1. Search Result

Search Result

Pathways Recommended: Stem Cell/Wnt Neuronal Signaling JAK/STAT Signaling
Targets Recommended: Wnt RGS Protein

Results for "Alternative wnt signaling Inhibitors" in MCE Product Catalog:

502

Inhibitors & Agonists

30

Screening Libraries

6

Dye Reagents

35

Peptides

1

MCE Kits

2

Inhibitory Antibodies

181

Natural
Products

1

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-114321
    Wnt/β-catenin agonist 1

    Wnt Cancer
    Wnt/β-catenin agonist 1 (compound 3f) is a Wnt/β-catenin signalling pathway agonist, with an EC50 of 0.27 μM.
  • HY-18959
    CWP232228

    β-catenin Wnt Cancer
    CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs).
  • HY-136073
    Wnt pathway activator 2

    Wnt Cancer
    Wnt pathway activator 2 is a potent Wnt activator extracted from patent WO2012024404A1, compound 2, has an IC50s of 13 nM.
  • HY-135516
    Wnt pathway activator 1

    Wnt Cancer
    Wnt pathway activator 1 is a potent Wnt activator extracted from patent WO2012024404A1, compound 1, has an IC50s of 28-29 nM.
  • HY-17545
    LGK974

    wnt974

    Porcupine Cancer
    LGK974 (WNT974) is an orally bioavailable and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM.
  • HY-15659
    Wnt-C59

    C59

    Porcupine Wnt Cancer
    Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC50 of 74 pM.
  • HY-N2907
    Atranorin

    Ras Endogenous Metabolite Cancer
    Atranorin is a lichen secondary metabolite. Atranorin inhibits lung cancer cell motility and tumorigenesis by affecting AP-1, Wnt, and STAT signaling and suppressing RhoGTPase activity.
  • HY-124697
    BMP signaling agonist sb4

    TGF-β Receptor Cancer
    BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC50 value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. BMP signaling agonist sb4 activates BMP4 target genes (inhibitors of DNA binding, Id1 and Id3) canonical BMP signaling.
  • HY-P1454A
    Fz7-21 TFA

    Ac-LPSDDLEFWCHVMY-NH2 TFA

    Wnt Cancer
    Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA , a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
  • HY-P1454
    Fz7-21

    Ac-LPSDDLEFWCHVMY-NH2

    Wnt Cancer
    Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2), a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
  • HY-15108
    Purmorphamine

    Shh signaling Antagonist VI

    Smo Autophagy Neurological Disease Cancer
    Purmorphamine (Shh Signaling Antagonist VI) is a smoothened receptor agonist with an EC50 of 1 μM.
  • HY-122816
    HLY78

    Wnt Cancer Neurological Disease
    HLY78 is an activator of the Wnt/β-catenin signaling pathway, which targets the DIX domain of Axin and potentiates the Axin-LRP6 association to promote Wnt signaling transduction.
  • HY-19987
    BML-284

    Wnt Cancer
    BML-284 is selective and cell-permeable Wnt signaling activator.
  • HY-12238
    IWR-1

    endo-IWR 1; IWR-1-endo

    Wnt Cancer
    IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
  • HY-A0293
    Pyrvinium pamoate

    Pyrvinium embonate

    Wnt Cancer
    Pyrvinium pamoate is an FDA-approved antihelmintic drug that inhibits WNT pathway signaling.
  • HY-135867
    NHC-triphosphate

    Topoisomerase HCV Infection
    NHC-triphosphate is an intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a triphosphate form. NHC-triphosphate is a weak alternative substrate for the viral polymerase and occasionally gets incorporated into HCV replicon RNA.
  • HY-100408
    GNF-6231

    Porcupine Cancer
    GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling.
  • HY-101275
    EMT inhibitor-1

    Hippo (MST) TGF-beta/Smad Wnt Cancer
    EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.
  • HY-19739
    JW74

    Wnt Cancer
    JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling with an IC50 of 420 nM.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-12292
    IM-12

    GSK-3 Cancer
    IM-12 is an inhibitor of GSK-3β, with an IC50 of 53 nM, and also enhances Wnt signalling.
  • HY-120675
    SSTC3

    Casein Kinase Wnt Cancer
    SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
  • HY-108642B
    AMG-548 dihydrochloride

    p38 MAPK Casein Kinase Inflammation/Immunology
    AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
  • HY-108642
    AMG-548

    p38 MAPK Casein Kinase Inflammation/Immunology
    AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
  • HY-108642A
    AMG-548 hydrochloride

    p38 MAPK Casein Kinase Inflammation/Immunology
    AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
  • HY-17439
    Salinomycin sodium salt

    Salinomycin sodium; Sodium salinomycin

    Wnt β-catenin Bacterial Autophagy Apoptosis Antibiotic Cancer
    Salinomycin sodium salt (Salinomycin sodium), an antibiotic potassium ionophore, is a potent inhibitor of Wnt/β-catenin signaling. Salinomycin sodium salt (Salinomycin sodium) acts on the Wnt/Fzd/LRP complex, blocks Wnt-induced LRP6 phosphorylation, and causes degradation of the LRP6 protein. Salinomycin sodium salt (Salinomycin sodium) shows selective activity against human cancer stem cells.
  • HY-P1416
    Foxy-5

    Wnt Cancer
    Foxy-5, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model.
  • HY-18285
    Longdaysin

    Casein Kinase ERK CDK Cancer
    Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.
  • HY-P1416A
    Foxy-5 TFA

    Wnt Cancer
    Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model.
  • HY-N0020
    Echinacoside

    Wnt Reactive Oxygen Species Neurological Disease
    Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche salsa, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity.
  • HY-16910
    WIKI4

    PARP β-catenin Cancer
    WIKI4 is a potent tankyrase inhibitor with an IC50 of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2. WIKI4 is cytotoxic to SCLC cells with an IC50 value of 0.02 μM.
  • HY-15597
    Salinomycin

    Procoxacin

    Bacterial Wnt β-catenin Mitophagy Autophagy Apoptosis Antibiotic Cancer
    Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of Wnt/β-catenin signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin (Procoxacin) shows selective activity against human cancer stem cells.
  • HY-109049
    Adavivint

    SM04690; Lorecivivint

    Wnt Inflammation/Immunology Cancer
    Adavivint (SM04690; Lorecivivint) is a potent and selective inhibitor of canonical Wnt signaling, with an EC50 of 19.5 nM via a high-throughput TCF/LEF-reporter assay in SW480 colon cancer cells.
  • HY-135145
    CB-103

    Notch Cancer
    CB-103 is a first-in-class orally active notch signaling pathway inhibitor extracted from patent US9296682B2. CB-103 has anti-tumor activity.
  • HY-N0008
    Orcinol glucoside

    Others Neurological Disease
    Orcinol glucoside (OG) is an active constituent isolated from Rhizoma Curculiginis, with antidepressant effects. Orcinol glucoside facilitates the shift of MSC fate to osteoblast and prevents adipogenesis via Wnt/β-catenin signaling pathway.
  • HY-108439
    Neurodazine

    Wnt Hedgehog Neurological Disease
    Neurodazine is an imidazole-based small molecule, serve as a promoter of neurogenesisin pluripotent cells. Neurodazine promotes neurogenesis by activating Wnt and Shh signaling pathways. Neurodazine selectively suppresses astrocyte differentiation of P19 cells.
  • HY-12681
    CCT251545

    Wnt Cancer
    CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC50 of 5 nM in 7dF3 cells. CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
  • HY-P2272
    NLS-StAx-h

    Wnt β-catenin Cancer
    NLS-StAx-h is a selective, stapled peptide inhibitor of Wnt signaling with an IC50 of 1.4 μM. NLS-StAx-h efficiently inhibits β-catenin-transcription factor interactions. NLS-StAx-h inhibits proliferation and migration of colorectal cancer cells.
  • HY-112799
    DK419

    Wnt β-catenin Cancer
    DK419 is a potent and orally active Wnt/β-catenin signaling inhibitor, with an IC50 of 0.19 μM. DK419 reduces protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin and induces production of pAMPK.
  • HY-124745
    KY-05009

    MAP4K Wnt Apoptosis Cancer
    KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.
  • HY-N2375
    L-Quebrachitol

    Wnt β-catenin Metabolic Disease
    L-Quebrachitol is a natural product isolated from many plants, promotes osteoblastogenesis by uppregulation of BMP-2, runt-related transcription factor-2 (Runx2), MAPK (ERK, JNK, p38α), and Wnt/β-catenin signaling pathway.
  • HY-W010231
    β-Cyclocitral

    Others Others
    β-Cyclocitral, a volatile oxidized derivative of β-carotene, is a grazer defence signal unique to the Cyanobacterium Microcystis. β-Cyclocitral, one of the predominant volatile terpenoid compounds, can upregulate the expression of defence genes to enhance excess light (EL) acclimation. β-Cyclocitral is a powerful repellent.
  • HY-101797
    Veralipride

    (±)-Veralipride; LIR166

    Dopamine Receptor Neurological Disease
    Veralipride is a D2 receptor antagonist. It is an alternative antidopaminergic treatment for menopausal symptoms.
  • HY-12170
    Prinomastat

    AG3340; KB-R9896

    MMP Cancer
    Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity.
  • HY-12170A
    Prinomastat hydrochloride

    AG3340 hydrochloride; KB-R9896 hydrochloride

    MMP Cancer
    Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity.
  • HY-125170
    Galiellalactone

    STAT Cancer
    Galiellalactone is a is a small non-toxic and non-mutagenic fungal metabolite, a selective inhibitor of STAT3 signaling, with an IC50 of 250-500 nM. Galiellalactone can be used to research castration-resistant prostate cancer.
  • HY-P9916
    Sarilumab

    Anti-Human IL6Rα, Human Antibody

    Interleukin Related Inflammation/Immunology
    Sarilumab (Anti-Human IL6Rα, Human Antibody) is a human immunoglobulin G1 monoclonal antibody. Sarilumab, a interleukin-6 (IL-6) receptor antagonist, binds to the IL-6 receptor with high affinity and inhibits cis and trans signaling by IL-6, resulting in reduced inflammation. Sarilumab can be used for the research of Rheumatoid arthritis.
  • HY-P1135
    M1145

    Neuropeptide Y Receptor Neurological Disease
    M1145, a chimeric peptide, is a selective galanin receptor type 2 (GAL2) agonist, with a Ki of 6.55 nM. M1145 shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). M1145 has an additive effect on the signal transduction of galanin.
  • HY-116035
    Nimbolide

    NF-κB CDK Apoptosis Cancer
    Nimbolide is a triterpene derived from the leaves and flowers of neem (Azadirachta indica L). Nimbolide induces apoptosis through inactivation of NF-κB. Nimbolide inhibits CDK4/CDK6 kinase activity. Nimbolide suppresses the NF-κB, Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways.
  • HY-P1135A
    M1145 TFA

    Neuropeptide Y Receptor Neurological Disease
    M1145 TFA, a chimeric peptide, is a selective galanin receptor type 2 (GAL2) agonist, with a Ki of 6.55 nM. M1145 TFA shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). M1145 TFA has an additive effect on the signal transduction of galanin.
  • HY-B1025
    Digoxigenin

    Lanadigenin

    Others Inflammation/Immunology
    Digoxigenin is a hapten, a small molecule with high antigenicity, that is used in many molecular biology applications, as an alternative probe labeling for in situ hybridization
  • HY-15147
    XAV-939

    β-catenin PARP Cancer
    XAV-939 is a potent tankyrase inhibitor that targets Wnt/β-catenin signaling. XAV-939 stabilizes axin by inhibiting tankyrase 1 and tankyrase 2 (IC50s of 5 and 2 nM, respectively), thereby stimulating β-catenin degradation. XAV939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 (Kds of 99 and 93 nM, respectively).
  • HY-N0665
    Specnuezhenide

    (8E)-Nuezhenide

    NF-κB Wnt Inflammation/Immunology
    Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and wnt/β-catenin signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA).
  • HY-15721
    FH535

    PPAR Wnt β-catenin Cancer
    FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities.
  • HY-103705
    iCRT3

    Wnt Apoptosis Cancer
    iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription.
  • HY-12879
    IWP-4

    Wnt Cancer
    IWP-4 is a small molecule Wnt inhibitor with an IC50 of 25 nM.
  • HY-117930
    Danicopan

    ACH-4471

    Complement System Inflammation/Immunology
    Danicopan (ACH-4471), a selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with Kd value of 0.54 nM. Danicopan (ACH-4471) inhibits alternative pathway of complement (APC) activity, has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS).
  • HY-N0054
    Osthole

    Osthol; Ostol; NSC 31868

    Histamine Receptor Apoptosis Parasite HBV Cancer Infection Endocrinology Inflammation/Immunology Cardiovascular Disease
    Osthole is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity. Osthole also suppresses the secretion of HBV in cells.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-B0911
    Sodium copper chlorophyllin A

    Others Cancer
    Sodium copper chlorophyllin A is a semi-synthetic mixture of water-soluble sodium copper salts derived from chlorophyll, primarily used as a food additive and in alternative medicine.
  • HY-N7378A
    N-Hydroxypipecolic acid potassium

    1-Hydroxy-2-piperidinecarboxylic acid potassium; NHP potassium

    Others Inflammation/Immunology
    N-Hydroxypipecolic acid potassium (1-Hydroxy-2-piperidinecarboxylic acid potassium), a plant metabolite and a systemic acquired resistance (SAR) regulator, orchestrates SAR establishment in concert with the immune signal salicylic acid. N-Hydroxypipecolic acid potassium accumulates systemically in the plant foliage in response to pathogen attack. N-Hydroxypipecolic acid potassium induces SAR to bacterial and oomycete infection.
  • HY-N7378
    N-Hydroxypipecolic acid

    1-Hydroxy-2-piperidinecarboxylic acid; NHP

    Others Inflammation/Immunology
    N-Hydroxypipecolic acid (1-Hydroxy-2-piperidinecarboxylic acid), a plant metabolite and a systemic acquired resistance (SAR) regulator, orchestrates SAR establishment in concert with the immune signal salicylic acid. N-Hydroxypipecolic acid accumulates systemically in the plant foliage in response to pathogen attack. N-Hydroxypipecolic acid induces SAR to bacterial and oomycete infection.
  • HY-131009
    Fluorescein-NAD+

    PARP Others
    Fluorescein-NAD+ is an alternative to radiolabeled NAD and a substrate for ADP-ribosylation. Fluorescein-NAD+ can be used in PARP assays by fluorescence microscopy. Extinction Coefficient: 262 nm.
  • HY-112055
    DIM-C-pPhOH

    Apoptosis Cancer
    DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively.
  • HY-101090
    KYA1797K

    Wnt β-catenin Cancer
    KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC50 of 0.75 µM.
  • HY-A0241
    Dalfopristin

    RP54476

    Bacterial Antibiotic Infection
    Dalfopristin is a semi-synthetic streptogramin antibiotic. Quinupristin/Dalfopristin (Q/D) is a valuable alternative antibiotic to vancomycin for the treatment of multi-drug resistant Enterococcus faecium infections.
  • HY-135717
    Norbiotinamine

