPGP is an oligopeptide exacted from Anthopleura anjunae. YVPGP has a significant antitumor activity by mediating PI3K/AKT/mTOR signaling pathway. YVPGP arrests DU-145 cells in the S phase and induces apoptosis via mitochondrial and death receptor pathways (caspase3, 7, 8, 9). YVPGP effectively inhibits tumor growth in DU-145 xenografts mice model, promising for prostate cancer research.
PI3K   Akt   mTOR   Caspase   Apoptosis   Bcl-2 Family  
/
HY-116755S2 Tiropramide-d5 oxalate
Tiropramide-d5 oxalate (CR 605-d5 oxalate) is the deuterium labeled Tiropramide oxalate. Tiropramide (CR 605) is a tyrosine derivative with antispastic properties. Tiropramide hydrochloride inhibits phosphodiesterase activity involved in cAMP catabolism in rabbit colon homogenates. Tiropramide relaxes smooth muscle in rabbit isolated colon. Tiropramide can be used for the research of irritable colon and biliary dyskinesia.
Isotope-Labeled Compounds   Phosphodiesterase (PDE)  
Neurological, Eye or Ear Disease  
/
HY-N3464 Isopedicin
Isopedicin potently and concentration-dependently inhibits superoxide anion (O2 U?) production in formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP)-activated cells. Isopedicin increases cAMP formation and PKA activity in FMLP-activated cells by inhibiting phosphodiesterase (PDE) activity.
Phosphodiesterase (PDE)  
Metabolic or Endocrine Disease  
/
HY-P3541 Dirucotide
Dirucotide (MBP8298) is a synthetic peptide that consists of 17 amino acids linked in a sequence identical to that of a portion of human myelin basic protein. Dirucotide can be used for the research in autoimmune disorder of the central nervous system, such as Multiple sclerosis (MS).
Others  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
/
HY-P5907 Helianorphin-19
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain.
Opioid Receptor  
Neurological, Eye or Ear Disease  
/
HY-P991725 Velvakiment
Velvakiment is a humanized VHH nanobody that targets IL-17A. Velvakiment can be used for autoimmune diseases such as multiple sclerosis and rheumatoid arthritis research.

Species: Human

Interleukin Related  
Inflammation or Immune System Disease  
/
HY-B0364AS Dyclonine-d9 hydrochloride
Dyclonine-d9 hydrochloride (Dyclocaine-d9 hydrochloride) is the deuterated-labeled Dyclonine hydrochloride (HY-B0364A). Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis.
Isotope-Labeled Compounds   TRP Channel   Aldehyde Dehydrogenase (ALDH)   Cholinesterase (ChE)   Keap1-Nrf2   Amyloid-β   Fungal   Apoptosis  
Cancer   Fungal Infection   Neurodegenerative Disease   Skin Inflammation  
/
HY-P4497 Prolylserine
Prolylserine, a dipeptide, is an inhibitor of melanogenesis production in Mel-Ab cells. Prolylserine decreases expression of microphthalmia-associated transcription factor (MITF) and tyrosinase, induces phorphosylation of ERK, but not cAMP response element binding protein (CREB).
ERK  
Cancer  
/
HY-175483S TrkB activator-1
TrkB activator-1 is a specific, orally active and brain-penetrant tropomyosin receptor kinase B (TrkB) activator. TrkB activator-1 shows potent antidepressant effects through activation of the activates the BDNF (brainderived neurotrophic factor)-Tropomyosin-related kinase B (TrkB)-CREB (cAMP response element binding protein) signaling aixs. TrkB activator-1 increaes neuroplasticity. TrkB activator-1 can be used for the research of neurological disease, such as depression.
Trk Receptor   Isotope-Labeled Compounds  
Neurological, Eye or Ear Disease  
/
HY-P991596 ANB004
ANB004 is a humanized monoclonal antibody inhibitor, targeting IL-17. ANB004 can be used for autoimmune and inflammatory diseases like multiple sclerosis and rheumatoid arthritis (RA) research.

Species: Human

Interleukin Related  
Inflammation or Immune System Disease  
/
HY-P3786 H-Arg-Gly-Tyr-Ala-Leu-Gly-OH
H-Arg-Gly-Tyr-Ala-Leu-Gly-OH is a competitive and CAMP dependent protein kinase inhibitor.
PKA   PKC  
Cancer  
/
HY-P3930 PKI (5-24),amide
PKI (5-24),amide (IP20-amide) is a 20-residue peptide that corresponds to the active portion of the heat-stable inhibitor protein of cAMP-dependent protein kinase. PKI (5-24),amide is a potent cAMP-dependent protein kinase (PKA) (PKA) inhibitor with a Ki of 2.3 nM.
PKA  
Neurological, Eye or Ear Disease  
/
HY-P10522 MBP Ac1-9
MBP Ac1-9 refers to a peptide fragment of myelin basic protein (MBP). MBP Ac1-9 is an immunodominant epitope in the experimental autoimmune encephalomyelitis (EAE) model, which can induce T cell immune response and lead to pathological changes similar to multiple sclerosis. MBP Ac1-9 can be used to study T cell activation and autoimmune response.
Others  
/
HY-D1187A 2-Aza-ε-cAMP sodium
2-Aza-ε-cAMP (sodium) is a multifunctional dye. Dyes are important tools in biological experiments. They can help researchers observe and analyze cell structures, track biomolecules, evaluate cell functions, distinguish cell types, detect biomolecules, study tissue pathology and monitor microorganisms. Their applications range from basic scientific research to clinical A wide range of diagnostics. Dyes are also widely used in traditional fields such as textile dyeing, as well as in emerging fields such as functional textile processing, food pigments and dye-sensitized solar cells.
Fluorescent Dye  
/
HY-N12399 Aplithianines A
Aplithianines A is a potent inhibitor against J-PKAcα with an IC50 of 1 μM , and inhibits wild-type PKA with an IC50 of 84 nM. Aplithianines A inhibits J-PKAcα catalytic activity by competitively binding to the ATP pocket.

Source: Aplidium sp.

PKA  
Inflammation or Immune System Disease  
/
HY-P991746 Anti-Mouse CXCR2 Antibody (Cx2Mab-1)
Anti-Mouse CXCR2 Antibody (Cx2Mab-1) reacts with mouse CXCR2 targeting the N-terminal extracellular domain of CXCR2. Recommend Isotype Controls: Rat IgG2b kappa, Isotype Control (HY-P990682).

Species: Mouse

CXCR  
Cancer  
/
HY-P11046 IIIM1
IIIM1 is an orally active anti-inflammatory peptide. IIIM1 ameliorates the symptoms of experimental autoimmune encephalomyelitis (EAE) by stimulating the proliferation of regulatory T cells and inducing them to produce RA1, and regulating the cytokine balance. IIIM1 can be used in the research of multiple sclerosis (MS).
Interleukin Related  
Inflammation or Immune System Disease  
/
HY-P10047 PKItide
PKItide exhibits an IC50 of 0.2 μM for cAMP-PK.
PKA  
/
HY-119695AS Simvastatin acid-d6 ammonium
Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
Isotope-Labeled Compounds   Endogenous Metabolite  
Blood or Cardio-cerebrovascular Disease  
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HY-N3550 Catalponol
Catalponol is a naphthoquinone derivative. Catalponol enhances dopamine biosynthesis by inducing tyrosine hydroxylase activity. Catalponol also increases the levels of cAMP and tyrosine hydroxylase phosphorylation in PC12 cells.
Others  
Cancer  
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HY-P3724 MBP (146-170)
MBP (146-170) is a myelin basic protein (MBP). MBP (146-170) can be used for the research of multiple sclerosis (MS).
Others  
Inflammation or Immune System Disease  
/
HY-N10319R Artepillin C (Standard)
Artepillin C (Standard) is the analytical standard of Artepillin C (HY-N10319). This product is intended for research and analytical applications. Artepillin C is an orally active CREB/CRTC2 inhibitor and TRPA1 covalent agonist (EC50=1.8 μM). Artepillin C inhibits CREB/CRTC2-mediated gene transcription and downregulates BMAL1 expression to regulate glucose and lipid metabolism. Artepillin C can also activate TRPA1 channels to induce spicy taste signals. Artepillin C can inhibit tumor cell proliferation, induce apoptosis, improve insulin resistance and inhibit liver lipid synthesis. Artepillin C can be used in the study of metabolic syndrome, tumor prevention and treatment, and inflammation.
Reference Standards   TRP Channel   Necroptosis   Epigenetic Reader Domain  
Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
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HY-W145108 Methyl red hydrochloride
Methyl red hydrochloride is a pH-sensitive acid-base indicator and colorimetric reagent with a pKa of 5.1. Methyl red hydrochloride achieves visual judgment of the titration endpoint through reversible structural changes of protonation (red, pH < 4.4) and deprotonation (yellow, pH > 6.2). Methyl red hydrochloride is widely used in acid-base titration in chemical analysis and buffer pH monitoring in biochemistry.
Fluorescent Dye  
/
HY-124371 Amentoflavone hexaacetate
Amentoflavone hexaacetate is a 3,5-cyclic nucleotide phosphodiesterase inhibitor with antiplatelet aggregation activity. Amentoflavone hexaacetate can inhibit the aggregation of eluted human platelets induced by ADP or collagen. Amentoflavone hexaacetate can also inhibit the cAMP phosphodiesterase activity in human platelets. Amentoflavone hexaacetate can significantly increase the cAMP level of platelets in the presence of prostaglandin E1. Amentoflavone hexaacetate has anti-angiogenic and anti-metastatic effects.
Phosphodiesterase (PDE)  
Blood or Cardio-cerebrovascular Disease  
/
HY-B1203S1 Fludrocortisone-d2
Fludrocortisone-d2 (9α-Fludrocortisone-d2) is the deuterium labeled Fludrocortisone (HY-B1203). Fludrocortisone is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency.
Isotope-Labeled Compounds   Mineralocorticoid Receptor   Glucocorticoid Receptor   Apoptosis  
Cancer   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-P11092 TLQP-62 (mouse,rat)
TLQP-62 (mouse,rat) is a secreted C-terminal peptide that can be derived from protein VGF. TLQP-62 activates the BDNF-TrkB signaling pathway, inducing acute, transient phosphorylation of TrkB receptor and downstream CREB (Ser133) phosphorylation. TLQP-62 demonstrates excellent efficacy in promoting long-term fear memory formationin wild-type mice and reversing memory impairment in VGF heterozygous knock-out mice. TLQP-62 can be used for the study of memory-related neurological disorders (e.g., Alzheimer’s disease, frontotemporal dementia).
Endogenous Metabolite  
Neurological, Eye or Ear Disease  
/
HY-13771S1 Ursodeoxycholic acid-13C
Ursodeoxycholic acid-13C is the 13C labeled Ursodeoxycholic acid. Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active.
Isotope-Labeled Compounds   G protein-coupled Bile Acid Receptor 1   FXR   Endogenous Metabolite  
Cancer  
/
HY-13749S2 Sitagliptin-d4
Sitagliptin-d4 (MK-0431-d4) is deuterium labeled Sitagliptin (HY-13749). Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
Isotope-Labeled Compounds   ERK   PKA   Dipeptidyl Peptidase   GLP Receptor   Endogenous Metabolite  
Metabolic or Endocrine Disease  
/
HY-153660S Bivamelagon-d8
Bivamelagon-d8 (MC-4R Agonist 2-d8) is the deuterium labeled Bivamelagon (HY-153660). Bivamelagon (MC-4R Agonist 2) is an orally active MC4R agonist with EC50 values of 0.562 nM (Luci assay) and 36.5 nM (cAMP assay), and a Ki of 65 nM. Bivamelagon can be used for the research of diseases such as obesity and diabetes.
Isotope-Labeled Compounds   Melanocortin Receptor  
Metabolic or Endocrine Disease  
/
HY-17453S Salmeterol-d3 xinafoate
Salmeterol-d3 (xinafoate) is the deuterium labeled Salmeterol xinafoate. Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
Isotope-Labeled Compounds   Adrenergic Receptor  
Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
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HY-P1996 Tiplimotide
Tiplimotide (NBI-5788) is an altered peptide ligand (APL) designed from an immunodominant region (83-99) of the neuroantigen myelin basic protein (MBP). Tiplimotide can selectively reduce the production of inflammatory cytokines by pathogenic T-cells. Tiplimotide can be used for the research of multiple sclerosis (MS).
Others  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
/
HY-W751179 Midostaurin-13C6
Midostaurin-13C6 (PKC412-13C6) is the 13C-labeled Midostaurin (HY-10230). Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects.
Isotope-Labeled Compounds   PKC   VEGFR   NO Synthase   Apoptosis   c-Kit  
Cancer  
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HY-P992233 Anti-GPR64 Antibody
Anti-GPR64 Antibody is a monoclonal antibody that targets GPR64/ADGRG2. Anti-GPR64 Antibody can be used in ELISA, FACS, and functional assays.

