Search Result
Results for "
ligand-binding
" in MedChemExpress (MCE) Product Catalog:
7
Biochemical Assay Reagents
5
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-13956
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Pioglitazone
Maximum Cited Publications
47 Publications Verification
U 72107
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PPAR
Ferroptosis
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Metabolic Disease
Cancer
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Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .
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- HY-P9977
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JNJ-61186372
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EGFR
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Inflammation/Immunology
Cancer
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Amivantamab (JNJ-61186372) is a human EGFR-MET bispecific antibody with immune anticancer activity. Amivantamab inhibits ligand binding, promotes endocytosis and degradation of receptor-antibody complexes, and induces Fc-dependent cytokinesis in macrophages and antibody-dependent cytotoxicity in natural killer cells .
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- HY-109176
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GDC-9545; RG6171
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Estrogen Receptor/ERR
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Cancer
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Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity .
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- HY-P99055
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TNF Receptor
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Inflammation/Immunology
Cancer
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Urelumab, a fully human, non-ligand binding, CD137 agonist IgG4 monoclonal antibody, enhances T-cell and natural killer-cell antitumor activity, and may enhance cytotoxic activity of Rituximab (HY-P9913). Urelumab can be used for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and other types of non-Hodgkin lymphoma (NHL) .
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- HY-14422
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ROR
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Cancer
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SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription .
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- HY-B1322
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- HY-B1322A
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- HY-N0010
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FXR
Sirtuin
TNF Receptor
Interleukin Related
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Metabolic Disease
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Geniposidic acid is an orally active FXR modulator and SIRT6 activator. Geniposidic acid binds to the Ser332 and His447 sites on the FXR ligand-binding domain, thereby driving nuclear translocation, coactivator recruitment, and transcription of downstream bile acid and cholesterol metabolism-related genes. Geniposidic acid improves metabolic dysfunction-related fatty liver disease by activating the SIRT6 signaling pathway. Geniposidic acid inhibits inflammation and modulates gut microbiota to alleviate colitis. Geniposidic acid can be used in research on drug-induced liver injury, inflammatory bowel disease, metabolic dysfunction-related fatty liver disease, and metabolic dysfunction-related steatohepatitis .
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- HY-23999
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BI-0115
2 Publications Verification
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LOX-1
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Cardiovascular Disease
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BI-0115 is a selective inhibitor of LOX-1 (IC50=5.4 μM) that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain .
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- HY-B1322B
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- HY-108822
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Arcalyst; IL 1 Trap; Interleukin 1 Trap
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Interleukin Related
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Inflammation/Immunology
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Rilonacept (Arcalyst), a dimeric fusion protein, is a interleukin 1 inhibitor. Rilonacept consists of the ligand-binding domains of the extracellular portions of the IL-1R components linked to the Fc portion of human IgG1. Rilonacept can be used for the research of cryopyrin-associated periodic syndromes .
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- HY-P99446
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TACI-Ig; TACI-Fc 5
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TNF Receptor
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Inflammation/Immunology
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Atacicept (TACI-Ig) is a is a recombinant fusion protein containing the extracellular, ligand-binding portion of the TACI receptor and the Fc portion of human IgG. Atacicept inhibits B cell stimulation by binding to B lymphocyte stimulator and a proliferation-inducing ligand. Atacicept can be used in research of B-cell autoimmune disease .
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- HY-NP002L
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Biochemical Assay Reagents
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Others
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Canine Serum Albumin is a plasma protein derived from dogs. Canine Serum Albumin exhibits greater flexibility than human serum albumin and bovine serum albumin. Serum albumin is a multifunctional protein with exceptional ligand-binding capacity, which enables it to act as a transport molecule for various metabolites, drugs, nutrients, metals and other molecules .
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- HY-N2025
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PPAR
Glycosidase
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Metabolic Disease
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Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
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- HY-130714
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TD-165
1 Publications Verification
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PROTACs
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Cancer
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TD-165 is a PROTAC-based cereblon (CRBN) degrader. TD-165 comprises a?cereblon (CRBN)?ligand binding group, a linker and an?von Hippel-Landau (VHL)?binding group .
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- HY-136242
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Estrogen Receptor/ERR
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Endocrinology
Cancer
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UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.
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- HY-132205
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Estrogen Receptor/ERR
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Metabolic Disease
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DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
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- HY-P991224
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CCR
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Inflammation/Immunology
Cancer
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CAP-100 is a monoclonal antibody that targets CCR7. CAP-100 neutralizes the ligand-binding site and signaling of CCR7. CAP-100 strongly inhibits CCR7-induced migration, extravasation, homing, and survival in chronic lymphocytic leukemia (CLL) samples. CAP-100 triggers potent tumor cell killing, mediated by host immune mechanism. CAP-100 shows a favorable toxicity profile on relevant hematopoietic subsets. CAP-100 is involved in research on anti-tumor and disease such as CLL .
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- HY-W073128
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PFTeDA
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PPAR
Apoptosis
PGC-1α
AMPK
Akt
mTOR
Reactive Oxygen Species (ROS)
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Endocrinology
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Perfluorotetradecanoic acid (PFTeDA) is an orally active perfluoroalkyl substance. Perfluorotetradecanoic acid directly binds to the ligand-binding domain of purified hPPARγ, with a Kd value of 157.8 μM. Perfluorotetradecanoic acid significantly reduces the activity of the SIRT1/PGC1α and AMPK signaling pathways while stimulating the activity of the AKT1/mTOR signaling pathway. Perfluorotetradecanoic acid significantly upregulates the expression of corticosterone biosynthesis genes. Perfluorotetradecanoic acid increases ROS levels and promotes Apoptosis. Perfluorotetradecanoic acid impairs Leydig cell function and male reproductive endocrine function in adult male rats .
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- HY-156190A
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Orphan Nuclear Receptor
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Cancer
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NR2F2-IN-1 (free base) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F2-IN-1 (free base) substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F2-IN-1 (free base) directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .
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- HY-18102
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Androgen Receptor
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Neurological Disease
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GLPG0492 is an orally active, non-steroidal selective androgen receptor modulator. GLPG0492 exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy .
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- HY-W587839
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Pregnane X Receptor (PXR)
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Endocrinology
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4,8-Dioxa-3H-perfluorononanoic acid is an ether-substituted polyfluoroalkyl compound and also a ligand of human pregnane X receptor (hPXR), which binds to the ligand-binding domain of hPXR. 4,8-Dioxa-3H-perfluorononanoic acid targets Arg-410, Lys-210, Lys-226, Met-323 and His-327 residues. Its binding process relies on long-range electrostatic interactions, and no significant hydrogen bonds form with hPXR residues. 4,8-Dioxa-3H-perfluorononanoic acid is used as a substitute for PFOA in Germany. 4,8-Dioxa-3H-perfluorononanoic acid is detectable in environmental matrices such as river water near fluoride production plants, accumulates in organisms including grass, deer liver and locusts, and is present in plasma samples of populations in southern Germany .
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- HY-171978
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Adrenergic Receptor
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Cardiovascular Disease
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LM-189 is a β2-adrenergic receptor (β2AR) ligand and G protein-biased modulator with a human β2AR Ki of 0.063 nM.LM-189 promotes β2AR coupling to Gαs and Gαi heterotrimers, stabilizes distinct β2AR conformations including a TM6 outward state, and increases β2AR ICL2 dynamics.LM-189 restricts β2AR ligand-binding pocket conformational heterogeneity, stabilizes polar ligand-receptor interaction networks, and exhibits bias toward Gαi signaling over Gαs signaling.LM-189 enabled cryo-EM structural characterization of the β2AR-Gi complex.LM-189 can be used for the research of congestive heart failure .
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- HY-P991222
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Phosphatase
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Cardiovascular Disease
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AMG-529 is a humanized monoclonal antibody against ASGR1 that binds to ASGR1, blocks ligand binding, and causes a dose-dependent increase in ALP (a biomarker of ASGR1 inhibition). AMG-529 can be used for the research of cardiovascular diseases .
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- HY-P990073
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REGN-5093
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c-Met/HGFR
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Cancer
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Davutamig (REGN-5093) is a human IgG4-kappa, anti-MET bispecific antibody. Davutamig binds 2 distinct epitopes of MET, blocking ligand binding and inducing MET internalization and degradation. Davutamig is applicable to the research of advanced non-small cell lung cancer with MET gene abnormalities .
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- HY-N4194
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PPAR
Influenza Virus
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Infection
Metabolic Disease
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Glabrone is an isoflavone found in Glycyrrhiza glabra roots. Glabrone exhibits significant PPAR-γ ligand binding activity. Glabrone is a specific UGT1A9 probe substrate, and its metabolites can block influenza virus release by inhibiting neuraminidase (NA). Glabrone can be used to screen for herb-drug interactions and for anti-influenza virus activity .
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- HY-P10579
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123B9
1 Publications Verification
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Ephrin Receptor
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Cancer
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123B9, a tumor-homing agent, is a potent and selective EphA2 agonist with a Kd value of 4.0 μM. 123B9 selectively targets the EphA2 tyrosine kinase receptor ligand-binding domain. 123B9 does not appreciably inhibit the ligand binding domains of the most closely related EphA3 and EphA4 receptors .
