Search Result
Results for "
binding models
" in MedChemExpress (MCE) Product Catalog:
4
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-NP009
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Biochemical Assay Reagents
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Others
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α-Lactalbumin is a Ca 2+-binding protein. α-Lactalbumin has a single strong Ca 2+-binding site and for this reason it frequently serves as a simple model Ca 2+-binding protein. α-Lactalbumin is a component of lactose synthase, an enzyme system, which consists of galactosyltransferase (GT) and α-Lactalbumin .
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- HY-153165
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RAR/RXR
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Others
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RXR antagonist 5 (compound 22) is a selective retinoic acid X receptor (RXR) antagonist with binding potential to RXR evaluated by modeling.
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- HY-43058
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- HY-112316
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Epigenetic Reader Domain
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Cancer
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BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
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- HY-103513
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GABA Receptor
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Others
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GABAA receptor agent 2 (compound 13) is a compound used to study the structure and orthosteric ligand binding of GABA(A) receptors. The relevant model of GABAA receptor agent 2 can be used to understand the details of orthosteric ligand binding, and a detailed binding mode hypothesis was created through structure-activity relationships with two homologous series of orthosteric GABA(A)R antagonists.
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- HY-106469
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MY-117
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Drug Derivative
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Neurological Disease
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Taltrimide (MY-117), a lipophilic derivative of Taurine (HY-B0351), strongly inhibits the sodium-independent binding of Taurine to synaptic membranes of brain, the effects on the binding of GABA being less pronounced. Taltrimide exhibits definitive anticonvulsive effects in experimental epilepsy models .
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- HY-121810
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Dopamine Transporter
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Others
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LBT-999 is a phenyltropane derivative used for positron emission tomography (PET) exploration of the dopamine transporter (DAT). It has high affinity binding to DAT on rat striatal membranes and human postmortem brain slices in vitro, high uptake in the striatum in rat and baboon models in vivo, and its binding can be blocked by specific compounds.
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- HY-P10010
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Galectin
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Cancer
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DB21, Galectin-1 Antagonist is a dibenzofuran conjugated peptidomimetic that acts as an allosteric inhibitor of galectin-1 (GAL1)binding to cell surface glycans. DB21, Galectin-1 Antagonis increases inhibition of angiogenesis and tumour growth in melanoma, lung adenocarcinoma and ovarian cancer models .
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- HY-14297
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Adrenergic Receptor
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Endocrinology
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Milveterol is a long-acting β(2)-adrenoceptor agonist with high binding activity. Milveterol exhibits high potency in vitro and a prolonged duration of action in a guinea pig bronchoprotection model. Milveterol has been structurally optimized to show enhanced binding potency compared to its parent monomer .
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- HY-148705
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SARS-CoV
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Infection
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Isomitomycin A is a potential inhibitor against SARS-CoV-2. Isomitomycin A targets to the hACE2 binding site of the modelled surface glycoprotein of SARS-CoV-2. Isomitomycin A can be used in studies of COVID-19 .
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- HY-16261
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INNO-206; DOXO-EMCH
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Topoisomerase
ADC Payload
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Cancer
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Aldoxorubicin (INNO-206) is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
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- HY-16261C
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INNO-206 hydrochloride; DOXO-EMCH hydrochloride
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Topoisomerase
ADC Payload
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Cancer
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Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
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- HY-177021
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin-IN-51 is an orally available, potent tubulin inhibitor (IC50 = 31 nM). Tubulin-IN-51 promotes tubulin polymerization in vitro and does not compete with Paclitaxel (HY-B0015) for binding. Tubulin-IN-51 inhibits the binding of Vinblastine (HY-13780) to tubulin. Tubulin-IN-51 downregulates the proportion of cells in the G1 phase and induces apoptosis. Tubulin-IN-51 inhibits tumor growth in multiple nude mouse xenograft models .
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- HY-100982
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trans-4-Hydroxycrotonic acid; trans-γ-Hydroxycrotonic acid; T‐HCA
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GABA Receptor
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Neurological Disease
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(E)-4-Hydroxycrotonic acid (T-HCA) is a high-affinity ligand for GHB binding sites, with a ki value of 1.1 μM. The introduction of diaryl substituents into (E)-4-Hydroxycrotonic acid significantly enhances its affinity for GHB binding sites, with ki values ranging from 0.023 to 0.075 μM. (E)-4-Hydroxycrotonic acid holds promise for optimizing GHB ligand structures and assisting in the development of effective three-dimensional pharmacophore models .
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- HY-177506
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Cholecystokinin Receptor
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Metabolic Disease
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FE100726 (Compound 39) is a Cholecystokinin 2 (CCK2) receptor agonist. FE100726 has a superior binding capacity on CCK2 receptor. FE100726 can induce gastric acid secretion in anaesthetized rat models. FE100726 can be used for diabetes research .
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- HY-117862
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Prostaglandin Receptor
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Inflammation/Immunology
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TASP0412098 is an orally available, potent and selective CRTH2/DP2 antagonist with high binding affinity (IC50 2.1 nM) and functional activity (IC50 12 nM). TASP0412098 has the potential to suppress asthma in mouse and guinea pig bronchial asthma models .
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- HY-103423
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Dopamine Receptor
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Neurological Disease
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PAOPA, an analog of L-proline-l-leucine-glycine amide (PLG) peptide, is an allosteric modulator of Dopamine D2 Receptor. PAOPA can effectively reduce behavioral abnormalities in rodent models of schizophrenia. PAOPA increases the high affinity dopamine D2 receptor and promotes its binding to agonists .
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- HY-N0830B
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HSP
Endogenous Metabolite
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Cancer
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Palmitic acid sodium is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid sodium can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells. Palmitic acid sodium is used to establish a cell steatosis model .
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- HY-N0830
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- HY-P991618
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Transmembrane Glycoprotein
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Cancer
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ST2485 is a monoclonal antitenascin antibody. ST2485 shows additivity in tenascin C binding in vitro as well as in a xenograft model. ST2485 binds human tenascin at an epitope partially shared with BC2. ST2485 cross-reacts with murine tenascin. ST2485 can be studied in antitumor research .
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- HY-119005A
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- HY-101119
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Estrogen Receptor/ERR
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Cancer
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GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC50=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.
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- HY-N0830A
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HSP
Endogenous Metabolite
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Cardiovascular Disease
Neurological Disease
Metabolic Disease
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Palmitic acid calcium is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells. Palmitic acid calcium is used to establish a cell steatosis model .
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- HY-106969A
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Glycine Receptor (GlyR)
iGluR
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Cardiovascular Disease
Neurological Disease
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ZD 9379 sodium is a competitive glycine/NMDA receptor antagonist, with an IC50 value of 75 nM (glutamate site). ZD 9379 sodium selectively antagonizes the glycine binding site (GlyB site) on the NMDA receptor, inhibiting the binding of glycine to the NMDA receptor and alleviating excitotoxicity. ZD 9379 sodium reduces the frequency of cortical spreading depression (SDs), alleviates energy depletion in the ischemic penumbra, and delays the expansion of infarction. ZD 9379 sodium reduces the infarct volume and improves neurological function in mouse models. ZD 9379 sodium can be used in studies of acute ischemic stroke, etc .
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- HY-B1864C
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Ksg sulfate
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Antibiotic
Bacterial
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Infection
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Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
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- HY-P2138
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HIV Protease
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Others
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U-85548E is an HIV protease inhibitor with nanomolar affinity for HIV-1 aspartic protease. By studying its structure-activity relationship, a potent nanomolar inhibitor with inhibitory effects on both HIV-1 and HIV-2 proteases was designed, and its binding mode was studied by X-ray crystallography and molecular modeling.
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- HY-170523
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SARS-CoV
DNA Methyltransferase
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Infection
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RU-0415529 is an orally active inhibitor for SARS-CoV-2 nonstructural protein 14 (NSP14) with an IC50 of 356 nM. RU-0415529 binds to the SAH-stabilized cap binding pocket, inhibits viral RNA methylation and the viral replication. RU-0415529 exhibits anti-infectious activity in mouse models .
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- HY-112316A
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Epigenetic Reader Domain
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Cancer
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(R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome .
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- HY-D0846
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Biochemical Assay Reagents
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Neurological Disease
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Diethyl pyrocarbonate is a potent, orally active, non-specific chemical inhibitor of RNase. Diethyl pyrocarbonate has been useful in vitro as an agent relatively specific for binding to imidazole of histidine. Diethyl pyrocarbonate inhibits central chemosensitivity in rabbits. Diethyl pyrocarbonate can modify Ser, Thr, His and Tyr residues. Diethyl pyrocarbonate can be used for modeling .
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- HY-117839
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Cholecystokinin Receptor
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Neurological Disease
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PD-135666 is a dipeptide inhibitor of cholecystokinin B (CCK B) receptors, binding to CCK B receptors in mouse cerebral cortex with IC50 of 0.1 nM. Its enantiomer, PD-140548, preferentially binds to CCK A receptors with IC50 of 2.8 nM in rat pancreas. PD-135666 exhibits anxiolytic effects in animal models .
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- HY-B1864B
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Ksg hydrochloride hydrate
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Antibiotic
Bacterial
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Infection
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Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
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- HY-B1864A
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Ksg hydrochloride
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Antibiotic
Bacterial
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Infection
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Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
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- HY-B0027
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Antibiotic
Bacterial
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Infection
Metabolic Disease
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Valnemulin hydrochloride is an orally effective truncated pleurotin antibiotic that inhibits protein synthesis in bacteria by binding to peptidyl transferase in the 50s ribosome subunit. Valnemulin hydrochloride effectively eliminates Mycobacterium bovis in the lungs in an experimental bovine model of Mycoplasma bovis infection. Valnemulin hydrochloride can reduce the mortality of epidemic rabbit enteropathy and has no adverse effect on the growth performance of rabbits .
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- HY-121490
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Apoptosis
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Cancer
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IMM-02 is a DID-DAD binding inhibitor with activity promoting actin assembly and microtubule stabilization. IMM-02 is able to trigger serum response factor-mediated gene expression and lead to cell cycle arrest and apoptosis. IMM-02 has shown the ability to slow tumor growth in a mouse colon cancer xenograft model .