    Others Cancer
    Norbiotinamine is an alternative to biotin. Norbiotinamine can be coupled with a carboxylic group of amino acids to give inverse peptides, having the amide linkage oriented in the opposite direction.
  • HY-135717A
    Norbiotinamine hydrochloride

    Others Cancer
    Norbiotinamine hydrochloride is an alternative to biotin. Norbiotinamine can be coupled with a carboxylic group of amino acids to give inverse peptides, having the amide linkage oriented in the opposite direction.
  • HY-10590
    TWS119

    GSK-3 Autophagy Neurological Disease Cancer
    TWS119 is a specific inhibitor of GSK-3β, with an IC50 of 30 nM, and activates the wnt/β-catenin pathway.
  • HY-100853
    IWP-O1

    Porcupine Wnt Cancer
    IWP-O1 is a highly potent Porcupine (Porcn) inhibitor, with an EC50 of 80 pM in L-Wnt-STF cells. IWP-O1 prevents the secretion of Wnt proteins. IWP-O1 suppresses the phosphorylation of Dvl2/3 and LRP6 in HeLa cells.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-126666
    PNU-159682 carboxylic acid

    ADC Cytotoxin Cancer Inflammation/Immunology
    PNU-159682 carboxylic acid (compound 53) is a potent ADCs cytotoxin and encodes a member of the C-type lectin/C-type lectin-like domain (CTL/CTLD) superfamily. PNU-159682 carboxylic acid has protein fold and diverse functions, such as cell adhesion, cell-cell signalling, glycoprotein turnover, and roles in inflammation and immune response.
  • HY-101130
    PNU-74654

    Wnt β-catenin Apoptosis Cancer
    PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.
  • HY-N0322
    Cholesterol

    Estrogen Receptor/ERR Endogenous Metabolite Metabolic Disease
    Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
  • HY-N0400
    Wogonin

    CDK Wnt Autophagy Apoptosis Cancer Inflammation/Immunology
    Wogonin is a naturally occurring mono-flavonoid, can inhibit the activity of CDK8 and Wnt, and exhibits anti-inflammatory and anti-tumor effects.
  • HY-136351
    THZ-P1-2

    Autophagy Cancer
    THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.
  • HY-10182B
    CHIR-99021 trihydrochloride

    CT99021 trihydrochloride

    GSK-3 Wnt β-catenin Autophagy Cancer
    CHIR-99021 trihydrochloride (CT99021 trihydrochloride) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 trihydrochloride enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 trihydrochloride induces autophagy.
  • HY-10182
    CHIR-99021

    CT99021

    GSK-3 Wnt β-catenin Autophagy Cancer
    CHIR-99021 (CT99021) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 induces autophagy.
  • HY-13912
    IWP-2

    Wnt Casein Kinase Cancer
    IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ.
  • HY-16665
    iCRT 14

    Wnt Cancer
    iCRT 14 is a novel potent inhibitor of β-catenin-responsive transcription (CRT), with IC50 of 40.3 nM against Wnt responsive STF16 luciferase.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-109079A
    Abeprazan hydrochloride

    DWP14012 hydrochloride

    Proton Pump Metabolic Disease
    Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases.
  • HY-109079
    Abeprazan

    DWP14012

    Proton Pump Metabolic Disease
    Abeprazan (DWP14012) is a potassium-competitive acid blocker. Abeprazan inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases.
  • HY-N2523
    Gigantol

    Wnt Cancer
    Gigantol is a bibenzyl compound derived from several medicinal orchids. Giganto shows promising therapeutic potential against cancer cells. Gigantol is a novel inhibitor of the Wnt/β-catenin pathway.
  • HY-102028
    KY1220

    Wnt β-catenin Cancer
    KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.
  • HY-126395
    Patent Blue V calcium salt

    Others Others
    Patent Blue V has been widely used in sentinel lymph node mapping. Patent Blue V is also a food coloring agent and an alternative dye for trypan blue (TB) in descemet membrane endothelial keratoplasty (DMEK).
  • HY-75342
    Methyl vanillate

    Wnt Reactive Oxygen Species Endogenous Metabolite Inflammation/Immunology Cancer
    Methyl vanillate, one of the ingredients in Hovenia dulcis Thunb, is a Wnt/β-catenin pathway activator. A benzoate ester that is the methyl ester of vanillic acid. It has a role as an antioxidant and a plant metabolite.
  • HY-10593
    IQ 1

    Wnt Cancer
    IQ 1 has many functions such as decreasing Wnt-stimulated phosphorylation, maintaining the pluripotency of murine ESCs, preventing PP2A/Nkd interaction and so on.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-101085
    SKL2001

    Wnt β-catenin Cancer
    SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction.
  • HY-10182A
    CHIR-99021 monohydrochloride

    CT99021 monohydrochloride

    GSK-3 Wnt β-catenin Autophagy Cancer
    CHIR-99021 monohydrochloride (CT99021 monohydrochloride) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 monohydrochloride enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 monohydrochloride induces autophagy.
  • HY-W040270
    Amino-PEG10-amine

    PROTAC Linker Cancer
    Amino-PEG10-amine, a PEG-based PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-130411
    Amino-PEG11-amine

    PROTAC Linker Cancer
    Amino-PEG11-amine, a PEG-based (12 units) PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer.
  • HY-117163
    FzM1.8

    Wnt β-catenin Cancer
    FzM1.8 derives from FzM1, is an allosteric agonist of FZD4 with pEC50 of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K.
  • HY-128693
    BpV(HOpic)

    PTEN Cancer Neurological Disease
    BpV(HOpic) is a potent and selective inhibitor of PTEN with an IC50 of 14 nM. Nanocarrier-BpV(HOpic) has neuroprotective activity.
  • HY-P2316
    Epinecidin-1 TFA

    Bacterial Antibiotic Infection
    Epinecidin-1 TFA is a multi-functional antimicrobial peptide (AMP) from Orange-spotted grouper (Epinephelus coioides). Epinecidin-1 TFA has antibacterial, antifungal, antiviral, anti-tumor, and immunomodulatory effects. Epinecidin-1 TFA has the potential to be an alternative for current antibiotics.
  • HY-122700
    Factor D inhibitor 6

    Complement System Inflammation/Immunology
    Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.
  • HY-112331
    SJ000291942

    TGF-β Receptor Cancer
    SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-129851
    NTP42

    Prostaglandin Receptor Cardiovascular Disease
    NTP42 is a thromboxane A2 (TXA2) receptor antagonist with an IC50 of 3.278 nM for antagonizing T prostanoid receptor (TP)- mediated [Ca 2+] mobilization following stimulation of cells with the alternative TP agonist U46609. NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH).
  • HY-B0389A
    D-Glucose-13C6

    Glucose-13C6

    Endogenous Metabolite Metabolic Disease
    D-Glucose-13C6 is a tracer used to trace glucose-related synthetic catabolism, is a low-cost alternative with the significant advantage that the sixth isotope of natural glucose has virtually zero natural abundance, which facilitates isotopomer analysis with <1% labeled glucose in the infusate.
  • HY-10858
    WAY 316606

    sFRP-1 Cancer
    WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM.
  • HY-N0224
    Epigoitrin

    Influenza Virus Infection Cancer
    Epigoitrin is a natural alkaloid from Isatis indigotica, with antiviral activities. Epigoitrin reduces susceptibility to influenza virus via mitochondrial antiviral signaling.
  • HY-125658
    Biotinyl tyramide

    Others Others
    Biotinyl tyramide is a biotin derivative used for tyramide signal amplification (TSA), as a reagent to amplify both immunohistochemical signals and in situ hybridization protocols.
  • HY-N2149A
    Tomatidine hydrochloride

    NF-κB JNK Autophagy Inflammation/Immunology Cardiovascular Disease
    Tomatidine hydrochloride acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling. Tomatidine hydrochloride activates autophagy either in mammal cells or C elegans.
  • HY-N2149
    Tomatidine

    NF-κB JNK Autophagy Inflammation/Immunology Cardiovascular Disease
    Tomatidine acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling. Tomatidine activates autophagy either in mammal cells or C elegans.
  • HY-121418
    Lusianthridin

    c-Myc Cancer
    Lusianthridin, a pure compound from Dendrobium venustum, have an anti-migratory effect. Lusianthridin enhances c-Myc degradation through the inhibition of Src-STAT3 signaling.
  • HY-119751
    Hematein

    Casein Kinase Akt Wnt Apoptosis Cancer
    Hematein is a oxidation product of hematoxylin acted as a dye. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells.
  • HY-128570
    FD-IN-1

    Complement System Inflammation/Immunology
    FD-IN-1 (Compound 12) is a factor D (FD) inhibitor with an IC50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5µM, respectively.
  • HY-106410A
    Zabofloxacin hydrochloride

    DW-224a

    Bacterial Topoisomerase Infection
    Zabofloxacin hydrochloride (DW-224a) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin hydrochloride has excellent activity against gram-positive pathogens including Steptococcus aureusStreptococcus pyogenes and S.pneumonia. Zabofloxacin hydrochloride is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
  • HY-N4127
    3'-Demethylnobiletin

    Others Cancer
    3'-Demethylnobiletin, a derivative of Nobiletin, is a polymethoxyflavonoid in citrus fruits. Nobiletin exhibits anticancer activity and inhibits tumor angiogenesis by regulating Src, FAK, and STAT3 signaling.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-106410
    Zabofloxacin

    DW-224a Free base

    Bacterial Topoisomerase Infection
    Zabofloxacin (DW-224a Free base) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin has excellent activity against gram-positive pathogens including Steptococcus aureusStreptococcus pyogenes and S.pneumonia. Zabofloxacin is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
  • HY-70075
    CCG-63808

    RGS Protein Cancer
    CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins.
  • HY-10917
    GW2580

    c-Fms Inflammation/Immunology Cancer
    GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.
  • HY-128590
    PHT-7.3

    Ras Cancer
    PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain, which inhibits mut-KRas, but not wild-type KRas cancer cell and tumor growth and signaling.
  • HY-100602
    HJC0152 hydrochloride

    STAT Apoptosis Cancer
    HJC0152 hydrochloride is a signal transducers and activators of transcription 3 (STAT3) inhibitor.
  • HY-12848B
    SAG hydrochloride

    Smo Cancer
    SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM.
  • HY-15860
    FLI-06

    Notch Cancer
    FLI-06 is an inhibitor of Notch signaling with an EC50 of 2.3 μM.
  • HY-N1513
    Ganoderic acid H

    Others Cancer
    Ganoderic acid H is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderic acid H suppresses growth and invasive behavior of breast cancer cells through the inhibition of transcription factors AP-1 and NF-kappaB signaling.
  • HY-114495
    Caerulomycin A

    Cerulomycin; Caerulomycin

    Fungal Antibiotic Infection Inflammation/Immunology
    Caerulomycin A (Cerulomycin; Caerulomycin), an antifungal compound, induces generation of T cells, enhances TGF-β-Smad3 protein signaling via suppressing interferon-γ-induced STAT1 signaling. Antifungal and antibiotic activity, and used in autoimmune diseases.
  • HY-12848
    SAG

    Smo Cancer
    SAG is a potent Smo receptor agonist which activates the Hedgehog signaling pathway with a Kd of 59 nM.
  • HY-A0181
    Adenosine monophosphate

    AMP

    Endogenous Metabolite Others
    Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-136145
    FIDAS-3

    Wnt Cancer
    FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A). FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-3 has anticancer activities.
  • HY-P1192
    GR-73632

    Neurokinin Receptor Neurological Disease Endocrinology
    GR-73632 is a novel tachykinin neurokinin 1 (NK-1) receptor agonist. GR-73632 acts directly on the peripheral terminals of primary sensory neurons through NK1 receptor which convey itch signals.
  • HY-N2491
    Deoxyelephantopin

    NF-κB Cancer
    Deoxyelephantopin, a natural bioactive sesquiterpene lactone from Elephantopus scaber, has shown promising anticancer effects against a broad spectrum of cancers. Deoxyelephantopin inhibits NF-κB, MAPK, PI3K/Akt, and β-catenin signaling.
  • HY-100831
    YM-58483

    BTP2

    CRAC Channel Inflammation/Immunology
    YM-58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca 2+ signals.
  • HY-N6577
    Astragaloside VI

    EGFR Inflammation/Immunology Neurological Disease
    Astragaloside VI could activate EGFR/ERK signalling pathway to improve wound healing.
  • HY-16587
    Saridegib

    IPI-926; Patidegib

    Smo Cancer
    Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway.
  • HY-N0837
    Veratramine

    NSC17821; NSC23880

    Others Cancer
    Veratramine(NSC17821; NSC23880) is useful as a signal transduction inhibitor for treating tumors.
  • HY-100492
    Fisogatinib

    BLU-554

    FGFR Cancer
    Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 5 nM. Fisogatinib has significant anti-tumor activity in models of hepatocellular carcinoma (HCC) that are dependent on FGFR4 signalling.
  • HY-130254
    Src Inhibitor 3

    Src Cancer Inflammation/Immunology
    Src Inhibitor 3 is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. Src Inhibitor 3 shows the ability to increase T cell proliferation induced by T cell receptor signaling.
  • HY-19726
    NSC59984

    MDM-2/p53 Cancer
    NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway. NSC59984 acts by targeting GOF-mutant p53 and stimulates p73 to restore the p53 pathway signaling.
  • HY-101098
    PD-1-IN-18

    PD-1/PD-L1 Inflammation/Immunology
    PD-1-IN-18 is a PD1 signaling pathway inhibitor, which acts as an immunomodulator.
  • HY-N1447
    Ganoderic acid A

    Apoptosis Autophagy Endogenous Metabolite Cancer
    Ganoderic acid A can inhibit of the JAK-STAT3 signaling pathway, also inhibit proliferation, viability, ROS.
  • HY-N1486
    Ursonic acid

    3-Ketoursolic acid

    Apoptosis Endogenous Metabolite Cancer
    Ursolic acid, a naturally occurring triterpenoid, induces the apoptosis of human cancer cells through multiple signaling pathways.
  • HY-70074
    CCG-63802

    RGS Protein Cancer
    CCG-63802 is a reversible inhibitor of regulator of G-protein signaling (RGS) protein; with greatest potency at RGS4.
  • HY-N0371
    Pachymic acid

    3-O-Acetyltumulosic acid

    Akt ERK Cancer
    Pachymic acid is a lanostrane-type triterpenoid from P. cocos. Pachymic acid inhibits Akt and ERK signaling pathways.
  • HY-126741
    Azadirachtin

    Apoptosis Others
    Azadirachtin, one of the most promising botanical insecticides, is widely used for pest control. Azadirachtin induces apoptosis in insect cell lines, including Sf9, SL-1 and BTI-Tn-5B1-4.
  • HY-13007A
    PF-3758309 hydrochloride

    PAK Apoptosis Cancer
    PF-3758309 hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-123952
    RTC-5