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- HY-P2264
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Ephrin Receptor
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Inflammation/Immunology
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KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC50:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses .
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- HY-143201
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Estrogen Receptor/ERR
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Metabolic Disease
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DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
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- HY-122742
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iGluR
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Neurological Disease
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HBT1 is an effective AMPA receptor AMPA-R potentiator. HBT1 specifically binds to the ligand-binding domain (LBD) of AMPAR and enhances receptor activity only when AMPA is present., HBT1 has almost no agonistic effect (i.e., reaching the optimal concentration, and then the efficacy decreases as the concentration continues to increase) compared with traditional AMPA-R potentiator, avoiding the bell-shaped reaction of brain-derived neurotrophic factor (BDNF) production in primary neurons. HBT1 can be applicable to a wider range of neurological and psychiatric diseases (such as depression, Alzheimer's disease, etc.) .
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- HY-135345
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PROTACs
FKBP
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Cancer
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PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader .
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- HY-120210
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ROR
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Inflammation/Immunology
Cancer
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XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD) .
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- HY-127024A
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Thyroid Hormone Receptor
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Metabolic Disease
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TR antagonist 2 (Compound 10a) is a competitive thyroid hormone receptors (TRα/β) antagonist (IC50=47 nM). TR antagonist 2 competes with triiodothyronine (T3) for binding to the ligand-binding domain of TR to block receptor-coactivator complex formation and inhibit target gene transcription, reducing thyroid hormone-mediated hypermetabolic effects. TR antagonist 2 is promising for research of hyperthyroidism (e.g., Graves' disease) and thyrotoxicosis .
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- HY-P5407
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SARS-CoV
Angiotensin-converting Enzyme (ACE)
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Infection
Cancer
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HD5 is an innate immune effector peptide and SARS-CoV Inhibitor. HD5 binds to the ligand-binding domain of angiotensin-converting enzyme-2 (ACE2) via multiple hydrogen bonds to competitively block the receptor, shielding it from viral recognition. HD5 can be used for the research of COVID-19, HPV16 infection, epithelial ovarian cancer, small-cell lung cancer, and colon cancer .
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- HY-164552
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Apoptosis
Androgen Receptor
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Cancer
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ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro .
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- HY-NP002K
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Biochemical Assay Reagents
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Others
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Rat Serum Albumin is a plasma protein derived from rat. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
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- HY-NP002O
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Biochemical Assay Reagents
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Others
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Cynomolgus Monkey serum albumin is a plasma protein derived from cynomolgus monkey. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules.
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- HY-164373
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Androgen Receptor
Apoptosis
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Cancer
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SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1 .
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- HY-156906
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MDM-2/p53
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Cancer
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UNC3474 is a small molecule ligand, binding with 53BP1. UNC3474 binds the aromatic methyl-lysine binding cage of 53BP1 TT, with a dissociation constant (Kd) of 1.0 ± 0.3 μM. UNC3474 inhibits the recruitment of 53BP1 to DSBs by stabilizing a pre-existing autoinhibited state of 53BP1 in cells .
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- HY-13956S1
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Isotope-Labeled Compounds
PPAR
Ferroptosis
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Metabolic Disease
Cancer
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Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively .
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- HY-156190
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Orphan Nuclear Receptor
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Cancer
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NR2F2-IN-1 (CIA1) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F2-IN-1 substantially inhibits COUP-TFII-driven NGFIA reporter expression. NR2F2-IN-1 directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .
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- HY-33821
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LXR
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Others
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LXRβ ligand 1 is a LXR β ligand-binding domain agonist, with an EC50 of 57 μM and a Ki of 28 μM against human LXR β. LXRβ ligand 1 forms hydrogen bonds with His435, stabilizes the His-Trp activation switch, and locks the ligand-binding domain in an agonist conformation; its tert-butyl moiety occupies a hydrophobic subpocket, while its phenyl moiety forms a π-π stacking interaction with Phe329. LXRβ ligand 1 serves as a structural unit for the development of LXRβ modulators .
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- HY-NP002C
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Biochemical Assay Reagents
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Others
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Rabbit Serum Albumin (globulin free) is a plasma protein derived from rabbits. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
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- HY-128838
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PROTACs
Estrogen Receptor/ERR
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Cancer
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PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader .
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- HY-111848A
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SNIPERs
PROTACs
Androgen Receptor
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Cancer
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PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs) .
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- HY-111848
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SNIPERs
PROTACs
Androgen Receptor
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Cancer
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PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs) .
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- HY-131188
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PROTACs
Bcl-2 Family
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Cancer
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PROTAC Bcl-xL degrader-1 is a PROTAC that comprises a Bcl-xL (Bcl-2 family member) ligand binding group, a linker and an IAP E3 ligases binding group. PROTAC Bcl-xL degrader-1 is a potent Bcl-xL degrader, and shows toxicity for human platelets and MyLa 1929 cells with IC50 values of 62 nM and 8.5 μM, respectively .
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- HY-13956B
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U 72107 potassium
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PPAR
Ferroptosis
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Metabolic Disease
Cancer
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Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research .
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- HY-13956R
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U 72107 (Standard)
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Reference Standards
PPAR
Ferroptosis
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Metabolic Disease
Cancer
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Pioglitazone (Standard) is the analytical standard of Pioglitazone. This product is intended for research and analytical applications. Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .
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- HY-120188
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PPAR
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Others
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CC618 is a selective PPARβ/δ antagonist. CC618 covalently modifies conserved Cys249 in the PPARβ/δ ligand-binding pocket via nucleophilic aromatic substitution, converting its thiol moiety to a 5-trifluoromethyl-2-pyridylthioether .
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- HY-P10430
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Transmembrane Glycoprotein
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Neurological Disease
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Stalk peptide is a GPR110 activator. Stalk peptide is released from GPCR Autoproteolysis INducing domain by autocatalytic process and then Stalk peptide is inserted into the ligand-binding pocket of the receptor to activate the receptor. Stalk peptide can promote nerve growth and synaptic formation. Stalk peptide can be used to study neurodevelopmental and neurodegenerative diseases .
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- HY-P4863
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CGRP Receptor
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Neurological Disease
Metabolic Disease
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Biotinyl-Amylin (human) is a biotin-labeled derivative of Amylin, amide, human (HY-P1070). Biotinyl-Amylin (human) acts as a competitive agonist for the Calcitonin Receptor (CTR) and for the Amylin receptors (AMY1, AMY2, and AMY3) formed by the association of CTR with RAMP1/2/3. By mimicking endogenous human amylin, Biotinyl-Amylin (human) binds to and activates CTR and AMY receptors, thereby initiating downstream signaling pathways involving cAMP, CREB, and ERK1/2, while retaining high-affinity receptor binding and activation capabilities. Biotinyl-Amylin (human) is primarily utilized in studies investigating the metabolic regulatory mechanisms underlying obesity and diabetes; it is also applicable to pharmacological research, receptor localization studies, and ligand-binding assays related to Amylin receptors in the context of Alzheimer's disease .
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- HY-178938
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Molecular Glues
Androgen Receptor
Caspase
Apoptosis
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Endocrinology
Cancer
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AR Degrader-3 is an orally active molecular glue that targets AR/ARV7 and induces the degradation of AR and ARV7 through the ubiquitin-proteasome pathway (UPP). AR Degrader-3 directly interacts with the ligand-binding domain (LBD) and the N-terminal domain (NTD) of AR. AR Degrader-3 effectively suppresses the transcriptional activity of wild-type AR (AR-WT), AR mutants, and ARV7. AR Degrader-3 downregulates the mRNA and protein levels of downstream AR target genes, thereby overcoming antiandrogen resistance mediated by ARV7 and AR point mutations. AR Degrader-3 induces apoptosis in Enzalutamide (HY-70002) (ENZa)-resistant cells and increases cleaved caspase-3 protein levels. AR Degrader-3 can be used for the study of castration-resistant prostate cancer (CRPC) .
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- HY-128839
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PROTACs
Estrogen Receptor/ERR
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Cancer
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PROTAC ERRα Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader .
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- HY-110392
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Estrogen Receptor/ERR
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Cancer
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CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively .
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- HY-135903
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GDC-9545 tartrate; RG6171 tartrate
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Estrogen Receptor/ERR
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Cancer
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Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity .
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- HY-113646
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FKBP
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Others
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Shield-2 is an efficient stabilizing ligand binding to the FKBP (F36V) protein with a dissociation constant of 29 nM. Shield-2 binds tightly to the FKBP mutants destabilizing domains and prevents degradation, thus providing small molecule regulation over intracellular protein levels .
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- HY-B1322AS
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Parasite
Histone Methyltransferase
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Infection
Neurological Disease
Inflammation/Immunology
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Amodiaquine-d10 is the deuterium labeled Amodiaquine. Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect .