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- HY-15350
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LY 300046 hydrochloride
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Reverse Transcriptase
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Others
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Trovirdine hydrochloride, a phenethylthiazolylthiourea (PETT) derivative, is an HIV reverse transcriptase (RT) non-nucleoside inhibitor (NNI). A novel computer model of the RT/NNI binding pocket revealed spatial gaps around Trovirdine hydrochloride's pyridyl ring. Docking studies suggested that replacing this planar ring with a nonplanar piperidinyl or piperazinyl ring could better occupy the binding pocket, enhancing anti-HIV activity. Synthesized heterocyclic compounds based on this modification demonstrated greater potency than Trovirdine hydrochloride, effectively inhibiting HIV replication at nanomolar concentrations without cytotoxicity in infected peripheral blood mononuclear cells .
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- HY-144549
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LXR
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Cardiovascular Disease
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LXR (Liver X receptor) agonist 1 is potent LXR agonist with AC50s of 1.5 nM and 12 nM for LXR-α and LXR-β, respectively. LXR agonist 1 has the potential for the research of atherosclerosis .
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- HY-115527
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SHP2
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Cancer
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SHP244 is a conformational inhibitor targeting the "latch allosteric site" (site 2) of the SHP2 protein with an IC50 value for SHP2 WT of 60 μM. SHP244 has no significant effect on the level of p-ERK alone. SHP244 combined with RMC-4550 (HY-116009) ("tunnel site" site 1 inhibitor) can reduce p-ERK and inhibit the rebound of p-ERK, thereby reducing drug resistance. SHP244 can be used to study drug resistance in FGFR-driven cancers .
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- HY-P99249
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Pogalizumab; MOXR 0916
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Orexin Receptor (OX Receptor)
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Cancer
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Vonlerolizumab (Pogalizumab; MOXR 0916) is a humanized IgG1 monoclonal antibody targeting OX40 (CD134). Pogalizumab partially blocks the interaction between OX40 and its natural ligand OX40L upon binding, thereby activating the NF-κB signaling pathway. Pogalizumab enhances T cell activation and proliferation and has shown antitumor activity in mouse models .
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- HY-170874
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PPAR
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Metabolic Disease
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PPARγ modulator-2 (Compound (R)-2n) is the reversible modulator for PPARγ that inhibits PPARγ ligand-binding domain (LBD) with an IC50 of 41 nM. PPARγ modulator-2 reduces blood glucose, improves the glucose tolerance and insulin tolerance, and exhibits anti-diabetic efficacy in db/db mouse models .
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- HY-117649
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Estrogen Receptor/ERR
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Cancer
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RU-39411 is a steroidal anti-estrogen with mixed estrogenic/antiestrogen activity. RU-39411 has shown inhibitory effects on cell growth in the MCF-7 breast cancer model, with the effect being correlated with its binding affinity to the estrogen receptor. RU-39411 was able to downregulate the estrogen binding capacity of cells, but did not reduce estrogen receptor mRNA levels, indicating that the grafting of its side chain prevents the antagonistic effects usually associated with steroidal estrogens. The administration of RU-39411 can promote the synthesis of progesterone receptors, further supporting its activity as an estrogen .
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- HY-122611
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Androgen Receptor
Apoptosis
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Cancer
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CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
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- HY-12168
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BAY 12-9566
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MMP
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Cancer
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Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models .
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- HY-147736
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GABA Receptor
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Neurological Disease
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GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression .
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- HY-147735
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GABA Receptor
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Neurological Disease
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GABAA receptor agonist 1 (compound 3e) is a potent GABAA receptor agonist. GABAA receptor agonist 1 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 1 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 1 has the potential for the research of depression .
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- HY-156483
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TT-012
2 Publications Verification
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Others
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Cancer
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TT-012 specifically binds to dynamic MITF and destroys the latter's dimer formation and DNA-binding ability. TT-012 inhibits the transcriptional activity of MITF in B16F10 melanoma cells. TT-012 inhibits the growth of high-MITF melanoma cells, and inhibits the tumor growth and metastasis with tolerable toxicity to liver and immune cells in animal models .
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- HY-122611A
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Androgen Receptor
Apoptosis
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Cancer
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CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model
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- HY-126336
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Calcium Channel
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Neurological Disease
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HM12 is a covalent inhibitor of L-/T-type calcium channels. HM12 can strongly inhibit the Cav1.2 (L-type) and Cav3.2 (T-type) calcium channels, and has selectivity for the N-type channels. HM12 produces an irreversible inhibition that persisted after washout. HM12 can be used to study diseases such as hypertension, pain, epilepsy, etc .
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- HY-W757743
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ACP-196-d3
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Isotope-Labeled Compounds
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Others
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Acalabrutinib-d3 (ACP-196-d3) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
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- HY-P11354
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TGF-β Receptor
Apoptosis
Interleukin Related
Integrin
Cadherin
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Inflammation/Immunology
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THR-123 is an orally active ALK3 peptide agonist. THR-123 has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 suppresses inflammation, apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 can be used for the study of kidney fibrosis .
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- HY-103552
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mGluR
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Neurological Disease
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LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research .
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- HY-P990033
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CC-95251; BMS-986351
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CD47
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Cancer
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Anzurstobart (CC-95251; BMS-986351) is a high-affinity, fully human monoclonal anti-SIRPα antibody that blocks the binding of CD47 to SIRPα. Anzurstobart enhances macrophage phagocytic activity against DLBCL cell lines in co-culture models when combined with the antibody Rituximab (HY-P9913). Anzurstobart has the potential for solid and hematologic malignancies research .
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- HY-11079
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Sodium Channel
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Neurological Disease
Inflammation/Immunology
Cancer
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A-803467 is a potent and selective tetrodotoxin-resistant Nav1.8 sodium channel blocker (IC50=8 nM). A-803467 has shown significant anti-nociception in neuropathic and inflammatory pain models. A-803467 enhances the chemosensitivity of conventional anticancer agents through interaction with the ATP-binding cassette subfamily G member 2 (ABCG2) transporter .
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- HY-112863
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ROR
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Inflammation/Immunology
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RORγt inhibitor 3 is an orally active and potent retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor. RORγt inhibitor 3 shows high binding affinity and inhibitory activity of Th17 cell differentiation. RORγt inhibitor 3 also shows efficacy in both mouse experimental autoimmune encephalomyelitis (EAE) and collagen induced arthritis (CIA) models .
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- HY-122255
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mGluR
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Neurological Disease
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LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research .
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- HY-168022
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Aurora Kinase
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Cancer
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CAM2602 is an Aurora A-TPX2 interaction inhibitor that has a binding affinity of 19 nM to Aurora A. CAM2602 can inhibit the growth of pancreatic cancer cells. In solid tumor transplant models, CAM2602 can increase the proportion of PH3 positive cells while reducing the proportion of P-Thr288 Aurora A positive cells, thereby inhibiting tumor growth .
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- HY-145644
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C-135-LS; BMS-986414
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SARS-CoV
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Infection
Cancer
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Ogalvibart (C-135-LS) is a human anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Ogalvibart binds to the spike (S) glycoprotein receptor-binding domain (RBD) of SARS-CoV-2. Ogalvibart in combination with C144LS (1:1 ratio) shows good preventive activity and can effectively block the development of COVID19 in a rhesus monkey disease model .
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- HY-144705
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Cannabinoid Receptor
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Neurological Disease
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GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma .
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- HY-170764
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YAP
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Cancer
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M3686 (Compound 29) is a potent, selective TEAD1 inhibitor with an IC50 value of 51 nM. M3686 also shows weaker binding activity on TEAD3. M3686 potently inhibits cell viability against YAP-dependent NCI-H226 cell line with an IC50 value of 0.06 uM. M3686 shows strong anti-tumor effects in the NCI-H226 xenograft model .
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- HY-175250
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TNF Receptor
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Inflammation/Immunology
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TNF-α-IN-25 is an orally active TNF-α inhibitor. TNF-α-IN-25 shows Fluorescence Polarization (FP) assay IC50 of 103 nM in FP binding assays and L929 assay IC50 of 505 nM in cell-based assays. TNF-α-IN-25 inhibits paw swelling in the glucose-6-phosphate isomerase (GPI) arthritis model. TNF-α-IN-25 can be used for the study of arthritis .
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- HY-P10793
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EGFR
Apoptosis
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Cancer
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Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model .
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- HY-B0027R
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Reference Standards
Antibiotic
Bacterial
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Metabolic Disease
Inflammation/Immunology
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Valnemulin (hydrochloride) (Standard) is the analytical standard of Valnemulin (hydrochloride). This product is intended for research and analytical applications. Valnemulin (hydrochloride) is an orally effective truncated pleurotin antibiotic that inhibits protein synthesis in bacteria by binding to peptidyl transferase in the 50s ribosome subunit. Valnemulin hydrochloride effectively eliminates Mycobacterium bovis in the lungs in an experimental bovine model of Mycoplasma bovis infection. Valnemulin hydrochloride can reduce the mortality of epidemic rabbit enteropathy and has no adverse effect on the growth performance of rabbits .
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- HY-P991353
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PD-1/PD-L1
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Cancer
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Sym-021 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. Sym-021 blocks the binding of PD-L1 and PD-L2 ligands, inducing the secretion of interferon IFN-γ and IL-2 and the proliferation of T cells. Sym-021 has anti-tumor activity in PDX mouse models .
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-
- HY-12168B
-
|
(Rac)-BAY 12-9566
|
MMP
|
Cancer
|
|
(Rac)-Tanomastat ((Rac)-BAY 12-9566) is the racemate of Tanomastat. Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models .
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-
- HY-158316
-
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Fc Receptor (FcR)
|
Others
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|
BTL-MK (Compound 19) an orally active antiallergic agent, that inhibits degranulation of mast cells with an IC50 of 6.7 μM, through binding to the inhibitory receptor FcγRIIB. BTL-MK improves the metaboilic stability in human liver microsomes. BTL-MK ameliorates the allergic response in Ovalbumins (HY-W250978)-induced food allergy mice model. BTL-MK exhibits a good pharmacokinetic character with metabolic stability .
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-
- HY-16999
-
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MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC50 value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model .
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-
- HY-170586
-
-
- HY-P3732
-
|
|
Integrin
|
Cancer
|
|
RGD-4C is a arginine-glycine-aspartic acid peptide (ACDCRGDCFC) with integrin binding activity. The Arg-Gly-Asp (RGD) sequence serves as the primary integrin recognition site in extracellular matrix proteins, and peptides containing this sequence can mimic the recognition specificity of the matrix proteins. RGD-4C is a αv-integrin ligand, can conjugate with bioactive molecule to exert antitumor effects in animal models .
