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ligand-induced

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31

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4

Inhibitory Antibodies

7

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-116624
    MAZ51
    Maximum Cited Publications
    7 Publications Verification

    VEGFR Apoptosis Cancer
    MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity .
    MAZ51
  • 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 .
    Necitumumab
  • HY-B2167R

    DHA (Standard); Cervonic acid (Standard)

    Reference Standards Endogenous Metabolite Neurological Disease Cancer
    Docosahexaenoic acid (Standard) is the analytical standard of Docosahexaenoic acid. This product is intended for research and analytical applications. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk. In Vitro: Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants. DHA is also required for maintenance of normal brain function in adults. The inclusion of plentiful DHA in the diet improves learning ability and memory . DHA is an essential requirement in every step of brain development like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple double bonds and unique structure allow DHA to impart special membrane characteristics for effective cell signaling. Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder, schizophrenia etc. are causally related to decreased level of DHA . DHA is a potent RXR ligand inducing robust RXR activation already at low micro molar concentrations. The EC50 for RXRα activation by DHA is about 5-10 μM fatty acid . In Vivo: Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memory errors, without affecting the number of working memory errors, and significantly increases the docosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampus and the cerebral cortex . DHA treatment exerts neuroprotective actions on an experimental mouse model of PD. There is a decrease tendency in brain lipid oxidation of MPTP mice but it does not significantly .
    Docosahexaenoic acid (Standard)
  • HY-N2453
    Convallatoxin
    1 Publications Verification

    PPAR NF-κB P-glycoprotein Inflammation/Immunology Cancer
    Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties .
    Convallatoxin
  • HY-N6777
    Penicillic acid
    1 Publications Verification

    Caspase Bacterial Apoptosis Antibiotic Infection Inflammation/Immunology Cancer
    Penicillic acid is a polyketide mycotoxin produced by several species of Aspergillus and Penicillium. Penicillic acid exhibits cytotoxicity in rat alveolar macrophages (AM) in vitro. Penicillic acid inhibits Fas ligand-induced apoptosis by blocking self-processing of caspase-8 .
    Penicillic acid
  • HY-103241
    Ro 90-7501
    3 Publications Verification

    Amyloid-β ATM/ATR Phosphatase Apoptosis Neurological Disease Cancer
    Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response . Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner . Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells .
    Ro 90-7501
  • HY-12397
    ZK159222
    1 Publications Verification

    VD/VDR Endocrinology
    ZK159222, a 25-carboxylic ester analogue of 1α,25-(OH)2D3, is a potent 1α,25-(OH)2D3 receptor (VDR) antagonist. The mechanism of ZK159222 antagonistic action is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivators. ZK159222 has a partial agonistic character .
    ZK159222
  • HY-130256

    PROTACs Epigenetic Reader Domain Cancer
    β-NF-JQ1 is a PROTAC that recruits Aryl Hydrocarbon Receptor E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity .
    β-NF-JQ1
  • HY-153840A

    Toll-like Receptor (TLR) Inflammation/Immunology
    ODN INH-18 sodium is a linear 24-mer class B INH-ODN in which the 5' INH-ODN 4084-F sequence was followed by a random stretch of 12 nucleotides lacking the ability to form significant secondary structures. ODN INH-18 sodium showes inhibitory potency for TLR9 ligand-induced IFN-α production.
    ODN INH 18 sodium
  • HY-P991048

    c-Fms Cancer
    AMG-820 is a fully human IgG2 antibody that targets CSF-1R. AMG-820 inhibits binding of the ligands CSF1 and IL34 and subsequent ligand-induced receptor activation. The isotype control for AMG-820 can refer to Human IgG2 kappa, Isotype Control (HY-P99002) .
    AMG-820
  • 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 .
    Ancriviroc
  • HY-P991571

    GC-1118A

    EGFR PERK Akt Cancer
    GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .
    GC1118
  • HY-160998