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- HY-W128798
-
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5-HT Receptor
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Neurological Disease
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Sulfabenz (Compound 9) is an amine-substituted N1-phenylsulfonyl indole derivative. Sulfabenz has binding activity to human 5-HT6 serotonin receptor (Ki: 200 nM). Sulfabenz can be used to study the ligand binding mechanism of 5-HT6 receptor and 5-HT6 receptor-related neurological diseases .
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- HY-B1322AR
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-
- HY-13956S
-
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U 72107-d4
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PPAR
Ferroptosis
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Metabolic Disease
Cancer
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Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively .
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-
- HY-13956C
-
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(R)-U 72107
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PPAR
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Neurological Disease
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(R)-Pioglitazone ((+)-pioglitazone) is the R enantiomer of Pioglitazone (HY-13956). (R)-Pioglitazone is an orally active and selective peroxisome proliferator-activated receptor (PPARγ) agonist with high affinity binding to the PPARγ ligand-binding domain. (R)-Pioglitazone can be used for the research of Alzheimer's disease .
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-
- HY-116205
-
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iGluR
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Others
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|
UBP684 is a novel positive allosteric modulator of NMDA receptors (NMDARs) that enhances receptor function by stabilizing the ligand-binding domains in a closed conformation, resulting in potentiated whole-cell currents and increased mean open time.
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-
- HY-170874
-
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PPAR
|
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-121372
-
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Estrogen Receptor/ERR
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Cancer
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Lactandrate is a D-high nitrogen steroid alkylating agent. It can interact with the ligand-binding domain (LBD) of estrogen receptor-alpha (ERα). Lactandrate has a growth inhibitory effect on breast cancer cells, with a GI50 value ranging from 5 to 65 μM. It shows anti-tumor activity in mouse breast tumors (MXT and CD8F1) as well as in human xenograft MX-1 .
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-
- HY-117182
-
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Apoptosis
VD/VDR
RAR/RXR
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Metabolic Disease
Inflammation/Immunology
Cancer
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LG190178 is a non-steroidal vitamin D receptor (VDR) ligand that can induce the formation of heterodimer complexes between VDR and retinoid X receptor (RXR), stabilizing the agonistic conformation of the VDR ligand-binding domain and promoting its interaction with co-activators. LG190178 has functions in regulating calcium homeostasis, bone mineralization, as well as cell proliferation, differentiation, and apoptosis, making it useful for research in psoriasis, osteoporosis, and cancer .
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- HY-P991553
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TNF Receptor
Apoptosis
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Inflammation/Immunology
Cancer
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HeFi-1 is a mouse anti-CD30 IgG1 monoclonal antibody. HeFi-1 recognizes the ligand-binding site on CD30. HeFi-1 can inhibit the growth of tumor cells with high expression of CD30. HeFi-1 can induce eosinophil apoptosis. HeFi-1 can be used for researches on cancer or inflammation conditions such as anaplastic large-cell lymphoma (ALCL) and asthma .
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- HY-N2025R
-
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Reference Standards
PPAR
Glycosidase
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Metabolic Disease
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Oroxin A (Standard) is the analytical standard of Oroxin A. This product is intended for research and analytical applications. Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
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-
- HY-18102BS
-
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Isotope-Labeled Compounds
Adrenergic Receptor
|
Neurological Disease
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GLPG0492- 13C,d3 racemate is 13C-labeled GLPG0492 (racemate) (HY-18102B). GLPG0492 racemate is an orally active, non-steroidal selective androgen receptor modulator. GLPG0492 racemate exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 racemate effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 racemate prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy .
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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-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-101601
-
-
- HY-119782
-
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Fluorescent Dye
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Others
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|
L-Argininamide is a hydrophilic amino acid derivative and can be used as a compound for ligand binding DNA aptamers. L-Argininamide has the potential for fluorescent aptasensors development .
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-
- HY-D2857
-
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Fluorescent Dye
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Metabolic Disease
|
|
NBD-Stearic acid is a stearic acid labeled with a nitrobenzoxadiazole (NBD) fluorophore. NBD-Stearic acid can be used as a probe for fatty acid uptake or the the ligand binding sites of fatty acid and sterol carrier proteins (FABP)
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-
- HY-D1398
-
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nAChR
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Neurological Disease
|
|
LtIA-F, a novel fluorescent analogue of LtIA, provides a wealth of pharmacological tools to explore the structure–function relationship, distribution, and ligand binding domain of the α3β2 nAChR subtype.
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-
- HY-NP0215
-
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Biochemical Assay Reagents
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Others
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|
Chicken Serum Albumin is a plasma protein derived from chicken. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
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-
- HY-NP002N
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Biochemical Assay Reagents
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Others
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Pigeon Serum Albumin is a plasma protein derived from pigeon. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
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-
- HY-174407
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Bacterial
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Infection
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|
Antibacterial agent 281 (Compound 95,186) can bacteriostatically inhibit the growth of GAS. Antibacterial agent 281 binds to the ligand binding pocket of SPs0871 and competes with the ligand. Antibacterial agent 281 shows concentration-dependent growth inhibition against S. pyogenes .
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- HY-174784
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mRNA
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Cancer
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Human ACVR1C mRNA encodes the human activin A receptor type 1C (ACVR1C) protein, a type I receptor for the TGFB family of signaling molecules. Upon ligand binding, type I receptors phosphorylate cytoplasmic SMAD transcription factors, which then translocate to the nucleus and interact directly with DNA or in complex with other transcription factors.
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- HY-128838A
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PROTACs
Estrogen Receptor/ERR
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Others
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(rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1. PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader .
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- HY-B1322AS1
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-
- HY-184126
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Androgen Receptor
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Cancer
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|
JZY3221 is an androgen receptor (AR) inhibitor. JZY3221 binds to the AR ligand-binding domain to inhibit AR function. JZY3221 constitutes the AR inhibitory moiety of DALTAC JZY3032 (HY-184124). JZY3221 is applicable to research related to prostate cancer .
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- HY-182395
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FXR
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Others
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|
DM175 is a partial agonist of FXR. DM175 binds to the ligand-binding domain of FXR and induces the outward movement of Trp454 .
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-
- HY-180398
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PPAR
PGC-1α
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Metabolic Disease
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|
PA-082 is a selective PPAR-γ modulator that functions as a partial agonist. PA-082 causes partial recruitment of SRC1, TIF2, SRC3 and full recruitment of PGC1-α to PPAR-γ ligand-binding domain. PA-082 prevents triglyceride accumulation during de novo adipogenesis and antagonizes Rosiglitazone (HY-17386)-induced lipid accumulation. PA-082 potentiates insulin-stimulated glucose uptake in adipocytes and protects against TNFα-induced insulin resistance. PA-082 can be used for the research of type 2 diabetes .
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-
- HY-P991781
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CXCR
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Inflammation/Immunology
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|
Anti-Mouse CXCR6 Antibody (Cx6Mab-1) reacts with the N-terminal extracellular ligand-binding domain of mouse CXCR6. Recommend Isotype Controls: Rat IgG1 kappa, Isotype Control (HY-P99979) .
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- HY-18314B
-
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Orphan Nuclear Receptor
Ferroptosis
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Cardiovascular Disease
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(Z)-GW 441756 is a hepatocyte nuclear factor 4α (HNF4α) activator, with an EC50 of 9.2 μM and a Ka of 4.6 μM in human systems. (Z)-GW 441756 directly interacts with the ligand-binding domain of HNF4α via persistent hydrogen bonds and hydrophobic interactions within the binding pocket. (Z)-GW 441756 reduces the accumulation of triglycerides and total cholesterol. (Z)-GW 441756 inhibits ferroptosis through a non-antioxidant mechanism. (Z)-GW 441756 decreases plasma triglyceride and total cholesterol levels in animal models of hyperlipidemia. (Z)-GW 441756 can be used in studies related to hyperlipidemia .
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- HY-181652
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PPAR
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Endocrinology
|
|
PPARδ agonist 13 is a potent, selective and orally active PPARδ agonist with an EC50 values of 0.50 nM. PPARδ agonist 13 binds to the PPARδ ligand-binding pocket and upregulates PPARδ target gene expression. PPARδ agonist 13 inhibits renal fibroblast activation, restores fatty acid oxidation, and attenuates TGF-β1-induced renal fibroblast activation. PPARδ agonist 13 exhibits anti-renal fibrosis effects in a mouse model of unilateral ureteral obstruction. PPARδ agonist 13 can be used for the research of renal fibrosis .
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-
- HY-165475
-
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iGluR
|
Neurological Disease
|
|
TDPAM02 is a positive allosteric modulator of AMPA receptor GluA2. TDPAM02 can specifically bind to the ligand-binding domain (LBD) of GluA2 and shows an IC50 of 1.4 nM for the GluA2 flop subtype. TDPAM02 can stabilize the activated conformation of GluA2 receptors, delay the receptor deactivation or desensitization process, maintaining the rapid excitatory synaptic transmission in the central nervous system .
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-
- HY-165474
-
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iGluR
|
Neurological Disease
|
|
TDPAM01 is a positive allosteric modulator of AMPA receptor GluA2. TDPAM01 can specifically bind to the ligand-binding domain (LBD) of GluA2 and shows an IC50 of 13.4 nM for the GluA2 flop subtype. TDPAM01 can stabilize the activated conformation of GluA2 receptors, delay the receptor deactivation or desensitization process, maintaining the rapid excitatory synaptic transmission in the central nervous system .