    EGFR Cancer
    RTC-5 is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling.
  • HY-126248
    Tankyrase-IN-2

    PARP Cancer
    Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model.
  • HY-123940
    SGC-AAK1-1

    Wnt Cancer
    SGC-AAK1-1, a chemical probe, is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor with an IC50 of 270 nM and a Ki of 9 nM. SGC-AAK1-1 also potently inhibits BMP2K. SGC-AAK1-1 is used to study Wnt pathway related to AAK1.
  • HY-10982
    Amonafide

    AS1413

    Topoisomerase Cancer
    Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA.
  • HY-N0138
    Theobromine

    3,7-Dimethylxanthine

    Adenosine Receptor Endogenous Metabolite Neurological Disease
    Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
  • HY-100347A
    SRI-011381 hydrochloride

    TGF-beta/Smad Neurological Disease
    SRI-011381 hydrochloride is an oral bioavailabile TGF-beta signaling agonist, exhibits neuroprotective effect.
  • HY-W015346
    Desaminotyrosine

    3-(4-Hydroxyphenyl)propionic acid

    Influenza Virus Endogenous Metabolite Infection
    Desaminotyrosine is a microbially associated metabolite protecting from influenza through augmentation of type I interferon signaling.
  • HY-100790
    Ciliobrevin A

    HPI-4

    Hedgehog Cancer
    Ciliobrevin A is a hedgehog (Hh) signaling pathway inhibitor with median inhibitory concentration (IC50) less than 10 μM.
  • HY-19566
    NQDI-1

    MAP3K Apoptosis Cancer
    NQDI-1 inhibits apoptosis signal-regulating kinase 1 (ASK1) with a Ki of 500 nM and an IC50 of 3 μM.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-16125
    Carboxyamidotriazole Orotate

    L-651582 Orotate; CAI Orotate

    Calcium Channel Cancer Inflammation/Immunology
    Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects.
  • HY-N2450
    Sulforaphene

    Apoptosis EGFR ERK NF-κB Cancer
    Sulforaphene, isolated from radish seeds, exhibits an ED50 against velvetleaf seedlings approximately 2 x 10 -4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1/2, NF‐κB and other signals.
  • HY-133028
    CKI-7 free base

    Casein Kinase CDK SGK Ribosomal S6 Kinase (RSK) Cancer
    CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases.
  • HY-N0486
    L-Leucine

    mTOR Metabolic Disease
    L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway.
  • HY-135905
    CL264

    Toll-like Receptor (TLR) Inflammation/Immunology
    CL264 is a TLR7-specific agonist for innate immune signals research.
  • HY-N6843
    Arnicolide D

    Caspase PI3K Akt mTOR STAT Cancer
    Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner.
  • HY-N1913
    Danshensu

    Dan shen suan A; Salvianic acid A

    Keap1-Nrf2 Autophagy Apoptosis Cardiovascular Disease Cancer
    Danshensu, an active ingredient of Salvia miltiorrhiza, shows wide cardiovascular benefit by activating Nrf2 signaling pathway.
  • HY-15735
    c-Met inhibitor 1

    c-Met/HGFR Cancer
    c-Met inhibitor 1 is an inhibitor of the c-Met receptor signaling pathway useful for the treatment of cancer including gastric, glioblastoma, and pancreatic cancer.
  • HY-106420
    16,16-Dimethyl prostaglandin E2

    16,16-dimethyl PGE2

    Prostaglandin Receptor Inflammation/Immunology
    16,16-Dimethyl prostaglandin E2 (16,16-dimethyl PGE2) is an orally active vertebrate Hematopoietic stem cells (HSCs) homeostasis critical regulator. 16,16-Dimethyl prostaglandin E2 can act through EP2/EP4 and has an interaction with the Wnt pathway.
  • HY-N6796
    Manumycin A

    Farnesyl Transferase Ras Apoptosis Cancer Infection
    Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (Ki =1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity . Manumycin A suppresses exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling.
  • HY-N0047
    Polyphyllin I

    JNK mTOR Akt PDK-1 Autophagy Apoptosis Cancer
    Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis.
  • HY-N7030
    5,7,3',4'-Tetramethoxyflavone

    Others Infection
    5,7,3',4'-Tetramethoxyflavone, one of the major polymethoxyflavones (PMFs) isolated from M. exotica, possesses various bioactivities, including anti-fungal, anti-malarial, anti-mycobacterial, and anti-inflammatory activities. 5,7,3',4'-Tetramethoxyflavone exhibits chondroprotective activity by targeting β-catenin signaling.
  • HY-N0628
    Kaempferitrin

    Lespedin; Lespenephryl

    Insulin Receptor Cancer Metabolic Disease Endocrinology
    Kaempferitrin is a natural flavonoid, possesses antinociceptive, anti-inflammatory, anti-diabetic, antitumoral and chemopreventive effects, and activates insulin signaling pathway.
  • HY-111360
    SPL-707

    Others Inflammation/Immunology
    SPL-707 is a potent, selective and orally available signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 80 nM.
  • HY-P0250
    Kassinin

    Neurokinin Receptor Neurological Disease Endocrinology
    Kassinin is a peptide derived from the Kassina frog. It belongs to tachykinin family of neuropeptides. It is secreted as a defense response, and is involved in neuropeptide signalling.
  • HY-128588
    STAT3-IN-3

    STAT Cancer
    STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3).
  • HY-12524
    Bikinin

    Abrasin

    GSK-3 Others
    Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3/Shaggy-like kinases and activates BR (brassinosteroids) signaling.
  • HY-N0637
    Eriodictyol

    Huazhongilexone

    Endogenous Metabolite Keap1-Nrf2 Inflammation/Immunology
    Eriodictyol is a flavonoid isolated from the Chinese herb, with antioxidant and anti-inflammatory activity. Eriodictyol induces Nrf2 signaling pathway.
  • HY-13018
    MRT67307

    IKK ULK Autophagy Cancer Inflammation/Immunology
    MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells.
  • HY-135892
    GNE-1858

    Others Inflammation/Immunology
    GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively.
  • HY-13018A
    MRT67307 hydrochloride

    IKK ULK Autophagy Cancer Inflammation/Immunology
    MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells.
  • HY-135985
    DCLK1-IN-1

    Others Cancer
    DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1 + pancreatic ductal adenocarcinoma (PDAC).
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-17397
    Strontium Ranelate

    Distrontium renelate; S12911

    CaSR Metabolic Disease
    Strontium Ranelate (S12911) is an antiosteoporotic agent that acts by reducing bone resorption and promoting bone formation, thereby inducing a positive bone balance. Strontium Ranelate also can activate the calcium-sensing receptor (CaSR) in non skeletal cells, resulting in the activation of inositol 1, 4, 5-triphosphate production and mitogen-activated protein kinase signaling.
  • HY-18287
    MRT-83

    Smo Cancer
    MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.
  • HY-N7452
    Coumermycin A1

    Bacterial Metabolic Disease
    Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.
  • HY-13288
    Org 27569

    Cannabinoid Receptor Neurological Disease
    Org 27569 is a potent CB1 receptor allosteric modulator, which increases agonist binding, yet blocks agonist-induced CB1 signaling.
  • HY-119720
    Neocryptotanshinone

    NF-κB NO Synthase Inflammation/Immunology
    Neocryptotanshinone, a fatty diterpenoids from Salvia Miltiorrhiza, inhibits lipopolysaccharide-induced inflammation by suppression of NF-κB and iNOS signaling pathways.
  • HY-B0837
    Emamectin Benzoate

    MK-244

    GABA Receptor Infection
    Emamectin Benzoate (MK-244) works as a chloride channel activator by binding gamma aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods.
  • HY-N0148A
    Rutin hydrate

    Rutoside hydrate; Quercetin 3-O-rutinoside hydrate

    JNK ERK mTOR Neurological Disease
    Rutin hydrate is a flavonol glycoside, able to cross the blood-brain barrier, and acts by inhibiting JNK and ERK1/2 activation and activating mTOR signalling.
  • HY-P1111
    Lyn peptide inhibitor

    Src Interleukin Related Inflammation/Immunology
    Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of  asthma, allergic, and other eosinophilic disorders.
  • HY-108742A
    Abaloparatide TFA

    BA 058 TFA; BIM 44058 TFA

    Thyroid Hormone Receptor Metabolic Disease Endocrinology
    Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue selected to be a potent and selective activator of the PTHR1 signaling pathway. Abaloparatide TFA enhances Gs/cAMP signaling (EC50 of 0.3 nM) and β-arrestin recruitment (EC50 of 0.9 nM) in MC3T3-E1 osteoblast cells.
  • HY-12695B
    Guanosine 5'-triphosphate trisodium salt hydrate

    5'-GTP trisodium salt hydrate

    Others Others
    5'-GTP trisodium salt hydrate is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.
  • HY-N2312
    Mogrol

    ERK STAT Cancer
    Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.
  • HY-U00431
    CCG 203769

    RGS Protein Neurological Disease
    CCG 203769 is a selective G protein signaling (RGS4) inhibitor, which blocks the RGS4-Gαo protein-protein interaction in vitro with an IC50 of 17 nM.
  • HY-N6940
    Prosapogenin A

    Progenin III

    Apoptosis Cancer
    Prosapogenin A, a natural product from Veratrum, induces apoptosis in human cancer cells in vitro via inhibition of the STAT3 signaling pathway and glycolysis.
  • HY-15872
    FTI-277

    Farnesyl Transferase Cancer
    FTI-277 is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.
  • HY-136390
    ML417

    Dopamine Receptor Neurological Disease
    ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons.
  • HY-121410
    Narasin

    Bacterial Parasite NF-κB Antibiotic Cancer Infection
    Narasin is a cationic ionophore and coccidiostat agent. Narasin inhibits NF-κB signaling and induces tumor cells apoptosis. Narasin has antimicrobial and anticancer activity.
  • HY-W011151
    trans-Zeatinriboside

    Others Others
    trans-Zeatinriboside is a type of cytokinin precursor, acts as a major long-distance signalling form in xylem vessels, regulates leaf size and meristem activity-related traits.
  • HY-W013093
    Uridine triphosphate trisodium salt

    UTP trisodium salt; Uridine 5'-triphosphate trisodium salt

    Others Cancer Inflammation/Immunology Cardiovascular Disease
    Uridine triphosphate trisodium salt is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
  • HY-16642A
    LY2828360

    Cannabinoid Receptor Neurological Disease
    LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
  • HY-N0436
    Engeletin

    NF-κB Infection Inflammation/Immunology
    Engeletin is a flavanonol glycoside isolated from hymenaea martiana, inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.
  • HY-U00002
    ZD-4190

    VEGFR EGFR Cancer
    ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.
  • HY-109010
    Poseltinib

    HM71224; LY3337641

    Btk BMX Kinase Toll-like Receptor (TLR) Metabolic Disease
    Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling.
  • HY-N2959
    Brevilin A

    JAK STAT Apoptosis Autophagy Cancer
    Brevilin A is a sesquiterpene lactone isolated from Centipeda minima with anti-tumor activity. Brevilin A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 µM) in Cancer Cells. Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K/AKT/mTOR inactivation in colon adenocarcinoma cell CT26.
  • HY-113038
    D-α-Hydroxyglutaric acid

    (R)-2-Hydroxypentanedioic acid

    Reactive Oxygen Species ATP Synthase mTOR Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    D-α-Hydroxyglutaric acid ((R)-2-Hydroxypentanedioic acid) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling.
  • HY-P1111A
    Lyn peptide inhibitor TFA

    Src Interleukin Related Inflammation/Immunology
    Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of  asthma, allergic, and other eosinophilic disorders.
  • HY-N1469
    Kaurenoic acid

    Others Inflammation/Immunology Neurological Disease
    Kaurenoic acid is a diterpene from Sphagneticola trilobata, inhibits Inflammatory Pain by the inhibition of cytokine production and activation of the NO–cyclic GMP–PKG–ATP-sensitive potassium channel signaling pathway.
  • HY-N0298
    Stachydrine

    NF-κB Endogenous Metabolite Cardiovascular Disease Cancer
    Stachydrine is a major constituent of Chinese herb leonurus heterophyllus sweet used to promote blood circulation and dispel blood stasis. Stachydrine can inhibit the NF-κB signal pathway.
  • HY-N0177
    Diosgenin

    STAT Metabolic Disease
    Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway. Diosgenin is an exogenous activator of Pdia3/ERp57.
  • HY-104031
    tCFA15

    Notch Neurological Disease
    tCFA15 is a trimethyl cyclohexenonic long chain fatty alcohol containing 15 carbon atoms on the side chain, promotes the differentiation of neurons, and may regulates Notch signaling.
  • HY-103640
    WR-1065 dihydrochloride

    MDM-2/p53 Cancer
    WR-1065 dihydrochloride can protect normal tissues from the toxic effects of certain cancer drugs and activate p53 through a JNK-dependent signaling pathway.
  • HY-100844
    GS-444217

    MAP3K Apoptosis Cancer
    GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM.
  • HY-W012078
    5-Methyl-2'-deoxycytidine

    5-Methyldeoxycytidine

    DNA Methyltransferase Endogenous Metabolite Others
    5-Methyl-2'-deoxycytidine in single-stranded DNA can act in cis to signal de novo DNA methylation.
  • HY-127105A
    LNP023 hydrochloride

    Complement System Metabolic Disease Inflammation/Immunology
    LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. LNP023 inhibits factor B with an IC50 value of 10 nM.
  • HY-127105
    LNP023

    Complement System Metabolic Disease Inflammation/Immunology
    LNP023 is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. LNP023 inhibits factor B with an IC50 value of 10 nM.
  • HY-15893
    DMOG

    Dimethyloxallyl Glycine

    HIF/HIF Prolyl-Hydroxylase Autophagy Cancer
    DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy.
  • HY-100848
    TX1-85-1

    EGFR Cancer
    TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.
  • HY-N0498
    Nitidine chloride

    Parasite Apoptosis STAT Topoisomerase ERK FAK p38 MAPK NF-κB Cancer Inflammation/Immunology
    Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.
  • HY-N2083
    Handelin

    Others Inflammation/Immunology
    Handelin is a guaianolide dimer from Chrysanthemum boreale that has potent anti-inflammatory activity by down-regulating NF-κB signaling and pro-inflammatory cytokine production.
  • HY-128356
    SPL-410

    Others Inflammation/Immunology
    SPL-410 is an orally active, highly potent and selective hydroxyethylamine based SPPL2a (Signal Peptide Peptidase Like 2a) inhibitor, with an IC50 of 9 nM.
  • HY-12212
    Omaveloxolone

    RTA 408

    Keap1-Nrf2 STING Apoptosis Cancer Inflammation/Immunology
    Omaveloxolone (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling.
  • HY-107372
    Uridine triphosphate

    UTP; Uridine 5'-triphosphate

    Endogenous Metabolite Cancer Inflammation/Immunology Cardiovascular Disease
    Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
  • HY-N0112
    Dihydromyricetin