    CCR Inflammation/Immunology
    YM-344031 is an orally active antagonist for CCR3. YM-344031 inhibits binding of Eotaxin-1 and RANTES to CCR3, with IC50 of 3.0 and 16.3 nM. YM-344031 inhibits ligand-induced rise in intracellular Ca [2+] and the ligand-induced chemotaxis. YM-344031 inhibits eotaxin-1-induced changes in eosinophil morphology in macaques blood, and prevents allergic skin reactions in a mouse allergy model .
    YM-344031
  • HY-134969

    LXR Metabolic Disease
    TFCA is a liver X receptor α (LXRα) antagonist. TFCA inhibits ligand-activated LXRα coactivation and transcriptional expression of the downstream target genes involved in fatty acid synthesis. TFCA attenuates ligand-induced lipogenesis and fatty liver by selectively inhibiting LXRα in the liver .
    TFCA
  • HY-153840

    Toll-like Receptor (TLR) Inflammation/Immunology
    ODN INH-18 is a linear 24-mer class B INH-ODN in which the 5' INH-ODN 4084-F sequence was followed by a random stretch of 12 nucleotides lacking the ability to form significant secondary structures. ODN INH-18 showes inhibitory potency for TLR9 ligand-induced IFN-α production.
    ODN INH 18
  • HY-169703
    SPA0355
    1 Publications Verification

    RANKL/RANK p38 MAPK Akt NF-κB Inflammation/Immunology
    SPA0355 is a thiourea derivative that has antioxidant and anti-inflammatory properties. SPA0355 inhibits the RANKL (receptor activator of nuclear factor κB ligand) induced osteoclast formation in primary bone marrow-derived macrophages. SPA0355 also suppresses the activation of the MAPKs, Akt, and NF-κB pathways. Additionally, SPA0355 promotes osteoblast differentiation, increases alkaline phosphatase activity, and enhances mineral nodule formation. SPA0355 can protect ovariectomized mice from bone loss by stimulating osteoblast differentiation and inhibiting osteoclast resorption, making it useful for studying postmenopausal osteoporosis .
    SPA0355
  • HY-N11494

    NF-κB Others
    Dauricumine is a chlorinated alkaloid that inhibits NF-κB ligand-induced differentiation of mouse bone marrow-derived macrophages into multinucleated osteoclasts .
    Dauricumine
  • HY-124382

    TRP Channel Neurological Disease
    AS1928370 is a novel and central nervous system (CNS) penetrant TRPV1 antagonist and can prevent ligand-induced activation in vivo. AS1928370 is a promising agent for neuropathic pain research .
    AS1928370
  • HY-116088

    LPL Receptor Inflammation/Immunology
    W123, a FTY720 analog, is a competitive sphingosine 1-phosphate type 1 (S1P1) receptor antagonist. W123 is measured by GTPγS activation, MAPK recruitment, cell migration, and ligand-induced receptor internalization .
    W123
  • HY-153840B

    Toll-like Receptor (TLR) Inflammation/Immunology
    ODN INH-18 triethylamine is a linear 24-mer class B INH-ODN in which the 5' INH-ODN 4084-F sequence was followed by a random stretch of 12 nucleotides lacking the ability to form significant secondary structures. ODN INH-18 triethylamine showes inhibitory potency for TLR9 ligand-induced IFN-α production.
    ODN INH 18 triethylamine
  • 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 .
    CP-96021
  • HY-N12561

    ERK p38 MAPK JNK Others
    Pestanoid A is a rearranged pimarane diterpenoid osteoclastogenesis inhibitor with an IC50 of 4.2 μM. Pestanoid A can be isolated from the marine mesophotic zone chalinidae sponge-associated fungus, Pestalotiopsis sp. NBUF145. Pestanoid A inhibits the receptor activator of NF-kB ligand-induced MAPK and NF-κB signaling by suppressing the phosphorylation of ERK1/2-JNK1/2-p38 MAPKs and NF-κB nuclear translocation. Pestanoid A can be used for the study of osteoporosis .
    Pestanoid A
  • HY-N2453R