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-
- HY-183602
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DNA/RNA Synthesis
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Cancer
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|
FRC-303 is a CHD1 inhibitor with a Kd of 0.14 μM and an IC50 of 0.18 μM. FRC-303 binds to the H3K4me3 binding site of CHD1 tandem chromodomain, forms aromatic cage interactions and extended ligand contacts, acts as a methyl-lysine mimic, and occupies natural peptide ligand-binding regions. FRC-303 can be used for the research of prostate cancer .
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-
- HY-P5407A
-
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SARS-CoV
Angiotensin-converting Enzyme (ACE)
|
Infection
Cancer
|
|
HD5 TFA is an innate immune effector peptide and SARS-CoV Inhibitor. HD5 TFA binds to the ligand-binding domain of angiotensin-converting enzyme-2 (ACE2) via multiple hydrogen bonds to competitively block the receptor, shielding it from viral recognition. HD5 TFA can be used for the research of COVID-19, HPV16 infection, epithelial ovarian cancer, small-cell lung cancer, and colon cancer .
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-
- HY-180554
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Synaptic Vesicle Proteins
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Neurological Disease
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UCB1244283 is a synaptic vesicle glycoprotein 2A (SV2A) allosteric modulator. UCB1244283 binds to a secondary ligand-binding site in SV2A and enhances orthosteric ligand engagement when the orthosteric site is occupied, by stabilizing the occluded state and slowing ligand dissociation. UCB1244283 shows a clear protective effect against both tonic and clonic convulsions in sound-sensitive mice. UCB1244283 can be used for epilepsy research .
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-
- HY-180944
-
|
|
REV-ERB
|
Neurological Disease
|
|
BE2012, SR8278 (HY-14415) derivative, is a potent and selective REV-ERBα/β Antagonist with EC50 values of 0.285 and 0.346 μM. BE2012 binds to the ligand-binding domain (LBD) of REV-ERB, preventing the receptor from recruiting co-inhibitory factors and thereby releasing the transcriptional repression on downstream target genes. BE2012 can upregulate the expression of myogenic transcription factors Myf5 and Myod, promoting muscle regeneration and repair in acute muscle injury micemodels .
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-
- HY-N1749
-
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FXR
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Others
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|
2-Oxokolavenol is a selective agonist targeting the farnesoid X receptor (FXR), with an EC50 of ~3.7 μM. 2-Oxokolavenol exerts its activity against Acetaminophen (HY-66005)-induced hepatocyte damage in an FXR-dependent manner by binding to the FXR ligand-binding pocket, recruiting co-activators, and inducing FXR transcriptional activity. 2-Oxokolavenol can be naturally extracted from Aglaia spectabilis (a plant of the Aglaia genus in the Meliaceae family) and can be used in research related to liver diseases .
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- HY-182624
-
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Na+/H+ Exchanger (NHE)
Wnt
Apoptosis
|
Cancer
|
|
FJ9 is a NHERF1/PDZ inhibitor with human NHERF1 PDZ1 IC50 1540 μM, NHERF1 PDZ2 IC50 160 μM, and Frizzled-7-Dishevelled PDZ complex Ki 10 μM. FJ9 binds ligand-binding pockets of NHERF1 PDZ domains to block cognate ligand interactions, disrupts Frizzled-7-Dishevelled interactions, and down-regulates canonical Wnt signaling. FJ9 induces apoptosis in cancer cells with intact β-catenin signaling. FJ9 can be used for the research of non-small cell lung cancer, melanoma .
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-
- HY-D3274
-
|
|
Fluorescent Dye
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Others
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|
PE-Cy5 is a tandem fluorescent dye commonly used in flow cytometry, immunofluorescence, and cell biology research. It is formed by the covalent linkage of two fluorescent molecules, namely phycoerythrin and CY5. PE-Cy5 binds to human FcγRI (CD64), and this binding can be blocked by human pooled serum, anti-CD64 monoclonal antibodies targeting the ligand-binding region, or aggregated IgG. PE-Cy5 supports three-color flow cytometry analysis, and whole blood staining can partially reduce its non-specific binding (Ex/Em = 450-500 nm/665 nm) .
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- HY-181588
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Nuclear Hormone Receptor 4A/NR4A
|
Neurological Disease
Inflammation/Immunology
|
|
NR4A agonist-2 is a selective pan-NR4A agonist designed based on Vidofludimus (HY-14908), with a Kd of 0.10 μM against NR4A1, and EC50 values of 0.098 μM, 0.092 μM and 0.09 μM against Nur77, Nurr1, NOR-1, respectively. NR4A agonist-2 exhibits 47-fold selectivity over DHODH, and shows no cytotoxic activity at concentrations up to 10 μM. By binding to a specific surface pocket in the ligand-binding domain of Nurr1, NR4A agonist-2 inhibits the formation of Nurr1 homodimers, activates response elements such as NBRE, NurRE, DR5, and then potently induces the expression of neuroprotective genes including BDNF, SOD2, thereby exerting neuroprotective activity. NR4A agonist-2 can be used in the research of neurodegenerative diseases such as Parkinson's disease, dementia and multiple sclerosis .
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-
- HY-NP002M
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Guinea Pig Serum Albumin is a plasma protein derived from guinea pig. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
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-
- HY-176822
-
|
|
Epigenetic Reader Domain
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Others
|
|
SGC-BRDVIII-NC (Compound 35) is a negative control compound of SMARCA2/4 and PB1 bromodomain (BRD) inhibitor. SGC-BRDVIII-NC completely abolishes protein-ligand binding capacity with the methylation of the phenolic hydroxyl moiety. SGC-BRDVIII-NC can be used for adipogenesis research .
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-
- HY-204388
-
|
|
iGluR
Calcium Channel
|
Neurological Disease
|
|
TAK-137 is an AMPA receptor potentiator with weak agonistic effect. TAK-137 binds to the AMPA receptor ligand binding domain in a glutamate-dependent manner. TAK-137 potentiates AMPA-induced currents and Ca 2+ influx. TAK-137 can be used for the research of neurological disease .
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-
- HY-122616
-
|
|
Trk Receptor
|
Neurological Disease
|
|
PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain .
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-
- HY-118260
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Phendioxan is a compound with binding activity at the α(1)-adrenaline receptor subtype. The facilitated membrane diffusion of phendioxan is thought to be associated with improved α(1d)-AR affinity. Docking simulations of phendioxan at biological targets supported the stoichiometric analysis and revealed the importance of polar, electrostatic, hydrophobic, and shape effects of its phenoxy terminal orthogonal substituents on ligand binding .
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-
- HY-144705
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
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-B1322BR
-
|
Amodiaquin dihydrochloride (Standard)
|
Nuclear Hormone Receptor 4A/NR4A
Parasite
Histone Methyltransferase
Reference Standards
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Amodiaquine (dihydrochloride) (Standard) is the analytical standard of Amodiaquine (dihydrochloride). This product is intended for research and analytical applications. Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect .
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-
- HY-W677684
-
|
|
Nuclear Hormone Receptor 4A/NR4A
|
Others
|
|
Nurr1 agonist 2 (Compound 7) is a Nurr1 agonist (EC50: 0.07 μM). Nurr1 agonist 2 binds to the recombinant Nurr1 ligand binding domain (LBD) with a Kd value of 0.14 μM. Nurr1 agonist 2 increases the Nurr1-regulated genes tyrosine hydroxylase (TH) and vesicular amino acid transporter 2 (VMAT2) mRNA expression .
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-
- HY-B1322R
-
|
Amodiaquin dihydrochloride dihydrate (Standard)
|
Nuclear Hormone Receptor 4A/NR4A
Reference Standards
Parasite
Histone Methyltransferase
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Amodiaquine (dihydrochloride dihydrate) (Standard) is the analytical standard of Amodiaquine (dihydrochloride dihydrate). This product is intended for research and analytical applications. Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect .
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-
- HY-107401
-
|
SCH-351125
|
HIV
CCR
Calcium Channel
|
Infection
|
|
Ancriviroc (SCH-351125) is an orally active CCR5 antagonist with an IC50 value of 13 nM against hCCR5. Ancriviroc specifically binds to hCCR5, blocks ligand-induced signal transduction, calcium influx, GTPγS binding, chemotaxis, ligand binding, and HIV-1 entry, induces conformational changes in CCR5, and inhibits infection and replication of R5-tropic HIV-1 .
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-
- HY-181171
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
HIT-2 is an estrogen receptor alpha (ERα) inhibitor that can bind to the ERα ligand binding domain. HIT-2 forms stable interactions including hydrogen bonds, π-π stacking, and hydrophobic contacts to disrupt ERα-driven signaling. HIT-2 exhibits antineoplastic activity against breast cancer. HIT-2 can be used for the research of breast cancer .