    Ampelopsin; Ampeloptin

    mTOR Autophagy Cancer
    Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2).
  • HY-N1382
    Asperuloside

    NO Synthase Inflammation/Immunology
    Asperuloside is an iridoid isolated from Hedyotis diffusa, with anti-inflammatory activity. Asperuloside inhibits inducible nitric oxide synthase (iNOS), suppresses NF-κB and MAPK signaling pathways.
  • HY-N0751
    Scutellarin

    STAT Akt HIV Cancer Infection
    Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively.
  • HY-100542
    D-α-Hydroxyglutaric acid disodium

    Disodium (R)-2-hydroxyglutarate

    Reactive Oxygen Species ATP Synthase mTOR Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling.
  • HY-50859
    Ruxolitinib sulfate

    INCB018424 sulfate

    JAK Autophagy Cancer
    Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
  • HY-131181
    LEI-401

    Phospholipase Neurological Disease
    LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice.
  • HY-N6017
    Bakkenolide A

    Others Cancer
    Bakkenolide A is a natural product extracted from Petasites tricholobus. Bakkenolide A inhibits leukemia by regulation of HDAC3 and PI3K/Akt-related signaling pathways.
  • HY-103316
    trans-Ned 19

    Calcium Channel Cardiovascular Disease
    trans-Ned 19, a NAADP antagonist and TPC blocker, suppresses the calcium signal in human umbilical vein endothelial cells (HUVEC) and the rat aorta relaxation in response to low histamine concentrations.
  • HY-N6651
    Isocryptotanshinone

    STAT Phosphatase Cancer
    Isocryptotanshinone is a potent signal transducer and activator of transcription 3 (STAT3) and protein tyrosine phosphatase 1B PTP1B inhibitor, with an IC50 of 56.1 μM for PTP1B.
  • HY-103473A
    Boc-MLF TFA

    Boc-Met-Leu-Phe-OH (TFA)

    Others Inflammation/Immunology
    Boc-MLF (TFA) is a peptide, used as a specific formyl peptide receptor (FPR) antagonist, also inhibits the signaling through formyl peptide receptor like 1 (FPRL1) at higher concentrations.
  • HY-18938
    Selonsertib

    GS-4997

    MAP3K Apoptosis Cancer
    Selonsertib, an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.
  • HY-113204
    N-Oleoyl glycine

    Endogenous Metabolite Cannabinoid Receptor Akt Metabolic Disease
    N-Oleoyl glycine is a lipoamino acid, which stimulates adipogenesis associated with activation of CB1 receptor and Akt signaling pathway in 3T3-L1 adipocyte.
  • HY-N6812
    Karacoline

    Others Endocrinology
    Karacoline, a diterpene alkaloid found in the plant Aconitum kusnezoffii, reduces degradation of the extracellular matrix (ECM) in intervertebral disc degeneration (IDD) via the NF-κB signaling pathway.
  • HY-P1868
    α2β1 Integrin Ligand Peptide

    Integrin Infection
    α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
  • HY-P1868A
    α2β1 Integrin Ligand Peptide TFA

    Integrin Others
    α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
  • HY-N6673
    Okanin

    Toll-like Receptor (TLR) NF-κB Inflammation/Immunology Neurological Disease Cardiovascular Disease
    Okanin, effective constituent of the flower tea Coreopsis tinctoria, attenuates LPS-induced microglial activation through inhibition of the TLR4/NF-κB signaling pathways.
  • HY-16126
    Carboxyamidotriazole

    L-651582; CAI

    Calcium Channel Cancer Inflammation/Immunology
    Carboxyamidotriazole (L-651582) is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole shows anti-tumor, anti-inflammatory and antiangiogenic effects.
  • HY-128854
    Dimethyl biphenyl-4,4'-dicarboxylate

    Others Metabolic Disease
    Dimethyl biphenyl-4,4'-dicarboxylate (Biphenyl dimethyl dicarboxylate) is a hepatoprotectant obtained from Schizandra fructus and may induce a signal transduction similar to that associated with IFN.
  • HY-N0738
    Stachydrine hydrochloride

    NF-κB Cardiovascular Disease Cancer
    Stachydrine hydrochloride is the major active constituent of Herba Leonuri, which is a potential therapy for cardiovascular diseases. Stachydrine can inhibit the NF-κB signal pathway. Anti-hypertrophic activities.
  • HY-N4176
    Ginkgolide K

    Autophagy Neurological Disease
    Ginkgolide K, isolated from Ginkgo biloba, induces protective autophagy through the AMPK/mTOR/ULK1 signaling pathway. Ginkgolide K possesses neuroprotective activity.
  • HY-N0635
    Prim-O-glucosylcimifugin

    NO Synthase COX Inflammation/Immunology
    Prim-O-glucosylcimifugin exerts anti-inflammatory effects through the inhibition of iNOS and COX-2 expression by through regulating JAK2/STAT3 signaling.
  • HY-16962A
    CC-115 hydrochloride

    DNA-PK mTOR Cancer
    CC-115 hydrochloride is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
  • HY-16962
    CC-115

    DNA-PK mTOR Cancer
    CC-115 is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
  • HY-112108
    Chitosan oligosaccharide

    COS

    AMPK Cancer Metabolic Disease
    Chitosan oligosaccharide (COS) is an oligomer of β-(1→4)-linked D-glucosamine. Chitosan oligosaccharide (COS) activates AMPK and inhibits inflammatory signaling pathways including NF-κB and MAPK pathways.
  • HY-13735A
    Quinacrine dihydrochloride

    Mepacrine dihydrochloride; SN-390 dihydrochloride

    Parasite Apoptosis Autophagy Mitophagy Cancer Infection
    Quinacrine dihydrochloride (Mepacrine dihydrochloride) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis.
  • HY-12695
    Guanosine 5'-triphosphate trisodium salt

    5'-GTP trisodium salt

    Endogenous Metabolite Others
    Guanosine 5'-triphosphate trisodium salt (5'-GTP trisodium salt) is an activator of the signal transducing G proteins which are involved in various cellular processes including proliferation, differentiation, and activation of several intracellular kinase cascades.
  • HY-114456B
    Ganglioside GM3 sodium salt

    Others Cancer Metabolic Disease
    Ganglioside GM3 sodium salt is a sialylated membrane-based glycosphingolipid that regulates insulin receptor signaling via direct association with the receptor. Ganglioside GM3 sodium salt possesses powerful effects on cancer development and progression.
  • HY-13735B
    Quinacrine hydrochloride hydrate

    Mepacrine hydrochloride hydrate; SN-390 hydrochloride hydrate

    Parasite Apoptosis Autophagy Mitophagy Cancer Infection
    Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis.
  • HY-W010104
    L-Methionine sulfoxide

    H-Met(O)-OH

    Endogenous Metabolite Metabolic Disease
    L-Methionine sulfoxide (H-Met(O)-OH), a metabolite of Methionine, induces M1/classical macrophage polarization, and modulates oxidative stress and purinergic signaling parameters.
  • HY-N0341
    Scopolin

    Sirtuin Metabolic Disease
    Scopolin is a coumarin isolated from Arabidopsis thaliana (Arabidopsis) roots. Scopolin attenuated hepatic steatosis through activation of SIRT1-mediated signaling cascades.
  • HY-10009
    Semagacestat

    LY450139

    γ-secretase Amyloid-β Notch Neurological Disease
    Semagacestat is a γ-secretase inhibitor, inhibits β-amyloid (Aβ42), Aβ38 and Aβ40 with IC50 of 10.9, 12 and 12.1 nM, respectively; also inhibits Notch signaling with IC50 of 14.1 nM.
  • HY-133021
    Arazine

    N-Acetyl-S-farnesyl-L-cysteine

    Others Inflammation/Immunology
    Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and G-protein coupled receptor signaling. Arazine can be a a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptors site.
  • HY-15771A
    Tirabrutinib hydrochloride

    ONO-4059 hydrochloride; GS-4059 hydrochloride

    Btk Cancer
    Tirabrutinib (ONO-4059) hydrochloride is a selective and novel inhibitor of BTK with IC50 2.2 nm, Tirabrutinib binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development.
  • HY-W001174
    2,5-Dihydroxyacetophenone

    ERK NF-κB Inflammation/Immunology
    2,5-Dihydroxyacetophenone, isolated from Rehmanniae Radix Preparata, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways.
  • HY-N1570
    Pterosin B

    Salt-inducible Kinase (SIK) Inflammation/Immunology
    Pterosin B, a indanone found in bracken fern (Pteridium aquilinum), is an inhibitor of salt-inducible kinase 3 (Sik3) signaling. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice by inhibiting Sik3.
  • HY-N4202
    Dihydrorotenone

    Mitochondrial Metabolism Apoptosis Neurological Disease
    Dihydrorotenone, a natural pesticide, is a potent mitochondrial inhibitor. Dihydrorotenone probably induces Parkinsonian syndrome. Dihydrorotenone induces human plasma cell apoptosis by triggering endoplasmic reticulum stress and activating p38 signaling pathway.
  • HY-N0109
    Salidroside

    Rhodioloside

    mTOR Apoptosis Cancer
    Salidroside is a prolyl endopeptidase Inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.
  • HY-13992
    AP20187

    B/B Homodimerizer

    FKBP Metabolic Disease
    AP20187 (B/B Homodimerizer) is a cell-permeable ligand used to dimerize FK506-binding protein (FKBP) fusion proteins and initiate biological signaling cascades and gene expression or disrupt protein-protein interactions.
  • HY-W010737
    Guanosine-5'-triphosphate disodium salt

    5'-GTP disodium salt

    Endogenous Metabolite Metabolic Disease
    Guanosine-5'-triphosphate disodium salt (5'-GTP trisodium salt) is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.
  • HY-N2460
    Aloesin

    Aloeresin

    Others Cancer Inflammation/Immunology
    Aloesin (Aloeresin) is an active constituent of the herb aloe vera and displays anti-inflammatory activity, ultraviolet protection, and antibacterium effects. Aloesin exerts its anticancer effect through the MAPK signaling pathway.
  • HY-133122
    UCB-9260

    TNF Receptor Inflammation/Immunology
    UCB-9260, an orally active compound, inhibits TNF signalling by stabilising an asymmetric form of the trimer. UCB-9260 is selective for TNF over other superfamily members, and binds TNF with a similar Kd of 13 nM.
  • HY-15872A
    FTI-277 hydrochloride

    Farnesyl Transferase Apoptosis Influenza Virus Cancer Infection
    FTI-277 hydrochloride is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. FTI-277 hydrochloride can inhibits hepatitis delta virus (HDV) infection.
  • HY-N0819
    Raddeanin A

    Apoptosis Cancer
    Raddeanin A is a natural triterpenoid saponin component of Anemone raddeana, with anti-cancer activities. Raddeanin A exerts anticancer effect on human osteosarcoma via the ROS/JNK and NF-κB signal pathway.
  • HY-101021
    Ascochlorin

    Ilicicolin D

    STAT Apoptosis Cancer Inflammation/Immunology
    Ascochlorin (Ilicicolin D), an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. Ascochlorin induces apoptosis. Anti-inflammatory activity.
  • HY-112730
    PEO-IAA

    2-(1H-Indol-3-yl)-4-oxo-4-phenyl-butyric acid

    Others Others
    PEO-IAA is an indole-3-acetic acid (IAA) antagonist. PEO-IAA is an auxin antagonist that binds to transport inhibitor response 1/auxin signaling F-box proteins (TIR1/AFBs).
  • HY-126242S
    Tyk2-IN-7

    JAK Inflammation/Immunology
    Tyk2-IN-7 (Compound 48) is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 (Compound 48) provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 (Compound 48) provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model.
  • HY-16563
    Narciclasine

    Lycoricidinol

    ROCK Cancer
    Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.
  • HY-13756
    Tacrolimus

    FK506; Fujimycin; FR900506

    Phosphatase FKBP Bacterial Autophagy Antibiotic Cancer Infection Inflammation/Immunology
    Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties.
  • HY-N2477
    Taraxerol

    Apoptosis NF-κB Cancer Inflammation/Immunology
    Taraxerol is isolated from Abroma augusta L, and has anti-inflammtory and anti-cancer effects. Taraxerol attenuates acute inlammation through inhibition of NF-κB signaling pathway. Taraxerol induces cell apoptosis.
  • HY-N1374
    Magnolin

    ERK Inflammation/Immunology
    Magnolin, a major component of Magnolia flos (Shin-Yi), inhibits the Ras/ERKs/RSK2 signaling axis by targeting the active pocket of ERK1 and ERK2 with IC50s of 87 nM and 16.5 nM, respectively.
  • HY-133554
    ASK1-IN-1

    p38 MAPK Inflammation/Immunology
    ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC50=138 nM; Biochemical IC50=21 nM).
  • HY-P1201
    Cyclosomatostatin

    Somatostatin Receptor Cancer
    Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
  • HY-W031727
    Hydroxychloroquine

    Parasite Toll-like Receptor (TLR) SARS-CoV Autophagy Cancer Infection
    Hydroxychloroquine is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro.
  • HY-N4019
    Maohuoside A

    Others Metabolic Disease
    Maohuoside A, a single compound isolated from the E. koreanum that potently promotes osteogenesis. Maohuoside A enhances the osteogenesis of bone marrow-derived mesenchymal stem cells via bone morphogenetic protein (BMP) and MAPK signaling pathways.
  • HY-N0439
    Asiaticoside

    TGF-beta/Smad Reactive Oxygen Species Apoptosis Endogenous Metabolite Inflammation/Immunology Neurological Disease Cardiovascular Disease Cancer
    Asiaticoside, a trisaccaride triterpene from Centella asiatica, suppresses TGF-β/Smad signaling through inducing Smad7 and inhibiting TGF-βRI and TGF-βRII in keloid fibroblasts; Asiaticoside shows antioxidant, anti-inflammatory, and anti-ulcer properties.
  • HY-N2357
    Eudesmin

    (-)-Eudesmin; Eudesmine; (-)-Eudesmine

    Ribosomal S6 Kinase (RSK) Cancer Infection Metabolic Disease Inflammation/Immunology
    Eudesmin ((-)-Eudesmin) impairs adipogenic differentiation via inhibition of S6K1 signaling pathway. Eudesmin possesses diverse therapeutic effects, including anti-tumor, anti-inflammatory, and anti-bacterial activities.
  • HY-N0171A
    Beta-Sitosterol (purity>98%)

    β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)

    Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Beta-Sitosterol (purity>98%) is a plant sterol. Beta-Sitosterol (purity>98%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
  • HY-136433
    N,N'-Dinitrosopiperazine

    1,4-Dinitrosopiperazine; DNP

    Others Cancer
    N,N'-Dinitrosopiperazine (1,4-Dinitrosopiperazine; DNP) is a carcinogen with specificity for nasopharyngeal epithelium and facilitates NPC metastasis. N,N'-Dinitrosopiperazine regulates multiple signaling pathways through protein phosphorylation, including LYRIC at serine 568.
  • HY-N6036
    Ganoderic acid F