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-
- HY-173474
-
|
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Estrogen Receptor/ERR
Androgen Receptor
|
Cancer
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|
ERβ agonist-1 (Compound 8) is a dual-active selective ERβ agonist (EC50: 46.8 nM) and AR antagonist (IC50: 1555 nM). ERβ agonist-1 activates ERβ signaling by binding to ERβ and inhibits AR activity. ERβ agonist-1 retains selective ERβ agonist activity in mouse models and can be used to study prostate cancer .
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-
- HY-118156
-
|
|
Others
|
Others
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|
L-699333 is a 5-lipoxygenase (5-LO) inhibitor belonging to the thieno[2,3,4-cd]indole class. This compound has a 2-ethoxybutyric acid side chain and is a potent inhibitor of the biosynthesis of 5-HPETE and LTB4 produced from human 5-LO, with ICm values of 22 nM, 7 nM, and 3.8 pM for human neutrophils and whole blood, respectively. L-699333 has shown anti-inflammatory and antiasthmatic effects in a variety of animal models, including rat pleurisy models, antigen-induced wheezing models, and awake macaque and sheep asthma models. Its inhibition of 5-LO is highly selective, with higher ICm values or stronger competitive inhibition in FLAP binding assays compared to inhibition of human 15-LO, porcine 12-LO, and ram epididymal cyclooxygenase. The racemic enantiomer 14g of L-699333 is the most potent enantiomer to date, with inhibitory effects similar to those of the known MK-0591, which has been shown in clinical trials to inhibit the biochemical effects of LTB4 biosynthesis in vitro and LTE4 excretion in urine.
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-
- HY-11052A
-
|
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Opioid Receptor
|
Neurological Disease
|
|
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases .
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-
- HY-B1864AR
-
|
Ksg hydrochloride (Standard)
|
Reference Standards
Antibiotic
Bacterial
|
Infection
|
|
Kasugamycin (Ksg) hydrochloride (Standard) is the analytical standard of Kasugamycin hydrochloride (HY-B1864A). This product is intended for research and analytical applications. Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
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-
- HY-157214
-
|
|
STING
Molecular Glues
|
Cancer
|
|
NVS-STG2 is a molecular glue that targets STINGbinding to pockets between adjacent STING dimer transmembrane domains, effectively acting as a molecular glue. NVS-STGI enhances the activity of cGAMP by inducing the formation of more abundant and larger oligomers. NVS-STG2 produces antitumor activity in animal models .
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-
- HY-169120
-
|
|
Telomerase
|
Cancer
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|
FKB04 is a telomeric repeat binding factor 2 (TRF2) inhibitor that exerts its antitumor activity by disrupting the telomere maintenance mechanism in liver cancer cells, leading to T-loop defects, telomere shortening, and cellular senescence. Additionally, FKB04 can inhibit tumor growth in a human liver cancer xenograft mouse model (with Huh-7 cells implanted in BALB/c mice). FKB04 can be used in liver cancer research .
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-
- HY-175750
-
|
|
DNA/RNA Synthesis
|
Cancer
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|
MOMA-341 is a selective Werner RecQ like helicase (WRN) inhibitor. MOMA-341 binds to WRN at cysteine 727 through an allosteric and ATP-competitive binding mechanism. MOMA-341 induces DNA damage, cell death, and tumor regressions in mismatch-repair deficient (dMMR)/microsatellite instability high (MSI-H) mice model. MOMA-341 has antitumor activity, promising for advanced and metastatic solid tumors research .
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-
- HY-173016
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
HINT1-IN-1 (Compound 8) is the inhibitor for histidine triad nucleotide-binding protein 1 (HINT1) with a Ki of 1.14 μM. HINT1-IN-1 affects the cross-regulation between μ-opioid receptor (MOR) and NMDA receptor (NMDAR). HINT1-IN-1 enhances the analgesic effect of morphine without causing opioid tolerance and has independent analgesic effects in mouse model .
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-
- HY-P99623
-
|
MGD006; S80880
|
CD3
|
Cancer
|
|
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
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-
- HY-160998
-
|
|
CCR
|
Inflammation/Immunology
|
|
YM-344031 is an orally active antagonist for CCR3. YM-344031 inhibits binding of Eotaxin-1 and RANTES to CCR3, with IC50 of 3.0 and 16.3 nM. YM-344031 inhibits ligand-induced rise in intracellular Ca [2+] and the ligand-induced chemotaxis. YM-344031 inhibits eotaxin-1-induced changes in eosinophil morphology in macaques blood, and prevents allergic skin reactions in a mouse allergy model .
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-
- HY-17600
-
|
Calquence; ACP-196
|
Btk
|
Cancer
|
|
Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL) . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-171317
-
|
|
Bacterial
|
Infection
|
|
SMARt751 targets the transcriptional regulatory factor VirS, inhibits its DNA binding ability, upregulates the mymA operon expression, thereby activating Ethionamide (HY-B0276), enhancing the antimicrobial activity of Ethionamide. SMARt751 enhances the antibacterial activity of Ethionamide against M. tuberculosis, reverses the Ethionamide resistance. SMARt751 improves the antibacterial effect of Ethionamide and reduces its effective dose in mouse models. SMARt751 can cross blood brain barrier .
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-
- HY-174375
-
|
|
Others
|
Cancer
|
|
NEDD4-IN-1 (Compound 32) is a potent inhibitor of NEDD4 (IC50 = 0.12 μM). NEDD4-IN-1 shows significant and comparable antiproliferative activity in H292 cell line. NEDD4-IN-1 demonstrates high plasma protein binding and medium-to-high in vitro clearance in both human and mouse models. NEDD4-IN-1 shows superior stability in mouse plasma. NEDD4-IN-1 has excellent potency, selectivity, and favourable in vitro ADME properties. NEDD4-IN-1 exhibits a systemic plasma clearance exceeding the hepatic blood flow in mouse model. NEDD4-IN-1 can be studied in anticancer research .
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-
- HY-165559
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
Trpvicin is a potent and subtype-selective TRPV3 inhibitor with IC50s of 0.41 and 0.22 μM for hTRPV3-WT and hTRPV3-G573S mutant, respectively. Trpvicin exhibits minimal effects on other TRP family members (such as TRPV1/2/4/5/6, TRPA1 and TRPM8). Trpvicin inhibits the TRPV3 channel by stabilizing it in a closed state via VSLD-PD binding. Trpvicin accesses additional binding sites inside the central cavity of the G573S mutant to remodel symmetry and block the channel. Trpvicin inhibits itch and hair loss in mouse models. Trpvicin can be used for study of inflammation and immunology .
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-
- HY-12193
-
|
|
Histamine Receptor
|
Others
|
|
A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .
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-
- HY-160921
-
|
SL65.0155 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Capeserod (SL65.0155 free base) is an agonist for serotonin receptor (5-HT receptor), with a Ki of 0.6 nM for 5-HT4 receptor. Capeserod enhances expression of phopshorilated cAMP-response element binding protein (p-CREB), vascular endothelium growth factor (VEGF), brain-derived neurotrophic factor (BDNF) and B cell lymphoma-2 (Bcl-2) proteins in hippocampus, and exhibits antidepressant-like efficacy in Wistar rats models .
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-
- HY-122611R
-
|
|
Reference Standards
Androgen Receptor
Apoptosis
|
Cancer
|
|
CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
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-
- HY-N1486R
-
|
3-Ketoursolic acid (Standard)
|
Reference Standards
Apoptosis
Endogenous Metabolite
NF-κB
|
Inflammation/Immunology
Cancer
|
|
CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
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-
- HY-175318S
-
|
|
MDM-2/p53
|
Cancer
|
|
p53 Activator 15 is an orally active p53 Y220C activator. p53 Activator 15 enhances the DNA binding of p53 Y220C (SC50 = 0.58 nM) and significantly inhibits NUGC-3 cell proliferation. p53 Activator 15 effectively inhibits tumor growth in NUGC-3 xenograft mouse and rat models. p53 Activator 15 can be used to study gastric cancer .
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-
- HY-P1220
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain .
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-
- HY-P1220A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain .
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-
- HY-B1864BR
-
|
Ksg hydrochloride hydrate (Standard)
|
Reference Standards
Antibiotic
Bacterial
|
Infection
|
|
Kasugamycin (Ksg) hydrochloride hydrate (Standard) is the analytical standard of Kasugamycin hydrochloride hydrate (HY-B1864B). This product is intended for research and analytical applications. Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
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-
- HY-144256
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
CHD1Li 6.11 is a potent and orally active Chromodomain Helicase DNA Binding Protein 1 Like (CHD1L) (oncogenic gene) inhibitor (IC50 = 3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 can inhibit EMT, induce mesenchymal-epithelial transition (reverse EMT) and promote apoptosis in tumor organoid models. CHD1Li 6.11 can be used for the research of cancer, such as colorectal cancer .