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-
- HY-P9977A
-
|
|
EGFR
|
Cancer
|
|
Amivantamab (FUT8-KO) is an anti-EGFR-MET monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the ADCC effect of the antibody. Amivantamab (FUT8-KO) inhibits ligand binding, promotes endocytosis and degradation of receptor-antibody complexes, and induces Fc-dependent cytokinesis in macrophages and antibody-dependent cytotoxicity in natural killer cells .
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-
- HY-163101
-
|
|
Platelet-activating Factor Receptor (PAFR)
Leukotriene Receptor
|
Inflammation/Immunology
|
|
CP-96021 is an orally active dual leukotriene D4 (LTD4) and platelet activating factor (PAF) receptor antagonist, featuring a guinea pig LTD4 receptor Ki of 34 nM and a rabbit PAF receptor Ki of 37 nM. CP-96021 blocks ligand binding to its target receptors, inhibits ligand-induced bronchoconstriction, and inhibits antigen-triggered airway obstructive effects. CP-96021 can be used for the research of asthma .
|
-
- HY-P99165
-
|
|
IGF-1R
TSH Receptor
|
Endocrinology
|
|
Teprotumumab is an IGF-1 receptor (IGF-1R) blocking human monoclonal antibody. Teprotumumab binds to the ligand binding extracellular α-subunit domain of IGF-1R. Teprotumumab inhibits TSH and IGF-1 action in fibrocytes. Teprotumumab attenuates TSH-dependent IL-6 and IL-8 expression and Akt phosphorylation. Teprotumumab can be used for thyroid-associated ophthalmopathy research .
|
-
- HY-125385
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Sulforhodamine 101 DHPE is a fluorescent probe made from the conjugation of the phospholipid 1,2-dipalmitoyl-sn-glycero-3-PE to sulforhodamine 101, a red fluorescent dye that displays excitation/emission spectra of 586/605 nm, respectively. It integrates into phospholipid bilayers and has been used for imaging of solid supported lipid bilayers, detection of protein-ligand binding on bilayers, and to monitor colocalization of lipid probes in liposomes via resonance energy transfer (RET).
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-
- HY-181020
-
|
|
Phosphodiesterase (PDE)
p38 MAPK
Akt
mTOR
ERK
|
Cancer
|
|
Deltafluorine is a phosphodiesterase delta (PDEδ) inhibitor with an IC50 of 27 nM, a KD of 148 nM. Deltafluorine covalently modifies the specific glutamate residue p.E88 in the ligand binding site of PDEδ, interfering with its chaperone function. Deltafluorine inhibits signaling through the MAPK and Akt-mTOR pathway, reduces ERK1/2 expression. Deltafluorine reduces tumor volume in an autochthonous mouse model of Kras-driven lung adenocarcinoma. Deltafluorine can be used for the research of lung adenocarcinoma .
|
-
- HY-141551
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GNE-274 is a structural analog of the ER degrader GDC-0927 and is a non-degrader. GNE-274 does not induce conversion of ER in breast cancer cell lines and functions as a partial ER agonist (partial ER agonist). GNE-274 increases the chromatin accessibility of ER-DNA binding sites, whereas GDC-0927 does not. GNE-274 is an effective ER ligand binding domain (LBD) inhibitor. GNE-274 can be used in cancer research.
|
-
- HY-175080
-
|
|
Drug Derivative
Fluorescent Dye
|
Others
|
|
8-DY547-cGMP is a fluorescent cGMP analogue composed of a dye DY547 to position 8 of cGMP. 8-DY547-cGMP is a Cyclic nucleotide-gated A2 (CNGA2) ligand. 8-DY547-cGMP can activated CNGA2 channel. 8-DY547-cGMP can be used for simultaneously detection CNG channel activation and ligand binding .
|
-
- HY-E70704
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR G719C Recombinant Human Active Protein Kinase is a recombinant EGFR G719C protein that can be used to study EGFR G719C-related functions .
|
-
- HY-174391
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
AR antagonist 15 is an orally active androgen receptor (AR) antagonist with the IC50 of 97 nM for ART787A. AR antagonist 15 disrupts AR nuclear translocation, hinders AR homodimerization, and suppresses transcription of AR-regulated genes by competitive binding to the ligand binding pocket. AR antagonist 15 can significantly lower the prostate-specific antigen (PSA) level. AR antagonist 15 induces apoptosis by reducing the expression of apoptosis pathway related proteins. AR antagonist 15 can be used for the research of prostate cancer.
|
-
- HY-E70695
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR C797S Recombinant Human Active Protein Kinase is a recombinant EGFR C797S protein that can be used to study EGFR C797S-related functions .
|
-
- HY-E70707
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L858R Recombinant Human Active Protein Kinase is a recombinant EGFR L858R protein that can be used to study EGFR L858R-related functions .
|
-
- HY-14863
-
|
CTA-018
|
VD/VDR
Cytochrome P450
|
Others
Endocrinology
|
|
Lunacalcipol (CTA-018), as a vitamin D analogue, has a dual role in the pathogenesis of Chronic Kidney Disease (CKD), as an agonist of vitamin D receptor and an antagonist of cytochrome P450 enzyme 24-hydroxylase. Lunacalcipol binds to VDR and regulates transcriptional activity of VDR by influencing ligand binding affinity, ligand-dependent coactivator recruitment or inhibitory factor dissociation, efficiency of ligand entry into target cells, tissue specificity and different metabolism of ligand. Lunacalcipol can be used in the study of CKD, especially Secondary Hyperparathyroidism (sHPT) .
|
-
- HY-P991529
-
|
|
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
AGEN-2373 is a conditionally active agonist antibody targeting the co-stimulatory receptor CD137. GEN-2373 binds to CD137 without disruption of ligand binding. AGEN-2373 stimulates CD137 under receptor clustering conditions. AGEN-2373 can enhance T cell activity when combined with other checkpoint modulators (e.g. PD-1 antagonist and OX40 agonist). AGEN-2373 can be studied in research for human malignancies .
|
-
- HY-E70708
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L861Q Recombinant Human Active Protein Kinase is a recombinant EGFR L861Q protein that can be used to study EGFR L861Q-related functions .
|
-
- HY-E70705
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR G719S Recombinant Human Active Protein Kinase is a recombinant EGFR G719S protein that can be used to study EGFR G719S-related functions .
|
-
- HY-E70706
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L718Q Recombinant Human Active Protein Kinase is a recombinant EGFR L718Q protein that can be used to study EGFR L718Q-related functions .
|
-
- HY-E70709
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR T790M Recombinant Human Active Protein Kinase is a recombinant EEGFR T790M protein that can be used to study EGFR T790M-related functions .
|
-
- HY-E70697
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d746-750 Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750 protein that can be used to study EGFR d746-750-related functions .
|
-
- HY-173393
-
|
|
LXR
|
Cancer
|
|
LXRα agonist 1 (Compound 40) is a selective LXRα agonist (EC50: 42 nM). LXRα agonist 1 also has a certain agonistic effect on LXRβ (EC50: 266 nM). LXRα agonist 1 promotes target gene transcription by stabilizing the ligand binding domain (LBD) of LXRα. LXRα agonist 1 exhibits potent antitumor effects in hepatocellular carcinoma cells when combined with the Raf inhibitor Sorafenib (HY-10201). LXRα agonist 1 can be used in the study of lipotoxic cancers .
|
-
- HY-E70703
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d752-759 Recombinant Human Active Protein Kinase is a recombinant EGFR d752-759 protein that can be used to study EGFR d752-759-related functions .
|
-
- HY-113329
-
|
Taurocyamine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Guanidinoethyl sulfonate (Taurocyamine) is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .
|
-
- HY-133830
-
|
(3β,7α,24S)-Cholest-5-ene-3,7,24-triol
|
Endogenous Metabolite
|
Others
|
|
7α,24(S)-Dihydroxycholesterol ((3β,7α,24S)-Cholest-5-ene-3,7,24-triol) serves as a ligand for liver X receptor (LXR), binding specifically to the ligand binding domains of both LXRα and LXRβ. This compound is synthetically produced from E-α,β-enone, utilizing Arsonium ylide and J-tert-butyldimethylsilyloxy-bisnor-5-cholenaldehyde as starting materials, followed by a series of transformations to yield 7α,24(S)-dihydroxycholesterol.
|
-
- HY-113329R
-
|
Taurocyamine (Standard)
|
Endogenous Metabolite
Reference Standards
|
Metabolic Disease
|
|
Guanidinoethyl sulfonate (Standard) is the analytical standard of Guanidinoethyl sulfonate. This product is intended for research and analytical applications. Guanidinoethyl sulfonate is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .
|
-
- HY-E70711
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR T790M/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR T790M/L858R protein that can be used to study EGFR T790M/L858R-related functions .
|
-
- HY-E70701
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d747-749/A750P Recombinant Human Active Protein Kinase is a recombinant EGFR d747-749/A750P protein that can be used to study EGFR d747-749/A750P-related functions .