Species: Human

Adhesion G Protein-coupled Receptors (AGPCRs)  
Inflammation or Immune System Disease  
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HY-N13132 Hellicoside
Hellicoside is a natural product that can be obtained from plantain. Hellicoside has inhibitory activity against cAMP phosphodiesterase and 5-lipoxygenase.
Phosphodiesterase (PDE)   Lipoxygenase  
/
HY-B1505G Acefylline (GMP)
Acefylline (Theophyllineacetic acid) (GMP), a xanthine derivative, is an Adenosine Receptor antagonist. Acefylline (GMP) is a peptidylarginine deiminase (PAD) activator. Acefylline (GMP) is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline (GMP) can be used in asthma research.
Adenosine Receptor   Protein Arginine Deiminase   Phosphodiesterase (PDE)  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
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HY-P992035 AMY109
AMY109 is an anti-human interleukin-8 (IL-8) monoclonal antibody, with a Ka of 36.8 pM for human IL-8, and a Ka of 380 pM for cynomolgus monkey IL-8. AMY109 binds to human and cynomolgus monkey IL-8 in a pH-dependent manner, inhibits IL-8-mediated activation of CXCR1 and CXCR2, and blocks the downstream biological activities of IL-8. AMY109 inhibits neutrophil recruitment to endometriotic lesions and suppresses monocyte chemoattractant protein-1 production by neutrophils. AMY109 is applicable to research related to endometriosis.

Species: Human

Interleukin Related  
Endometriosis  
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HY-N3324 Mangostanol
Mangostanol ((+)-Mangostanol) is a polyoxygenated xanthone mangostanol, which can be isolated from the shell of Garcinia mangostana, and has inhibitory effect on cAMP phosphodiesterase (PDE).
Phosphodiesterase (PDE)  
/
HY-P3907 Kemptide (amide)
Kemptide (amide) is a heptapeptide with properties of a cytophilic substrate. Kemptide is a molecule preserving cell membrane intactness, is phosphorylated by PKI, the inhibitory protein specific for cAMP-dependent protein kinase (PK).
Others  
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HY-N2573 Corydalmine
Corydalmine (L-Corydalmine) inhibits spore germination of some plant pathogenic as well as saprophytic fungi. Corydalmine acts as an oral analgesic agent, exhibiting potent analgesic activity. Corydalmine alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway.
Fungal   CXCR  
Infection   Neurological, Eye or Ear Disease  
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HY-W701397 Nicotinamide N-oxide-d4
Nicotinamide N-oxide-d4 is the deuterium labeled Nicotinamide N-oxide (HY-101407). Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.
Isotope-Labeled Compounds   Endogenous Metabolite   Drug Metabolite   CXCR   Oxidative Phosphorylation  
Inflammation or Immune System Disease  
/
HY-175310S Voderdeucitinib
Voderdeucitinib (Compoudn I) is a TYK2 inhibitor with an anti-inflammatory activity. Voderdeucitinib can be used for inflammatory and autoimmune disease research, such as rheumatoid arthritis (RA), multiple sclerosis and intestinal bowel disease (IBD).
JAK  
Inflammation or Immune System Disease  
/
HY-N0164R Matrine (Standard)
Matrine (Standard) is the analytical standard of Matrine. This product is intended for research and analytical applications. Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI).
Reference Standards   PINK1/Parkin   Opioid Receptor   Autophagy   Mitophagy   Ferroptosis   Apoptosis  
Cancer   Inflammation or Immune System Disease  
/
HY-16900G Rolipram (GMP)
Rolipram GMP is Rolipram (HY-16900) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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.
Phosphodiesterase (PDE)   Epigenetic Reader Domain   Amyloid-β  
Depression   Glioblastoma Multiforme   Alzheimer's Disease   Multiple Sclerosis  
/
HY-W654256 Matrine-d3
Matrine-d3 (Matridin-d3) is a deuterium labeled Matrine (HY-N0164). Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI).
Isotope-Labeled Compounds   Autophagy   Apoptosis   Opioid Receptor   Ferroptosis   PINK1/Parkin   Mitophagy  
Inflammation or Immune System Disease  
/
HY-126754 Archangelicin
Archangelicin is an inhibitor for cAMP-phosphodiesterase (cAMP-PDE) with IC50 >400 μM. Archangelicin inhibits nuclear factor of activated T cell (NFAT) with IC50 of 9 μM. Archangelicin exhibits antitumor and anti-inflammatory.
Nuclear Factor of activated T Cells (NFAT)   Phosphodiesterase (PDE)  
Cancer   Inflammation or Immune System Disease  
/
HY-16950AR (E/Z)-4-Hydroxytamoxifen (Standard)
(E/Z)-4-Hydroxytamoxifen (Standard) is the analytical standard of (E/Z)-4-Hydroxytamoxifen. This product is intended for research and analytical applications. (E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is a selective estrogen receptor modulator with mixed estrogenic and antiestrogenic activity, which is also an active metabolite of Tamoxifen (HY-13757A). (E/Z)-4-Hydroxytamoxifen is an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100-1000 nM). (E/Z)-4-Hydroxytamoxifen is promising for research of cyclical mastalgia, such as breast pain, tenderness, and nodularity.
Reference Standards   Estrogen Receptor/ERR   Endogenous Metabolite  
Cancer  
/
HY-N1189 DL-Syringaresinol diacetate
DL-Syringaresinol diacetate is a glucoside. DL-Syringaresinol inhibits cAMP phosphodiesterase and alleviation of stress.
Others  
Cancer  
/
HY-P1594 Dynorphin A (1-10)
Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.
Opioid Receptor   iGluR  
Neurological, Eye or Ear Disease  
/
HY-N0378BGL D-Mannitol, M100 (GMP Like)
D-Mannitol, M100 (GMP Like) (Mannitol, M100 (GMP Like)) is the GMP Like class D-Mannitol that can be used as pharmaceutical excipients. D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells.
Endogenous Metabolite   PGC-1α   Adrenergic Receptor   Apoptosis   PKA  
Cancer   Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
/
HY-W019787 BAM-12P
BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM.
Opioid Receptor   CXCR  
Neurological, Eye or Ear Disease  
/
HY-N2942 Bisdemethoxycurcumin
Bisdemethoxycurcumin is an orally effective curcuminoid. Bisdemethoxycurcumin downregulates pro-inflammatory cytokines in macrophages by inhibiting the phosphorylation of PI3K/Akt and p38 MAPK. Bisdemethoxycurcumin relieves autophagy inhibition and promotes lipophagy to clear vascular smooth muscle foam cells by inhibiting the PDK1/Akt/mTOR pathway. Bisdemethoxycurcumin activates the cAMP/Epac/AMPKα axis and the NRF2/HO-1 antioxidant axis, thereby indirectly inhibiting the phosphorylation of NF-κB p65 and pro-inflammatory outputs such as IL-1β/IL-6/TNF-α, so as to alleviate pulmonary oxidative stress, inflammatory infiltration and pulmonary edema. Bisdemethoxycurcumin blocks NLRP3-mediated pyroptosis and protects cartilage extracellular matrix degradation by activating NRF2/HO-1. Bisdemethoxycurcumin also exerts a synergistic effect with potassium iodide against Candida.
PI3K   Akt   p38 MAPK   PDK-1   mTOR   Autophagy   AMPK   Keap1-Nrf2   Interleukin Related   TNF Receptor   NOD-like Receptor (NLR)   Pyroptosis   Bacterial  
Candida Infection   Acute Lung Injury   Atherosclerosis   Ulcerative Colitis   Osteoarthritis  
/
HY-P1595A CREBtide TFA
CREBtide TFA is a CREB (cAMP response element binding protein)-like peptide. CREBtide TFA a synthetic 13 amino acid peptide, has been reported as a PKA and PKC substrate.
PKA   PKC  
Metabolic or Endocrine Disease  
/
HY-17453S1 Salmeterol-13C6 xinafoate
Salmeterol-13C6 (xinafoate) is the 13C6 labeled Salmeterol (xinafoate). Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
Isotope-Labeled Compounds   Adrenergic Receptor  
Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-W127485 cis-9,10-Methyleneoctadecanoic Acid
cis-9,10-Methyleneoctadecanoic acid is a cyclopropane fatty acid that has been found in bacteria and in the digestive glands of P. globosa. It is a component of the cell membrane of Staphylococcus aureus, and levels were reduced after treatment with carvacrol. cis-9,10-Methyleneoctadecanoic acid is secreted by H. pylori and enhances histamine- and dibutyryl cAMP-stimulated acid secretion in isolated guinea pig parietal cells. It also activates protein kinase C (PKC) in a calcium-dependent manner.
Biochemical Assay Reagents  
/
HY-B0531S Triflusal-d3
Triflusal-d3 is deuterium labeled Triflusal (HY-B0531). Triflusal is an orally bioavailable, blood-brain barrier-permeable dual Cyclooxygenase-1 (COX-1)/cAMP phosphodiesterase inhibitor. Triflusal inhibits platelet aggregation, NF-κB activation, iNOS activity, and prostaglandin synthesis in ischaemic tissue. Triflusal stimulates neutrophil nitric oxide production, eNOS protein expression, and cNOS activity. Triflusal alleviates cerebral ischemic injury in rats and ameliorates pathological lesions and related gene expression in transgenic Alzheimer’s disease models. Triflusal can be used for the research of thromboembolic/ischemic cardiovascular and cerebrovascular diseases, and Alzheimer’s disease.
Isotope-Labeled Compounds   COX   NF-κB   Phosphodiesterase (PDE)   NO Synthase   Prostaglandin Receptor  
Colorectal Cancer   Prostate Cancer   Pancreatic Cancer   Depression   SARS-CoV-2 Infection   Rheumatoid Arthritis  
/
HY-14302S1 Salmeterol-d5
Salmeterol-d5 is a deuterated labeled Salmeterol. Salmeterol (GR33343X) is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
Isotope-Labeled Compounds   Adrenergic Receptor  
Metabolic or Endocrine Disease  
/
HY-186252 GPR133 agonist 1
GPR133 agonist 1 is an orally active GPR133/ADGRD1 agonist with an EC50 of 1.6 nM (293T cells). GPR133 agonist 1 activates GPR133, thereby regulating the downstream cAMP signaling pathway. GPR133 agonist 1 enhances muscle strength and endurance in mice. GPR133 agonist 1 can be used in research related to muscular atrophy, myasthenia, sarcopenia, erectile dysfunction, vestibular dysfunction, obesity, and non-alcoholic fatty liver disease.
Adhesion G Protein-coupled Receptors (AGPCRs)  
Digestive System Disease   Digestive System Inflammation   Obesity   Erectile Dysfunction   Muscular Dystrophy  
/
HY-D2310 CXCR2 Probe 1
CXCR2 Probe 1 (Compound 16b) is a selective ligand for CXCR2 and is a radiotracer for PET imaging of neutrophils in inflammatory diseases.
CXCR  
Inflammation or Immune System Disease  
/
HY-P10297 PLP (190-209)
PLP (190-209) is a myelin proteolipid protein (PLP) fragment. PLP (190-209) is used to induce experimental autoimmune encephalomyelitis (EAE) animal models for multiple sclerosis research.
Biochemical Assay Reagents  
Inflammation or Immune System Disease  
/
HY-P10680 TFE-IDAtp1-LinA
TFE-IDAtp1-LinA is a highly potent amphiphilic carrier, containing a trifluoroethyl-iminodiacetic acid analog of Stp. TFE-IDAtp1-LinA, formed nanoparticles with Cas9 RNP/ssDNA, achieved enhanced green fluorescent protein knockouts with an ED50 of 0.38 nM Cas9/sgRNA ribonucleoproteins (RNP).
Liposome  
/
HY-N12302A (E/Z)-Scotanamine D
(E/Z)-Scotanamine D is a hydroxycinnamic acid amide found in the roots of Scopolia tangutica. (E/Z)-Scotanamine D is inactive against μ-, δ-, and κ-opioid receptors.
Drug Derivative  
/
HY-15244G Alpelisib (GMP)
Alpelisib GMP is Alpelisib (HY-15244) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Alpelisib (BYL-719) is an orally active PI3Kα-selective inhibitor that blocks the conversion of PIP2 to PIP3, thereby inhibiting pathways including PI3K/AKT/mTOR, MAPK/ERK, Notch and JAK-STAT. Alpelisib also induces apoptosis, G0/G1 phase arrest and senescence; it significantly inhibits the proliferation, self-renewal, stemness and epithelial-mesenchymal transition (EMT) of tumor cells, reduces cancer stem cell populations and decreases the expression of stem cell markers. Alpelisib not only enhances the sensitivity to Eribulin (HY-13442) and exerts a synergistic effect with Paclitaxel (HY-B0015), but may also induce drug resistance by upregulating the SGK3/GSK3β/β-catenin signaling pathway. Alpelisib can be applied to research related to breast cancer, gastric cancer and lipomas associated with PTEN hamartoma tumor syndrome.
PI3K   Apoptosis  
/
HY-P992036 Anti-CXCR2 Antibody
Anti-CXCR2 Antibody is an anti-CXCR2 antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

