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dual modulator

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24

Inhibitors & Agonists

1

Inhibitory Antibodies

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-114863

    THCCC

    mGluR Neurological Disease
    PHCCC(4Me) (THCCC), a PHCCC analog, is a dual mGluR2 (IC50 of 1.5 μM) negative allosteric modulator and mGluR3 (EC50 of 8.9 μM) positive allosteric modulator .
    PHCCC(4Me)
  • HY-147361

    Apoptosis Lactate Dehydrogenase Cancer
    LDCA is a dual-hit metabolic modulator and inhibits LDH-A enzyme activity to stimulate apoptosis in the malignant population. LDCA can be used for the research of oncogenic progression .
    LDCA
  • HY-152254

    FAAH Cannabinoid Receptor Infection Neurological Disease Inflammation/Immunology Cancer
    CB2R/FAAH modulator-3 (compound 27) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-3 are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection .
    CB2R/FAAH modulator-3
  • HY-169964

    Carbonic Anhydrase Neurological Disease
    TSPO/Carbonic Anhydrase Modulator 1 (Compound 3) is a dual modulator for mitochondrial translocator protein and Carbonic Anhydrase with a Ki of 1.340 μM for TSPO and a KA of 10.7 μM for CA VII. TSPO/Carbonic Anhydrase Modulator 1 promotes the production of neurosteroid, increases BDNF gene expression, exhibits neuroprotective efficacy .
    TSPO/Carbonic Anhydrase Modulator 1
  • HY-170944

    HSP Apoptosis Caspase Cancer
    BAG3/HSP70-IN-1 (compound 16) is the first-in-class BAG3 and HSP70 dual inhibitor. BAG3/HSP70-IN-1 binds to BAG3 full-length, BAG3-BD, and HSP70 proteins with Kds of 33.10 μM, 27.90 μM, and 33.80 μM, respectively. BAG3/HSP70-IN-1 inhibits HeLa cells with an IC50 of 49.46 μM. BAG3/HSP70-IN-1 induces apoptosis by activating caspase 3 and caspase 9 levels in HeLa cells. BAG3/HSP70-IN-1 elevates p21 levels while reduces FOXM1 expression in HeLa cells. BAG3/HSP70-IN-1 decreases ATPase activity .
    BAG3/HSP70-IN-1
  • HY-118397

    PPAR Others
    RB394 is a potent dual sEH/PPARγ modulator isoform that promotes adipocyte browning and exhibits cardioprotective activity, and can be used to suppress metabolic syndrome.
    RB394
  • HY-151963

    PPAR Glucocorticoid Receptor Metabolic Disease
    PPARγ/GR modulator 1 is an orally active dual agonist of PPARγ and glucocorticoid receptor (GR), with Kis of 3.3 and 33.6 μM, respectively. PPARγ/GR modulator 1 can be used for the research of metabolic diseases, such as diabetes .
    PPARγ/GR modulator 1
  • HY-152253

    FAAH Cannabinoid Receptor Infection Neurological Disease Inflammation/Immunology Cancer
    CB2R/FAAH modulator-2 (compound 26) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-2 are 10.8 and 152.9 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 6.2 μM. CB2R/FAAH modulator-2 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection .
    CB2R/FAAH modulator-2
  • HY-117965

    CORT 118335

    Glucocorticoid Receptor Mineralocorticoid Receptor Endocrinology
    Miricorilant (CORT 118335) is a dual selective glucocorticoid (GR) modulator/mineralocorticoid (MR) antagonist. Miricorilant can be used for the research of hypothalamic-pituitary-adrenal (HPA) axis related disorders .
    Miricorilant
  • HY-172231

    Estrogen Receptor/ERR Cardiovascular Disease Cancer
    Hexolame is an estrogen receptors agonist with dual anticoagulant and estrogenic properties. Hexolame binds to estrogen receptors to induce anticoagulant effects by modulating clotting factors or platelet activity. Hexolame is promising for research of prostatic cancer and prevention of thrombosis .
    Hexolame
  • HY-149831