|
-
- HY-151071
-
|
|
Ligands for Target Protein for PROTAC
CDK
|
Cancer
|
|
TMX-3013 is a CDK inhibitor capable of inhibiting the activity of CDK1, CDK2, CDK4, CDK5, and CDK6, with IC50 values of 0.9 nM, <0.5 nM, 24.5 nM, 0.5 nM, and 15.6 nM, respectively. TMX-3013 can be used as a target protein ligand, conjugated with the PROTAC linker and the CRBN ligand Thalidomide (HY-14658) for the synthesis of PROTAC TMX-2138 (HY-164906). TMX-3013 can also act as an effector ligand, binding to target proteins HaloTag or FKBP, and can be used in the synthesis of regulated induced proximity targeting chimeras (RIPTACs) .
|
-
- HY-E70696
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR C797S/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR C797S/L858R protein that can be used to study EGFR C797S/L858R-related functions .
|
-
- HY-E70698
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d746-750/C797S Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750/C797S protein that can be used to study EGFR d746-750/C797S-related functions .
|
-
- HY-403733A
-
|
|
Androgen Receptor
|
Cancer
|
|
(-)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). (-)-JJ-450 is more potent than (+)-JJ-450 (HY-403733B) in inhibiting androgen-induced AR activity, and the mechanism of AR inhibition by (+)-JJ-450 is different from that of Enzalutamide (MDV3100) (HY-70003), which may target the ligand binding domain (LBD) of AR. (-)-JJ-450 inhibits the transcriptional activity of wild-type AR and mutant AR F876L by inhibiting AR nuclear translocation and promoting nuclear degradation of unbound AR. (-)-JJ-450 can be used in the study of castration-resistant prostate cancer (CRPC) resistant to Enzalutamide .
|
-
- HY-E70702
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d747-752/P753S Recombinant Human Active Protein Kinase is a recombinant EGFR d747-752/P753S protein that can be used to study EGFR d747-752/P753S-related functions .
|
-
- HY-P9964
-
|
11F8; IMC-11F8; LY3012211
|
EGFR
|
Cancer
|
|
Necitumumab (11F8; IMC-11F8; LY3012211) is a human IgG monoclonal antibody directed against EGFR. Necitumumab binds to the EGF binding site of EGFR, blocks ligand binding, neutralizes ligand-induced EGFR phosphorylation and downstream signaling, induces EGFR internalization and degradation, and mediates antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. Necitumumab enhances antitumour activity in combination with Gemcitabine (HY-17026) and Cisplatin (HY-17394) in murine non-small-cell lung cancer xenograft models. Necitumumab can be used in research on cancers such as non-small cell lung cancer and colorectal cancer .
|
-
- HY-P992434
-
|
|
PD-1/PD-L1
SHP1
Interleukin Related
|
Cancer
|
|
OSE-279 is a high-affinity humanized monoclonal bivalent antibody targeting PD-1, the recommended isotype control is HY-P99003. OSE-279 blocks PD-1 ligand binding, inhibits PDL1-induced SHP1 phosphorylation, restores T cell activation, and promotes reactivation of primary T cell effector functions. OSE-279 binds hFcRn receptor, predicts long half-life, induces CD4 and CD8 T cell proliferation, and promotes interleukin 2 and interferon gamma secretion. OSE-279 can be used for the research of advanced malignancies, colon cancer, hepatocarcinoma, mesothelioma .
|
-
- HY-160250
-
|
|
Fluorescent Dye
UGT
|
Metabolic Disease
|
|
UGT1A1-IN-1 is a UGT1A1 inhibitor and fluorescent probe (Ex=370 nm, Em=520 nm), with an IC50 of 1.33 μM and a Ki of 5.02 μM. UGT1A1-IN-1 is selectively glucuronidated by UGT1A1 at the bilirubin homologous binding site, and its PET effect is blocked along with this reaction, triggering fluorescence changes. UGT1A1-IN-1 can serve as a substitute for bilirubin to detect UGT1A1 activity and perform high-throughput screening of UGT1A1 modulators .
|
-
- HY-403733B
-
|
|
Androgen Receptor
Prostaglandin Receptor
|
Cancer
|
|
(+)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR) that inhibits AR nuclear localization and transcriptional activity in the absence of androgen. (+)-JJ-450 is less active than (-)-JJ-450 (HY-403733A) in inhibiting prostate-specific antigen (PSA) expression in LN95 cells, possibly because (+)-JJ-450 targets the ligand binding domain (LBD) of AR. (+)-JJ-450 inhibits the transcriptional activity of AR and its splice variants (e.g., ARv7) by promoting the degradation of unliganded AR in the nucleus and reducing the binding of AR to androgen response elements (AREs). (+)-JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to enzalutamide (MDV3100) (HY-70003) .
|
-
- HY-P990951
-
|
REGN-5381
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
|
|
Vixticibart (REGN-5381) is a fully human IgG4 monoclonal antibody and NPR1 agonist that targets NPR1. Vixticibart stabilizes the receptor in an activated conformation by binding to the N-terminal domain of NPR1, and enhances the activity of endogenous ligands ANP and BNP without blocking ligand binding when these ligands are present. Vixticibart exerts vasodilatory and hypotensive effects by inducing cGMP production, preferentially dilating venous vessels to reduce systolic and venous pressure, but does not induce diuresis and may trigger a compensatory increase in heart rate. Vixticibart produces a synergistic hypotensive effect when combined with angiotensin-converting enzyme inhibitors or angiotensin receptor blockers, and is currently mainly used in research related to heart failure and hypertension .
|
-
- HY-403733C
-
|
|
Androgen Receptor
|
Cancer
|
|
JJ-450 is a non-competitive antagonist androgen receptor (AR) that inhibits the transcriptional activity of wild-type AR and mutant AR F876L. JJ-450 has an IC50 of approximately 1-10 μM in inhibiting AR transcriptional activity in PC3 cells. It is selective for AR binding and does not compete with androgens for binding to the ligand binding domain (LBD) of AR. JJ-450 inhibits the transcriptional activity of AR and its splice variants (such as AR F876L) by inhibiting AR nuclear translocation and promoting the degradation of unliganded AR in the nucleus. JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to Enzalutamide (MDV3100) (HY-70003) .
|
-
- HY-173408
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Ferroptosis
Reactive Oxygen Species (ROS)
Glutathione Peroxidase
|
Cancer
|
|
Nur77 agonist-1 (Compound 8f) is an orally active Nur77 agonist. Nur77 agonist-1 induces ferroptosis by upregulating Nur77 protein expression, increasing reactive oxygen species (ROS) and lipid peroxidation levels, and decreasing GPX4 protein expression. Nur77 agonist-1 has binding affinity to the ligand binding domain (LBD) of Nur77 (KD: 13.80 μM). Nur77 agonist-1 exhibits significant antiproliferative activity against a variety of breast cancer cells (IC50: 2.15-3.26 μM) and has low toxicity to normal cells. Nur77 agonist-1 can be used in breast cancer research .
|
-
- HY-181761
-
|
|
FXR
|
Metabolic Disease
|
|
FXR agonist 16 is a FXR agonist with an EC50 of 2.2 μM. FXR agonist 16 activates FXR transcriptional activity, upregulates SHP and BSEP, and downregulates Cyp7a1. FXR agonist 16 exhibits hepatoprotective activity and reduces AST and ALT levels in free fatty acid-induced hepatocellular injury models. FXR agonist 16 can be used for the research of liver injury .
|
-
- HY-E70699
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d746-750/T790M/C797S Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750/T790M/C797S protein that can be used to study EGFR d746-750/T790M/C797S-related functions .
|
-
- HY-B1403
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Dienestrol is an orally active nonsteroidal estrogen. Dienestrol prevents the formation of implantation swellings in the uterus by inhibiting ovum discharge .
|
-
- HY-157281
-
|
PLIII
|
Endogenous Metabolite
Drug Derivative
MHC
|
Inflammation/Immunology
|
|
Photolumazine III (PLIII) is a microbial metabolite and derivative of Riboflavin (HY-B0456). Photolumazine III binds MR1 with high specificity. Photolumazine III supports efficient TCR binding. Photolumazine III acts as an antigen to activate cells. Responses to Photolumazine III trigger immune reactions .
|
-
- HY-183274
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Apoptosis
PARP
|
Cancer
|
|
Nur77 modulator 5 is a Nur77 modulator. Nur77 modulator 5 induces lysosomal dysfunction, impaired autophagic flux, and apoptosis with increased PARP cleavage, TUNEL positivity, and Annexin V/PI staining. Nur77 modulator 5 can be used for the research of gastric cancer .
|
-
- HY-P2917
-
|
GyK
|
Nuclear Hormone Receptor 4A/NR4A
|
Metabolic Disease
Inflammation/Immunology
|
|
Glycerol kinase, microorganism (GyK) acts as a NR4A1 inhibitor with enzymatic activity. It directly binds to and inhibits the transcription factor NR4A1, thereby negatively regulating hepatic gluconeogenesis and reducing blood glucose levels. Glycerol kinase, microorganism positively regulates UCP1 expression via partial dependence on the β-adrenergic receptor-cAMP-CREB pathway, promotes browning of white adipose tissue and thermogenesis, and further modulates intracellular fatty acid composition and energy metabolism. In diabetic mouse models, overexpression of Glycerol kinase effectively antagonizes NR4A1-induced hyperglycemia, demonstrating potential for improving glucose homeostasis. Glycerol kinase, microorganism can be used for studies on diabetes and obesity .