    Others Cancer
    Ganoderic acid F is a ganoderic acid. Ganoderic acid F exhibits antitumor and antimetastatic activities through inhibition of angiogenesis and alteration of proteins involving cell proliferation and/or cell death, carcinogenesis, oxidative stress, calcium signaling, and endoplasmic reticulum stress.
  • HY-N2031
    Parishin

    Others Neurological Disease
    Parishin is a phenolic glucoside isolated from Gastrodia elata. Parishin exhibits antiaging effects and extends the lifespan of yeast via regulation of Sir2/Uth1/TOR signaling pathway.
  • HY-P2233
    Globomycin

    Bacterial Infection
    Globomycin is a lipopeptide antibiotic and a signal peptidase II (LspA) inhibitor. Globomycin inhibits processing of the prolipoprotein by binding irreversibly to the peptidase. Globomycin has toxic for the mollicute Spiroplasma melliferum with a MIC in the range 6.25-12.5 μM.
  • HY-N0608
    Myrislignan

    NF-κB Inflammation/Immunology
    Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.
  • HY-B0497C
    Niclosamide olamine

    BAY2353 olamine

    STAT Parasite Antibiotic Autophagy
    Niclosamide olamine is an anthelmintic that disrupts mitochondrial metabolism in parasitic worms and animal models. Niclosamide olamine inhibits STAT3 (IC50 = 0.25 μM) and stimulates autophagy by reversibly inhibiting mammalian target of Rapamycin complex 1 (mTORC1) signaling.
  • HY-11011
    A-770041

    Src Inflammation/Immunology
    A-770041 is selective and orally active Src-family Lck inhibitor; A-770041 is a 147 nM inhibitor of Lck (1 mM ATP) and is 300-fold selective against Fyn, the other Src family kinase involved in T-cell signaling.
  • HY-13756A
    Tacrolimus monohydrate

    FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate

    Phosphatase FKBP Autophagy Bacterial Antibiotic Cancer Infection Inflammation/Immunology
    Tacrolimus monohydrate (FK506 monohydrate), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex and inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties.
  • HY-D0254
    Gallein

    Pyrogallol phthalein

    Others Cancer
    Gallein is a G protein βγ (Gβγ) subunit signalling inhibitor. Gallein disrupts the interaction of Gβγ subunits with the PI3Kγ. Anticancer agent. Gallein used as a red dye, an acid-base indicator and as a detection reagent for phosphates.
  • HY-N2255
    Crebanine

    Akt Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Crebanine, an alkaloid from Stephania venosa, induces G1 arrest and apoptosis in human cancer cells. Crebanine exhibits anti-inflammatory activity via suppressing MAPKs and Akt signaling. Crebanine also possesses antiarrhythmic effect.
  • HY-P1201A
    Cyclosomatostatin TFA

    Somatostatin Receptor Cancer
    Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
  • HY-P9926
    Dupilumab

    REGN-668; SAR-231893

    Interleukin Related Inflammation/Immunology
    Dupilumab (REGN-668) is a fully human mAb to IL-4 receptor α (IL-4Rα) that inhibits both IL-4 and IL-13 signaling, markedly improved moderate-to-severe atopic dermatitis.
  • HY-109039
    Praliciguat

    IW-1973

    Guanylate Cyclase Cardiovascular Disease
    Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase stimulator, enhances NO signaling, acts as a vasodilator. Praliciguat (IW-1973) stimulates sGC in HEK-293 cells with an EC50 of 197 nM.
  • HY-N6679A
    10,11-Dehydrocurvularin

    HSP TGF-beta/Smad Cancer Infection
    10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity.
  • HY-116213
    Sparstolonin B

    Toll-like Receptor (TLR) HIV Cancer Infection Inflammation/Immunology
    Sparstolonin B acts as a selective TLR2 and TLR4 antagonist and selectively blocks TLR2- and TLR4-mediated inflammatory signaling. Sparstolonin B has anti-HIV and anticancer activities.
  • HY-110066
    (Z)-Guggulsterone

    Apoptosis VEGFR Akt Cancer
    Z-guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. Z-guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis.
  • HY-N6076
    Tenuifoliside A

    ERK Neurological Disease
    Tenuifoliside A is isolated from Polygala tenuifolia, has anti-apoptotic and antidepressant-like effects. Tenuifoliside A exhibits its neneurotrophic effects and promotes cell proliferation through the ERK/CREB/BDNF signal pathway in C6 cells.
  • HY-100016
    AZD0156

    ATM/ATR Apoptosis Cancer
    AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis.
  • HY-122935
    Nigranoic acid

    HIV Reverse Transcriptase Infection
    Nigranoic acid is a triterpenoid separated from Schisandra chinensis. Nigranoic acid inhibits HIV-1 reverse transcriptase. Nigranoic acid exhibits protective effects on brain through PARP/AIF signaling pathway in cerebral ischemia-reperfusion animal model.
  • HY-100461
    C29

    Toll-like Receptor (TLR) Inflammation/Immunology
    C29 is a Toll-like receptor 2 (TLR2) inhibitor. C29 blocks hTLR2/1 and hTLR2/6 signaling with IC50s of 19.7 and 37.6 μM, respectively.
  • HY-N1419
    Vaccarin

    AMPK Metabolic Disease
    Vaccarin is an active flavonoid glycoside associated with various biological functions. Vaccarin significantly promote wound healing and endothelial cells and fibroblasts proliferation in the wound site. Vaccarin ameliorates insulin resistance and steatosis by activating the AMPK signaling pathway.
  • HY-N6674
    Diazepinomicin

    ECO-4601; TLN-4601; BU 4664L

    Ras Apoptosis Cancer
    Diazepinomicin (TLN-4601) is a secondary metabolite produced by Micromonospora sp. Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. An anti-tumor agent for K-Ras mutant models.
  • HY-103316A
    Ned 19

    Calcium Channel Cancer
    Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca 2+ signaling, with an IC50 of 65 nM. Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice.
  • HY-124237A
    N-Octanoyl-L-homoserine lactone

    Bacterial
    N-octanoyl-L-Homoserine lactone is a small diffusible signaling molecule involved in quorum sensing, thereby controlling gene expression and affecting cellular metabolism. N-octanoyl-L-Homoserine lactone can be used for the infection prevention and regulation of virulence in general and in cystic fibro.
  • HY-15185
    Nirogacestat

    PF-3084014; PF-03084014

    γ-secretase Apoptosis Cancer
    Nirogacestat (PF-3084014) is a reversible, noncompetitive, and selective γ-secretase inhibitor with IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers.
  • HY-125829
    Erythropterin

    Others Others
    Erythropterin is a Pterin derivative that belongs in a group of heterocyclic compounds that are frequently found in biological systems. Pterin derivatives are responsible for the characteristic warning coloration of some Heteroptera and other insects, signaling noxiousness or unpalatability and are used to discourage potential predators from attacking.
  • HY-19706
    ARS-853

    Ras Apoptosis Cancer
    ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.
  • HY-N0188
    Esculin

    p38 MAPK Inflammation/Immunology Cancer
    Esculin, a fluorescent coumarin glucoside, is an active ingredient of ash bark. Esculin ameliorates cognitive impairment in experimental diabetic nephropathy (DN), and exerts anti‑oxidative stress and anti‑inflammatory effects, via the MAPK signaling pathway.
  • HY-N0705
    Curculigoside

    JAK STAT NF-κB Inflammation/Immunology Neurological Disease Cancer
    Curculigoside is the main saponin in C. orchioide, exerts significant antioxidant, anti-osteoporosis, antidepressant and neuroprotection effects. Curculigoside possesses significant anti-arthritic effects in vivo and in vitro via regulation of the JAK/STAT/NF-κB signaling pathway.
  • HY-122219
    R243

    CCR Inflammation/Immunology
    R243 is a potent and selective CCR8 antagonist. R243 inhibits CCL1/CCR8 interaction and inhibits CCR8 signaling and chemotaxis. R243 has antinociceptive and anti-inflammatory effects.
  • HY-122632
    Ciliobrevin D

    Hedgehog Cancer
    Ciliobrevin D is a cell-permeable, reversible and specific inhibitor of AAA+ ATPase motor cytoplasmic dynein. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation. Ciliobrevin D inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.
  • HY-113764
    N-Butanoyl-DL-homoserine lactone

    (Rac)-C4-HSL

    Others Infection
    N-Butanoyl-DL-homoserine lactone ((Rac)-C4-HSL) is a quorum sensing (QS) signaling molecule. N-Butanoyl-DL-homoserine lactone aptamers blocks qurom sensing and inhibits biofilm formation in Pseudomonas aeruginosa.
  • HY-19356A
    Didesmethylrocaglamide

    Eukaryotic Initiation Factor (eIF) Apoptosis Cancer
    Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity.
  • HY-B1370A
    (S)-Hydroxychloroquine

    (S)-HCQ

    Parasite Toll-like Receptor (TLR) SARS-CoV Autophagy Infection
    (S)-Hydroxychloroquine ((S)-HCQ) is the enantiomer of Hydroxychloroquine. Hydroxychloroquine, a synthetic antimalarial drug, inhibits Toll-like receptor 7/9 (TLR7/9) signaling, and shows efficiently inhibits SARS-CoV-2 infection in vitro.
  • HY-N0608A
    (Rac)-Myrislignan

    NF-κB Inflammation/Immunology
    (Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.
  • HY-114267
    Cbz-B3A

    mTOR Others
    Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).
  • HY-N0366
    Sennoside B

    PDGFR Cancer
    Sennoside B is an anthraquinone glycoside, found in large quantities in leaves and pods of Senna (Cassia angustifolia). Sennoside B can inhibit PDGF-stimulated cell proliferation by binding to PDGF-BB and its receptor and by down-regulating the PDGFR-beta signaling pathway.
  • HY-B1370
    Hydroxychloroquine sulfate

    HCQ sulfate

    Parasite Toll-like Receptor (TLR) SARS-CoV Autophagy Cancer Infection
    Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro.
  • HY-100224
    SANT-1

    Smo Hedgehog Cancer
    SANT-1, a potent Smo antagonist, inhibits Hedgehog signaling. SANT-1 shows IC50s of 20 nM and 30 nM in Shh-LIGHT2 and SmoA1-LIGHT2 assay, respectively.
  • HY-N2350
    Cynaropicrin

    MMP NF-κB TNF Receptor Cancer
    Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
  • HY-N6857
    Armepavine

    NF-κB Inflammation/Immunology
    Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades.
  • HY-118697
    N-dodecanoyl-L-Homoserine lactone

    C12-HSL

    Others Infection
    N-dodecanoyl-L-Homoserine lactone (C12-HSL) is a quorum sensing (QS) signaling molecule. N-dodecanoyl-L-Homoserine lactone (C12-HSL) aptamers blocks qurom sensing and inhibits biofilm formation in Pseudomonas aeruginosa.
  • HY-B1370B
    (R)-Hydroxychloroquine

    (R)-HCQ

    Parasite Toll-like Receptor (TLR) SARS-CoV Autophagy Infection
    (R)-Hydroxychloroquine is the enantiomer of Hydroxychloroquine. Hydroxychloroquine is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro.
  • HY-P1453
    CMD178

    STAT Cancer
    CMD178 is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 also is an inhibitor of STAT5 and inhibit Treg cell development.
  • HY-N6795
    Leptomycin A

    CRM1 HIV Infection
    Leptomycin A, a Streptomyces metabolite, is an inhibitor of CRM1 (exportin 1) that blocks CRM1 interaction with nuclear export signals, preventing the nuclear export of a broad range of proteins. Leptomycin A suppresses HIV-1 replication. Less potent than Leptomycin B.
  • HY-131262
    Hydroxychloroquine Impurity E

    4-[(7-Chloro-4-quinolinyl)amino]-1-pentanol

    Others Others
    Hydroxychloroquine Impurity E is the impurity of Hydroxychloroquine. Hydroxychloroquine is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro.
  • HY-12316
    20(S)-Hydroxycholesterol

    20α-Hydroxycholesterol

    Smo Endogenous Metabolite Cancer
    20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells.
  • HY-N7496
    Odoroside A

    Apoptosis Cancer
    Odoroside A is an active ingredient extracted from the leaves of Nerium oleander Linn. Odoroside A has anti-cancer activity. Odoroside A could induce apoptosis and cell cycle arrest through ROS/p53 signaling pathway, leading to the tumor cell death.
  • HY-P1453A
    CMD178 TFA

    STAT Inflammation/Immunology
    CMD178 (TFA) is a lead peptide that consistently reduces the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 (TFA) also is an inhibitor of STAT5 and inhibits Tregcells development.
  • HY-N0003
    Honokiol

    NSC 293100

    Akt ERK Autophagy HCV Cancer
    Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2. Honokiol can readily cross the blood brain barrier.
  • HY-119917
    Gossypetin

    p38 MAPK Bacterial Cancer Infection
    Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities.
  • HY-N0119
    Naringin Dihydrochalcone

    Naringin DC

    NF-κB Cancer
    Naringin Dihydrochalcone is an artificial sweetener derived from naringin. Naringin is a major flavanone glycoside obtained from tomatoes, grapefruits, and many other citrus fruits. Naringin exhibits biological properties such as antioxidant, anti-inflammatory, and antiapoptotic activities. Naringin suppresses NF-κB signaling pathway.
  • HY-110302
    6'-GNTI dihydrochloride

    Opioid Receptor Neurological Disease
    6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.
  • HY-125171
    IAXO-102

    Toll-like Receptor (TLR) Inflammation/Immunology
    IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. It inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development.
  • HY-126329
    AZD9898

    Gutathione S-transferase Inflammation/Immunology
    AZD9898 is an orally active leukotriene-C4 synthetase (LTC4S, glutathione S-transferase II) inhibitor, with an IC50 of 0.28 nM. AZD9898 mitigates the GABA binding and hepatic toxicity signal. AZD9898 has the potential to treat asthma.
  • HY-N0781
    Linderalactone

    Apoptosis Cancer
    Linderalactone is an important sesquiterpene lactone isolated from Radix linderae. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 µM.
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-135750
    VAF347

    Aryl Hydrocarbon Receptor Inflammation/Immunology
    VAF347 is a cell permeable and highly affinity aryl hydrocarbon receptor (AhR) agonist and induces AhR signaling. VAF347 inhibits the development of CD14 +CD11b + monocytes from granulo-monocytic (GM stage) precursors. VAF347 has anti-inflammatory effects.
  • HY-P2282
    APTSTAT3-9R

    STAT Cancer
    APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity.
  • HY-N0316
    Mollugin

    Others Cancer
    Mollugin is a major bioactive component isolated from Rubia cordifolia L.. Mollugin has an anti-cancer therapeutic effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 via the p38-Smad signaling pathway .
  • HY-125355
    SEC

    Apoptosis Cancer
    SEC induces activation of ANXA7 GTPase via the AMPK/mTORC1/STAT3 signaling pathway. SEC selectively promotes apoptosis in cancer cells, expressing a high level of ITGB4 by inducing ITGB4 nuclear translocation.
  • HY-12068
    PI3K-IN-1