Species: Human

CXCR  
/
HY-P3770 Phosphate acceptor peptide
Phosphate acceptor peptide is a substrate for cAMP-dependent protein kinase (PKA). phosphate acceptor peptide is also a weak PKC inhibitor.
PKC  
/
HY-B0965S Thioridazine 2-Sulfone-d3
Thioridazine-d3 2-Sulfone is the deuterium labeled Thioridazine hydrochloride. Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
Isotope-Labeled Compounds   Bacterial   Apoptosis   5-HT Receptor   Dopamine Receptor   Autophagy  
Cancer   Infection   Neurological, Eye or Ear Disease  
/
HY-17609S Difelikefalin-d5
Difelikefalin-d5 (CR-845-d5; FE-202845-d5) is the deuterated-labeled Difelikefalin (HY-17609). Difelikefalin (CR-845; FE-202845) is an orally active peripherally acting kappa opioid receptor agonist. Difelikefalin reduces acute kidney injury, decreases oliguria, maintains urine flow, inhibits cytokine expression, and improves survival in endotoxemia after ischemia/reperfusion. Difelikefalin suppresses pruritus signals and exhibits neuromodulatory antipruritic activity. Difelikefalin can be used in research related to acute kidney injury, chronic kidney disease-associated pruritus, and atopic dermatitis.
Isotope-Labeled Compounds   Opioid Receptor   Interleukin Related  
Renal Disease   Atopic Dermatitis  
/
HY-Y0699R Methyl red (Standard)
Methyl red (Standard) is the analytical standard of Methyl red (HY-Y0699). This product is intended for research and analytical applications. Methyl red is a pH-sensitive acid-base indicator and colorimetric reagent with a pKa of 5.1. Methyl red achieves visual judgment of the titration endpoint through reversible structural changes of protonation (red, pH < 4.4) and deprotonation (yellow, pH > 6.2). Methyl red is widely used in acid-base titration in chemical analysis and buffer pH monitoring in biochemistry.
Reference Standards   Fluorescent Dye   Environmental Pollutants  
/
HY-13749S3 Sitagliptin-d6
Sitagliptin-d6 (MK-0431-d6) is deuterium labeled Sitagliptin (HY-13749). Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
Isotope-Labeled Compounds   PKA   Endogenous Metabolite   GLP Receptor   Dipeptidyl Peptidase   ERK  
Metabolic or Endocrine Disease  
/
HY-12366S Ubrogepant-d5
Ubrogepant-d5 (MK-1602-d5) is deuterium labeled Ubrogepant. Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine.
Isotope-Labeled Compounds   CGRP Receptor  
Neurological, Eye or Ear Disease   Blood or Cardio-cerebrovascular Disease  
/
HY-W110780 Methyl red sodium
Methyl red sodium is a pH-sensitive acid-base indicator and colorimetric reagent with a pKa of 5.1. Methyl red sodium achieves visual judgment of the titration endpoint through reversible structural changes of protonation (red, pH < 4.4) and deprotonation (yellow, pH > 6.2). Methyl red sodium is widely used in acid-base titration in chemical analysis and buffer pH monitoring in biochemistry.
Fluorescent Dye  
/
HY-N0259R Epimedin B (Standard)
Epimedin B (Standard) (Epmedin B (Standard)) is the analytical standard of Epimedin B (HY-N0259). This product is intended for research and analytical applications. Epimedin B (Epmedin B) is a flavonoid active component found in Epimedium, with oral activity, and exhibits anti-osteoporotic and neuroprotective effects. Epimedin B inhibits RANKL-induced osteoclast differentiation, F-actin ring formation, and mature osteoclast bone resorption, inhibits the phosphorylation of JNK, p38 MAPK, PI3K, and AKT, activates the AMPK-Nrf2 antioxidant pathway, and reduces cellular and mitochondrial ROS. Epimedin B acts on ESR1 and exerts its effects via GPER. Epimedin B alleviates bone loss and improves bone microstructure in vivo, and in Parkinson's models protects dopaminergic neurons and maintains striatal dopamine levels through anti-apoptotic and anti-endoplasmic reticulum stress effects. Epimedin B can be used for research related to osteoporosis, diabetic osteoporosis, and Parkinson's disease.
Reference Standards   JNK   Estrogen Receptor/ERR   p38 MAPK   PI3K   Akt   AMPK   Keap1-Nrf2   Reactive Oxygen Species (ROS)   Apoptosis   Bcl-2 Family  
Glucose Metabolism   Parkinson's Disease   Osteoporosis  
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HY-W013935R Bisphenol B (Standard)
Bisphenol B (Standard) is the analytical standard of Bisphenol B. This product is intended for research and analytical applications. Bisphenol B is a close structural analog of Bisphenol A (BPA) (HY-18260). Bisphenol B is a potent, orally active endocrine disruptor (ED). Bisphenol B binds to G protein-coupled estrogen receptor (GPER) (IC50 = 3.3 μM) with higher affinity and agonistic activity than BPA. Bisphenol B promotes GPER mediated cell migration. Bisphenol B exerts estrogenic effects via GPER pathway at nanomolar concentration. Bisphenol B is used in the manufacture of polycarbonate resin with ED properties.
Reference Standards   Endogenous Metabolite   Estrogen Receptor/ERR   Reactive Oxygen Species (ROS)  
Metabolic or Endocrine Disease  
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HY-19436S Solabegron-d8
Solabegron-d8 (GW 427353-d8) is deuterium labeled Solabegron. Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM. Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome.
Isotope-Labeled Compounds   Adrenergic Receptor  
Metabolic or Endocrine Disease  
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HY-187424 GPCR antagonist-1
GPCR antagonist-1 is an orally active G protein-coupled receptor (GPCR) antagonist as well as an insecticide. GPCR antagonist-1 induces intestinal microvillus destruction, reduces microfilarial secretion, increases the proportion of malformed embryos, inhibits nematode motility and L3-stage molting, and exerts L4-stage larvicidal activity. GPCR antagonist-1 can be used for the research of filarial infections.
Adhesion G Protein-coupled Receptors (AGPCRs)   Insecticide  
Parasitic Infection  
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HY-13599S2 Cladribine-15N
Cladribine-15N (2-Chloro-2′-deoxyadenosine-15N) is 15N labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.
Isotope-Labeled Compounds   Adenosine Deaminase   Apoptosis  
Cancer   Blood or Cardio-cerebrovascular Disease  
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HY-N0005S1 Curcumin-d3
Curcumin-d3 (Diferuloylmethane-d3 ) is deuterium labeled Curcumin (HY-N0005). 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.
Isotope-Labeled Compounds   Keap1-Nrf2   Epigenetic Reader Domain   Histone Acetyltransferase   Mitophagy   Autophagy   Influenza Virus   Ferroptosis  
Cancer   Infection   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
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HY-13599S Cladribine-d4
Cladribine-d4 (2-Chloro-2′-deoxyadenosine-d4) is deuterium labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.
Isotope-Labeled Compounds  
Cancer   Blood or Cardio-cerebrovascular Disease  
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HY-N14662 Griseolic acid B
Griseolic acid B (7′-Desoxygriseolic acid) has the activity of inhibiting cyclic adenosine monophosphate (cAMP) phosphodiesterase [EC 3.1.4.17] with an IC50 of 0.16 μM.

Source: Streptomyces griseoaurantiacus

Phosphodiesterase (PDE)  
Neurological, Eye or Ear Disease  
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HY-D2324 EE-Flipper 33
EE-Flipper 33 is a Flipper probe designed to evaluate the mechanism of early endocytosis. EE-Flipper has a pKa value of 10.6 and is capable of tracking approximately 70% of early endosomes (EE) in live cells. Furthermore, EE-Flipper 33 can also label the Golgi apparatus in live cells with an internal pH ranging from 6.0 to 6.7.
Fluorescent Dye  
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HY-184966 PF-07976016
PF-07976016 (GIPR antagonist 4) is an orally active GIPR antagonist with an IC50 of 4.1 nM. PF-07976016 (GIPR antagonist 4) exerts its antagonistic effect by competitively binding to GIPR and blocking the increase in Gαs-mediated cAMP production induced by GIP agonists. The combination of GIPR antagonist 4 and Liraglutide (HY-P0014) can enhance the weight loss effect of the single drug. PF-07976016 (GIPR antagonist 4) can be used for research related to obesity and metabolic diseases.
Adhesion G Protein-coupled Receptors (AGPCRs)  
Obesity  
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HY-13599S1 Cladribine-13C5,15N2
Cladribine-13C5,15N2 (2-Chloro-2′-deoxyadenosine-13C5,15N2) is 13C and 15N labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.
Isotope-Labeled Compounds  
Cancer   Blood or Cardio-cerebrovascular Disease  
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HY-B0188AS Mianserin-d3 hydrochloride
Mianserin-d3 hydrochloride is the deuterium labeled Mianserin. Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy.
Isotope-Labeled Compounds   Histamine Receptor   Opioid Receptor   ERK   p38 MAPK  
Neurological, Eye or Ear Disease   Metabolic or Endocrine Disease  
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HY-107216A (3aS,4R,9bR)-G-1
(3aS,4R,9bR)-G-1 is a highly selective G protein-coupled receptor GPR30 (GPER) agonist with a Ki value of approximately 7 nM. (3aS,4R,9bR)-G-1 activates rapid signaling pathways such as intracellular calcium mobilization and PI3K signaling through GPR30, promoting uterine epithelial cell proliferation and exerting antidepressant effects. (3aS,4R,9bR)-G-1 is promising for research of breast cancer and depression.
Adhesion G Protein-coupled Receptors (AGPCRs)   PI3K  
Neurological, Eye or Ear Disease  
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HY-10230S Midostaurin-d5
Midostaurin-d5 (PKC412-d5) is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
Isotope-Labeled Compounds   PKC   Syk   Akt   PKA   c-Kit  
Cancer  
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HY-17609S1 Difelikefalin-d5 hydrochloride
Difelikefalin-d5 hydrochloride (CR-845-d5 hydrochloride; FE-202845-d5 hydrochloride) is the deuterated-labeled Difelikefalin (HY-17609). Difelikefalin (CR-845; FE-202845) is an orally active peripherally acting kappa opioid receptor agonist. Difelikefalin reduces acute kidney injury, decreases oliguria, maintains urine flow, inhibits cytokine expression, and improves survival in endotoxemia after ischemia/reperfusion. Difelikefalin suppresses pruritus signals and exhibits neuromodulatory antipruritic activity. Difelikefalin can be used in research related to acute kidney injury, chronic kidney disease-associated pruritus, and atopic dermatitis.
Isotope-Labeled Compounds   Opioid Receptor   Interleukin Related  
Renal Disease   Atopic Dermatitis  
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HY-P0228A PKA RII peptide TFA
PKA RII peptide TFA is a PKA substrate that, after being phosphorylated at the serine residue, can be used for the detection of calcineurin activity.
PKA  
Metabolic or Endocrine Disease  
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HY-N0378S D-Mannitol-d8
D-Mannitol-d8 is the deuterium labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells. D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed.
Isotope-Labeled Compounds   PGC-1α   Apoptosis   PKA   Endogenous Metabolite   Adrenergic Receptor  
Cancer   Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
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HY-B0725S Doxepin-d3 hydrochloride
Doxepin-d3 hydrochloride is the deuterated-labeled Doxepin Hydrochloride (HY-B0725). Doxepin Hydrochloride is an orally active, blood-brain barrier penetrant tricyclic antidepressant with multiple activities including hypnosis, sedation, analgesia and vasodilation. Doxepin Hydrochloride enhances the expression of PSD-95 and synapsin 1 via the PI3K/AKT/mTOR signaling pathway, and is metabolized to DesmethylDoxepin Hydrochloride in vivo. Doxepin Hydrochloride can be used in research related to various diseases such as depression, anxiety, obesity and atopic dermatitis.
Isotope-Labeled Compounds   Akt   mTOR   Drug Intermediate  
Depression   Atopic Dermatitis   Obesity  
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HY-101407R Nicotinamide N-oxide (Standard)
Nicotinamide N-oxide (Standard) is the analytical standard of Nicotinamide N-oxide. This product is intended for research and analytical applications. Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.
Reference Standards   CXCR   Drug Metabolite   Endogenous Metabolite  
Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
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HY-W674241A 4-Ethylphenyl sulfate sodium
4-Ethylphenyl sulfate sodium is an orally active and brain-penetrant gut microbial metabolite. 4-Ethylphenyl sulfate sodium downregulates Bcl2 expression, upregulates Bax expression, and induces cancer cell apoptosis via the endogenous apoptotic pathway. 4-Ethylphenyl sulfate sodium induces G2/M cell cycle arrest and reactive oxygen species (ROS) production. 4-Ethylphenyl sulfate sodium impairs oligodendrocyte maturation, reduces oligodendrocyte-neuron interactions, decreases axonal myelination levels, and shifts the oligodendrocyte population toward immature precursor cells. 4-Ethylphenyl sulfate sodium alters brain region-specific neural activity and functional connectivity in mice, and correlates with anxiety-like behaviors in mice.