|
-
- HY-148611
-
|
|
iGluR
|
Neurological Disease
|
|
NSC339614 potassium is a selective GluN1/GluN2C and GluN1/GluN2D receptor enhancer with the activity of enhancing neuronal responses to specific NMDA receptors. NSC339614 potassium can selectively enhance the signaling of GluN1/GluN2C and GluN1/GluN2D receptors without affecting other NMDA receptors. The mechanism of action of NSC339614 potassium does not compete with agonists of L-glutamate or glycine, nor does it depend on membrane potential. The activity of NSC339614 potassium depends on the specific structure of the agonist ligand binding domain, showing its potential as a novel pharmacological agent for studying the function of NMDA receptor subtypes and providing new lead compounds for a variety of neurological diseases .
|
-
- HY-N8075
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Artonin U is an artonin. Artonin U can be isolated from Artocarpus species. Artonin U binds to hERα, as measured by docking score and Prime MM-GBSA binding free energy evaluation. Artonin U can be used in breast cancer research .
|
-
- HY-E70700
-
|
|
EGFR
|
Cancer
|
|
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d746-750/T790M/C797S/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750/T790M/C797S/L858R protein that can be used to study EGFR d746-750/T790M/C797S/L858R-related functions .
|
-
- HY-W017113
-
|
|
Environmental Pollutants
Endogenous Metabolite
|
Metabolic Disease
|
|
2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC50 value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .
|
-
- HY-114402
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study of castration-resistant prostate cancer (mCRPC) .
ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).
|
-
- HY-112288
-
|
TTI-101
|
STAT
Apoptosis
DNA Methyltransferase
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
C188-9 (TTI-101) is a STAT3 inhibitor with a Kd value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia .
|
-
-
-
HY-L152
-
|
|
5,123 compounds
|
|
19F-NMR has proved to be a detection mode in fragment-based drug discovery (FBDD) for studies of protein structure and interactions. 19F shows high sensitivity for NMR detection, and the exquisite sensitivity of 19F chemical shifts and linewidths to ligand binding all make it a valuable approach in FBDD.F (Fluorine) -Fragments can be used for 19F-NMR detection after binding to target proteins, and can be used as an effective 19F-NMR tool for FBDD.
MCE designs a unique collection of 5,123 F-fragments, all of which obey a heuristic rule called the “Rule of Three (RO3)”, in which molecular weight ≤300 Da, the number of hydrogen bond donors (H-donors) ≤3, the number of hydrogen bond acceptors (H-acceptors) is ≤3 and cLogP is ≤3. This F-fragments library is an important source of lead-like drugs.
|
| Cat. No. |
Product Name |
Type |
-
- HY-D2857
-
|
|
Fluorescent Dyes
|
|
NBD-Stearic acid is a stearic acid labeled with a nitrobenzoxadiazole (NBD) fluorophore. NBD-Stearic acid can be used as a probe for fatty acid uptake or the the ligand binding sites of fatty acid and sterol carrier proteins (FABP)
|
-
- HY-D3274
-
|
|
Fluorescent Dyes
|
|
PE-Cy5 is a tandem fluorescent dye commonly used in flow cytometry, immunofluorescence, and cell biology research. It is formed by the covalent linkage of two fluorescent molecules, namely phycoerythrin and CY5. PE-Cy5 binds to human FcγRI (CD64), and this binding can be blocked by human pooled serum, anti-CD64 monoclonal antibodies targeting the ligand-binding region, or aggregated IgG. PE-Cy5 supports three-color flow cytometry analysis, and whole blood staining can partially reduce its non-specific binding (Ex/Em = 450-500 nm/665 nm) .
|
| Cat. No. |
Product Name |
Type |
-
- HY-NP002L
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Biochemical Assay Reagents
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Canine Serum Albumin is a plasma protein derived from dogs. Canine Serum Albumin exhibits greater flexibility than human serum albumin and bovine serum albumin. Serum albumin is a multifunctional protein with exceptional ligand-binding capacity, which enables it to act as a transport molecule for various metabolites, drugs, nutrients, metals and other molecules .
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- HY-NP002K
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Biochemical Assay Reagents
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Rat Serum Albumin is a plasma protein derived from rat. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
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- HY-NP002O
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Biochemical Assay Reagents
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Cynomolgus Monkey serum albumin is a plasma protein derived from cynomolgus monkey. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules.
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- HY-NP002C
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Biochemical Assay Reagents
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Rabbit Serum Albumin (globulin free) is a plasma protein derived from rabbits. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
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- HY-NP0215
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Biochemical Assay Reagents
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Chicken Serum Albumin is a plasma protein derived from chicken. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
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- HY-NP002N
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Biochemical Assay Reagents
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Pigeon Serum Albumin is a plasma protein derived from pigeon. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
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- HY-NP002M
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Biochemical Assay Reagents
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Guinea Pig Serum Albumin is a plasma protein derived from guinea pig. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10579
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123B9
1 Publications Verification
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Ephrin Receptor
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Cancer
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123B9, a tumor-homing agent, is a potent and selective EphA2 agonist with a Kd value of 4.0 μM. 123B9 selectively targets the EphA2 tyrosine kinase receptor ligand-binding domain. 123B9 does not appreciably inhibit the ligand binding domains of the most closely related EphA3 and EphA4 receptors .
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- HY-P2264
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Ephrin Receptor
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Inflammation/Immunology
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KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC50:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses .
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- HY-P5407
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SARS-CoV
Angiotensin-converting Enzyme (ACE)
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Infection
Cancer
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HD5 is an innate immune effector peptide and SARS-CoV Inhibitor. HD5 binds to the ligand-binding domain of angiotensin-converting enzyme-2 (ACE2) via multiple hydrogen bonds to competitively block the receptor, shielding it from viral recognition. HD5 can be used for the research of COVID-19, HPV16 infection, epithelial ovarian cancer, small-cell lung cancer, and colon cancer .
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- HY-P10430
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Transmembrane Glycoprotein
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Neurological Disease
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Stalk peptide is a GPR110 activator. Stalk peptide is released from GPCR Autoproteolysis INducing domain by autocatalytic process and then Stalk peptide is inserted into the ligand-binding pocket of the receptor to activate the receptor. Stalk peptide can promote nerve growth and synaptic formation. Stalk peptide can be used to study neurodevelopmental and neurodegenerative diseases .
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- HY-P4863
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CGRP Receptor
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Neurological Disease
Metabolic Disease
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Biotinyl-Amylin (human) is a biotin-labeled derivative of Amylin, amide, human (HY-P1070). Biotinyl-Amylin (human) acts as a competitive agonist for the Calcitonin Receptor (CTR) and for the Amylin receptors (AMY1, AMY2, and AMY3) formed by the association of CTR with RAMP1/2/3. By mimicking endogenous human amylin, Biotinyl-Amylin (human) binds to and activates CTR and AMY receptors, thereby initiating downstream signaling pathways involving cAMP, CREB, and ERK1/2, while retaining high-affinity receptor binding and activation capabilities. Biotinyl-Amylin (human) is primarily utilized in studies investigating the metabolic regulatory mechanisms underlying obesity and diabetes; it is also applicable to pharmacological research, receptor localization studies, and ligand-binding assays related to Amylin receptors in the context of Alzheimer's disease .
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- HY-119782
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Fluorescent Dye
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Others
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L-Argininamide is a hydrophilic amino acid derivative and can be used as a compound for ligand binding DNA aptamers. L-Argininamide has the potential for fluorescent aptasensors development .
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- HY-P5407A
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SARS-CoV
Angiotensin-converting Enzyme (ACE)
|
Infection
Cancer
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HD5 TFA is an innate immune effector peptide and SARS-CoV Inhibitor. HD5 TFA binds to the ligand-binding domain of angiotensin-converting enzyme-2 (ACE2) via multiple hydrogen bonds to competitively block the receptor, shielding it from viral recognition. HD5 TFA can be used for the research of COVID-19, HPV16 infection, epithelial ovarian cancer, small-cell lung cancer, and colon cancer .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P9977
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JNJ-61186372
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EGFR
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Inflammation/Immunology
Cancer
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Amivantamab (JNJ-61186372) is a human EGFR-MET bispecific antibody with immune anticancer activity. Amivantamab inhibits ligand binding, promotes endocytosis and degradation of receptor-antibody complexes, and induces Fc-dependent cytokinesis in macrophages and antibody-dependent cytotoxicity in natural killer cells .
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-
(5)
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- HY-P99055
-
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TNF Receptor
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Inflammation/Immunology
Cancer
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Urelumab, a fully human, non-ligand binding, CD137 agonist IgG4 monoclonal antibody, enhances T-cell and natural killer-cell antitumor activity, and may enhance cytotoxic activity of Rituximab (HY-P9913). Urelumab can be used for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and other types of non-Hodgkin lymphoma (NHL) .