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-
- HY-P99171
-
|
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .
|
-
- HY-117006
-
E1231
1 Publications Verification
1-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-one
|
Sirtuin
|
Cardiovascular Disease
|
|
E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE -/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases .
|
-
- HY-159585
-
|
|
Cytochrome P450
Fungal
|
Infection
|
|
CYP51-IN-20 (compound 5b) is an inhibitor of CYP51 and has antifungal activity. CYP51-IN-20 has a significant inhibitory effect on Candida albicans ATCC 10231, downregulates ERG11 (Cyp51) gene expression, and significantly reduces the yeast-to-hyphae morphological transition. CYP51-IN-20 can synergize with Voriconazole (HY-76200) to occupy the entire CYP51 binding site and exert a synergistic inhibitory effect in the Glechoma moth model .
|
-
- HY-17600R
-
|
ACP-196 (Standard)
|
Reference Standards
Btk
|
Cancer
|
|
Acalabrutinib (Standard) is the analytical standard of Acalabrutinib. This product is intended for research and analytical applications. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL) . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-124388
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PDE4-IN-20 is a selective submicromolar phosphodiesterase-4 (PDE4) inhibitor with anti-TNF-α properties. PDE4-IN-20 exhibits significant biological activity in vitro and in vivo. The mechanism of action of PDE4-IN-20 is supported by molecular modeling studies, which reveal its binding mode with PDE4. PDE4-IN-20 was optimized in further conformational analysis and showed pharmacological characteristics similar to those of known PDE4 inhibitors .
|
-
- HY-12927
-
|
|
CXCR
|
Inflammation/Immunology
|
|
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca 2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model .
|
-
- HY-168948
-
|
|
Bacterial
|
Infection
|
|
Quorum sensing-IN-9 (Compound 7d) inhibits quorum sensing in Pseudomonas aeruginosa by binding PqsR proteins. Quorum sensing-IN-9 inhibits the expression of quorum sensing systems related genes lasB, rhlA and pqsA, blocks the generation of virulence factors elastase, pyocyanin and rhamnolipid. Quorum sensing-IN-9 destorys the motility of P. aeruginosa, inhibits the biofilm formation, decreasing the virulence and pathogenicity of P. aeruginosa. Quorum sensing-IN-9 exhibits anti-infectious activity in Galleria mellonella larval model .
|
-
- HY-176758
-
|
|
Glutathione Peroxidase
|
Cancer
|
|
GPX4-IN-17 (Compound 9i) is an inhibitor of GPX4 with potent cytotoxicity (IC50 = 0.3 nM). GPX4-IN-17 shows strong binding affinity against GPX4 (KD = 20.4 nM). GPX4-IN-17 inhibits tumor growth in the xenograft tumor mouse model without detectable cytotoxicity. GPX4-IN-17 can enhance cancer chemotherapy and overcome tumor resistance. GPX4-IN-17 can be studied in antitumor reseach .
|
-
- HY-170925
-
|
|
Cholinesterase (ChE)
Apoptosis
|
Neurological Disease
|
|
AChE-IN-81 (compound 22) is a potent, irreversible and selective AChE inhibitor. AChE-IN-81 inhibits activity on AChE with inhibitory rates of 80.0%, with an IC50 of 3.7 μM. AChE-IN-81 binds to AChE with a binding affinity (Kd) of 5.37 μM. AChE-IN-81 effectively reduces in zebrafish brain cells. AChE-IN-81 exhibits potential neuroprotective activities on H2O2-induced SH-SY5Y cell injury model .
|
-
- HY-146432
-
|
|
Apoptosis
Raf
Ras
ROS Kinase
MDM-2/p53
|
Cancer
|
|
Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model .
|
-
- HY-N11768
-
|
|
NF-κB
Interleukin Related
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
4-Methoxylonchocarpin is an orally active anti-inflammatory agent. 4-methoxylonchocarpin inhibits the binding of LPS to Toll-like Receptor (TLR) TLR4 to inhibit NF-κB activation and TNF Receptor and IL-6 expression. 4-Methoxylonchocarpin also inhibits the phosphorylation of TGF-beta activated kinase 1 and TNBS-induced expression of IL-1β, IL-17A, and TNF. 4-methoxylonchocarpin can improve 2,4, 6-trinitrobenzene sulfonic acid (TNBS)-induced colitis mouse model .
|
-
- HY-19487
-
|
|
Bacterial
|
Infection
|
|
Ribocil is a selective inhibitor targeting the bacterial FMN riboswitch, regulating the bacterial riboflavin riboswitch. Ribocil competitively binds to the FMN binding site, mimicking the natural ligand FMN to induce conformational changes in the riboswitch, inhibiting ribB gene expression, reducing riboflavin synthesis, and thus inhibiting bacterial growth. Ribocil strongly inhibits GFP expression (EC50=0.3 μM). Ribocil exhibits in vivo antibacterial activity in a mouse model and can be used to study antibacterial drugs related to drug-resistant bacterial infections and bacterial riboflavin metabolic pathways[1][2].
|
-
- HY-P991447
-
|
|
VISTA
|
Cancer
|
|
Anti-VSIR/VISTA Antibody (SG7) is a human monoclonal antibody (mAb) targeting VISTA/B7-H5. Anti-VSIR/VISTA Antibody (SG7) inhibits VISTA function and prevents PSGL-1 and VSIG3 from binding to VISTA. Anti-VSIR/VISTA Antibody (SG7) has anti-tumor activity in the mouse B16F10 melanoma model. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-176537
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
RGN6024 is a brain-penetrant, orally active and reversible small molecule tubulin destabilizer. RGN6024 inhibits microtubule polymerization both in biochemical and cellular assays, binds to the colchicine binding pocket of β-tubulin (SPR: Kd = 6.7 μM; tryptophan assay: Kd = 7.4 μM), and triggers G2/M arrest in glioblastoma (GB) cells. RGN6024 retains activity in βIII-tubulin overexpressing cells. RGN6024 inhibits tumor growth in a GB xenograft mouse model. RGN6024 can be used for the study of glioblastoma (GB) .
|
-
- HY-155356
-
|
|
PROTACs
Ras
|
Cancer
|
|
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
|
-
- HY-178342
-
|
|
Xanthine Oxidase
Reactive Oxygen Species (ROS)
SOD
|
Metabolic Disease
Inflammation/Immunology
|
|
Xanthine oxidase-IN-18 is a potent orally activeXanthine oxidase (XO) inhibitor (IC50 = 0.263 μM). Xanthine oxidase-IN-18 exerts inhibition by directly and stably binding to the xanthine oxidase Mo-co active site. Xanthine oxidase-IN-18 exhibits reactive oxygen species (ROS) scavenging activity. Xanthine oxidase-IN-18 shows anti-hyperuricemia effects in a Potassium oxonate (HY-17511)-induced hyperuricemic rat model. Xanthine oxidase-IN-18 can be used for hyperuricemia, breast and lung cancer research .
|
-
- HY-122179
-
|
|
TGF-β Receptor
|
Inflammation/Immunology
|
|
NUCC-555 is an activin antagonist. NUCC-555 interacts with Trp25, Trp28, Phe55, Tyr93, Lys103, and Asn107 in the Activin A binding pocket. NUCC-555 blocks Activin A-mediated hepatic stellate cells (HSCs) activation. NUCC-555 promotes liver regeneration and halts fibrosis progression in chronic liver disease models. NUCC-555 inhibits Activin A-mediated ovarian cell proliferation. NUCC-555 decreases FSH levels in ovariectomized mice .
|
-
- HY-174346
-
|
|
E1/E2/E3 Enzyme
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
Skp2-IN-4 is an Skp2 inhibitor with a IC50 of 0.38 μM for Skp2-Cks1 binding. Skp2-IN-4 improves anti-tumor activity, inhibits the proliferation and induces S phase arrest by targeting Skp2. Skp2-IN-4 significantly enhances Cisplatin (HY-17394) chemosensitivity by suppressing the tumor cell stemness in NCl-H1299 xenograft mice model, promising for lung cancer and esophageal cancer research .
|
-
- HY-33299
-
|
BTCA
|
Biochemical Assay Reagents
|
Cancer
|
|
Serpin B9-IN-1 (BTCA) is an inhibitor that specifically targets Serpin B9 (SB9); SB9 is a natural inhibitor of granzyme B (GrB) , but may promote the metastasis of lung cancer cells into the bone marrow. SB9-overexpressing cancer cells promote proliferation and metastasis in an immune cell-dependent manner by binding to GrB. Inhibition of SB9 by Serpin B9-IN-1 significantly inhibits immunotherapy of lung cancer bone metastases in the caudal artery (CA) mouse model (LCBM) .
|
-
- HY-163410
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
AU-24118 is a selective and orally bioavailable PROTAC degrader of mSWI-SNF ATPases (SMARCA2 and SMARCA4) and PBRM1. AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase. AU-24118 demonstrates tumor regression in prostate cancer model. AU-24118 can be studied to combat prostate cancer. (Pink: PBRM1/SMARCA2,4 ligand (HY-171774); Blue: CRBN ligand (HY-171775)) .
|
-
- HY-P991598
-
|
MOR12743; MOR03207
|
Interleukin Related
NF-κB
|
Inflammation/Immunology
|
|
MOR-106 (MOR12743) is a humanized anti-IL-17C IgG1 monoclonal antibody. MOR-106 inhibits the NF-κB signaling pathway by specifically binding to IL-17C (IC50 = 59 pM for human IL-17C, IC50 = 55 pM for mouse IL-17C). MOR-106 can effectively inhibit skin inflammation and reduce related inflammatory factors in animal models of psoriasis and atopic dermatitis .
|
-
- HY-107588
-
TC-I 15
1 Publications Verification
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Integrin
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Cardiovascular Disease
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TC-I 15 (TC-I-15) is a type of allosteric collagen-binding integrin α2β1 inhibitor, and it also inhibits α1β1 and α11β1. TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition. TC-I 15 prevents the formation of a pre-metastatic microenvironment by inhibiting the uptake of cancer-associated fibroblast (CAF) extracellular vesicles (EVs) by lung fibroblasts, which reduces the metastasis of salivary gland adenocystic carcinoma (SACC) to the lungs in mouse models, .
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- HY-19210
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Endothelin Receptor
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Cardiovascular Disease
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SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
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- HY-P990004
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Tim3
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Inflammation/Immunology
Cancer
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Anti-Mouse TIM-3 Antibody (B8.2C12) is an anti-mouse TIM-3 IgG1 monoclonal antibody. Anti-Mouse TIM-3 Antibody (B8.2C12) can block the binding of Tim-3 with Phosphatidylserine (PtdSer) and CEACAM1 without interfering with the binding to Galectin-9. Anti-Mouse TIM-3 Antibody (B8.2C12) can inhibit tumor growth and activate tumor infiltrating CD8 + T cells. Anti-Mouse TIM-3 Antibody (B8.2C12) can be used for studying cancer such as breast cancer and colon cancer and constructing experimental autoimmune encephalomyelitis (EAE) models .
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- HY-129085
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C5OH
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Drug Derivative
Apoptosis
NF-κB
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Cancer
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5-Methyl cromolyn (C5OH) disodium, an analog of Cromolyn (HY-B1619), is a S100P inhibitor. 5-Methyl cromolyn disodium inhibits the binding of S100P to its receptor RAGE, NF-κB activity and cell proliferation, and promotes Gemcitabine (HY-17026)-induced apoptosis. 5-Methyl cromolyn disodium reduces tumor growth and metastasis, and prolongs survival in mouse models of syngeneic PDAC. 5-Methyl cromolyn disodium can be used for pancreatic cancer like pancreatic ductal adenocarcinoma (PDAC) research .