Source: goat urine

Endogenous Metabolite   Apoptosis   Bcl-2 Family   Reactive Oxygen Species (ROS)  
Cancer   Neurological, Eye or Ear Disease  
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HY-N6901 Luteolin 7-sulfate
Luteolin 7-sulfate is isolated from Phyllospadix iwatensis Makino, a marine plant. Luteolin 7-sulfate attenuates TYR gene expression through the intervention of a cAMP-responsive element binding protein (CREB)- and microphthalmia-associated transcription factor (MITF)-mediated signaling pathway, leading to the decreased melanin synthesis.
Epigenetic Reader Domain  
Metabolic or Endocrine Disease  
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HY-D0867A BES sodium
BES sodium is a secondary standard biochemical buffer with effective pH range of 6.4 to 7.8 (pKa: 7.15 at 20 °C). BES sodium is used in the diagnostic testing area.
Biochemical Assay Reagents  
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HY-P4331 Boc-Gln-Gly-Arg-AMC
Boc-Gln-Gly-Arg-AMC is a fluorogenic substrate for kallikrein (PKa), coagulation factor XIIa (FXIIa) and coagulation factor XIa (FXIa). Boc-Gln-Gly-Arg-AMC enables fluorescence-based activity assays for PKa, FXIIa and FXIa.
Fluorescent Dye   Ser/Thr Protease  
Blood or Cardio-cerebrovascular Disease  
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HY-W040263 TAPS sodium
TAPS sodium is a biological buffer that protects the structural integrity of lysozyme bacteria and prevents them from thermal denaturation at high temperatures. A pKa of 8.1 for TAPS results in half-maximal connexin channel activity.
Biochemical Assay Reagents  
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HY-B0188S Mianserin-d3
Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy.
Histamine Receptor   Isotope-Labeled Compounds   Opioid Receptor   ERK   p38 MAPK  
Neurological, Eye or Ear Disease  
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HY-P3570 Adipokinetic hormone II (Locusta migratoria)
Adipokinetic hormone II (Locusta migratoria) (Lom-AKH-II) is a insect adipokinetic hormone (AKH), enhances fat body cAMP levels in vitro. Insect adipokinetic hormones (AKHs) controls flight-directed mobilization of carbohydrate and lipid from fat body stores, which depends on AKH receptor(s) coupling to cAMP formation and glycogen phosphorylase activation via the stimulatory guanine nucleotide-binding protein (Gs).
Endogenous Metabolite  
Metabolic or Endocrine Disease  
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HY-P990610 KHK-2898
KHK-2898 is a monoclonal antibody targeting CD98, which binds to the extracellular domain of CD98 on the tumor cell membrane in a non-covalent antigen-specific mode. KHK-2898 can disrupt the heterodimeric complex formed by CD98 with LAT1 and xCT light chains, reduce the amino acid uptake capacity of tumor cells, block the PI3K/AKT/mTOR proliferative signaling cascade, and mediate antibody-dependent cytotoxicity. KHK-2898 can be used for cancer-related research. The isotype control of KHK-2898 can be found in Human IgG1 kappa, Isotype Control (HY-P99001).

Species: Human

Akt   mTOR   PI3K  
Cancer  
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HY-P1052A Myelin Basic Protein(87-99) TFA
Myelin Basic Protein(87-99) TFA is an encephalitogenic peptide that induces basic protein-specific T cell proliferation. Myelin Basic Protein(87-99) TFA causes a Th1 polarization in peripheral blood mononuclear cells with is implicated of multiple sclerosis (MS).
PKC  
Inflammation or Immune System Disease  
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HY-P3572 Adipokinetic hormone I (Locusta migratoria)
Adipokinetic hormone I (Locusta migratoria) (Lom-AKH-I) is a insect adipokinetic hormone (AKH), enhances fat body cAMP levels in vitro. Insect adipokinetic hormones (AKHs) controls flight-directed mobilization of carbohydrate and lipid from fat body stores, which depends on AKH receptor(s) coupling to cAMP formation and glycogen phosphorylase activation via the stimulatory guanine nucleotide-binding protein (Gs).
Endogenous Metabolite  
Metabolic or Endocrine Disease  
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HY-N10173 (+)-Epiloliolide
(+)-Epiloliolide is a megastigmane that can be isolated from Annona muricata. (+)-epiloliolide increased the nuclear localization of p53. (+)-Epiloliolide has anti-inflammatory effect through upregulating phosphorylation of the PKA/CREB pathway. (+)-Epiloliolide also effectively increases the proliferation and migration of human periodontal ligament cells by downregulating NLRP3 activated by PG-LPS.
MDM-2/p53   NOD-like Receptor (NLR)   PKA  
Inflammation or Immune System Disease  
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HY-13010S Laquinimod-d5
Laquinimod-d5 (ABR-215062-d5) is deuterium labeled Laquinimod. Laquinimod (ABR-215062), an orally available carboxamide derivative, is a potent immunomodulator that prevents neurodegeneration and inflammation in the central nervous system. Laquinimod reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod has the potential for relapsing-remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research.
Isotope-Labeled Compounds   NF-κB   Apoptosis  
Inflammation or Immune System Disease  
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HY-B0188AR Mianserin hydrochloride (Standard)
Mianserin hydrochloride (Org GB 94) (Standard) is the analytical standard of Mianserin hydrochloride. This product is intended for research and analytical applications. Mianserin hydrochloride is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy.
Reference Standards   Histamine Receptor   Opioid Receptor   ERK   p38 MAPK  
Neurological, Eye or Ear Disease   Metabolic or Endocrine Disease  
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HY-W009330 TAPSO sodium
TAPSO sodium is a commonly used biological buffer and pH-stabilizing reagent, with an effective pH range of 7-8 and a pKa range of 7.5-9. TAPSO sodium contains a Tris group, exhibits considerable reactivity, and can interact with zwitterionic glycine peptides.
Biochemical Assay Reagents  
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HY-P99855 Divozilimab
Divozilimab (BCD-132) is a humanised monoclonal antibody against CD20 (CD20). Divozilimab can be used for multiple sclerosis research.