    FXR Metabolic Disease
    ZLY28 is the first-in-class intestinal restricted and orally active FXR and FABP1 dual modulator. ZLY28 also is a novel anti-NASH agent. ZLY28 can be used for the research of nonalcoholic steatohepatitis (NASH) .
    ZLY28
  • HY-116273

    Phospholipase Cancer
    ML299 is a selective allosteric modulator and a dual inhibitor of phospholipases D1 and D2 (IC50 values are 6 and 12 nM, respectively). ML299 decreases invasive migration in U87-MG glioblastoma cells .
    ML299
  • HY-P990706

    ALPN-303

    TNF Receptor Inflammation/Immunology
    Povetacicept (ALPN-303), an Fc fusion protein of an engineered TACI domain, is a dual APRIL/BAFF antagonist. Povetacicept modulates B lymphocytes and pathogenic autoantibodies for the study of Lupus and other B cell-related autoimmune diseases .
    Povetacicept
  • HY-128677

    Casein Kinase Neurological Disease
    NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms .
    NCC007
  • HY-124478

    Ethyl 2,5-dihydroxybenzoate

    Phosphatase Metabolic Disease
    Ethyl gentisate (Ethyl 2,5-dihydroxybenzoate) is a dual modulator for cell differentiation, that enhances the osteogenic differentiation of human mesenchymal stem cells (hMSCs) and alkaline phosphatase activity, inhibits RANKL-activated osteoclastogenesis in RAW264.7 cells, and balances the bone remodeling process .
    Ethyl gentisate
  • HY-159484

    HSP Guanylate Cyclase Cardiovascular Disease
    Hsp110/sGC-modulator-1 (compound 17i), an orally active Hsp110/sGC dual-target regulator, exhibits optimal Hsp110 and sGC molecular activities as well as remarkable cell malignant phenotypes inhibitory and vasodilatory effects. Hsp110/sGC-modulator-1 (compound 17i) attenuates pulmonary vascular remodeling and right ventricular hypertrophy via Hsp110 suppression .
    Hsp110/sGC-modulator-1
  • HY-121736

    AGI-026

    Isocitrate Dehydrogenase (IDH) Neurological Disease
    AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma .
    AGI-12026
  • HY-163065

    Opioid Receptor Sigma Receptor Neurological Disease
    σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC50: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (Ki: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models .
    σ1 Receptor/μ Opioid receptor modulator 2
  • HY-155672

    5-HT Receptor Neurological Disease
    JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
    JPC0323
  • HY-158627

    5-HT Receptor Others
    JPC0323 Oleate is a derivative of JPC0323 (HY-155672). JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
    JPC0323 Oleate
  • HY-176731

    P2X Receptor Neurological Disease
    MSK-9 is a positive allosteric modulator of the P2X4 receptor with dual activities of enhancing ion conductance and delaying receptor inactivation. MSK-9 stabilizes the open state of the P2X4 receptor through rigid 3-piperidinyl and hydrophobic menthyl substituents. MSK-9 can be used in the study of multiple sclerosis (MS) .
    MSK-9
  • HY-117459

    PPAR Metabolic Disease
    E-3030 free acid is a potent dual activator of peroxisome proliferator-activated receptor (PPAR) alpha and PPARgamma, exhibiting significant antidiabetic and lipid-modulating effects. E-3030 decreases blood glucose, triglyceride, non-esterified fatty acids, and insulin levels, while increasing blood adiponectin levels. E-3030 improves glucose tolerance and shows remarkable triglyceride- and non-high-density lipoprotein cholesterol-lowering effects in animal models.
    E-3030 free acid
  • HY-144501

    Toll-like Receptor (TLR) PD-1/PD-L1 Inflammation/Immunology Cancer
    D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC50=24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases PD-L1 expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2 .
    D18
  • HY-176287

    Dopamine Receptor GSK-3 PKA Neurological Disease
    ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-gp-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders .
    ARN25657

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