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(5)
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- HY-P99165
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IGF-1R
TSH Receptor
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Endocrinology
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Teprotumumab is an IGF-1 receptor (IGF-1R) blocking human monoclonal antibody. Teprotumumab binds to the ligand binding extracellular α-subunit domain of IGF-1R. Teprotumumab inhibits TSH and IGF-1 action in fibrocytes. Teprotumumab attenuates TSH-dependent IL-6 and IL-8 expression and Akt phosphorylation. Teprotumumab can be used for thyroid-associated ophthalmopathy research .
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-
(5)
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- HY-P9964
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11F8; IMC-11F8; LY3012211
|
EGFR
|
Cancer
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Necitumumab (11F8; IMC-11F8; LY3012211) is a human IgG monoclonal antibody directed against EGFR. Necitumumab binds to the EGF binding site of EGFR, blocks ligand binding, neutralizes ligand-induced EGFR phosphorylation and downstream signaling, induces EGFR internalization and degradation, and mediates antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. Necitumumab enhances antitumour activity in combination with Gemcitabine (HY-17026) and Cisplatin (HY-17394) in murine non-small-cell lung cancer xenograft models. Necitumumab can be used in research on cancers such as non-small cell lung cancer and colorectal cancer .
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(5)
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- HY-108822
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Arcalyst; IL 1 Trap; Interleukin 1 Trap
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Interleukin Related
|
Inflammation/Immunology
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Rilonacept (Arcalyst), a dimeric fusion protein, is a interleukin 1 inhibitor. Rilonacept consists of the ligand-binding domains of the extracellular portions of the IL-1R components linked to the Fc portion of human IgG1. Rilonacept can be used for the research of cryopyrin-associated periodic syndromes .
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(5)
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- HY-P99446
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TACI-Ig; TACI-Fc 5
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TNF Receptor
|
Inflammation/Immunology
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Atacicept (TACI-Ig) is a is a recombinant fusion protein containing the extracellular, ligand-binding portion of the TACI receptor and the Fc portion of human IgG. Atacicept inhibits B cell stimulation by binding to B lymphocyte stimulator and a proliferation-inducing ligand. Atacicept can be used in research of B-cell autoimmune disease .
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(5)
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- HY-P991224
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CCR
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Inflammation/Immunology
Cancer
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CAP-100 is a monoclonal antibody that targets CCR7. CAP-100 neutralizes the ligand-binding site and signaling of CCR7. CAP-100 strongly inhibits CCR7-induced migration, extravasation, homing, and survival in chronic lymphocytic leukemia (CLL) samples. CAP-100 triggers potent tumor cell killing, mediated by host immune mechanism. CAP-100 shows a favorable toxicity profile on relevant hematopoietic subsets. CAP-100 is involved in research on anti-tumor and disease such as CLL .
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(5)
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- HY-P990951
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REGN-5381
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Natriuretic Peptide Receptor (NPR)
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Cardiovascular Disease
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Vixticibart (REGN-5381) is a fully human IgG4 monoclonal antibody and NPR1 agonist that targets NPR1. Vixticibart stabilizes the receptor in an activated conformation by binding to the N-terminal domain of NPR1, and enhances the activity of endogenous ligands ANP and BNP without blocking ligand binding when these ligands are present. Vixticibart exerts vasodilatory and hypotensive effects by inducing cGMP production, preferentially dilating venous vessels to reduce systolic and venous pressure, but does not induce diuresis and may trigger a compensatory increase in heart rate. Vixticibart produces a synergistic hypotensive effect when combined with angiotensin-converting enzyme inhibitors or angiotensin receptor blockers, and is currently mainly used in research related to heart failure and hypertension .
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(5)
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- HY-P991222
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Phosphatase
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Cardiovascular Disease
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AMG-529 is a humanized monoclonal antibody against ASGR1 that binds to ASGR1, blocks ligand binding, and causes a dose-dependent increase in ALP (a biomarker of ASGR1 inhibition). AMG-529 can be used for the research of cardiovascular diseases .
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(5)
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- HY-P990073
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REGN-5093
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c-Met/HGFR
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Cancer
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Davutamig (REGN-5093) is a human IgG4-kappa, anti-MET bispecific antibody. Davutamig binds 2 distinct epitopes of MET, blocking ligand binding and inducing MET internalization and degradation. Davutamig is applicable to the research of advanced non-small cell lung cancer with MET gene abnormalities .
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(5)
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- HY-P9977A
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EGFR
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Cancer
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Amivantamab (FUT8-KO) is an anti-EGFR-MET monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the ADCC effect of the antibody. Amivantamab (FUT8-KO) inhibits ligand binding, promotes endocytosis and degradation of receptor-antibody complexes, and induces Fc-dependent cytokinesis in macrophages and antibody-dependent cytotoxicity in natural killer cells .
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-
(5)
-
- HY-P991553
-
|
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TNF Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
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HeFi-1 is a mouse anti-CD30 IgG1 monoclonal antibody. HeFi-1 recognizes the ligand-binding site on CD30. HeFi-1 can inhibit the growth of tumor cells with high expression of CD30. HeFi-1 can induce eosinophil apoptosis. HeFi-1 can be used for researches on cancer or inflammation conditions such as anaplastic large-cell lymphoma (ALCL) and asthma .
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-
(5)
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- HY-P991529
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|
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TNF Receptor
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Inflammation/Immunology
Cancer
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AGEN-2373 is a conditionally active agonist antibody targeting the co-stimulatory receptor CD137. GEN-2373 binds to CD137 without disruption of ligand binding. AGEN-2373 stimulates CD137 under receptor clustering conditions. AGEN-2373 can enhance T cell activity when combined with other checkpoint modulators (e.g. PD-1 antagonist and OX40 agonist). AGEN-2373 can be studied in research for human malignancies .
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-
(5)
-
- HY-P991781
-
|
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CXCR
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Inflammation/Immunology
|
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Anti-Mouse CXCR6 Antibody (Cx6Mab-1) reacts with the N-terminal extracellular ligand-binding domain of mouse CXCR6. Recommend Isotype Controls: Rat IgG1 kappa, Isotype Control (HY-P99979) .
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-
(5)
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- HY-P992434
-
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PD-1/PD-L1
SHP1
Interleukin Related
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Cancer
|
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OSE-279 is a high-affinity humanized monoclonal bivalent antibody targeting PD-1, the recommended isotype control is HY-P99003. OSE-279 blocks PD-1 ligand binding, inhibits PDL1-induced SHP1 phosphorylation, restores T cell activation, and promotes reactivation of primary T cell effector functions. OSE-279 binds hFcRn receptor, predicts long half-life, induces CD4 and CD8 T cell proliferation, and promotes interleukin 2 and interferon gamma secretion. OSE-279 can be used for the research of advanced malignancies, colon cancer, hepatocarcinoma, mesothelioma .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-113329
-
-
-
- HY-N0010
-
-
-
- HY-W017113
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|
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Structural Classification
Natural Products
Classification of Application Fields
Metabolic Disease
Endogenous metabolite
Disease Research Fields
Source Classification
|
Environmental Pollutants
Endogenous Metabolite
|
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2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC50 value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .
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-
-
- HY-N2025
-
-
-
- HY-N4194
-
-
-
- HY-113329R
-
|
Taurocyamine (Standard)
|
Structural Classification
Natural Products
Other disease
Disease markers
Endogenous metabolite
|
Endogenous Metabolite
Reference Standards
|
|
Guanidinoethyl sulfonate (Standard) is the analytical standard of Guanidinoethyl sulfonate. This product is intended for research and analytical applications. Guanidinoethyl sulfonate is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .
|
-
-
- HY-13956R
-
|
U 72107 (Standard)
|
Human Gut Microbiota Metabolites
Endogenous metabolite
Source Classification
|
Reference Standards
PPAR
Ferroptosis
|
|
Pioglitazone (Standard) is the analytical standard of Pioglitazone. This product is intended for research and analytical applications. Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .
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-
-
- HY-N2025R
-
-
-
- HY-N1749
-
-
-
- HY-N8075
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13956S1
-
|
|
|
Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively .
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-
-
- HY-B1322AS
-
|
|
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Amodiaquine-d10 is the deuterium labeled Amodiaquine. Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect .
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-
-
- HY-13956S
-
|
|
|
Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively .
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-
-
- HY-18102BS
-
|
|
|
GLPG0492- 13C,d3 racemate is 13C-labeled GLPG0492 (racemate) (HY-18102B). GLPG0492 racemate is an orally active, non-steroidal selective androgen receptor modulator. GLPG0492 racemate exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 racemate effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 racemate prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy .
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-
-
- HY-B1322AS1
-
|
|
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Amodiaquine-d10 hydrochloride is deuterated labeled Amodiaquine (HY-B1322A). Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect .
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-114402
-
|
|
|
PROTAC Synthesis
|
ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study of castration-resistant prostate cancer (mCRPC) .
ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).
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| Cat. No. |
Product Name |
|
Classification |
-
- HY-174784
-
|
|
|
mRNA
|
|
Human ACVR1C mRNA encodes the human activin A receptor type 1C (ACVR1C) protein, a type I receptor for the TGFB family of signaling molecules. Upon ligand binding, type I receptors phosphorylate cytoplasmic SMAD transcription factors, which then translocate to the nucleus and interact directly with DNA or in complex with other transcription factors.
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