Species: Human

CD20  
Inflammation or Immune System Disease  
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HY-B0965AS Thioridazine-d3 hydrochloride
Thioridazine-d3 (hydrochloride) is the deuterium labeled Thioridazine. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
Dopamine Receptor   Apoptosis   5-HT Receptor   Autophagy   Bacterial  
Neurological, Eye or Ear Disease  
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HY-D0878 TAPSO
TAPSO is a commonly used biological buffer and pH-stabilizing reagent, with an effective pH range of 7-8 and a pKa range of 7.5-9. TAPSO contains a Tris group, exhibits considerable reactivity, and can interact with zwitterionic glycine peptides.
Biochemical Assay Reagents  
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HY-P10927A BRP TFA
BRP (BRINP2-related peptide) TFA is a 12-peptide derived from BRINP2 that can cross the blood-brain barrier. BRP TFA induces the central activation of FOS in neuronal cells via the cAMP-PKA-CREB signaling pathway. BRP TFA exerts anorectic and anti-obesity effects without triggering nausea or aversive responses. The action of BRP TFA is independent of the leptin, GLP-1 receptor and melanocortin 4 receptor pathways. BRP TFA is applicable to obesity-related research.
PKA   AP-1  
Metabolic or Endocrine Disease  
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HY-13749S1 Sitagliptin-d4 hydrochloride
Sitagliptin-d4 hydrochloride is the deuterium labeled Sitagliptin hydrochloride (HY-13749E). Sitagliptin hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin hydrochloride blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin hydrochloride can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes.
Dipeptidyl Peptidase   PKA   Isotope-Labeled Compounds   GLP Receptor   Endogenous Metabolite   ERK  
Metabolic or Endocrine Disease  
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HY-100845 Salvinorin A
Salvinorin A is a potent, unique and short-acting high efficacy kappa-opioid receptor (KOPr) agonist with Ki value of 4.3 nm. Salvinorin A is a non-nitrogenous neoclerodane isolated from Salvia divinorum.
Opioid Receptor  
Blood or Cardio-cerebrovascular Disease  
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HY-N0378S1 D-Mannitol-13C
D-Mannitol-13C is the 13C labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells. D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed.
Isotope-Labeled Compounds   PGC-1α   Apoptosis   PKA   Endogenous Metabolite   Adrenergic Receptor  
Cancer   Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
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HY-N8303 Gardenin A
Gardenin A is an orally active and synthetic PMF analogue with the neurotrophic effect for neurite outgrowth and neuronal differentiation. Gardenin A promotes neuritogenesis via activating MAPK/ERK, PKC, and PKA, but not TrkA, CREB signaling pathways. Gardenin A also has sedative, anxiolytic, antidepressant, and anticonvulsant effects.
ERK   PAK  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
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HY-114146 CID 1375606
CID 1375606 is a surrogate agonist of orphan G protein-coupled receptor GPR27.
Orphan GPCR  
Neurological, Eye or Ear Disease   Metabolic or Endocrine Disease  
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HY-135119 Salmeterol-d3
Salmeterol-d3 is a deuterium labeled Salmeterol. Salmeterol is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
Adrenergic Receptor  
Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
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HY-13749AS Sitagliptin-d4 phosphate
Sitagliptin-d4 phosphate (MK-0431-d4) is the deuterium labeled Sitagliptin phosphate (HY-13749A). Sitagliptin phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes.
PKA   Dipeptidyl Peptidase   Endogenous Metabolite   ERK   GLP Receptor  
Metabolic or Endocrine Disease  
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HY-W001242 1-(Tetrahydropyran-2-yl)-1H-pyrazole-5-boronic acid pinacol ester
1-(Tetrahydropyran-2-yl)-1H-pyrazole-5-boronic acid pinacol ester is a pharmaceutical intermediate used in the synthesis of naphthyl FXIa/PKa inhibitors.
Biochemical Assay Reagents   Drug Intermediate  
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HY-N1420AR Rhamnose monohydrate (Standard)
Rhamnose monohydrate (Standard) is the analytical standard of Rhamnose monohydrate (HY-N1420A). Rhamnose monohydrate (L-Rhamnose monohydrate) is an orally active deoxysugar. Rhamnose monohydrate can inhibit levels of pro-inflammatory interleukin and matrix metalloproteinases (MMPs) in skin aging models. Rhamnose can promote the phosphorylation levels of PKA substrates and HSL in SVF-derived adipocytes, stimulating PKA signaling. Rhamnose monohydrate can act against obesity in mice by stimulating fat dopamine receptors and inducing thermogenesis. Rhamnose monohydrate shows anti-aging effects. Rhamnose monohydrate can be used in the study of Ehrlich’s solid tumors and sarcomas.
Reference Standards   Endogenous Metabolite   MMP   Interleukin Related   PKA  
Cancer   Infection   Metabolic or Endocrine Disease  
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HY-N6076 Tenuifoliside A
Tenuifoliside A is isolated from Polygala tenuifolia, has anti-apoptotic and antidepressant-like effects. Tenuifoliside A exhibits its neneurotrophic effects and promotes cell proliferation through the ERK/CREB/BDNF signal pathway in C6 cells.
ERK  
Inflammation or Immune System Disease   Colorectal Cancer   Prostate Cancer   Liver Cancer   Depression   Pain   Obesity  
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HY-111896 7-Methoxyrosmanol
7-Methoxyrosmanol (7-O-Methoxyrosmanol), a phenolic diterpene isolated from rosemary, suppresses the cAMP responsiveness of PEPCK and G6Pase promoters.
PEPCK  
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HY-P10602 PKA Regulatory Subunit II Substrate
PKA Regulatory Subunit II Substrate (RII phosphopeptide) is a tool peptide derived from the regulatory subunit Type II (RII) of cyclic AMP-dependent protein kinase (PKA). PKA Regulatory Subunit II Substrate is commonly used to mimic the phosphorylation of protein kinases and as a specific substrate for protein phosphatases to assess the activities of these enzymes.
PKA  
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HY-N0050 Allomatrine
Allomatrine ((+)-Allomatrine) is an alkaloid from the bark of Sophora japonica. Allomatrine has antinociceptive properties mediated mainly through the activation ofκ-opioid receptors.
Others  
Neurological, Eye or Ear Disease  
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HY-W004284R Heptadecanoic acid (Standard)
Heptadecanoic acid (Standard) is the analytical standard of Heptadecanoic acid. This product is intended for research and analytical applications. Heptadecanoic acid is an odd-chain saturated fatty acid (OCS-FA) with oral activity. Heptadecanoic acid can inhibit cell proliferation and induce Apoptosis. Heptadecanoic acid has antitumor activity. Heptadecanoic acid is associated with a number of diseases, including coronary heart disease, pre-diabetes and type 2 diabetes, and multiple sclerosis[1].
Reference Standards   Apoptosis   PI3K   Akt  
Cancer   Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
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HY-W011927R 4,4'-Sulfonyldiphenol (Standard)
4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone) (Standard) is the analytical standard of 4,4'-Sulfonyldiphenol (HY-W011927). This product is intended for research and analytical applications. 4,4'-Sulfonyldiphenol, a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC50 values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.
Reference Standards   Estrogen Receptor/ERR   Histone Methyltransferase   Thyroid Hormone Receptor   PI3K   Akt   mTOR   Androgen Receptor   Drug Derivative  
Cancer   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
/
HY-17363R Dimethyl fumarate (Standard)
Dimethyl fumarate (Standard) is the analytical standard of Dimethyl fumarate. This product is intended for research and analytical applications. Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research.
Reference Standards   Keap1-Nrf2   Reactive Oxygen Species (ROS)   HIV   Autophagy   Endogenous Metabolite  
Cancer   Infection   Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
/
HY-N2590 Lupenone
Lupenone is an orally active lupine-type triterpenoid that can be isolated from Musa basjoo. Lupenone Lupenone plays a role through the PI3K/Akt/mTOR and NF-κB signaling pathways. Lupenone has anti-inflammatory, antiviral, antidiabetic and anticancer activities.
Parasite   PI3K   Akt   mTOR   NF-κB  
Breast Cancer   Pancreatic Cancer   Parasitic Infection   Pain   Digestive System Inflammation   Glucose Metabolism  
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HY-N0378S2 D-Mannitol-13C6
D-Mannitol-13C6 is the 13C labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells. D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed.
Isotope-Labeled Compounds   PGC-1α   Apoptosis   PKA   Endogenous Metabolite   Adrenergic Receptor  
Cancer   Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
/
HY-N10319 Artepillin C
Artepillin C is an orally active CREB/CRTC2 inhibitor and TRPA1 covalent agonist (EC50=1.8 μM). Artepillin C inhibits CREB/CRTC2-mediated gene transcription and downregulates BMAL1 expression to regulate glucose and lipid metabolism. Artepillin C can also activate TRPA1 channels to induce spicy taste signals. Artepillin C can inhibit tumor cell proliferation, induce necroptosis, improve insulin resistance and inhibit liver lipid synthesis. Artepillin C can be used in the study of metabolic syndrome, tumor prevention and treatment, and inflammation.
Epigenetic Reader Domain   Necroptosis   TRP Channel  
Digestive System Disease   Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pain   Digestive System Inflammation   Glucose Metabolism   Obesity  
/
HY-P3942 SDP116
SDP116 is a synthetic Stachel-derived peptide of GPR116 Stachel peptide. SDP116 has ADGRF5 agonist effect.
Adhesion G Protein-coupled Receptors (AGPCRs)  
/
HY-W674241 4-Ethylphenyl sulfate
4-Ethylphenyl sulfate is an orally active and brain-penetrant gut microbial metabolite. 4-Ethylphenyl sulfate downregulates Bcl2 expression, upregulates Bax expression, and induces cancer cell apoptosis via the endogenous apoptotic pathway. 4-Ethylphenyl sulfate induces G2/M cell cycle arrest and reactive oxygen species (ROS) production. 4-Ethylphenyl sulfate impairs oligodendrocyte maturation, reduces oligodendrocyte-neuron interactions, decreases axonal myelination levels, and shifts the oligodendrocyte population toward immature precursor cells. 4-Ethylphenyl sulfate alters brain region-specific neural activity and functional connectivity in mice, and correlates with anxiety-like behaviors in mice.

Source: goat urine

Endogenous Metabolite   Apoptosis   Bcl-2 Family   Reactive Oxygen Species (ROS)  
Cancer   Neurological, Eye or Ear Disease  
/
HY-P3445A Anrikefon acetate
Anrikefon (HSK21542) acetate is a kappa opioid receptor agonist with analgesic effect.
Opioid Receptor  
Depression   Pain  
/
HY-P99403 Refanezumab
Refanezumab (GSK249320) is a brain-penetrant IgG1-type humanized monoclonal antibody directed against myelin-associated glycoprotein (MAG). Refanezumab binds to MAG and blocks MAG-mediated inhibition of axonal regeneration. Refanezumab has the potential for the enhancement of recovery of function poststroke.

Species: Human

Others  
Neurological, Eye or Ear Disease  
/
HY-D0867 BES
BES is a secondary standard biochemical buffer with effective pH range of 6.4 to 7.8 (pKa: 7.15 at 20 °C). BES is used in the diagnostic testing area.
Biochemical Assay Reagents  
/
HY-P1299A UFP-101 TFA
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect.
Opioid Receptor  
Neurological, Eye or Ear Disease  
/
HY-N7144A Citronellyl acetate
Citronellyl acetate, a monoterpene product of the secondary metabolism of plants, is an orally active antinociceptive agent. Citronellyl acetate modulates TRPV1, TRPM8, ASIC, glutamate receptors, PKC, and PKA-mediated nociception. Citronellyl acetate can be used for the research of acute pain.
Environmental Pollutants   PKA   TRP Channel   PKC  
Neurological, Eye or Ear Disease  
/
HY-W010448 Imidazol-1-yl-acetic acid
Imidazol-1-yl-acetic acid is a BRS-3 agonist that mediates anorectic effects through activation of orphan G protein-coupled receptors (Orphan GPCR) in peripheral tissues; it also serves as a green, water-soluble, recyclable bifunctional organocatalyst for transformations such as Biginelli multicomponent reactions and epoxide ring opening. Imidazol-1-yl-acetic acid is used in the study of obesity.
Bombesin Receptor   Orphan GPCR  
Obesity  
/
HY-W004121 4-Biphenylsulfonyl chloride
4-Biphenylsulfonyl chloride is a synthetic intermediate that participates in the sulfonamide formation reaction to synthesize antiproliferative compounds. The derivatives of 4-Biphenylsulfonyl chloride inhibit human head and neck squamous cell carcinoma (HNSCC) cells by increasing PTEN expression and inhibiting the PI3K/Akt/mTOR pathway. 4-Biphenylsulfonyl chloride can be used in the development of anticancer drugs for HNSCC.
Drug Intermediate  
/
HY-N3138 Ombuoside
Ombuoside has antioxidant properties, inhibiting ROS production and apoptosis. Ombuoside exerts neuroprotective effects through the ERK-JNK-caspase-3 system. Ombuoside promotes Dopamine biosynthesis through TH and CREB activation. Ombuoside exhibits antimicrobial activity against several Gram-positive and Gram-negative bacteria, as well as Candida albicans
Bacterial   Apoptosis   Reactive Oxygen Species (ROS)   ERK   JNK   Caspase   SOD   Fungal  
Colorectal Cancer   Prostate Cancer   Liver Cancer   Pancreatic Cancer   Bacterial Infection   Fungal Infection   Depression   Pain   Digestive System Inflammation   Parkinson's Disease   Obesity   Lung Fibrosis  
/
HY-P990246 Anti-Mouse F4/80 Antibody (CI:A3-1)
Anti-Mouse F4/80 Antibody (CI:A3-1) is an anti-mouse F4/80 IgG2b monoclonal antibody. Anti-Mouse F4/80 Antibody (CI:A3-1) can clear macrophages. Anti-Mouse F4/80 Antibody (CI:A3-1) can be used for research on inflammation conditions such as endometriosis. Anti-Mouse F4/80 Antibody (CI:A3-1) often used for flow cytometry analysis and immunohistochemical analysis.

Species: Mouse

Adhesion G Protein-coupled Receptors (AGPCRs)  
Inflammation or Immune System Disease  
/
HY-17363S1 Dimethyl fumarate-d2
Dimethyl fumarate-d2 is the deuterium labeled Dimethyl fumarate. Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research.
Autophagy   HIV   Keap1-Nrf2   Endogenous Metabolite   Reactive Oxygen Species (ROS)  
Cancer  
/
HY-P10365 VPM-p15
Vmm-p15 is a peptide agonist optimized for the adhesion G protein-coupled receptor GPR64 (also known as ADGRG2 or HE6). The affinity of VPM-p15 with GPR64 is significantly higher than that of the original p15 peptide. The cAMP level induced by VMM-P15 increased significantly, activated GPR64, and triggered downstream Gs, Gq, and G12/13 signaling. VPM-p15 can be used to study the activation mechanism of adherent GPCR family members.
Adhesion G Protein-coupled Receptors (AGPCRs)  
/
HY-P3840 Head activator neuropeptide
Head activator neuropeptide is a mitogen for mammalian cell lines of neuronal or neuroendocrine origin. Head activator neuropeptide signals by binding GPR37 and stimulates cells to enter mitosis.
Mitosis  
Cancer   Neurological, Eye or Ear Disease  
/
HY-163087 PT-91
PT-91 is an agonist of GPR27. PT-91 exhibits high metabolic stability and brain exposure in mice.
Orphan GPCR  
Neurological, Eye or Ear Disease   Metabolic or Endocrine Disease  
/
HY-P1595 CREBtide
CREBtide is a CREB (cAMP response element binding protein)-like peptide. CREBtide, a synthetic 13 amino acid peptide, has been reported as a PKA and PKC substrate.
PKA   PKC  
Metabolic or Endocrine Disease  
/
HY-W004284S1 Heptadecanoic acid-d33
Heptadecanoic acid-d33 is the deuterium labeled Heptadecanoic acid. Heptadecanoic acid is an odd chain saturated fatty acid (OCS-FA). Heptadecanoic acid is associated with several diseases, including the incidence of coronary heart disease, prediabetes and type 2 diabetes as well as multiple sclerosis.
Endogenous Metabolite  
Cancer   Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
/
HY-P99213 Ozanezumab
Ozanezumab (GSK1223249) is a humanized, Fc-inactivated monoclonal antibody that targets the nervous system protein Nogo-A. Ozanezumab promotes neurite outgrowth and axonal regeneration by neutralizing Nogo-A signaling. Ozanezumab is used for research on neurodegenerative diseases such as amyotrophic lateral sclerosis and multiple sclerosis[1].