    XL-147 derivative 1

    PI3K Cancer
    PI3K-IN-1 (XL-147 derivative 1) is a potent inhibitor of PI3K. PI3K-IN-1 (25 μM) blocks PI3K/Akt signaling pathways.
  • HY-N2112
    Glaucocalyxin A

    PI3K Akt Apoptosis Cancer
    Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect.
  • HY-P2141
    TRV-120027

    Angiotensin Receptor Cardiovascular Disease
    TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment.
  • HY-107794
    Clodronate disodium tetrahydrate

    Disodium clodronate tetrahydrate

    Others Inflammation/Immunology Neurological Disease
    Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl - competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain.
  • HY-N1356
    Reticuline

    JAK STAT NF-κB Inflammation/Immunology
    Reticuline, isolated from Litsea cubeba, shows anti-inflammatory effects through JAK2/STAT3 and NF-κB signaling pathways. Reticuline inhibits mRNA expressions of TNF-α, and IL-6 and reduces the phosphorylation levels of JAK2 and STAT3.
  • HY-N1778
    3,4-Dimethoxycinnamic acid

    O-Methylferulic acid

    Reactive Oxygen Species Virus Protease Cancer Infection
    3,4-Dimethoxycinnamic acid (O-Methylferulic acid) is a monomer extracted and purified from Securidaca inappendiculata Hassk. 3,4-Dimethoxycinnamic acid exerts anti-apoptotic effects on L-02 cells via the ROS-mediated signaling pathway. Anti-apoptotic effects.
  • HY-N0728
    α-Linolenic acid

    PI3K Akt Cancer Cardiovascular Disease
    α-Linolenic acid, isolated from seed oils, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer.
  • HY-126390
    (E/Z)-BCI

    NSC 150117

    Phosphatase Cancer Inflammation/Immunology
    (E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.
  • HY-11005
    BX-912

    PDK-1 Apoptosis Cancer
    BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis.
  • HY-N0171B
    Beta-Sitosterol (purity>75%)

    β-Sitosterol (purity>75%); 22,23-Dihydrostigmasterol (purity>75%)

    Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Beta-Sitosterol (purity>75%) includes 75% β-sitosterol and 10% campesterol. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>75%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
  • HY-103258
    TC ASK 10

    MAP3K Apoptosis Cancer
    TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM).
  • HY-14650
    DHEA

    Prasterone; Dehydroisoandrosterone; Dehydroepiandrosterone

    Androgen Receptor Endogenous Metabolite Endocrinology Cancer
    DHEA (Prasterone) is one of the most abundant steroid hormones. DHEA (Prasterone) mediates its action via multiple signaling pathways involving specific membrane receptors and via transformation into androgen and estrogen derivatives (e.g., androgens, estrogens, 7α and 7β DHEA, and 7α and 7β epiandrosterone derivatives) acting through their specific receptors.
  • HY-14788
    Drinabant

    AVE1625

    Cannabinoid Receptor Metabolic Disease
    Drinabant (AVE1625) is an orally active CB1 receptor antagonist. Drinabant (AVE1625) inhibits the agonist-stimulated calcium signal with IC50 values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective for the hCB2-R.
  • HY-N2204
    Swertiajaponin

    Tyrosinase Inflammation/Immunology
    Swertiajaponin is a tyrosinase inhibitor, forms multiple hydrogen bonds and hydrophobic interactions with the binding pocket of tyrosinase, with an IC50 of 43.47 μM. Swertiajaponin also inhibits oxidative stress-mediated MAPK/MITF signaling, leading to decrease in tyrosinase protein level. Swertiajaponin suppresses melanin accumulation and exhibits strong anti-oxidative activity.
  • HY-123503
    Salicortin

    JNK NF-κB Inflammation/Immunology Neurological Disease
    Salicortin, a phenolic glycoside, has been isolated from many plants such as Populus and Salix species. Salicortin inhibits osteoclast differentiation and bone resorption by down-regulating JNK and NF-κB/NFATc1 signaling pathways. Salicortin has anti-amnesic, anti-adipogenic, and immune-modulatory activity.
  • HY-N2485
    4'-Methoxyresveratrol

    4'-O-Methylresveratrol

    Others Inflammation/Immunology
    4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a polyphenol derived from Dipterocarpaceae, with antiandrogenic, antifungal and anti-inflammatory activities. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation.
  • HY-18366A
    RU-SKI 43 hydrochloride

    Hedgehog Cancer
    RU-SKI 43 hydrochloride is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 hydrochloride reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 hydrochloride has anti-cancer activity.
  • HY-18366
    RU-SKI 43

    Hedgehog Cancer
    RU-SKI 43 is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 has anti-cancer activity.
  • HY-124748A
    ENMD-1068 hydrochloride

    Protease-Activated Receptor (PAR) Inflammation/Immunology Cardiovascular Disease
    ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist with antiangiogenic and anti-inflammatory activities. ENMD-1068 hydrochloride reduces epatic stellate cells (HSCs) activation and collagen expression through the inhibiton of TGF-β1/Smad signal transduction.
  • HY-P2141A
    TRV-120027 TFA

    Angiotensin Receptor Cardiovascular Disease
    TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment.
  • HY-136244
    PF-06952229

    TGF-β Receptor Cancer
    PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction. PF-06952229 is a promising antineoplastic agent for the study solid tumors, especifically metastatic breast cancer.
  • HY-129390
    Orelabrutinib

    ICP-022

    Btk Cancer
    Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.
  • HY-B0094
    Artemisinin

    Qinghaosu; NSC 369397

    HCV Parasite Akt Ferroptosis Cancer Infection Neurological Disease
    Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial drug isolated from the aerial parts of Artemisia annua L. plants. Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects.
  • HY-110193
    SPP-86

    RET Cancer
    SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
  • HY-13894
    Tyrphostin AG1296

    AG1296

    PDGFR c-Kit FLT3 Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.
  • HY-13968
    JW 55

    PARP Cancer
    JW 55 is a potent and selective β-catenin signaling pathway inhibitor, which functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). JW 55 decreases auto-PARsylation of TNKS1/2 in vitro with IC50s of 1.9 μM and 830 nM respectively.
  • HY-N6901
    Luteolin 7-sulfate

    Others Metabolic Disease
    Luteolin 7-sulfate is isolated from Phyllospadix iwatensis Makino, a marine plant. Luteolin 7-sulfate attenuates TYR gene expression through the intervention of a cAMP-responsive element binding protein (CREB)- and microphthalmia-associated transcription factor (MITF)-mediated signaling pathway, leading to the decreased melanin synthesis.
  • HY-N6973
    Boldine

    Others Inflammation/Immunology
    Boldine is an aporphine isoquinoline alkaloid extracted from the root of Litsea cubeba and also possesses these properties, including antioxidant, anti-inflammatory and cytoprotective effects. Boldine suppresses osteoclastogenesis, improves bone destruction by down-regulating the OPG/RANKL/RANK signal pathway and may be a potential therapeutic agent for rheumatoid arthritis.
  • HY-N0392
    Polygalasaponin F

    Toll-like Receptor (TLR) PI3K Akt NF-κB Inflammation/Immunology
    Polygalasaponin F, an oleanane-type triterpenoid saponin extracted from Polygala japonica, decreases the release of the inflammatory cytokine tumor necrosis factor a (TNFa). Polygalasaponin F reduces neuroinflammatory cytokine secretion through the regulation of the TLR4-PI3K/AKT-NF-kB signaling pathway .
  • HY-130149
    MRTX849

    Ras Cancer
    MRTX849 is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. MRTX849 covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction.
  • HY-N6704
    Enniatin A1

    ERK Apoptosis Cancer
    Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in rat liver microsomes.
  • HY-17514
    Itraconazole

    R51211

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Infection Cancer
    Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects.
  • HY-N0171
    Beta-Sitosterol (purity>80%)

    β-Sitosterol (purity>80%); 22,23-Dihydrostigmasterol (purity>80%)

    Endogenous Metabolite Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Beta-Sitosterol (purity>80%) includes β-sitosterol (≥80%), stigmasterol, campesterol and brassicasterol mainly. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>98%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
  • HY-126397
    MnTBAP chloride

    NF-κB Inflammation/Immunology
    MnTBAP chloride is a superoxide dismutase (SOD) mimetic and peroxynitrite scavenger. MnTBAP chloride is a manganic porphyrin complex and has anti-oxidative property. MnTBAP chloride mediates anti-inflammatory effects through upregulation of BMPR-II and inhibition of the NFκB signaling. MnTBAP chloride has the potential for the fibrotic response in chronic kidney diseases (CKDs) research.
  • HY-13306
    Pyrintegrin

    Integrin Metabolic Disease
    Pyrintegrin is an β1-integrin agonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. Pyrintegrin can be used as a podocyte-protective agent and has robustly adipogenic.
  • HY-124418
    SBI-477

    Others Metabolic Disease
    SBI-477 is a chemical probe stimulated insulin signaling by deactivating the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain–containing 4 (ARRDC4). SBI-477 coordinately inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes.
  • HY-N2438
    Methylophiopogonanone B

    Ras Others
    Methylophiopogonanone B, homoisoflavonoid, is extracted from the root of Ophiopogon japonicas, shows high antioxidant ability. Methylophiopogonanone B increases GTP-Rho and acts via the Rho signaling pathway, inducing cell morphological change via actin cytoskeletal reorganization, including dendrite retraction and stress fiber formation.
  • HY-120006A
    (rel)-AR234960

    ERK Cardiovascular Disease
    (rel)-AR234960 is an active relative configuration of AR234960. AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts.
  • HY-136563
    RA375

    Proteasome Apoptosis Reactive Oxygen Species Cancer
    RA375 is a RPN13 (26S proteasome regulatory subunit) inhibitor. RA375 activates UPR signaling, ROS production and apoptosis. RA375 exhibits ten-fold greater activity against cancer lines than RA190, reflecting its nitro ring substituents and the addition of a chloroacetamide warhead.
  • HY-N6950
    Hederacolchiside A1

    PI3K Akt mTOR Parasite Apoptosis Cancer Infection
    Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro.
  • HY-N1967
    Dihydrocurcumin

    Fatty Acid Synthase (FASN) Metabolic Disease
    Dihydrocurcumin, a major metabolites of curcumin, reduces lipid accumulation and oxidative stress. Dihydrocurcumin regulates mRNA and protein expression levels of SREBP-1C, PNPLA3 and PPARα, increases protein expression levels of pAKT and PI3K, and reduced the levels of cellular NO and ROS via Nrf2 signaling pathways.
  • HY-109854A
    (R)-Lisofylline

    (R)-Lisophylline

    STAT Metabolic Disease Inflammation/Immunology
    (R)-Lisofylline ((R)-Lisophylline) is a (R)-enantiomer of the metabolite of Pentoxifylline with anti-inflammatory properties. (R)-Lisofylline is a lysophosphatidic acid acyltransferase inhibitor with an IC50 of 0.6 µM and interrupts IL-12 signaling-mediated STAT4 activation. (R)-Lisofylline has the potential for type 1 diabetes, autoimmune disorders research.
  • HY-10585A
    Valproic acid sodium salt

    Sodium Valproate

    HDAC Autophagy Mitophagy HIV Notch Cancer
    Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
  • HY-130307
    Rubrofusarin

    Bacterial Cancer Inflammation/Immunology Neurological Disease
    Rubrofusarin is an orange polyketide pigment from Fusarium graminearum. Rubrofusarin is also an active ingredient of the Cassia species and ameliorates chronic restraint stress (CRS) -induced depressive symptoms through PI3K/Akt signaling. Rubrofusarin has anticancer, antibacterial, and antioxidant effects.
  • HY-136555
    GSK717

    NOD-like Receptor (NLR) Inflammation/Immunology
    GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells.
  • HY-N0527
    Pentagalloylglucose

    Penta-O-galloyl-β-D-glucose; 1,2,3,4,6-Pentagalloyl glucose

    Influenza Virus Infection
    Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is a gallotannin isolated from various plants. It suppressed interleukin (IL)-4 induced signal pathway in B cell, and inhibited IgE production partially caused by increasing a population of Treg cells in conjunction with Treg-inducing factors. Pentagalloylglucose possesses significant anti-rabies virus (RABV) activity.
  • HY-N7363
    Isolongifolene

    (-)-Isolongifolene

    Others Cancer Inflammation/Immunology Neurological Disease
    Isolongifolene ((-)-Isolongifolene) is a tricyclic sesquiterpene isolated from Murraya koenigii. Isolongifolene attenuates Rotenone-induced oxidative stress, mitochondrial dysfunction and apoptosis through the regulation of P13K/AKT/GSK-3β signaling pathways. Isolongifolene has antioxidant, anti-inflammatory, anticancer and neuroprotective properties.
  • HY-Y0189
    Methyl Salicylate

    Wintergreen oil

    COX Inflammation/Immunology
    Methyl Salicylate (Wintergreen oil) is a topical analgesic and anti-inflammatory agent. Also used as a pesticide, a denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products. A systemic acquired resistance (SAR) signal in tobacco. A topical nonsteroidal anti-inflammatory drug (NSAID). Methyl salicylate lactoside is a COX inhibitor.
  • HY-13755
    Sulforaphane

    HDAC Keap1-Nrf2 Apoptosis Cancer Inflammation/Immunology
    Sulforaphane is an isothiocyanate present naturally in widely consumed vegetables. Sulforaphane increases tumor suppressor protein transcription and inhibits histone deacetylase activity. Sulforaphane activates Nrf2 and inhibits high glucose-induced progression of pancreatic cancer via AMPK dependent signaling. Sulforaphane has shown anti-cancer and anti-inflammatory activities.
  • HY-116961
    TH1020

    Toll-like Receptor (TLR) Bacterial Infection Inflammation/Immunology
    TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC50 of 0.85 μM. TH1020 inhbits flagellin-induced TLR5 signaling. TH1020 is inactive against TLR2, TLR3, TLR4, TLR7 and TLR8.
  • HY-112143
    STOCK2S-26016

    Others Cardiovascular Disease
    STOCK2S-26016 is a WNK signalling inhibitors. STOCK2S-26016 inhibits WNK4 and WNK1 with IC50s of 16 μM and 34.4 μM, respectively. STOCK2S-26016 has potential for antihypertensive research.
  • HY-N2095
    Atractylone

    Atractylon

    Influenza Virus Infection Inflammation/Immunology
    Atractylone (Atractylon) is a sesquiterpenoid extracted from Atractylodis Rhizoma. Atractylone (Atractylon) alleviates influenza A virus (IAV)-induced lung injury via regulating the TLR7 signaling pathway, and acts as a promising agent for IAV treatment. Atractylone (Atractylon) inhibits the degranulation of mast cell and exhibits potential for the treatment of mast cell-mediated allergic reactions.
  • HY-N0636
    Eriocitrin