    Reference Standards PPAR NF-κB P-glycoprotein Inflammation/Immunology Cancer
    Convallatoxin (Standard) is the analytical standard of Convallatoxin. This product is intended for research and analytical applications. Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties .
    Convallatoxin (Standard)
  • HY-N9790

    Notch Others
    Procyanidin B2, 3,3'-di-O-gallate is an active constituent. Procyanidin B2, 3,3'-di-O-gallate can be isolated from grape seed extract (GSE) procyanidin mix. Procyanidin B2, 3,3' -di-o-gallate target cancer stem cells (CSCs) in prostate cancer (PCa). Procyanidin B2, 3,3'-di-O-gallate targets both unsorted and sorted CSCs at lower doses. Procyanidin B2, 3,3'-di-O-gallate strongly suppresses the constitutive as well as Jagged1 (Notch1 ligand)-induced activated Notch1 pathway .
    Procyanidin B2 3,3'-di-O-gallate
  • HY-146441

    STAT Cardiovascular Disease Inflammation/Immunology
    Prohibitin ligand 1 (Compound 22i), a cardioprotectant prohibitin ligand, induces a phosphorylation of the pro-survival factor STAT3. Prohibitin ligand 1 exhibits in vitro cardioprotectant activities at nanomolar concentrations .
    Prohibitin ligand 1
  • HY-168586

    PROTACs IRAK Cancer
    PROTAC IRAK4 degrader-12 is a PROTAC based on Cereblon ligand, inducing a maximum degradation rate of IRAK4 of 108.46% in K562 cells with an IC50 value of 4.87 nM ( Structure Note: Pink, IRAK4 inhibitor (HY-168611); Blue, E3 (HY-W733885); Black, linker (HY-168613)) .
    PROTAC IRAK4 degrader-12
  • HY-P991353

    PD-1/PD-L1 Cancer
    Sym-021 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. Sym-021 blocks the binding of PD-L1 and PD-L2 ligands, inducing the secretion of interferon IFN-γ and IL-2 and the proliferation of T cells. Sym-021 has anti-tumor activity in PDX mouse models .
    Sym-021
  • HY-N6777S

    Isotope-Labeled Compounds Cancer
    Penicillic acid- 13C8 is the 13C-labeled Penicillic acid (HY-N6777). Penicillic acid is a polyketide mycotoxin produced by several species of Aspergillus and Penicillium. Penicillic acid exhibits cytotoxicity in rat alveolar macrophages (AM) in vitro. Penicillic acid inhibits Fas ligand-induced apoptosis by blocking self-processing of caspase-8 .
    Penicillic acid-13C8
  • HY-118668

    NF-κB Others
    ABD-350 is an antiresorptive agent that inhibits osteoclast activity without affecting osteoblast activity and preventing ovariectomy-induced bone loss. ABD-350 inhibits NF-κB ligand-induced inhibitor of NF-κB phosphorylation, leading to osteoclast apoptosis, but has no inhibitory effect on osteoblast function, effectively preventing bone loss in ovariectomized mice, and does not inhibit parathyroid hormone-induced bone formation.
    ABD-350
  • HY-182736

    CCR Histamine Receptor Calcium Channel Inflammation/Immunology
    YM-344484 is an orally active dual antagonist of chemokine CCR3 receptor and histamine histamine H1 receptor. YM-344484 inhibits ligand-induced Ca 2+ influx, chemotaxis of CCR3-expressing cells, histamine-induced Ca 2+ influx, increased vascular permeability and eosinophil accumulation. YM-344484 suppresses vascular permeability and inhibits eosinophil infiltration in a mouse asthma model. YM-344484 can be used in research related to asthma, allergic rhinitis and atopic dermatitis .
    YM-344484
  • HY-103241R

    Reference Standards Amyloid-β ATM/ATR Phosphatase Apoptosis Neurological Disease Cancer
    Ro 90-7501 (Standard) is the analytical standard of Ro 90-7501 (HY-103241). This product is intended for research and analytical applications. Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response . Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner . Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells .
    Ro 90-7501 (Standard)

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