Species: Human

Others  
Amyotrophic Lateral Sclerosis   Multiple Sclerosis  
/
HY-156354 GPR61 Inverse agonist 1
GPR61 Inverse agonist 1 (Compound 1) is a GPR61 inverse agonist (IC50: 11 nM). GPR61 Inverse agonist 1 can be used for research of disorders of metabolism and body weight, such as obesity and cachexia.
Orphan GPCR  
Metabolic or Endocrine Disease  
/
HY-N0005S Curcumin-d6
Curcumin-d6 (Diferuloylmethane-d6 ) is deuterium labeled Curcumin (HY-N0005). 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.
Isotope-Labeled Compounds   Keap1-Nrf2   Ferroptosis   Autophagy   Histone Acetyltransferase   Epigenetic Reader Domain   Mitophagy   Influenza Virus  
Cancer   Infection   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-155417 GPR34 receptor antagonist 3
GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680 μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .
Orphan GPCR   ERK  
Colorectal Cancer   Prostate Cancer   Liver Cancer   Pain   Obesity  
/
HY-P1594A Dynorphin A (1-10) TFA
Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC50 of 42.0 μM.
Opioid Receptor   iGluR  
Neurological, Eye or Ear Disease  
/
HY-N2180 (+)-Eudesmin
Pinoresinol dimethyl ether ((+)-Eudesmin) is a non-phenolic furanoid lignin. Pinoresinol dimethyl ether can be isolated from Magnolia biondii. Pinoresinol dimethyl ether activates MAPK, PKC, and PKA upstream pathways and inhibits NO levels. Pinoresinol dimethyl ether has neuroprotective activity.
PKC   PKA   p38 MAPK   NO Synthase  
Digestive System Disease   Lung Cancer   Neurodegenerative Disease   Pain   Digestive System Inflammation  
/
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  
/
HY-N2038 3,5,6,7,8,3',4'-Heptemthoxyflavone
3,5,6,7,8,3',4'-Heptemthoxyflavone, a flavonoid from satsuma peel, is an orally available CREB activator with anti-tumor and anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-Heptemthoxyflavone inhibits collagenase activity and increases the content of type I procollagen in human dermal fibroblast neoblast (HDFn) cells. 3,5,6,7,8,3',4'-Heptemthoxyflavone induces brain-derived neurotrophic factor (BDNF) expression through the cAMP/ERK/CREB signaling pathway and reduces phosphodiesterase activity in C6 glioma.
Phosphodiesterase (PDE)  
Colorectal Cancer   Prostate Cancer   Depression   Pain   Alzheimer's Disease   Obesity  
/
HY-B1511S Cyclic AMP-13C5
Cyclic AMP-13C5 is a deuterated cyclic AMP.
Isotope-Labeled Compounds  
/
HY-P10927 BRP
BRP is a 12-peptide derived from BRINP2 that can cross the blood-brain barrier. BRP induces the central activation of FOS in neuronal cells via the cAMP-PKA-CREB signaling pathway. BRP exerts anorectic and anti-obesity effects without triggering nausea or aversive responses. The action of BRP is independent of the leptin, GLP-1 receptor and melanocortin 4 receptor pathways. BRP is applicable to obesity-related research.
AP-1   PKA  
Obesity  
/
HY-P4776 Acetyl-(D-Phe2,Lys15,Arg16,Leu27)-VIP (1-7)-GRF (8-27)
Acetyl-(D-Phe2,Lys15,Arg16,Leu27)-VIP (1-7)-GRF (8-27) is a high-affinity, selective VPAC1 receptor antagonist, with IC50 values of 10 nM and 2000 nM for binding to human VPAC1 and VPAC2, respectively. Acetyl-(D-Phe2,Lys15,Arg16,Leu27)-VIP (1-7)-GRF (8-27) inhibits VIP-induced VPAC1/Gs/adenylate cyclase signaling with a Ki of 2 nM, and its VPAC1 selectivity is mainly determined by the N-terminal extracellular domain of the receptor. Acetyl-(D-Phe2,Lys15,Arg16,Leu27)-VIP (1-7)-GRF (8-27) can be used in studies related to VPAC1 receptor pharmacology, VIP signaling, and the structure and function of class B GPCRs.
PACAP Receptor   Adenylate Cyclase  
Metabolic or Endocrine Disease  
/
HY-13771R Ursodeoxycholic acid (Standard)
Ursodeoxycholic acid (Standard) is the analytical standard of Ursodeoxycholic acid. This product is intended for research and analytical applications. Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection. Orally active.
Reference Standards   G protein-coupled Bile Acid Receptor 1   FXR   Angiotensin-converting Enzyme (ACE)   Endogenous Metabolite  
Cancer   Metabolic or Endocrine Disease   SARS-CoV-2 Infection  
/
HY-155318A GPR3 agonist-2
GPR3 agonist-2(compound 32) is a potent full agonist of G protein-coupled receptor 3, with the IC50of 260 nM.
Orphan GPCR  
Metabolic or Endocrine Disease  
/
HY-P0088 Porcine dynorphin A(1-13)
Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations.
Opioid Receptor  
/
HY-124151 Adenosine-2'-monophosphate
Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation.
Adenosine Receptor   Endogenous Metabolite  
Cancer   Pain  
/
HY-P3507 Dalazatide
Dalazatide (ShK-186) is a specific Kv1.3 potassium channel peptide inhibitor. Dalazatide can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease.
Potassium Channel  
Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-P99780 Opicinumab
Opicinumab (BIIB033) is a human IgG1 monoclonal antibody targeting LINGO-1. Opicinumab binds LINGO-1 to block its negative regulatory signaling, suppress axonal degeneration, enhance axonal regeneration, promote remyelination, and exert neuroprotective effects. Opicinumab maintains axonal protective effects during co-administration with methylprednisolone. Opicinumab can be used for the research of multiple sclerosis, acute optic neuritis, and optic neuritis..

Species: Human

Transmembrane Glycoprotein  
Experimental Autoimmune Encephalomyelitis   Multiple Sclerosis   Experimental Autoimmune Encephalomyelitis  
/
HY-P3507A Dalazatide TFA
Dalazatide (ShK-186) TFA is a specific Kv1.3 potassium channel peptide inhibitor. Dalazatide TFA can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease.
Potassium Channel  
Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-N15721 Tryptophan-cholic acid
Tryptophan-cholic acid (Trp-CA) is a microbial amino acid-conjugated bile acid that acts as an endogenous ligand and agonist (EC50=9.6 μM) for the orphan G protein-coupled receptor (GPCR) MRGPRE (Mas-related G protein-coupled receptor family member E). Tryptophan-cholic acid is orally effective but has poor oral absorption and does not cross the blood-brain barrier. Tryptophan-cholic acid promotes the secretion of glucagon-like peptide GLP-1, thereby improving glucose tolerance in diabetic mice. Tryptophan-cholic acid improves glucose tolerance, promotes insulin secretion, and alleviates high-fat diet-induced hepatic steatosis without causing pruritus side effects. Tryptophan-cholic acid is primarily used in research on type 2 diabetes (T2D).
Orphan GPCR   GLP Receptor  
Type 2 Diabetes  
/
HY-P9960 Ocrelizumab
Ocrelizumab (Ocrevus) is a humanized anti-CD20 monoclonal antibody. Ocrelizumab can induce B cell depletion and inhibit multiple sclerosis lesions in mice through antibody dependent cytotoxicity (ADCC).

Species: Human

CD20  
Inflammation or Immune System Disease  
/
HY-177108 AP-503
AP-503 is a selective GPR133/ADGRD1 agonist with an EC50 of 1.21 nM. AP-503 is used in research on the prevention of muscle-related diseases and vestibular dysfunction.
Adhesion G Protein-coupled Receptors (AGPCRs)  
/
HY-156815 YL-365
YL-365 is a potent and selective GPR34 antagonist with an IC50 of 17 nM. YL-365 binds to a portion of the orthosteric binding pocket of GPR34 and induces allosteric changes that stabilize the receptor in an inactive conformation. YL-365 down-regulates expression of the proinflammatory gene iNOS in M1 microglia and suppresses proinflammatory responses. YL-365 reduces mechanical allodynia in a dose-dependent manner in a mouse model of neuropathic pain. YL-365 can be used for the research of neuropathic pain.
Orphan GPCR  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
/
HY-109556 Insulin Detemir
Insulin Detemir is an artificial insulin, shows effect on controlling blood sugar levels. Insulin Detemir stimulates GLP-1 secretion as a consequence of enhanced Gcg expression by a mechanism involving activation of Akt- and/or extracellular signal-regulated kinase (ERK)-dependent-cat and CREB signaling pathways. Insulin Detemir can be used for type 2 diabetes research.
Akt   ERK  
Type 2 Diabetes  
/
HY-W011927 4,4'-Sulfonyldiphenol
4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone), a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an oally ative estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC50 values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.
Estrogen Receptor/ERR   Histone Methyltransferase   Thyroid Hormone Receptor   PI3K   Akt   mTOR   Androgen Receptor   Drug Derivative  
Metabolic or Endocrine Disease   Breast Cancer   Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Depression   Pain   Digestive System Inflammation   Cardiovascular Disease  
/
HY-110252 Salvinorin B
Salvinorin B is a selective and brain-penetrant kappa opioid receptor (KOPr) agonist with an EC50 of 248 nM and Ki of 2.95 μM. Salvinorin B activates downstream signaling pathways by binding to KOPr, inhibits pain transmission and reduces inflammatory response. Salvinorin B can be used for the researches of inflammation, immunology and neurological disease, such as neuropathic pain, multiple sclerosis and anxiety.
Opioid Receptor  
Inflammation or Immune System Disease   Depression   Pain  
/
HY-P99486 Briakinumab
Briakinumab (ABT-874) is a fully human anti-IL-12/23p40 monoclonal antibody. Briakinumab targets and neutralizes IL-12 and IL-23. Briakinumab can be used for the research of rheumatoid arthritis, inflammatory bowel disease, and multiple sclerosis.

Species: Human

Interleukin Related  
Inflammation or Immune System Disease  
/
HY-P991202 Anti-TSHR Antibody (M22)
Anti-TSHR Antibody (M22) is a selective agonist targeting TSHR (thyroid-stimulating hormone receptor), acting through competitive binding to the extracellular domain of TSHR. Anti-TSHR Antibody (M22) can mimic the biological effects of thyroid-stimulating hormone (TSH), activating downstream cAMP-PKA and other signaling pathways. Anti-TSHR Antibody (M22) can stimulate the proliferation of thyroid follicular epithelial cells and human umbilical vein endothelial cells (HUVECs), promote angiogenesis and tube formation, cell migration, and also upregulate the expression of angiogenesis-related proteins such as PROX1. Anti-TSHR Antibody (M22) can be used in research areas such as the mechanisms of goiter formation in Graves' disease (GD), angiogenesis regulation, and TSHR antagonist screening.

Species: Human

TSH Receptor   PKA  
Blood or Cardio-cerebrovascular Disease   Graves’ Disease  
/
HY-P75796 GPR56 Protein, Human (HEK293, His)
GPR56, a cell adhesion receptor, mediates cell-matrix adhesion in developing neurons and hematopoietic stem cells. It acts as a receptor for collagen III (COL3A1), influencing cortical development and hematopoietic stem cell maintenance. Additionally, GPR56 plays a pivotal role in cancer progression by inhibiting angiogenesis via PRKCA-mediated signaling and is essential for testis development. GPR56 Protein, Human (HEK293, His) is the recombinant human-derived GPR56 protein, expressed by HEK293 , with C-His labeled tag.

Species: Human; Source: HEK293

Receptor Proteins G-Protein-Coupled Receptors (GPCRs) Adhesion GPCRs Adhesion G Protein-Coupled Receptor G1 (GPR56)

/
HY-P700536 CXCR2 Protein, Human (His-SUMO)
CXCR2, the receptor for interleukin-8 (IL-8), orchestrates neutrophil activation through a G-protein-mediated phosphatidylinositol-calcium second messenger system upon IL-8 binding. Exhibiting high-affinity binding to IL-8, CXCR2 also interacts with other ligands like CXCL3, GRO/MGSA, and NAP-2. The involvement of GNAI2 underscores the intricate signaling mechanisms regulating neutrophil function through CXCR2. CXCR2 Protein, Human (His-SUMO) is the recombinant human-derived CXCR2 protein, expressed by E. coli , with N-SUMO, N-6*His labeled tag.

Species: Human; Source: E. coli

Cytokines and Growth Factors Receptor Proteins Chemokine & Receptors G-Protein-Coupled Receptors (GPCRs) CXC Chemokine Receptor Chemokine Receptor CXCR2

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HY-P790083 CXCR2 Protein, Human (Cell-Free, His)
CXCR2, the receptor for interleukin-8 (IL-8), orchestrates neutrophil activation through a G-protein-mediated phosphatidylinositol-calcium second messenger system upon IL-8 binding. Exhibiting high-affinity binding to IL-8, CXCR2 also interacts with other ligands like CXCL3, GRO/MGSA, and NAP-2. The involvement of GNAI2 underscores the intricate signaling mechanisms regulating neutrophil function through CXCR2. CXCR2 Protein, Human (Cell-Free, His) is the recombinant human-derived CXCR2, expressed by E. coli Cell-free, with N-10*His labeled tag. The total length of CXCR2 Protein, Human (Cell-Free, His) is 360 a.a..

Species: Human; Source: E. coli Cell-free

Cytokines and Growth Factors Chemokine & Receptors CXC Chemokine Receptor CXCR2

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HY-P702257 CXCR2 Protein, Mouse (Cell-Free, His)
CXCR2 protein acts as a receptor for interleukin-8 and induces neutrophil activation through the G protein-mediated phosphatidylinositol-calcium second messenger system. In addition to IL-8, CXCR2 also exhibits high-affinity binding to ligands such as CXCL3, GRO/MGSA, and NAP-2. CXCR2 Protein, Mouse (Cell-Free, His) is the recombinant mouse-derived CXCR2 protein, expressed by E. coli Cell-free , with N-10*His labeled tag.

Species: Mouse; Source: E. coli Cell-free

Cytokines and Growth Factors Receptor Proteins Chemokine & Receptors G-Protein-Coupled Receptors (GPCRs) Cytokine Receptors CXC Chemokine Receptor Chemokine Receptor CXCR2

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HY-P701961 PDE4D Protein, Human (His)
PDE4D (Phosphodiesterase 4D) protein, as a hydrolytic enzyme, degrades the second messenger cAMP, a crucial regulator in various physiological processes. Its enzymatic activity in breaking down cAMP underscores PDE4D's pivotal role in modulating cellular signaling cascades, maintaining the intricate balance of intracellular communication mediated by this critical second messenger. PDE4D Protein, Human (His) is the recombinant human-derived PDE4D protein, expressed by E. coli , with N-6*His labeled tag.

Species: Human; Source: E. coli

Enzymes & Regulators Hydrolases (EC 3)

/
HY-P701068 PKA/PRKACA Protein, Canine (His)
PKA/PRKACA Protein, Canine (His) is the recombinant canine-derived PKA/PRKACA protein, expressed by E. coli, with N-His labeled tag.

Species: Canine; Source: E. coli

Enzymes & Regulators Kinases Transferases (EC 2) Serine/Threonine Kinase Proteins AGC PKA PRKACA/PKAc alpha

/
HY-P701753 PKA/PRKACA Protein, Human (Active, sf9, GST)
PKACα protein is a key kinase that phosphorylates a variety of substrates, including CDC25B, ABL1, NFKB1, and VASP, affecting a variety of cellular processes, such as cell cycle progression, platelet regulation, and adipogenic differentiation. It also negatively regulates mTORC1 through RPTOR phosphorylation, thereby modulating signaling networks. PKA/PRKACA Protein, Human (sf9, GST) is the recombinant human-derived PKACα protein, expressed by sf9 insect cells , with GST tagged.

Species: Human; Source: Sf9 insect cells

Enzymes & Regulators Kinases Transferases (EC 2) Serine/Threonine Kinase Proteins AGC PKA PRKACA/PKAc alpha

/
HY-P702637 PRKACB Protein, Human (Active, sf9)
PRKACB Protein, Human (sf9) is the recombinant human-derived PRKACB, expressed by Sf9 insect cells , with tag Free labeled tag. ,

Species: Human; Source: Sf9 insect cells

Enzymes & Regulators Kinases Transferases (EC 2) Serine/Threonine Kinase Proteins AGC PKA PRKACB/PKAc beta

/
HY-P74408 ATF2 Protein, Human (sf9, His-GST)
The ATF2 protein is a transcriptional activator that regulates anti-apoptotic genes, cell growth, and DNA damage responses. It binds to CRE and AP-1 sequences and plays a key role in nuclear transcription. ATF2 Protein, Human (sf9, His-GST) is the recombinant human-derived ATF2 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.

Species: Human; Source: Sf9 insect cells

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HY-P706128 Atf4 Protein, Mouse (His)

Species: Mouse; Source: E. coli

/
HY-P701960 PDE4D Protein, Human
PDE4D (Phosphodiesterase 4D) protein, as a hydrolytic enzyme, degrades the second messenger cAMP, a crucial regulator in various physiological processes. Its enzymatic activity in breaking down cAMP underscores PDE4D's pivotal role in modulating cellular signaling cascades, maintaining the intricate balance of intracellular communication mediated by this critical second messenger. PDE4D Protein, Human is the recombinant human-derived PDE4D protein, expressed by E. coli , with tag free.

Species: Human; Source: E. coli

Enzymes & Regulators Hydrolases (EC 3)

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HY-P702638 PRKACG Protein, Human (Active, sf9)
PRKACG Protein, Human (sf9) is the recombinant human-derived PRKACG, expressed by Sf9 insect cells , with tag Free labeled tag. ,

Species: Human; Source: Sf9 insect cells

Enzymes & Regulators Kinases Transferases (EC 2) Serine/Threonine Kinase Proteins AGC PKA PRKACG/PKAc gamma

/
HY-P702661 DCLK2 Protein, Human (sf9, GST)
DCLK2 Protein, Human (sf9, GST) is the recombinant human-derived DCLK2, expressed by Sf9 insect cells , with GST labeled tag.

Species: Human; Source: Sf9 insect cells

Enzymes & Regulators Kinases Transferases (EC 2) Serine/Threonine Kinase Proteins CAMK DCAMKL DCLK2/DCAMKL2

/
HY-P702891 CREBBP Protein, Human (GST)
CREBBP Protein, Human (GST) is the recombinant human-derived CREBBP, expressed by E. coli , with N-GST labeled tag.

Species: Human; Source: E. coli

Enzymes & Regulators Transferases (EC 2)

/
HY-P71209 PKI-beta Protein, Human (His)
The PKI-β protein emerged as an extremely potent competitive inhibitor of cAMP-dependent protein kinase activity. This protein operates at the molecular level, binding to the catalytic subunit of the enzyme after cAMP induces dissociation of its regulatory chain. PKI-beta Protein, Human (His) is the recombinant human-derived PKI-beta protein, expressed by E. coli , with N-6*His labeled tag.

Species: Human; Source: E. coli

Enzymes & Regulators Protein Kinase Inhibitor Peptide (PKI) cAMP-Dependent Protein Kinase A Inhibitor beta

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HY-P76284 CREB3L1 Protein, Human (HEK293, His)
CREB3L1 protein is located on the endoplasmic reticulum membrane and is converted into a transcription factor processing cyclic AMP response element binding protein 3-like protein 1. During endoplasmic reticulum stress or DNA damage, it translocates to the Golgi apparatus, is cleaved by S1P/MBTPS1 and S2P/MBTPS2, and releases a cytoplasmic domain that activates gene transcription in the nucleus. CREB3L1 Protein, Human (HEK293, His) is the recombinant human-derived CREB3L1 protein, expressed by HEK293 , with C-His labeled tag.

Species: Human; Source: HEK293

/
HY-P76191 CAMKI gamma/CAMK1G Protein, Human (Active, sf9, His, GST)
The CAMK1G protein is a calcium/calmodulin-dependent protein kinase and a key component of the proposed calcium-triggered signaling cascade. This kinase exhibits the ability to phosphorylate the transcription factor CREB1 in vitro, suggesting its involvement in regulating cellular processes related to gene expression and transcriptional control. CAMKI gamma/CAMK1G Protein, Human (sf9, His, GST) is the recombinant human-derived CAMKI gamma/CAMK1G protein, expressed by Sf9 insect cells , with His, GST labeled tag.

Species: Human; Source: Sf9 insect cells

Enzymes & Regulators Kinases Transferases (EC 2) Serine/Threonine Kinase Proteins CAMK CAMK1 CAMK1G/CaMKI gamma

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HY-P76376 GPR37 Protein, Human (HEK293, His)
GPR37 Protein, a receptor for prosaposin, undergoes endocytosis upon ligand binding, initiating an ERK phosphorylation cascade. It forms a complex with PRKN, STUB1, and HSP70, with STUB1 association increasing during ER stress. STUB1 facilitates HSP70 dissociation from PRKN, promoting PRKN-mediated ubiquitination of GPR37. GPR37 also interacts with PACRG, indicating a complex regulatory network in its cellular functions. GPR37 Protein, Human (HEK293, His) is the recombinant human-derived GPR37, expressed by HEK293, with C-His labeled tag.

Species: Human; Source: HEK293

Receptor Proteins G-Protein-Coupled Receptors (GPCRs) GPR37

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HY-P706260 Atf4 Protein, Human (His)

Species: Human; Source: E. coli

/
HY-P702890 CREBBP Protein, Human (His)
CREBBP Protein, Human (His) is the recombinant human-derived CREBBP, expressed by E. coli , with N-6*His labeled tag.

Species: Human; Source: E. coli

Enzymes & Regulators Transferases (EC 2)

/
HY-P702959 CREBBP Protein, Human (392a.a, GST)
CREBBP Protein, Human (1319-1710, GST) is the recombinant human-derived CREBBP, expressed by E. coli , with GST labeled tag.

Species: Human; Source: E. coli

Enzymes & Regulators Transferases (EC 2)

/
HY-P702980 PRKAR1B Protein, Human (sf9, His)
PRKAR1B Protein, Human (sf9, His) is the recombinant human-derived PRKAR1B, expressed by Sf9 insect cells , with His labeled tag. ,

Species: Human; Source: Sf9 insect cells

Enzymes & Regulators

/
HY-P705954 GPR17 Protein, Human (Cell-Free, His)

Species: Human; Source: E. coli Cell-free

/
HY-P704128 PDE4A Protein, Human (sf9, His)
PDE4A Protein, Human (sf9, His) is the recombinant human-derived PDE4A protein, expressed by Sf9 insect cells, with C-His tag.

Species: Human; Source: Sf9 insect cells

Enzymes & Regulators Phosphatase

/
HY-P704646 GPR56 Protein-VLP, Human (HEK293)
GPR56 Protein-VLP, Human (HEK293) is recommended for animal immunization, ELISA. It is not recommended for receptor-ligand interaction detection and SPR/BLI assay since there are other irrelevant membrane proteins of the host on the VLP envelope, and the receptor-ligand interaction will have strong background interference. High requirements for chips and experimental protocols are needed for SPR/BLI assays. If VLP control is required, it is recommended HY-P705433.

Species: Human; Source: HEK293

Receptor Proteins G-Protein-Coupled Receptors (GPCRs) Adhesion GPCRs Adhesion G Protein-Coupled Receptor G1 (GPR56)

/
HY-P705803 DCLK2 Protein, Human (sf9, Flag)

Species: Human; Source: sf9 insect cells

Enzymes & Regulators Kinases Transferases (EC 2) CAMK DCAMKL DCLK2/DCAMKL2

/
HY-P705862 PKA/PRKACA Protein, Human (K48R, L96Q, M121L, V124A, Q182K, T184A)

Species: Human; Source: E. coli

Enzymes & Regulators Kinases Transferases (EC 2) AGC PKA PRKACA/PKAc alpha

/
HY-P705863 PRKACA-DNAJB1 Protein, Human (sf9, His-GST)

Species: Human; Source: sf9 insect cells

Enzymes & Regulators Kinases Transferases (EC 2) AGC PKA PRKACA/PKAc alpha

/
HY-P81127 PKA alpha+beta Antibody
PKA alpha+beta Antibody is a Rabbit-derived and non-conjugated IgG polyclonal antibody, targeting to PKA alpha+beta.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Polyclonal Antibodies Primary Antibodies

/
HY-P81150 GPR30 Antibody
GPR30 Antibody is a Rabbit-derived and non-conjugated IgG polyclonal antibody, targeting to GPR30.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Polyclonal Antibodies Flow Cytometry Antibodies Primary Antibodies

/
HY-P80092 CREB Antibody (YA491)
CREB Antibody (YA491) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to CREB.

Host: Rabbit; Reactivity: Human, Mouse, Rat, Zebrafish

Monoclonal Antibodies Recombinant Antibodies Flow Cytometry Antibodies Primary Antibodies

/
HY-P80805 Phospho-CREB (Ser133) Antibody (YA209)
Phospho-CREB (Ser133) Antibody (YA209) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Phospho-CREB (Ser133).

Host: Rabbit; Reactivity: Human, Rat

Monoclonal Antibodies Recombinant Antibodies Modification Specific Antibodies Primary Antibodies

/
HY-P86462 PKA C-alpha Antibody (YA6154)
PKA C-alpha Antibody (YA6154) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to PKA C-alpha.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P84126 CREB1 Antibody (YA3823)
CREB1 Antibody (YA3823) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to CREB1.

Host: Mouse; Reactivity: Human, Mouse, Rat, Monkey

Monoclonal Antibodies Primary Antibodies

/
HY-P81158 CXCR2 Antibody
CXCR2 Antibody is a Rabbit-derived and non-conjugated IgG polyclonal antibody, targeting to CXCR2.

Host: Rabbit; Reactivity: Human

Polyclonal Antibodies Primary Antibodies

/
HY-P82578 Epac2 Antibody (YA2323)
Epac2 Antibody (YA2323) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Epac2.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P87988 phospho-PKA C alpha/beta/gamma (T197) Antibody (YA7673)
phospho-PKA C alpha/beta/gamma (T197) Antibody (YA7673) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to phospho-PKA C alpha/beta/gamma (T197).

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Modification Specific Antibodies Primary Antibodies

/
HY-P84207 CXCR2 Antibody (YA3904)
CXCR2 Antibody (YA3904) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to CXCR2.

Host: Mouse; Reactivity: Human

Monoclonal Antibodies Flow Cytometry Antibodies Primary Antibodies

/
HY-P80428 PKA 2 beta (regulatory subunit)Antibody (YA133)
PKA 2 beta (regulatory subunit)Antibody (YA133) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to PKA 2 beta (regulatory subunit).

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Flow Cytometry Antibodies Primary Antibodies

/
HY-P80429 PKA R2/PKR2 Antibody (YA132)
PKA R2/PKR2 Antibody (YA132) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to PKA R2/PKR2.

Host: Rabbit; Reactivity: Human

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P81981 PKA C gamma Antibody (YA1726)
PKA C gamma Antibody (YA1726) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to PKA C gamma.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P83206 GPR37 Antibody (YA2951)
GPR37 Antibody (YA2951) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to GPR37.

Host: Rabbit; Reactivity: Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P89859 ARPP-21 Antibody (YA9203)
ARPP-21 Antibody (YA9203) is a Mouse-derived and non-conjugated IgM monoclonal antibody, targeting to ARPP-21.

Host: Mouse; Reactivity: human

Monoclonal Antibodies Primary Antibodies

/
HY-P86398 CREB-1 Antibody (YA6090)
CREB-1 Antibody (YA6090) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to CREB-1.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P810911 PKA C beta Antibody
PKA C beta Antibody is a Rabbit-derived and non-conjugated IgG Polyclonal antibody, targeting to PKA C beta.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Polyclonal Antibodies Primary Antibodies

/
HY-P84148 ATF4 Antibody (YA3845)
ATF4 Antibody (YA3845) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to ATF4.

Host: Mouse; Reactivity: Human

Monoclonal Antibodies Primary Antibodies

/
HY-P84207A CXCR2 Antibody (YA3904)(PBS only)
CXCR2 Antibody (YA3904) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to CXCR2.

Host: Mouse; Reactivity: Human

Monoclonal Antibodies Primary Antibodies

/
HY-P811059 ICER Antibody
ICER Antibody is a Rabbit-derived and non-conjugated IgG Polyclonal antibody, targeting to ICER.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Polyclonal Antibodies Primary Antibodies

/
HY-P811705 ICER Antibody (YA10176)
ICER Antibody (YA10176) is a Rabbit-derived and non-conjugated IgG recombinant monoclonal antibody, targeting to ICER.

Host: Rabbit; Reactivity: Human

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P84901 GPR56 Antibody (YA4598)
GPR56 Antibody (YA4598) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to GPR56.

Host: Mouse; Reactivity: Human

Monoclonal Antibodies Flow Cytometry Antibodies Primary Antibodies

/
HY-P811708 EPAC 1 Antibody (YA10179)
EPAC 1 Antibody (YA10179) is a Rabbit-derived and non-conjugated IgG recombinant monoclonal antibody, targeting to EPAC 1.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P811708A EPAC 1 Antibody (YA10179) (PBS only)
EPAC 1 Antibody (YA10179) is a Rabbit-derived and non-conjugated IgG recombinant monoclonal antibody, targeting to EPAC 1.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P811772 RapGEF5 Antibody (YA10243)
RapGEF5 Antibody (YA10243) is a Rabbit-derived and non-conjugated IgG recombinant monoclonal antibody, targeting to RapGEF5.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Flow Cytometry Antibodies Primary Antibodies

/
HY-P811772A RapGEF5 Antibody (YA10243) (PBS only)
RapGEF5 Antibody (YA10243) is a Rabbit-derived and non-conjugated IgG recombinant monoclonal antibody, targeting to RapGEF5.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Flow Cytometry Antibodies Primary Antibodies

/
HY-P81981A PKA C gamma Antibody (YA1726)(PBS only)
PKA C gamma Antibody (YA1726) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to PKA C gamma.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P83206A GPR37 Antibody (YA2951)(PBS only)
GPR37 Antibody (YA2951) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to GPR37.

Host: Rabbit; Reactivity: Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P83387 kappa Opioid Receptor Antibody (YA3132)
kappa Opioid Receptor Antibody (YA3132) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to kappa Opioid Receptor.

Host: Rabbit; Reactivity: Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P83387A kappa Opioid Receptor Antibody (YA3132)(PBS only)
kappa Opioid Receptor Antibody (YA3132) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to kappa Opioid Receptor.

Host: Rabbit; Reactivity: Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P84126A CREB1 Antibody (YA3823)(PBS only)
CREB1 Antibody (YA3823) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to CREB1.

Host: Mouse; Reactivity: Human, Mouse, Rat, Monkey

Monoclonal Antibodies Primary Antibodies

/
HY-P84148A ATF4 Antibody (YA3845)(PBS only)
ATF4 Antibody (YA3845) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to ATF4.

Host: Mouse; Reactivity: Human

Monoclonal Antibodies Primary Antibodies

/
HY-P84901A GPR56 Antibody (YA4598)(PBS only)
GPR56 Antibody (YA4598) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to GPR56.

Host: Mouse; Reactivity: Human

Monoclonal Antibodies Primary Antibodies

/
HY-P85014 GPR56 Antibody (YA4706)
GPR56 Antibody (YA4706) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to GPR56.

Host: Mouse; Reactivity: Human

Monoclonal Antibodies Recombinant Antibodies Flow Cytometry Antibodies Nanobodies Primary Antibodies

/
HY-P85732 CREB-1 Antibody (YA5424)
CREB-1 Antibody (YA5424) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to CREB-1.

Host: Mouse; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Primary Antibodies

/
HY-P86731 CREB-1 Antibody (YA6423)
CREB-1 Antibody (YA6423) is a Mouse-derived and non-conjugated IgG monoclonal antibody, targeting to CREB-1.

Host: Mouse; Reactivity: Human, Mouse

Monoclonal Antibodies Primary Antibodies

/
HY-P86731A CREB-1 Antibody (YA6423)(PBS only)
CREB-1 Antibody (YA6423) is a Mouse-derived and non-conjugated IgG monoclonal antibody, targeting to CREB-1.

Host: Mouse; Reactivity: Human, Mouse

Monoclonal Antibodies Primary Antibodies

/
HY-P87329 PER3 Antibody (YA7012)
PER3 Antibody (YA7012) is a Mouse-derived and non-conjugated IgG2b monoclonal antibody, targeting to PER3.

Host: Mouse; Reactivity: Human

Monoclonal Antibodies Flow Cytometry Antibodies Primary Antibodies

/
HY-P87329A PER3 Antibody (YA7012)(PBS only)
PER3 Antibody (YA7012) is a Mouse-derived and non-conjugated IgG2b monoclonal antibody, targeting to PER3.

Host: Mouse; Reactivity: Human

Monoclonal Antibodies Primary Antibodies

/
HY-P87358 PDE10A Antibody (YA7041)
PDE10A Antibody (YA7041) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to PDE10A.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Flow Cytometry Antibodies Primary Antibodies

/
HY-P88362 GPR17 Antibody (YA8046)
GPR17 Antibody (YA8046) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to GPR17.

Host: Mouse; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Primary Antibodies

/
HY-P88362A GPR17 Antibody (YA8046)(PBS only)
GPR17 Antibody (YA8046) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to GPR17.

Host: Mouse; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Primary Antibodies

/
HY-P88614 PRKAR1B (PKA regulatory subunit I beta) Antibody (YA8298)
PRKAR1B (PKA regulatory subunit I beta) Antibody (YA8298) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to PRKAR1B (PKA regulatory subunit I beta).

Host: Mouse; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Flow Cytometry Antibodies Primary Antibodies

/
HY-P810621 Phospho-PKA alpha/beta/gamma (catalytic subunit) (Thr197) Antibody (YA9883)
Phospho-PKA alpha/beta/gamma (catalytic subunit) (Thr197) Antibody (YA9883) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to Phospho-PKA alpha/beta/gamma (catalytic subunit) (Thr197).

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Modification Specific Antibodies Primary Antibodies

/

References

[1]. McDonald JK, et al. G Protein-Coupled Receptor Signaling in CNS (Re)Myelination. J Neurochem. 2025;169(11):e70286.  

[2]. Mei F, et al. Identification of the Kappa-Opioid Receptor as a Therapeutic Target for Oligodendrocyte Remyelination. J Neurosci. 2016;36(30):7925-7935.  

[3]. Hirahara Y, et al. G protein-coupled receptor 30 contributes to improved remyelination after cuprizone-induced demyelination. Glia. 2013;61(3):420-431.  

[4]. Giera S, et al. Microglial transglutaminase-2 drives myelination and myelin repair via GPR56/ADGRG1 in oligodendrocyte precursor cells. eLife. 2018;7:e33385.  

[5]. Simon K, et al. The Orphan G Protein-coupled Receptor GPR17 Negatively Regulates Oligodendrocyte Differentiation via Gαi/o and Its Downstream Effector Molecules. J Biol Chem. 2016;291(2):705-718.  

[6]. Hennen S, et al. Decoding signaling and function of the orphan G protein-coupled receptor GPR17 with a small-molecule agonist. Sci Signal. 2013;6(298):ra93.  

[7]. Ou Z, et al. Olig2-Targeted G-Protein-Coupled Receptor Gpr17 Regulates Oligodendrocyte Survival in Response to Lysolecithin-Induced Demyelination. J Neurosci. 2016;36(41):10560-10573.  [Content Brief]

[8]. Merten N, et al. Repurposing HAMI3379 to Block GPR17 and Promote Rodent and Human Oligodendrocyte Differentiation. Cell Chem Biol. 2018;25(6):775-786.e5.  

[9]. Wang L, et al. CXCR2 antagonism promotes oligodendrocyte precursor cell differentiation and enhances remyelination in a mouse model of multiple sclerosis. Neurobiol Dis. 2020;134:104630.  

[10]. Qian Z, et al. Osteocalcin attenuates oligodendrocyte differentiation and myelination via GPR37 signaling in the mouse brain. Sci Adv. 2021;7(43):eabi5811.  

Keywords

GPCR signaling | myelin regeneration | remyelination | oligodendrocyte precursor cells | oligodendrocyte differentiation | multiple sclerosis | GPR17 | GPR56 | ADGRG1 | GPER | GPR37 | CXCR2 | κ-opioid receptor | cAMP | PKA | CREB | EPAC | PI3K/AKT/mTOR