    Apoptosis Cancer
    Eriocitrin is a flavonoid isolated from lemon, which is a strong antioxidant agent. Eriocitrin could inhibit the proliferation of hepatocellular carcinoma cell lines by arresting cell cycle in S phase through up-regulation of p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating mitochondria-involved intrinsic signaling pathway.
  • HY-113498
    Sphingomyelin

    Endogenous Metabolite Metabolic Disease Inflammation/Immunology Neurological Disease
    Sphingomyelin is a eukaryotic sphingolipid and one of the major constituents of cell membranes and particularly abundant in the myelin sheath that surrounds neuronal axons. Sphingomyelin plays an important role in cell processes, the regulation of inflammatory responses, and signal transduction. Sphingomyelin metabolism is associated with various central nervous system diseases and Niemann–Pick disease.
  • HY-112801
    F-1

    ALK ROS Cancer
    F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK WT, ROS1 WT, ALK L1196M and ALK G1202R, respectively.
  • HY-W010970
    5'-Guanylic acid disodium salt

    5'-GMP disodium salt; 5'-guanosine monophosphate disodium salt

    Endogenous Metabolite Others
    5'-Guanylic acid disodium salt (5'-GMP disodium salt) is composed of guanine, ribose, and phosphate moieties and it is a nucleotide monomer in messenger RNA. Guanosine derivatives are involved in intracellular signal transduction and have been identified in repetitive genomic sequences in telomeres, in ribosomal DNA, immunoglobulin heavy‐chain switch regions, and in the control regions of proto-oncogenes.
  • HY-N0587
    Demethylzeylasteral

    Apoptosis Cancer Inflammation/Immunology
    Demethylzeylasteral is a triterpene compound isolated from Tripterygium wilfordii Hook F, with anti-inflammatory, immunosuppressive and anti-tumor activities. Demethylzeylasteral can significantly alleviates atherosclerosis (AS). Demethylzeylasteral inhibits triple-negative breast cancer invasion by blocking the canonical and non-canonical TGF-β signaling pathways.
  • HY-10585
    Valproic acid

    VPA; 2-Propylpentanoic Acid

    HDAC Autophagy Mitophagy HIV Notch Cancer
    Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
  • HY-125817
    BI-3406

    Ras p38 MAPK Cancer
    BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity.
  • HY-N3298
    Meranzin

    Adrenergic Receptor Neurological Disease Cardiovascular Disease
    Meranzin is an absorbed bioactive compound from the Traditional Chinese Medicine (TCM) Chaihu-Shugan-San (CSS). Meranzin, isolated from leaves of Murraya exotica L., regulates the shared alpha 2-adrenoceptor and involves the AMPA-ERK1/2–BDNF signaling pathway. Meranzin has the potential for the prevention of the comorbidity of atherosclerosis and depression.
  • HY-N0232
    Psoralidin

    COX Lipoxygenase Notch Reactive Oxygen Species Bacterial Cancer
    Psoralidin, isolated from the seed of Psoralea corylifolia, is a dual inhibitor of COX-2 and 5-LOX, regulates ionizing radiation (IR)-induced pulmonary inflammation.Anti-cancer, anti-bacterial, and anti-inflammatory properties. Psoralidin significantly downregulates NOTCH1 signaling. Psoralidin also greatly induces ROS generation.
  • HY-113965
    CUR61414

    Hedgehog Smo Apoptosis Inflammation/Immunology
    CUR61414 is a novel, potent and cell permeable Hedgehog signaling pathway inhibitor (IC50 =100-200 nM). CUR61414 is a small-molecule aminoproline class compound and selectively binds to smoothened (Smo) with a Ki  value of 44 nM. CUR-61414 can induce apoptosis in cancer cells without affecting neighboring non-tumor cells.
  • HY-121246
    Fluorofenidone

    AKF-PD

    Others Inflammation/Immunology
    Fluorofenidone (AKF-PD), an analogue of AMR69, shows equivalent antifibrotic activity, lower toxicity and longer half-life. Fluorofenidone (AKF-PD) attenuates the progression of renal interstitial fibrosis partly by suppressing NADPH oxidase and extracellular matrix (ECM) deposition via the PI3K/Akt signalling pathway.
  • HY-15959
    Savolitinib

    Volitinib; HMPL-504; AZD-6094

    c-Met/HGFR Cancer
    Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity.
  • HY-111557
    YM-254890

    P2Y Receptor Cardiovascular Disease
    YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y1 signal transduction pathway, with an IC50 value below 0.6 μM.
  • HY-101364A
    CHPG sodium salt

    mGluR NF-κB ERK Akt Inflammation/Immunology Neurological Disease
    CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways..
  • HY-14340
    WAY-181187

    SAX-187

    5-HT Receptor Neurological Disease
    WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.
  • HY-116171
    (Rac)-Calpain Inhibitor XII

    Proteasome
    (Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM), with lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). (Rac)-Calpain Inhibitor XII has been used to study the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.
  • HY-107818
    4-Hydroxychalcone

    NF-κB Inflammation/Immunology Cardiovascular Disease
    4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity. 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice.
  • HY-126113
    KIN101

    Influenza Virus HCV Infection
    KIN101 is a potent RNA viral inhibitor with IC50s of 2 μM, >5 μM for influenza virus and Dengue virus (DNV), respectively. KIN101, an isoflavone agonist of IRF-3 dependent signaling, induces IRF-3 nuclear translocation. KIN101 has broad-spectrum activity against RNA viruses.
  • HY-N7110
    6-Hydroxyflavone

    Others Inflammation/Immunology
    6-Hydroxyflavone is a naturally occurring flavone, with anti-inflammatory activity. 6-Hydroxyflavone exhibits inhibitory effect towards bovine hemoglobin (BHb) glycation. 6-Hydroxyflavone can activate AKT, ERK 1/2, and JNK signaling pathways to effectively promote osteoblastic differentiation. 6-Hydroxyflavone inhibits the LPS-induced NO production .
  • HY-N6246
    Asperulosidic Acid

    NF-κB ERK Cancer Inflammation/Immunology
    Asperulosidic Acid (ASPA), a bioactive iridoid glycoside, is extracted from the herbs of Hedyotis diffusa Willd. Asperulosidic Acid (ASPA) has anti-tumor, anti-oxidant, and anti-inflammatory activities. ASPA is related to the inhibition of inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways.
  • HY-B0151
    Pregnenolone

    3β-Hydroxy-5-pregnen-20-one

    Cannabinoid Receptor Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication.
  • HY-101364
    CHPG

    mGluR NF-κB ERK Akt Inflammation/Immunology Cardiovascular Disease
    CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways.
  • HY-128932
    Cefminox sodium

    MT-141

    Bacterial PPAR Prostaglandin Receptor Antibiotic Infection Cardiovascular Disease Endocrinology
    Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity. Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension.
  • HY-13653
    (-)-Epigallocatechin Gallate

    EGCG; Epigallocatechol Gallate

    Autophagy Reactive Oxygen Species HIV Ferroptosis Mitochondrial Metabolism Endogenous Metabolite Cancer
    (-)-Epigallocatechin Gallate is a tea flavonoid with potent antioxidant, antiinflammatory, and anticarcinogenic properties. (-)-Epigallocatechin Gallate is reported to inhibit EGFR signaling and thereby exert anticancer effects. (-)-Epigallocatechin Gallate (EGCG) is a glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) inhibitor. Epigallocatechin-3-gallate induces oxidative phosphorylation by activating cytochrome c oxidase.
  • HY-B0185A
    Lidocaine hydrochloride

    Lignocaine hydrochloride

    Sodium Channel MEK ERK NF-κB Apoptosis Cancer Cardiovascular Disease
    Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative commonly used to anesthetize. hydrochloride is a a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
  • HY-126154
    L48H37

    Toll-like Receptor (TLR) Inflammation/Immunology
    L48H37 is an analog of Curcumin (HY-N0005) with improved chemical stability. L48H37 is a potent and specific myeloid differentiation protein 2 (MD2) inhibitor and inhibits the interaction and signaling transduction of LPS-TLR4/MD2. L48H37 is used for the research of sepsis or lung injury treatment.
  • HY-N2082
    Isorhamnetin 3-O-galactoside

    Cacticin

    Others Inflammation/Immunology Cardiovascular Disease
    Isorhamnetin 3-O-galactoside (Cacticin), a flavonoid glycoside isolated from Artemisia capillaris Thunberg, which ameliorates CCl4-induced hepatic damage by enhancing the anti-oxidative defense system and reducing the inflammatory signaling pathways. Isorhamnetin 3-O-galactoside (Cacticin) has antithrombotic and anti-inflammatory activities.
  • HY-18766
    EW-7195

    TGF-β Receptor p38 MAPK Cancer
    EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung.
  • HY-136174
    RBN-2397

    PARP Cancer
    RBN-2397 is a potent, accross species and orally active NAD + competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores interferon (Type I) signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors.
  • HY-B0185
    Lidocaine

    Lignocaine

    Sodium Channel MEK ERK NF-κB Apoptosis Cancer Cardiovascular Disease
    Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative commonly used to anesthetize. Lidocaine is a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
  • HY-111024
    2,2,5,7,8-Pentamethyl-6-Chromanol

    PMC

    Androgen Receptor Cancer
    2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines.
  • HY-110358
    QAQ dichloride

    Sodium Channel Inflammation/Immunology
    QAQ dichloride, a photoswitchable voltage-gated Nav and Kv channels blocker, blocks channels in its trans form (of the azobenzene photoswitch), but not in its cis form. QAQ dichloride is membrane-impermeant and only infiltrates pain-sensing neurons that express endogenous import channels. QAQ dichloride acts as a light-sensitive analgesic and can be used for studying of signaling mechanisms in acute and chronic pain.
  • HY-13440
    AMG 511

    PI3K Cancer
    AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model.
  • HY-116084
    Trimethylamine N-oxide

    NOD-like Receptor (NLR) Reactive Oxygen Species TGF-beta/Smad Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease
    Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.
  • HY-100487
    TAK-243

    MLN7243

    E1/E2/E3 Enzyme NF-κB Apoptosis Cancer
    TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
  • HY-14621
    Zingerone

    Vanillylacetone; Gingerone

    NF-κB Cancer Metabolic Disease Inflammation/Immunology
    Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antilipolytic, antidiarrhoeic, antispasmodic and anti-tumor properties. Zingerone alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways. Zingerone acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells.
  • HY-131031
    KCC-07

    DNA Alkylator/Crosslinker Cancer
    KCC-07 is a potent, selective and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity.
  • HY-13065
    Isobavachalcone

    Corylifolinin; Isobacachalcone

    Akt Reactive Oxygen Species Apoptosis Autophagy Cancer
    Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity.
  • HY-13027
    DAPT

    GSI-IX

    γ-secretase Amyloid-β Autophagy Notch Apoptosis Cancer Inflammation/Immunology Neurological Disease
    DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and 42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.
  • HY-130234
    SP-8356

    NF-κB Apoptosis Cancer Cardiovascular Disease
    SP-8356, an anti-inflammatory synthetic verbenone derivative, is a potent, orally active cluster of differentiation 147 (CD147) inhibitor. SP-8356 inhibits CD147-cyclophilin A (CypA) interaction and reduces MMP-9 activity. SP-8356 exerts anti-breast cancer effects by inhibiting NF-κB signaling. Anti-atherosclerotic effects.
  • HY-16697
    CID 16020046

    GPR55 Cancer
    CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function.
  • HY-B1640
    Ethacrynic acid

    Gutathione S-transferase NF-κB Calcium Channel Cancer Inflammation/Immunology
    Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
  • HY-11109
    Resatorvid

    TAK-242; CLI-095

    Toll-like Receptor (TLR) TNF Receptor Interleukin Related Autophagy Inflammation/Immunology Cancer
    Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-R and IL-6 production with IC50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases.
  • HY-B1739
    Pregnenolone monosulfate

    3β-Hydroxy-5-pregnen-20-one monosulfate

    Cannabinoid Receptor Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication.
  • HY-N2259
    Curcumenol

    (+)-Curcumenol

    Cytochrome P450 Cancer Inflammation/Immunology Neurological Disease
    Curcumenol ((+)-Curcumenol) is a potent CYP3A4 inhibitor with an IC50 of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. Curcumenol ((+)-Curcumenol) suppresses Akt-mediated NF-κB activation and p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells.
  • HY-P1432
    K-(D-1-Nal)-FwLL-NH2

    GHSR
    K-(D-1-Nal)-FwLL-NH2 is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
  • HY-18980
    Rottlerin

    Mallotoxin; NSC 56346; NSC 94525

    PKC Autophagy Apoptosis Infection Cancer
    Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation.
  • HY-P1812
    AUNP-12

    NP-12

    PD-1/PD-L1 Cancer
    AUNP-12 (NP-12) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs).
  • HY-15509A
    Semapimod tetrahydrochloride

    CNI-1493; CPSI-2364 tetrahydrochloride

    TNF Receptor Interleukin Related p38 MAPK Inflammation/Immunology
    Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders.
  • HY-110189
    Pregnenolone monosulfate sodium salt

    3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt

    Cannabinoid Receptor Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone monosulfate sodium salt (3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication.
  • HY-N0222
    Avicularin

    Others Cancer Inflammation/Immunology
    Avicularin is a bio-active flavonoid from plants, anti-inflammatory, anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities. Avicularin exhibits anti-inflammatory activity through the suppression of ERK signaling pathway in LPS-stimulated RAW 264.7 macrophage cells. Avicularin ameliorates human hepatocellular carcinoma via the regulation of NF κB (p65), COX 2 and PPAR γ activities.
  • HY-15672
    FM19G11

    HIF/HIF Prolyl-Hydroxylase Cancer Neurological Disease
    FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions.
  • HY-120327
    KY-226

    Phosphatase Metabolic Disease Neurological Disease
    KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury.
  • HY-N0631
    Cornuside

    p38 MAPK NF-κB Inflammation/Immunology
    Cornuside is a secoiridoid glucoside isolated from the fruit of Cornus officinalis Sieb. et Zucc., which is a traditional oriental medicine for treating inflammatory diseases and invigorating blood circulation. Cornuside inhibits mast cell-mediated allergic response by down-regulating MAPK and NF-κB signaling pathways. Cornuside has anti-allergic effects in vivo and in vitro which suggests a therapeutic application of this agent in inflammatory allergic diseases.
  • HY-B0097
    Floxuridine

    5-Fluorouracil 2'-deoxyriboside

    Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Bacterial CMV HSV Cancer Infection
    Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis. Floxuridine has antiviral effects against HSV and CMV.
  • HY-N0678
    Icaritin

    Anhydroicaritin

    Autophagy Apoptosis Cancer
    Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium Genusis and potently inhibits proliferation of K562 cells (IC50 of 8 µM) and primary CML cells (IC50 of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis[3.
  • HY-W017212
    Methyl cinnamate