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- HY-100555
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HSP
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Infection
Cancer
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CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
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- HY-P10870
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Peptide-Drug Conjugates (PDCs)
FGFR
Apoptosis
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Cancer
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Pep1-DNP conjugate 9 is a functionalized peptide which is composed of the DNP-Hapten and the FGFR1 binding peptide. Pep1-DNP conjugate 9 exhibits good affinity to FGFR1 with KD of 5.01 μM. Pep1-DNP conjugate 9 recruits anti-DNP antibodies to the surface of FGFR1-positive cells, inhibits the FGF2-induced proliferation in rat skeletal myoblast cells, and induces apoptosis. Pep1-DNP conjugate 9 exhibits antitumor efficacy in mouse models .
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- HY-P991270
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Interleukin Related
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Inflammation/Immunology
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MT204 is a humanized IgG1 antibody inhibitor targeting IL-2 of human and rhesus monkey origin. MT204 prevents soluble IL-2 from binding to intermediate-affinity IL-2 receptors and blocks CD25-bound IL-2 on high-affinity IL-2 receptors. MT204 has potently anti-proliferative activity with NKL cells and primary NK cells. MT204 has good tolerability and potent immunosuppressive activity in allogeneic skin graft model of rhesus monkey, promising for immunosuppressive and anti-proliferative therapy .
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- HY-W181530
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Molecular Glues
CDK
Apoptosis
Ligands for E3 Ligase
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Cancer
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NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models .
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- HY-123960
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Raphin1
3 Publications Verification
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Phosphatase
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Neurological Disease
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Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease .
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- HY-123960A
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Phosphatase
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Neurological Disease
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Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease .
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- HY-117380
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Neurokinin Receptor
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Neurological Disease
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SB 235375 is a potent and selective antagonist of the human neurokinin-3 (hNK-3) receptor designed by optimizing the structure of 2-phenyl-4-quinolinecarboxylic acid amide. SB 235375 displays high affinity for the hNK-3 receptor, with significantly higher binding affinities than hNK-2 and hNK-1 receptors. In vitro studies demonstrated its ability to block NK-3 receptor-mediated contraction and calcium mobilization, while in vivo, SB 223412 demonstrated oral and intravenous activity against NK-3 receptor-driven responses in animal models .
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- HY-103490
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EDHS-206
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MAP3K
Apoptosis
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Infection
Inflammation/Immunology
Cancer
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Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
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- HY-P991571
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GC-1118A
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EGFR
PERK
Akt
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Cancer
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GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .
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- HY-P991584
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FGFR
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Cancer
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HuGAL-FR21 is a humanized antiFGFR2IIIb IgG1 monoclonal antibody. HuGAL-FR21 can block the binding of FGF2, FGF7, and FGF10 to FGFR2IIIb and inhibit FGF-induced phosphorylation of FGFR2IIIb. HuGAL-FR21 can downregulate the expression of FGFR2 in SNU-16 cells. HuGAL-FR21 shows the significant anti-tumor activity in athymic nude mice bearing gastric cancer xenograft models. HuGAL-FR21 can be used for research on cancer such as gastric cancer .
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- HY-110333
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EGFR
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Cancer
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BMS-599626 dihydrochloride is a small molecule pan-HER (human epidermal growth factor receptor) kinase inhibitor. BMS-599626 dihydrochloride primarily targets HER1 (IC50=20 nmol/L) and HER2 (IC50=30 nmol/L) kinase activity in the HER family. BMS-599626 inhibits the kinase activity of HER1 and HER2 by competing with their ATP-binding sites, and can inhibit the downstream signaling pathway by blocking the heterodimer formation of HER1 and HER2. BMS-599626 dihydrochloride can be used to study the antitumor effects of multiple HER1 or HER2 overexpressed tumor models .
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- HY-116142
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iGluR
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Neurological Disease
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CP-283097 is a conformationally restricted and NR2B subtype-selective NMDA antagonist. CP-283097 efficiently competitively inhibits the binding of [³H]CP-101,606 to the rat meninges, with an IC50 value of 18 nM. CP-283097 exhibits nearly complete inhibition of the current mediated by the NR2B receptor (IC50 = 206 nM), while the inhibitory effect on the NR2A or NR2C receptors is very weak. CP-283097 demonstrates excellent central nervous system permeability and in vivo efficacy in animal models. CP-283097 can be used for neurological diseases related to excessive activation of NMDA receptors .
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- HY-147081
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AS 1411
2 Publications Verification
AGRO-100
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Histone Methyltransferase
Bcl-2 Family
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Cancer
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AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
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- HY-103151A
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5-HT Receptor
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Others
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CP94253 is a selective, orally active agonist for serotonin receptor 1B (5-HT1B), through competitive binding with iodocyanopindolol (ICP) to the 5-HT1 receptor. CP94253 binds to the 5-HT1B, 5-HT1A, 5-HT1D, 5-HT1C and 5-HT2 receptors, with Kis of 2, 89, 49, 860 and 1600 nM. CP94253 causes satiety, anorexia, weight loss and hyperlocomotion in rats model .
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- HY-P990259
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Transmembrane Glycoprotein
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Inflammation/Immunology
Cancer
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Anti-Mouse CD96 Antibody (3.3) is a rat-derived anti-mouse CD96 IgG1 λ type antibody inhibitor. Anti-Mouse CD96 Antibody (3.3) blocks binding of CD155 to CD96. Anti-Mouse CD96 Antibody (3.3) can enhance the antitumor efficacy of multiple immune-checkpoint inhibitors. Anti-Mouse CD96 Antibody (3.3) shows potent anti-tumor and anti-metastatic activity in various tumor models. Anti-Mouse CD96 Antibody (3.3) can be used for the researches of cancer and inflammation, such as mammary carcinoma .
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- HY-P10786
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Transmembrane Glycoprotein
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Cancer
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LinTT1 peptide is a tumor-penetrating peptide with the amino acid sequence AKRGARST. LinTT1 peptide targets peritoneal carcinoma (PC) by binding to the p32 (gC1qR) receptor. It can conjugate with iron oxide nanoworms (NWs) to form a nanocarrier. This nanocarrier is taken up by peritoneal carcinoma cells in vitro and enters the mitochondria; it also exhibits significant tumor targeting and penetration effects in mice. Moreover, LinTT1-functionalized nanocarriers, combined with the pro-apoptotic peptide [D(KLAKLAK)2], show significant tumor suppression in a mouse peritoneal tumor model. LinTT1 peptide holds promise as a delivery carrier for peritoneal cancer research .
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- HY-P10393
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ERα (295-311)
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Apoptosis
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Cancer
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ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
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- HY-175698
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Ferroptosis
Microtubule/Tubulin
COX
Glutathione Peroxidase
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Cancer
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Ferroptosis inducer-9 is a ferroptosis inducer and colchicine site tubulin polymerization inhibitor. Ferroptosis inducer-9 inhibits MCF-7 cell growth with an IC50 of 14 nM and inhibits [ 3H]colchicine binding. Ferroptosis inducer-9 reduces expression of GPX4 and FTH, increases COX2 and ACSL4, lowers GSH, NADP+, and NADPH levels, increases LPO, MDA, and Fe(II) levels, and decreases SOD concentrations. Ferroptosis inducer-9 demonstrates significant anti-tumor efficacy in HCT116 CRC xenograft model. Ferroptosis inducer-9 can be used for the study of triple negative breast cancer (TNBC) and colorectal cancer (CRC) .
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- HY-178169
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Toll-like Receptor (TLR)
p38 MAPK
TNF Receptor
ERK
JNK
NF-κB
Interleukin Related
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Inflammation/Immunology
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ETI60 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.68 μM) and TLR9 (IC50 = 0.12 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI60 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI60 modulates the expression of genes associated with inflammation. ETI60 effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI60 can be used for autoimmune and inflammatory diseases research .
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- HY-178343
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Aurora Kinase
Apoptosis
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Cancer
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Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research .
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- HY-178166
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Toll-like Receptor (TLR)
p38 MAPK
TNF Receptor
ERK
JNK
NF-κB
Interleukin Related
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Inflammation/Immunology
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ETI41 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.63 μM) and TLR9 (IC50 = 0.16 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI41 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI41 suppresses the expression of inflammation-associated genes and effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI41 can be used for autoimmune and inflammatory diseases research .
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- HY-173182
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Microtubule/Tubulin
P-glycoprotein
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Cancer
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Antitumor agent-200 (Compound 2g) is a microtubule synthesis inhibitor. By binding to the colchicine site of tubulin, it causes G2/M cell cycle arrest and generates reactive oxygen species (ROS). Antitumor agent-200 exhibits significant inhibitory activity against MCF7/ADR and KBV200 cell lines with overexpression of P-glycoprotein (P-gp), with drug resistance indices (DRI) of 0.83 and 0.58 respectively. In the MCF-7 xenograft model, Antitumor agent-200 (25 mg/kg, intraperitoneal injection) can achieve a tumor growth inhibition rate of 57.2%. Antitumor agent-200 can be used in the research of the anti-cancer field .
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- HY-175455
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PROTACs
Androgen Receptor
Akt
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Cancer
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LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR). LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002)-insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC). (Pink: AR-DBD ligand-1: HY-175456, Blue: Thalidomide: HY-14658, Pink + Black: AR-DBD ligand-Linker Conjugate 1: HY-175457, Black: Boc-piperidine-oxopiperidin: HY-175458) .
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- HY-101741
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A-289099
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Microtubule/Tubulin
Apoptosis
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Cancer
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A-259745 is an orally active antimitotic agent that binds to the colchicine-binding site of tubulin. A-259745 exhibits potent in vitro cytotoxic activity against both multi-drug-resistant and non-multi-drug-resistant cancer cell lines, with ED50 values of 0.018 μM against HCT-15 and 0.028 μM against NCI-H460 cell lines. A-259745 inhibits tubulin polymerization, disrupts the dynamic equilibrium of the mitotic spindle, arrests dividing cells in metaphase, and subsequently induces apoptosis. A-259745 shows dose-dependent antitumor efficacy in murine tumor models. A-259745 can be used for the study of cancer .
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- HY-103490R
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EDHS-206 (Standard)
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Reference Standards
MAP3K
Apoptosis
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Infection
Inflammation/Immunology
Cancer
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Takinib (Standard) is the analytical standard of Takinib. This product is intended for research and analytical applications. Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
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- HY-N0837
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NSC17821; NSC23880
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PI3K
Akt
mTOR
Autophagy
Apoptosis
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Neurological Disease
Metabolic Disease
Cancer
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Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
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- HY-128574
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DS11252927
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GLUT
PI3K
Akt
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Metabolic Disease
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D927 (DS11252927) is an orally active glucose transporter type 4 (GLUT4) translocation activator with an EC50 of 0.14 μM. D927 enhances the binding affinity of PI3Kα catalytic subunit p110α to canonical RAS proteins (KRAS4A, KRAS4B) and RRAS, RRAS2, MRAS. D927 activates the PI3Kα-AKT pathway (increasing phosphorylation of AKT, p70S6 kinase) without affecting the RAF-ERK1/2 pathway. D927 improves hyperglycemia in type 1 and type 2 diabetes mice model. D927 can be used for the study of glucose homeostasis disorders and diabetes .
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- HY-117093
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HDAC
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Cancer
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H8-A5 is a novel human histone deacetylase 8 (HDAC8) inhibitor. A highly specific ZBG-based pharmacophore model was developed by incorporating a custom zinc-binding group (ZBG) feature. Pharmacophore-based virtual screening identified three novel HDAC8 inhibitors with low micromolar IC50 values (1.8-1.9 μM). Further studies showed that H8-A5 was more selective for HDAC8 than HDAC1/4 and exhibited antiproliferative activity in MDA-MB-231 cancer cells. Molecular docking and molecular dynamics studies showed that H8-A5 could bind to HDAC8, providing a good starting point for the development of HDAC8 inhibitors for cancer treatment.
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- HY-141878
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PROTACs
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Neurological Disease
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Di-Ellipticine-RIBOTAC (Compound 7) is a RNA RIBOTAC degrader, capable of specifically binding and degrading r(G4C2)exp. Di-Ellipticine-RIBOTAC only cuts the expanded GGGGCC repeat RNA in the pathogenic factor of amyotrophic lateral sclerosis/ frontotemporal dementia (c9ALS/FTD) - the chromosome 9 open reading frame 72 (9orf72) gene (r(G4C2)exp), and has no effect on normal short repetitive sequences. Di-Ellipticine-RIBOTAC significantly improves the pathological phenotype of c9ALS/FTD in cells and mouse models. Di-Ellipticine-RIBOTAC can be used for the study of c9ALS/FTD .
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- HY-151096
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CXCR
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Inflammation/Immunology
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ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research .
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- HY-W013403
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IFNAR
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Infection
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2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
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- HY-P99395
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JNJ 56022473; CSL 362
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Interleukin Related
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Cancer
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Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
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- HY-170524
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SARS-CoV
DNA Methyltransferase
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Infection
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TDI-015051 is an orally active inhibitor for SARS-CoV-2 nonstructural protein 14 (NSP14) with an IC50 ≤0.15 nM. TDI-015051 inhibits SARS-CoV-2 NSP14 in Huh-7.5 cell (EC50=11.4 nM) and in ACE2-TMPRSS2 expressing A549 cell (EC50=64.7 nM). TDI-015051 also inhibits other coronaviruses like α-hCoV-NL63, α-hCoV-229E and β-hCoV-MERS with IC50s of 1.7, 2.6 and 3.6 nM, respectively. TDI-015051 binds to the SAH-stabilized cap binding pocket, inhibits viral RNA methylation and viral replication, and exhibits anti-infectious activity in mouse models .
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- HY-N7368
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Adenosine Deaminase
Bacterial
Caspase
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Infection
Neurological Disease
Inflammation/Immunology
Cancer
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Hibifolin is a flavonol glycoside that can be isolated from Helicteres isora. Hibifolin is an inhibitor of adenosine deaminase (ADA) (Ki = 49.92 μM). Hibifolin protects neurons against β-amyloid-induced neurotoxicity. Hibifolin possesses a potent protective activity against cell death induced by aggregated Aβ. Hibifolin can abolish Aβ-induced caspase-3 and caspase-7 activation. Hibifolin induces Akt phosphorylation in cortical neurons. Hibifolin is also a natural sortase A (SrtA) inhibitor (IC50 = 31.2 μM) through direct binding to SrtA protein. Hibifolin attenuates the pathogenic behavior of Staphylococcus aureus including adhesion, invasion, and biofilm formation. Hibifolin improves the survival of pneumonia induced by Staphylococcus aureus in mouse model and alleviates pathological damage. Hibifolin shows a synergistic antibacterial effect with Cefotaxime (HY-A0088A) .
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- HY-159922
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Androgen Receptor
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Cancer
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AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .
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- HY-125938
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Cycloartenol ferulate; Cycloartenol ferulic acid ester
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Drug Derivative
Apoptosis
Reactive Oxygen Species (ROS)
JAK
STAT
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Inflammation/Immunology
Cancer
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Cycloartenyl ferulate (Cycloartenol ferulate; Cycloartenol ferulic acid ester) is a derivative of γ-oryzanol (HY-B2194) with multiple biological activities including antioxidant, anti-inflammatory, and anti-tumor properties. Cycloartenyl ferulate selectively binds to IFNγR1 (binding affinity Kd = 0.5 μM) to activate the canonical JAK1/2-STAT1 signaling pathway. Cycloartenyl ferulate inhibits paraquat (PQ)-triggered apoptosis and ROS in HK2 cells. Cycloartenyl ferulate enhances the activation and cytolytic activity of natural killer (NK) cells by upregulating the expression of NK cell activation receptors (NKG2D, NKp30, NKp44) and the release of cytotoxic molecules and cytokine IFNγ. Cycloartenyl ferulate exerts anti-cancer effects in tumor mice models. Cycloartenyl ferulate can be used for the study of cancer and allergic inflammation intervention .
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- HY-N8146
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STAT
Bcl-2 Family
Ser/Thr Kinase
Survivin
c-Myc
Apoptosis
Necroptosis
CDK
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Infection
Cancer
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Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells .
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- HY-12875
-
|
|
Ras
|
Cancer
|
|
BQU57 is a selective inhibitor of RalA/RalB small GTPases, with a binding potency (Kb) of 7.7 μM for RalB-GDP. BQU57 can block its interaction with effector proteins (such as SEC5 and EXO84), inhibiting tumor cell migration, invasion and non-adherent growth. BQU57 downregulates the NF-κB signaling pathway, reduces the expression of IL-6, IL-8 and MMP-13, and inhibits apoptosis by regulating the Bcl-2/Bax balance. BQU57 also protects the extracellular matrix by inhibiting the Ral/NF-κB pathway and can be used for the study of degenerative diseases. BQU57 exhibits significant antitumor activity in triple-negative breast cancer (TNBC) models, inhibiting orthotopic tumor growth and lung metastasis and enhancing paclitaxel chemotherapy sensitivity .
|
-
- HY-174403
-
|
|
Bcl-2 Family
c-Myc
Apoptosis
Caspase
|
Cancer
|
|
c-MYC/BCL2 ligand 1 iodide is a dual-targeting c-MYC/Bcl-2 G4 ligand with Kd values of 0.90 μM (c-MYC G4) and 0.56 μM (Bcl-2 G4). c-MYC/BCL2 ligand 1 iodide inhibits c-MYC and Bcl-2 gene transcription by binding to G4-forming sequences and downregulates their protein expression. c-MYC/BCL2 ligand 1 iodide inhibits suppresses migration, induces caspase-dependent apoptosis, and triggers cell cycle G1 arrest in MCF-7 cells. c-MYC/BCL2 ligand 1 iodide significantly suppresses tumor growth in a 4T1 syngeneic model with no observable toxicity. c-MYC/BCL2 ligand 1 iodide can be used for the research of breast cancer.
|
-
- HY-N7368R
-
|
|
Reference Standards
Adenosine Deaminase
Bacterial
Caspase
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Hibifolin (Standard) is the analytical standard of Hibifolin. This product is intended for research and analytical applications. Hibifolin is a flavonol glycoside that can be isolated from Helicteres isora. Hibifolin is an inhibitor of adenosine deaminase (ADA) (Ki = 49.92 μM). Hibifolin protects neurons against β-amyloid-induced neurotoxicity. Hibifolin possesses a potent protective activity against cell death induced by aggregated Aβ. Hibifolin can abolish Aβ-induced caspase-3 and caspase-7 activation. Hibifolin induces Akt phosphorylation in cortical neurons. Hibifolin is also a natural sortase A (SrtA) inhibitor (IC50 = 31.2 μM) through direct binding to SrtA protein. Hibifolin attenuates the pathogenic behavior of Staphylococcus aureus including adhesion, invasion, and biofilm formation. Hibifolin improves the survival of pneumonia induced by Staphylococcus aureus in mouse model and alleviates pathological damage. Hibifolin shows a synergistic antibacterial effect with Cefotaxime (HY-A0088A) .
|
-
- HY-N0837R
-
|
NSC17821 (Standard); NSC23880 (Standard)
|
Reference Standards
PI3K
Akt
mTOR
Autophagy
Apoptosis
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Veratramine (NSC17821; NSC23880) (Standard) is the analytical standard of Veratramine (HY-N0837). This product is intended for research and analytical applications. Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
|
-
- HY-175236
-
|
|
PD-1/PD-L1
Apoptosis
ERK
JNK
Cadherin
p38 MAPK
GSK-3
IFNAR
Caspase
Bcl-2 Family
|
Cancer
|
|
SF-9-2 is a PD-L1/PD-1 binding inhibitor (IC50 = 24.9 nM). SF-9-2 inhibits epithelial-mesenchymal transition, migration, invasion, and proliferation of SK-N-SH cells, and also induces apoptosis and cell cycle arrest. SF-9-2 blocks PD-L1-induced SK-N-SH cell growth through the MAPK signaling pathway. SF-9-2 restores GSK-3β activity and enhances PD-L1 degradation through the ubiquitin-proteasome pathway. SF-9-2 inhibits tumor growth in the SK-N-SH NOG mouse model without significant toxicity. SF-9-2 also acts as an immune checkpoint inhibitor, blocking PD-L1 to restore T cell function. SF-9-2 can be used in neuroblastoma research .
|
-
- HY-176220
-
|
|
AUTACs
Autophagy
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
|
GPX4-AUTAC is a GPX4-targeting autophagy-mediated degrader (AUTAC). GPX4-AUTAC consists of an inhibitor ML162-yne (HY-153748), a degradation tag FBnG (HY-W073762) and a glycol linker (HY-W021401). GPX4-AUTAC promotes the ubiquitination of GPX4 by E3 ligase TRAF6, and enhances the binding with GPX4 and p62, leading to the selective autophagy-dependent degradation of GPX4. GPX4-AUTAC significantly induces ferroptosis and shows a potent anti-cancer activity in breast cancer cells, breast cancer-derived organoids (PDOs) and MDA-MB-231 tumor xenograft mice model, with potent synergistic effects when combined with Sulfasalazine (SAS) (HY-14655) or chemotherapy drugs (Paclitaxel (HY-B0015) or Cisplatin (HY-17394)) .
|
-
- HY-161483
-
|
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Neurological Disease
Cancer
|
|
CBP/p300 ligand 3 is a target protein ligand of CBPD-268 (HY-161369). CBP and p300 are two proteins with histone acetyltransferase (HAT) activity, and CBP and p300 play key roles in regulating biological processes such as gene expression, cell proliferation, differentiation and DNA repair. Through its acetyltransferase activity, CBP/p300 can acetylate histones and other proteins, thereby regulating chromatin structure and gene expression. CBP/p300 ligand 3 regulates the function of CBP/p300 by binding to a specific domain of the CBP/p300 protein (the bromine domain or HAT domain), inhibiting its enzyme activity or altering its interactions with other proteins (transcription factors). CBP/p300 ligand 3 can be used in cancer, neurodegenerative diseases and other disease models associated with abnormal CBP/p300 function .
|
-
- HY-W013403S
-
|
|
IFNAR
|
Infection
|
|
2'-Deoxy-2'-fluorouridine-d2 is the deuterium labeled 2'-Deoxy-2'-fluorouridine . 2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
|
-
- HY-177578
-
|
|
Antibody-Drug Conjugates (ADCs)
c-Kit
Apoptosis
Microtubule/Tubulin
ERK
Akt
Caspase
|
Cancer
|
|
NN3201 is a c-Kit-targeting antibody-drug conjugate (ADC) with high affinity (KD = 0.19 pM). NN3201 is composed of 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE (HY-178219) and an anti-c-Kit human monoclonal antibody NN2101 (HY-P991293). NN3201 rapidly internalizes and inhibits stem cell factor (SCF)-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits no Fc-mediated effector functions antibody-dependent cell-mediated cytotoxicity (ADCC)/complement-dependent cytotoxicity (CDC) due to reduced FcγR binding. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models. NN3201 can be used in small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST) and acute myeloid leukemia (AML) research [1][2].
|
-
- HY-162275
-
|
|
Histone Demethylase
Histone Methyltransferase
STAT
|
Cancer
|
|
JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC50 = 0.59 μM, Kd = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells .
|
-
- HY-137055
-
|
|
Others
|
Others
|
|
PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
|
-
- HY-NP008
-
|
|
Lipocalin Family
|
Inflammation/Immunology
|
|
β-Lactoglobulin, a major whey protein, is a small globular protein from the lipocalin family. β-Lactoglobulin is an important source of the essential and branched-chain amino acids (leucine, isoleucine, and valine). β-Lactoglobulin shows antioxidant properties, because it contains two disulfide bonds and one free thiol group. β-Lactoglobulin is a ligand transport agent. β-Lactoglobulin is one of the major allergens in milk and can be utilized in the research for developing safe hypoallergenic dairy products .
|
-
-
-
HY-L0115V
-
|
|
10,091 compounds
|
|
ASINEX has elaborated a library of diverse macrocycles using an effective tool box of synthetic methods. The resulting scaffolds are novel, tremendously diverse, medchem-relevant, macrocyclic frameworks.
Macrocyles tend to be larger than traditional screening molecules which make them perfect discovery tools for targets with shallow or extended binding sites. At the same time, their unique character based on restricted flexibility and ability to form intra-molecular hydrogen bonds allows for design approaches effectively optimizing properties such asaqueous solubility and membrane permeability. Many of these macrocycles have been tested for aqueous and DMSO solubility with cut-offs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4) followed by PAMPA permeability assay.
|
| Cat. No. |
Product Name |
Type |
-
- HY-NP009
-
|
|
Native Proteins
|
|
α-Lactalbumin is a Ca 2+-binding protein. α-Lactalbumin has a single strong Ca 2+-binding site and for this reason it frequently serves as a simple model Ca 2+-binding protein. α-Lactalbumin is a component of lactose synthase, an enzyme system, which consists of galactosyltransferase (GT) and α-Lactalbumin .
|
-
- HY-N0830B
-
|
|
Cell Assay Reagents
|
|
Palmitic acid sodium is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid sodium can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells. Palmitic acid sodium is used to establish a cell steatosis model .
|
-
- HY-D0846
-
|
|
Biochemical Assay Reagents
|
|
Diethyl pyrocarbonate is a potent, orally active, non-specific chemical inhibitor of RNase. Diethyl pyrocarbonate has been useful in vitro as an agent relatively specific for binding to imidazole of histidine. Diethyl pyrocarbonate inhibits central chemosensitivity in rabbits. Diethyl pyrocarbonate can modify Ser, Thr, His and Tyr residues. Diethyl pyrocarbonate can be used for modeling .
|
-
- HY-NP008
-
|
|
Native Proteins
|
|
β-Lactoglobulin, a major whey protein, is a small globular protein from the lipocalin family. β-Lactoglobulin is an important source of the essential and branched-chain amino acids (leucine, isoleucine, and valine). β-Lactoglobulin shows antioxidant properties, because it contains two disulfide bonds and one free thiol group. β-Lactoglobulin is a ligand transport agent. β-Lactoglobulin is one of the major allergens in milk and can be utilized in the research for developing safe hypoallergenic dairy products .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3732
-
|
|
Integrin
|
Cancer
|
|
RGD-4C is a arginine-glycine-aspartic acid peptide (ACDCRGDCFC) with integrin binding activity. The Arg-Gly-Asp (RGD) sequence serves as the primary integrin recognition site in extracellular matrix proteins, and peptides containing this sequence can mimic the recognition specificity of the matrix proteins. RGD-4C is a αv-integrin ligand, can conjugate with bioactive molecule to exert antitumor effects in animal models .
|
-
- HY-P1220A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain .
|
-
- HY-P10010
-
|
|
Galectin
|
Cancer
|
|
DB21, Galectin-1 Antagonist is a dibenzofuran conjugated peptidomimetic that acts as an allosteric inhibitor of galectin-1 (GAL1)binding to cell surface glycans. DB21, Galectin-1 Antagonis increases inhibition of angiogenesis and tumour growth in melanoma, lung adenocarcinoma and ovarian cancer models .
|
-
- HY-P2138
-
|
|
HIV Protease
|
Others
|
|
U-85548E is an HIV protease inhibitor with nanomolar affinity for HIV-1 aspartic protease. By studying its structure-activity relationship, a potent nanomolar inhibitor with inhibitory effects on both HIV-1 and HIV-2 proteases was designed, and its binding mode was studied by X-ray crystallography and molecular modeling.
|
-
- HY-P11354
-
|
|
TGF-β Receptor
Apoptosis
Interleukin Related
Integrin
Cadherin
|
Inflammation/Immunology
|
|
THR-123 is an orally active ALK3 peptide agonist. THR-123 has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 suppresses inflammation, apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 can be used for the study of kidney fibrosis .
|
-
- HY-P10793
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model .
|
-
- HY-P1220
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain .
|
-
- HY-P10870
-
|
|
Peptide-Drug Conjugates (PDCs)
FGFR
Apoptosis
|
Cancer
|
|
Pep1-DNP conjugate 9 is a functionalized peptide which is composed of the DNP-Hapten and the FGFR1 binding peptide. Pep1-DNP conjugate 9 exhibits good affinity to FGFR1 with KD of 5.01 μM. Pep1-DNP conjugate 9 recruits anti-DNP antibodies to the surface of FGFR1-positive cells, inhibits the FGF2-induced proliferation in rat skeletal myoblast cells, and induces apoptosis. Pep1-DNP conjugate 9 exhibits antitumor efficacy in mouse models .
|
-
- HY-P10786
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
LinTT1 peptide is a tumor-penetrating peptide with the amino acid sequence AKRGARST. LinTT1 peptide targets peritoneal carcinoma (PC) by binding to the p32 (gC1qR) receptor. It can conjugate with iron oxide nanoworms (NWs) to form a nanocarrier. This nanocarrier is taken up by peritoneal carcinoma cells in vitro and enters the mitochondria; it also exhibits significant tumor targeting and penetration effects in mice. Moreover, LinTT1-functionalized nanocarriers, combined with the pro-apoptotic peptide [D(KLAKLAK)2], show significant tumor suppression in a mouse peritoneal tumor model. LinTT1 peptide holds promise as a delivery carrier for peritoneal cancer research .
|
-
- HY-P10393
-
|
ERα (295-311)
|
Apoptosis
|
Cancer
|
|
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99249
-
|
Pogalizumab; MOXR 0916
|
Orexin Receptor (OX Receptor)
|
Cancer
|
|
Vonlerolizumab (Pogalizumab; MOXR 0916) is a humanized IgG1 monoclonal antibody targeting OX40 (CD134). Pogalizumab partially blocks the interaction between OX40 and its natural ligand OX40L upon binding, thereby activating the NF-κB signaling pathway. Pogalizumab enhances T cell activation and proliferation and has shown antitumor activity in mouse models .
|
-
- HY-P990033
-
|
CC-95251; BMS-986351
|
CD47
|
Cancer
|
|
Anzurstobart (CC-95251; BMS-986351) is a high-affinity, fully human monoclonal anti-SIRPα antibody that blocks the binding of CD47 to SIRPα. Anzurstobart enhances macrophage phagocytic activity against DLBCL cell lines in co-culture models when combined with the antibody Rituximab (HY-P9913). Anzurstobart has the potential for solid and hematologic malignancies research .
|
-
- HY-P99623
-
|
MGD006; S80880
|
CD3
|
Cancer
|
|
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
|
-
- HY-P99171
-
|
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .
|
-
- HY-P990004
-
|
|
Tim3
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse TIM-3 Antibody (B8.2C12) is an anti-mouse TIM-3 IgG1 monoclonal antibody. Anti-Mouse TIM-3 Antibody (B8.2C12) can block the binding of Tim-3 with Phosphatidylserine (PtdSer) and CEACAM1 without interfering with the binding to Galectin-9. Anti-Mouse TIM-3 Antibody (B8.2C12) can inhibit tumor growth and activate tumor infiltrating CD8 + T cells. Anti-Mouse TIM-3 Antibody (B8.2C12) can be used for studying cancer such as breast cancer and colon cancer and constructing experimental autoimmune encephalomyelitis (EAE) models .
|
-
- HY-P991618
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
ST2485 is a monoclonal antitenascin antibody. ST2485 shows additivity in tenascin C binding in vitro as well as in a xenograft model. ST2485 binds human tenascin at an epitope partially shared with BC2. ST2485 cross-reacts with murine tenascin. ST2485 can be studied in antitumor research .
|
-
- HY-145644
-
|
C-135-LS; BMS-986414
|
SARS-CoV
|
Infection
Cancer
|
|
Ogalvibart (C-135-LS) is a human anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Ogalvibart binds to the spike (S) glycoprotein receptor-binding domain (RBD) of SARS-CoV-2. Ogalvibart in combination with C144LS (1:1 ratio) shows good preventive activity and can effectively block the development of COVID19 in a rhesus monkey disease model .
|
-
- HY-P991353
-
|
|
PD-1/PD-L1
|
Cancer
|
|
Sym-021 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. Sym-021 blocks the binding of PD-L1 and PD-L2 ligands, inducing the secretion of interferon IFN-γ and IL-2 and the proliferation of T cells. Sym-021 has anti-tumor activity in PDX mouse models .
|
-
- HY-P991447
-
|
|
VISTA
|
Cancer
|
|
Anti-VSIR/VISTA Antibody (SG7) is a human monoclonal antibody (mAb) targeting VISTA/B7-H5. Anti-VSIR/VISTA Antibody (SG7) inhibits VISTA function and prevents PSGL-1 and VSIG3 from binding to VISTA. Anti-VSIR/VISTA Antibody (SG7) has anti-tumor activity in the mouse B16F10 melanoma model. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-P991598
-
|
MOR12743; MOR03207
|
Interleukin Related
NF-κB
|
Inflammation/Immunology
|
|
MOR-106 (MOR12743) is a humanized anti-IL-17C IgG1 monoclonal antibody. MOR-106 inhibits the NF-κB signaling pathway by specifically binding to IL-17C (IC50 = 59 pM for human IL-17C, IC50 = 55 pM for mouse IL-17C). MOR-106 can effectively inhibit skin inflammation and reduce related inflammatory factors in animal models of psoriasis and atopic dermatitis .
|
-
- HY-P991270
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
MT204 is a humanized IgG1 antibody inhibitor targeting IL-2 of human and rhesus monkey origin. MT204 prevents soluble IL-2 from binding to intermediate-affinity IL-2 receptors and blocks CD25-bound IL-2 on high-affinity IL-2 receptors. MT204 has potently anti-proliferative activity with NKL cells and primary NK cells. MT204 has good tolerability and potent immunosuppressive activity in allogeneic skin graft model of rhesus monkey, promising for immunosuppressive and anti-proliferative therapy .
|
-
- HY-P991571
-
|
GC-1118A
|
EGFR
PERK
Akt
|
Cancer
|
|
GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .
|
-
- HY-P991584
-
|
|
FGFR
|
Cancer
|
|
HuGAL-FR21 is a humanized antiFGFR2IIIb IgG1 monoclonal antibody. HuGAL-FR21 can block the binding of FGF2, FGF7, and FGF10 to FGFR2IIIb and inhibit FGF-induced phosphorylation of FGFR2IIIb. HuGAL-FR21 can downregulate the expression of FGFR2 in SNU-16 cells. HuGAL-FR21 shows the significant anti-tumor activity in athymic nude mice bearing gastric cancer xenograft models. HuGAL-FR21 can be used for research on cancer such as gastric cancer .
|
-
- HY-P990259
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse CD96 Antibody (3.3) is a rat-derived anti-mouse CD96 IgG1 λ type antibody inhibitor. Anti-Mouse CD96 Antibody (3.3) blocks binding of CD155 to CD96. Anti-Mouse CD96 Antibody (3.3) can enhance the antitumor efficacy of multiple immune-checkpoint inhibitors. Anti-Mouse CD96 Antibody (3.3) shows potent anti-tumor and anti-metastatic activity in various tumor models. Anti-Mouse CD96 Antibody (3.3) can be used for the researches of cancer and inflammation, such as mammary carcinoma .
|
-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Interleukin Related
|
Cancer
|
|
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0830
-
-
-
- HY-B1864A
-
-
-
- HY-N11768
-
-
-
- HY-N0837
-
|
NSC17821; NSC23880
|
Alkaloids
Piperidine Alkaloids
other families
Classification of Application Fields
Source classification
Plants
Disease Research Fields
Cancer
|
PI3K
Akt
mTOR
Autophagy
Apoptosis
|
|
Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
|
-
-
- HY-N7368
-
|
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Flavonols
Flavonoids
other families
Neurological Disease
Classification of Application Fields
Source classification
Phenols
Polyphenols
Plants
Inflammation/Immunology
Disease Research Fields
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Adenosine Deaminase
Bacterial
Caspase
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Hibifolin is a flavonol glycoside that can be isolated from Helicteres isora. Hibifolin is an inhibitor of adenosine deaminase (ADA) (Ki = 49.92 μM). Hibifolin protects neurons against β-amyloid-induced neurotoxicity. Hibifolin possesses a potent protective activity against cell death induced by aggregated Aβ. Hibifolin can abolish Aβ-induced caspase-3 and caspase-7 activation. Hibifolin induces Akt phosphorylation in cortical neurons. Hibifolin is also a natural sortase A (SrtA) inhibitor (IC50 = 31.2 μM) through direct binding to SrtA protein. Hibifolin attenuates the pathogenic behavior of Staphylococcus aureus including adhesion, invasion, and biofilm formation. Hibifolin improves the survival of pneumonia induced by Staphylococcus aureus in mouse model and alleviates pathological damage. Hibifolin shows a synergistic antibacterial effect with Cefotaxime (HY-A0088A) .
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- HY-125938
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Cycloartenol ferulate; Cycloartenol ferulic acid ester
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Triterpenes
Monophenols
other families
Classification of Application Fields
Terpenoids
Source classification
Phenols
Plants
Inflammation/Immunology
Disease Research Fields
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Drug Derivative
Apoptosis
Reactive Oxygen Species (ROS)
JAK
STAT
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Cycloartenyl ferulate (Cycloartenol ferulate; Cycloartenol ferulic acid ester) is a derivative of γ-oryzanol (HY-B2194) with multiple biological activities including antioxidant, anti-inflammatory, and anti-tumor properties. Cycloartenyl ferulate selectively binds to IFNγR1 (binding affinity Kd = 0.5 μM) to activate the canonical JAK1/2-STAT1 signaling pathway. Cycloartenyl ferulate inhibits paraquat (PQ)-triggered apoptosis and ROS in HK2 cells. Cycloartenyl ferulate enhances the activation and cytolytic activity of natural killer (NK) cells by upregulating the expression of NK cell activation receptors (NKG2D, NKp30, NKp44) and the release of cytotoxic molecules and cytokine IFNγ. Cycloartenyl ferulate exerts anti-cancer effects in tumor mice models. Cycloartenyl ferulate can be used for the study of cancer and allergic inflammation intervention .
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- HY-N8146
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- HY-N0830A
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- HY-B1864AR
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- HY-N1486R
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- HY-N7368R
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Flavonols
Flavonoids
other families
Source classification
Phenols
Polyphenols
Plants
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Reference Standards
Adenosine Deaminase
Bacterial
Caspase
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Hibifolin (Standard) is the analytical standard of Hibifolin. This product is intended for research and analytical applications. Hibifolin is a flavonol glycoside that can be isolated from Helicteres isora. Hibifolin is an inhibitor of adenosine deaminase (ADA) (Ki = 49.92 μM). Hibifolin protects neurons against β-amyloid-induced neurotoxicity. Hibifolin possesses a potent protective activity against cell death induced by aggregated Aβ. Hibifolin can abolish Aβ-induced caspase-3 and caspase-7 activation. Hibifolin induces Akt phosphorylation in cortical neurons. Hibifolin is also a natural sortase A (SrtA) inhibitor (IC50 = 31.2 μM) through direct binding to SrtA protein. Hibifolin attenuates the pathogenic behavior of Staphylococcus aureus including adhesion, invasion, and biofilm formation. Hibifolin improves the survival of pneumonia induced by Staphylococcus aureus in mouse model and alleviates pathological damage. Hibifolin shows a synergistic antibacterial effect with Cefotaxime (HY-A0088A) .
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- HY-N0837R
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NSC17821 (Standard); NSC23880 (Standard)
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Alkaloids
Piperidine Alkaloids
other families
Source classification
Plants
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Reference Standards
PI3K
Akt
mTOR
Autophagy
Apoptosis
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Veratramine (NSC17821; NSC23880) (Standard) is the analytical standard of Veratramine (HY-N0837). This product is intended for research and analytical applications. Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-W757743
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Acalabrutinib-d3 (ACP-196-d3) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
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- HY-175318S
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p53 Activator 15 is an orally active p53 Y220C activator. p53 Activator 15 enhances the DNA binding of p53 Y220C (SC50 = 0.58 nM) and significantly inhibits NUGC-3 cell proliferation. p53 Activator 15 effectively inhibits tumor growth in NUGC-3 xenograft mouse and rat models. p53 Activator 15 can be used to study gastric cancer .
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- HY-W013403S
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2'-Deoxy-2'-fluorouridine-d2 is the deuterium labeled 2'-Deoxy-2'-fluorouridine . 2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
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| Cat. No. |
Product Name |
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Classification |
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- HY-175421
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Alkynes
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ArMan is an aryl mannoside ligand that can be chemically functionalized onto the surface of virus-like particles (VLPs) through click chemistry. VLPs can be used to target DC-SIGN dendritic cells, promote the selective co-binding of DC-SIGN and TLR7, and lead to a Th1-type immune response. VLP-ArMan-OvaI/II can significantly inhibit tumor growth in the mouse melanoma model .
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| Cat. No. |
Product Name |
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Classification |
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- HY-43058
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5'-O-DMT-N2-isobutyrylguanosine
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Nucleoside Phosphoramidites
Guanine
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5'-O-DMT-ibu-rG is a useful model for a new class of DNA binding molecules for the development of potent and selective anti-cancer agents .
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- HY-147081
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AS 1411
2 Publications Verification
AGRO-100
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Aptamers
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AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
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