    Methyl 3-phenylpropenoate

    Tyrosinase Bacterial AMPK Infection Metabolic Disease
    Methyl cinnamate (Methyl 3-phenylpropenoate), an active component of Zanthoxylum armatum, is a widely used natural flavor compound. Methyl cinnamate (Methyl 3-phenylpropenoate) possesses antimicrobial activity and is a tyrosinase inhibitor that can prevent food browning. Methyl cinnamate (Methyl 3-phenylpropenoate) has antiadipogenic activity through mechanisms mediated, in part, by the CaMKK2-AMPK signaling pathway.
  • HY-N2329
    Piperlongumine

    Piplartine

    ERK Reactive Oxygen Species Autophagy Apoptosis Bacterial Ferroptosis Cancer Infection Cardiovascular Disease
    Piperlongumine is a natural alkaloid isolated from Piper longum Linn, possesses ant-inflammatory, antibacterial, antiangiogenic, antioxidant, antitumor, and antidiabetic activities. Piperlongumine induces ROS, and induces apoptosis in cancer cell lines. Piperlongumine shows anti-cardiac fibrosis activity, suppresses myofibroblast transformation via suppression of the ERK1/2 signaling pathway.
  • HY-131001
    DPNB-ABT594

    nAChR Neurological Disease
    DPNB-ABT594 is a nitrobenzyl-caged ABT594 (HY-14316A) and activates nAChRs containing the α4β2 subunits with good selectivity than the α7 subunit. DPNB-ABT594 can be used to map the distribution of nAChRs on neurons of the medial habenula (MHb) and helps to gain a deeper understanding of the nAChR‐mediated Ca 2+ signalling in the MHb.
  • HY-N2573
    Corydalmine

    L-Corydalmine

    Fungal CXCR Infection Neurological Disease
    Corydalmine (L-Corydalmine), an alkaloid isolated from roots of Corydalis Chaerophylla, inhibits spore germination of some plant pathogenic as well as saprophytic fungi. Corydalmine acts as an oral analgesic agent, exhibiting potent analgesic activity. Corydalmine alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway.
  • HY-103565
    AMN082

    mGluR Neurological Disease
    AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
  • HY-W008947
    SEW​2871

    LPL Receptor Inflammation/Immunology Neurological Disease
    SEW2871 is a highly selective, orally active S1P1 agonist with an EC50 of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood and has therapeutic implications in contexts of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses.
  • HY-P1432A
    K-(D-1-Nal)-FwLL-NH2 TFA

    GHSR
    K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
  • HY-135318
    NBDHEX

    Glutathione Peroxidase Apoptosis Autophagy Cancer
    NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
  • HY-N6953
    Garcinone D

    STAT Keap1-Nrf2 Reactive Oxygen Species Neurological Disease
    Garcinone D, a natural xanthone from mangosteen, promotes the proliferation of C17.2 neural stem cell. Garcinone D increases the protein levels of phosphorylated signal transducer and activator of transcription 3 (p-STAT3), Cyclin D1 and nuclear factor erythroid 2-related factor (Nrf2), heme oxygenase-1 (HO-1) in concentration- and time- dependent manners.
  • HY-107390A
    AX-024 hydrochloride

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-N2484
    Methylnissolin

    Astrapterocarpan

    PDGFR ERK Cardiovascular Disease
    Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM. Methylnissolin inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinase. Methylnissolin inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibition of the ERK1/2 MAP kinase cascade.
  • HY-P1812A
    AUNP-12 TFA

    NP-12 TFA

    PD-1/PD-L1 Cancer
    AUNP-12 TFA (NP-12 TFA) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 TFA exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs).
  • HY-121222
    alpha-Bisabolol

    Apoptosis Cancer
    alpha-Bisabolol is a nontoxic sesquiterpene alcohol present in natural essential oil, with anticancer activity. alpha-Bisabolol exerts selective anticancer effect on A549 NSCLC cells (IC50=15 μM) via induction of cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol also strongly induces apoptosis in glioma cells.
  • HY-107390
    AX-024

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-108538
    Ethacrynic acid D5

    Gutathione S-transferase NF-κB Calcium Channel Inflammation/Immunology
    Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
  • HY-113466
    4-Hydroxynonenal

    4-HNE

    Aldehyde Dehydrogenase (ALDH) Endogenous Metabolite Cancer Neurological Disease Cardiovascular Disease
    4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
  • HY-121629
    PS210

    PDK-1 Cancer
    PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K.
  • HY-N1970
    5,7-Dihydroxychromone

    Keap1-Nrf2 Arenavirus Caspase PARP Neurological Disease
    5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells.
  • HY-13509
    CCG-50014

    RGS Protein Inflammation/Immunology
    CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test.
  • HY-14743B
    Golotimod hydrochloride

    SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod hydrochloride (SCV 07 hydrochloride), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod hydrochloride (SCV 07 hydrochloride) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod hydrochloride (SCV 07 hydrochloride) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-13686
    PQ401

    IGF-1R Apoptosis Cancer
    PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis.
  • HY-N1372A
    Fangchinoline

    HIV FAK Apoptosis Autophagy Cancer Infection
    Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK. Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer.
  • HY-N2205
    Esculentoside H

    NF-κB JNK Cancer
    Esculentoside H (EsH) is a water-soluble saponin isolated and purified from the root extract of perennial plant Phytolacca esculenta. Esculentoside H (EH) has anti-tumor activity, the mechanism is related to the capacity for TNFrelease. Esculentoside H (EsH) suppresses colon cancer cell migration through blockage of the JNK1/2 and NF-κB signaling-mediated matrix metalloproteinases-9 (MMP-9) expression.
  • HY-100434
    PD-161570

    FGFR PDGFR EGFR Src TGF-β Receptor Cancer Cardiovascular Disease
    PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
  • HY-107024
    Osteogenic Growth Peptide (10-14)

    OGP(10-14); Historphin

    Src Others
    Osteogenic Growth Peptide (10-14) (OGP(10-14)), the C-terminal truncated pentapeptide of osteogenic growth peptide (OGP), retains the full OGP-like activity. Osteogenic Growth Peptide (10-14) is responsible for the binding to the OGP receptor and activates an intracellular Gi-protein-MAP kinase signaling pathway. Osteogenic Growth Peptide (10-14) is a potent mitogen and stimulator of osteogenesis and hematopoiesis. Osteogenic Growth Peptide (10-14) acts as a Src inhibitor.
  • HY-P9917
    Tocilizumab

    Anti-Human IL6R, Humanized Antibody

    Interleukin Related Cancer Inflammation/Immunology
    Tocilizumab (Anti-Human IL6R, Humanized Antibody) is an anti-human interleukin-6 receptor (IL-6R) neutralizing antibody, prevents binding of IL-6 to the IL-6R, thereby inhibiting both classic and trans-signaling. Tocilizumab (Anti-Human IL6R, Humanized Antibody) can be used for the treatment of rheumatoid arthritis. Tocilizumab is remarkablely effective for the study of severe COVID-19 (coronavirus disease).
  • HY-N1746
    (2S)-2'-Methoxykurarinone

    2'-O-Methylkurarinone

    Others Cancer Metabolic Disease Inflammation/Immunology
    (2S)-2'-Methoxykurarinone, a compound isolated from the roots of Sophora flavescens, has anti-inflammatory, antipyretic, antidiabetic, and antineoplastic effects. (2S)-2'-Methoxykurarinone (MK) inhibits osteoclastogenesis and bone resorption through down-regulation of RANKL signaling. (2S)-2'-Methoxykurarinone (MK) displays cytotoxic activity against human myeloid leukemia HL-60 cells.
  • HY-13811
    NSC697923

    E1/E2/E3 Enzyme Apoptosis Cancer
    NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity.
  • HY-14743A
    Golotimod TFA

    SCV 07 TFA; Gamma-D-glutamyl-L-tryptophan TFA

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod TFA (SCV 07 TFA), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod TFA (SCV 07 TFA) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod TFA (SCV 07 TFA) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-112146
    MMG-11

    Toll-like Receptor (TLR) Inflammation/Immunology
    MMG-11 is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7 µM for Pam3CSK4-induced hTLR2/1 and 5.7 µM for Pam2CSK4-induced hTLR2/6 responses.
  • HY-135805
    JBJ-04-125-02

    EGFR Cancer
    JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.
  • HY-14743
    Golotimod

    SCV 07; Gamma-D-glutamyl-L-tryptophan

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-N0261
    Aurantio-obtusin

    Others Inflammation/Immunology Cardiovascular Disease
    Aurantio-obtusin is an anthraquinone isolated from Semen Cassiae, with anti-Inflammatory, anti-oxidative, anti-coagulating and anti-hypertension activities. Aurantio-obtusin relaxes systemic arteries through endothelial PI3K/AKT/eNOS-dependent signaling pathway in rats, thus acts as a new potential vasodilator. Aurantio-obtusin inhibits allergic responses in IgE-mediated mast cells and anaphylactic models and is potential for treatment for allergy-related diseases.
  • HY-126247
    BI-2852

    Ras Cancer
    BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRAS G12C inhibitor (binds to switch II pocket) because it binds to a different pocket present in both the active and inactive forms of KRAS. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
  • HY-125751
    UCSF924

    Dopamine Receptor Neurological Disease
    UCSF924 is a potent and specific dopamine D4 receptor (DRD4) partial agonist with a EC50 of 4.2 nM. UCSF924 has a high-affinity with a Ki value of 3 nM for DRD4 and shows no measurable affinity for D2, D3 or the F261V/L328F D4 mutant. UCSF924 is a 7.4-fold bias toward arrestin over Gαi/o signaling, referenced to quinpirole.
  • HY-N0632
    Esculentoside A

    COX NF-κB Inflammation/Immunology
    Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta. Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models, has selective inhibitory activity towards cyclooxygenase-2 (COX-2). Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways.
  • HY-128892
    EN6

    Autophagy Proton Pump Neurological Disease
    EN6 is a small-molecule in vivo activator of autophagy that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal the vacuolar H + ATPase (v-ATPase). EN6-mediated ATP6V1A modification decouples the v-ATPase from the Rags, leading to inhibition of mTORC1 signaling, increased lysosomal acidification and activation of autophagy. EN6 clears TDP-43 aggregates, a causative agent in frontotemporal dementia, in a lysosome-dependent manner.
  • HY-N2447
    Amarogentin

    AMPK Apoptosis Cancer Metabolic Disease
    Amarogentin is a secoiridoid glycoside that is mainly extracted from Swertia and Gentiana roots. Amarogentin exhibits many biological effects, including anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin exerts hepatoprotective and immunomodulatory effects. Amarogentin promotes apoptosis, arrests G2/M cell cycle and downregulates of PI3K/Akt/mTOR signalling pathways. Amarogentin exerts beneficial vasculo-metabolic effect by activating AMPK.
  • HY-108464A
    Phenamil methanesulfonate

    Sodium Channel TRP Channel Metabolic Disease Inflammation/Immunology
    Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca 2+ transport with an IC50 of 140 nM in a Ca 2+ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.
  • HY-123823
    Nitroaspirin

    NCX 4016

    COX Apoptosis Cancer
    Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins.
  • HY-19744
    T6167923

    MyD88 Inflammation/Immunology
    T6167923 is a potent and selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with an 50 of 2.7  μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively.
  • HY-110353
    CU-T12-9

    Toll-like Receptor (TLR) Cancer Infection Inflammation/Immunology
    CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
  • HY-122575
    Aurintricarboxylic acid

    P2X Receptor Influenza Virus Topoisomerase Infection Inflammation/Immunology Neurological Disease
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway.
  • HY-135680
    I-OMe-Tyrphostin AG 538

    I-OMe-AG 538

    IGF-1R Cancer Metabolic Disease
    I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM.
  • HY-12326A
    c-di-AMP sodium

    Cyclic diadenylate sodium; Cyclic-di-AMP sodium

    STING Bacterial Endogenous Metabolite Inflammation/Immunology
    c-di-AMP (Cyclic diadenylate) sodium is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP sodium is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP sodium acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.
  • HY-N1445
    Isoquercetin

    Quercetin 3-glucoside

    NF-κB NO Synthase Inflammation/Immunology Cancer
    Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway. Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies.
  • HY-N0103
    Sophocarpine

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-N0103A
    Sophocarpine monohydrate

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine (monohydrate) significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-18676
    OSU-T315

    Integrin Autophagy Apoptosis Cancer
    OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.
  • HY-12326
    c-di-AMP

    Cyclic diadenylate; Cyclic-di-AMP

    STING Bacterial Inflammation/Immunology
    c-di-AMP (Cyclic diadenylate) is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP (Cyclic diadenylate) is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP (Cyclic diadenylate) acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.
  • HY-N2038
    3,​5,​6,​7,​8,​3',​4'-​Heptemthoxyflavone

    Others Cancer Neurological Disease
    3,5,6,7,8,3',4'-heptamethoxyflavone, a flavonoid in C. unshiu peels, exhibits anti-tumor-initiating effect and Anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-heptamethoxyflavone inhibits collagenase activity and increased type I procollagen content in HDFn cells. 3,5,6,7,8,3',4'-heptamethoxyflavone induces brain-derived neurotrophic factor (BDNF) expression via cAMP/ERK/CREB signaling and reduces phosphodiesterase activity in C6 cells.
  • HY-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.
  • HY-N5072
    Desmethylglycitein

    4',6,7-Trihydroxyisoflavone

    CDK PI3K PKC Cancer
    Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.
  • HY-10624
    THIQ

    Melanocortin Receptor Metabolic Disease
    THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants.
  • HY-N2515
    Ginsenoside Rk1

    NF-κB PI3K JAK Apoptosis Cancer Inflammation/Immunology
    Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures. Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB. Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis. Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway.
  • HY-N1992
    Theaflavin 3,3'-digallate

    TF3

    Akt NF-κB MEK ERK Cancer
    Theaflavin 3,3'-digallate (TF3), the typical pigment in black tea, is a good antitumor agent. Theaflavin 3,3'-digallate is generally regarded as the effective component for the inhibitory effects against carcinogenesis without adverse side effects by affecting multiple signal transduction pathways, such as upregulating p53 and p21, inhibiting phosphorylation of the cell survival protein Akt and MAPK pathway, downregulation of NF-κB, shifting the ratio between pro-/antiapoptotic proteins. Theaflavin 3,3'-digallate causes a rapid and sustained decrease in phospho-ERK1/2 and -MEK1/2 protein expression. Theaflavin 3,3'-digallate inhibits HCT116 cell growth with an IC50 of 17.26 μM.
  • HY-12379
    NS-2028

    Guanylate Cyclase Inflammation/Immunology
    NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor with IC50 values of 30 nM and 200 nM for basal and NO-stimulated enzyme activity. NS-2028 inhibits soluble Guanylyl Cyclase activity in homogenates of mouse cerebellum and neuronal NO synthase with IC50 values of 17 nM and 20 nM. NS-2028 inhibits 3-morpholino-sydnonimine (SIN-1)-elicited formation of cyclic GMP in human cultured umbilical vein endothelial cells with an IC50 of 30 nM. NS-2028 is commonly used in the research of nitric oxide signaling pathways, it inhibits NO-dependent relaxant responses in non-vascular smooth muscle completely (1 μM). NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability.