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Results for "Also Recruited to Activated Integrins: Inhibitors" in MCE Product Catalog:

9835

Inhibitors & Agonists

67

Screening Libraries

47

Dye Reagents

23

Biochemical Assay Reagents

446

Peptides

6

MCE Kits

9

Inhibitory Antibodies

1640

Natural
Products

6

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-119339
    SX-682

    CXCR Cancer Inflammation/Immunology Endocrinology
    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.
  • 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-P0297
    Protease-Activated Receptor-4

    Protease-Activated Receptor (PAR) Others
    Protease-Activated Receptor-4 is the agonist of proteinase-activated receptor-4 (PAR4).
  • HY-P0283
    Protease-Activated Receptor-2, amide

    Protease-Activated Receptor (PAR) Cancer
    Protease-Activated Receptor-2, amide (SLIGKV-NH2) is a highly potent protease-activated receptor-2 (PAR2) activating peptide.
  • HY-133137A
    SJF620 hydrochloride

    PROTAC Btk Cancer
    SJF620 hydrochloride is a potent PROTAC BTK degrader with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN.
  • HY-133137
    SJF620

    PROTAC Btk Cancer
    SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN.
  • HY-101810
    Tazanolast

    to 188; Tazalest; Tazanol

    Others Inflammation/Immunology
    Tazanolast is a selective mast-cell-stabilizing drug, on ozone-induced airway hyperresponsiveness in guinea pigs.
  • HY-12290
    Arg-Gly-Asp-Ser

    RGDS peptide; Fibronectin tetrapeptide

    Integrin Inflammation/Immunology
    Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function, decreases systemic inflammation via inhibition of collagen-triggered activation of leukocytes and attenuates expression of inflammatory cytokines, iNOS and MMP-9.
  • HY-119486A
    (Rac)-Tavapadon

    (Rac)-PF-06649751; (Rac)-CVL-751

    Dopamine Receptor Neurological Disease
    (Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity.
  • HY-136572
    CEM114

    Epigenetic Reader Domain CRISPR/Cas9 Cancer
    CEM114 is an effective chemical epigenetic modifier (CEM) that recruits endogenous chromatin machinery through CRISPR-Cas9 systems.
  • HY-P2518
    Protease-Activated Receptor-1, PAR-1 Agonist

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    Protease-Activated Receptor-1, PAR-1 Agonist is a thrombin-specific, protease-activated receptor 1 (PAR-1)-specific agonist peptide.
  • HY-P1308
    SLIGRL-NH2

    Protease-Activated Receptor-2 Activating Peptide

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) is an agonist of Protease-Activated Receptor-2 (PAR-2).
  • HY-P1682
    Balixafortide

    POL6326

    CXCR Cancer
    Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects.
  • HY-P1682A
    Balixafortide TFA

    POL6326 TFA

    CXCR Cancer
    Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects.
  • HY-P2519
    Protease-Activated Receptor-3 (PAR-3) (1-6), human

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    Protease-Activated Receptor-3 (PAR-3) (1-6), human is a proteinase-activated receptor (PAR-3) agonist peptide.
  • HY-P1308A
    SLIGRL-NH2 TFA

    Protease-Activated Receptor-2 Activating Peptide TFA

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    SLIGRL-NH2 TFA (Protease-Activated Receptor-2 Activating Peptide TFA) is an agonist of Protease-Activated Receptor-2 (PAR-2).
  • HY-115537
    NAE-IN-M22

    Apoptosis Cancer
    NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.
  • HY-P2519A
    Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA is a proteinase-activated receptor (PAR-3) agonist peptide.
  • HY-43722
    Lenalidomide-Br

    Ligand for E3 Ligase Cancer
    Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC STAT3 degrader SD-36 (HY-129602).
  • HY-100506
    GLPG0187

    Integrin Cancer
    GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
  • 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-70073
    Zaurategrast

    CT7758

    Integrin Inflammation/Immunology
    Zaurategrast (CT7758) is a potent and oral-effective α4-integrin inhibitor.
  • HY-P1375
    [D-Trp7,9,10]-Substance P

    mAChR Endocrinology
    [D-Trp7,9,10]-Substance P is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P does not inhibit Gi/o activation by M2 ACh receptors.
  • HY-P1375A
    [D-Trp7,9,10]-Substance P TFA

    mAChR Endocrinology
    [D-Trp7,9,10]-Substance P TFA is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P TFA does not inhibit Gi/o activation by M2 ACh receptors.
  • HY-133987
    AP-1/NF-κB activation inhibitor 1

    NF-κB Inflammation/Immunology
    AP-1/NF-κB activation inhibitor 1 is a potent AP-1 and NF-κB mediated transcriptional activation inhibitor (IC50=1 μM), without blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells.
  • HY-128756
    SIAIS178

    PROTAC Bcr-Abl Cancer
    SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.
  • HY-P1328
    TAT-14

    Keap1-Nrf2 Others
    TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
  • HY-P0290A
    GRGDSP TFA

    Integrin Cancer
    GRGDSP (TFA) is an integrin inhibitor.
  • HY-P0178
    LXW7

    Integrin Inflammation/Immunology
    LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.
  • HY-P1740
    RGD peptide (GRGDNP)

    Integrin Apoptosis Inflammation/Immunology
    RGD peptide (GRGDNP) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
  • HY-N3196
    Neotuberostemonine

    Others Infection Inflammation/Immunology
    Neotuberostemonine, one of the main antitussive alkaloids in the root of Stemona tuberosa Lour, attenuates bleomycin-induced pulmonary fibrosis by suppressing the recruitment and activation of macrophages.
  • HY-P0178A
    LXW7 TFA

    Integrin Inflammation/Immunology
    LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.
  • HY-10255AS
    Sunitinib D10

    SU 11248 D10

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib D10 (SU 11248 D10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-P1740A
    RGD peptide (GRGDNP) (TFA)

    Integrin Apoptosis Inflammation/Immunology Cancer
    RGD peptide (GRGDNP) (TFA) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) (TFA) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
  • HY-P1376
    G-Protein antagonist peptide

    mAChR Adrenergic Receptor Endocrinology
    G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
  • HY-P0290
    GRGDSP

    Integrin Cancer
    GRGDSP, a synthetic linear RGD peptide, is an integrin inhibitor.
  • HY-P1376A
    G-Protein antagonist peptide TFA

    mAChR Adrenergic Receptor Endocrinology
    G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-50937
    ST 2825

    MyD88 Inflammation/Immunology
    ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity.
  • HY-100445
    αvβ1 integrin-IN-1

    Integrin Cancer Cardiovascular Disease
    αvβ1 integrin-IN-1 (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC50 of 0.63 nM. Antifibrotic effects.
  • HY-100431
    IMR-1

    Notch Cancer
    IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with an IC50 of 26 μM. IMR-1 prevents the recruitment of Mastermind-like 1 (Maml1) to the Notch Ternary Complex (NTC) on chromatin, inhibits Notch target gene transcription and dramatically inhibits tumor growth.
  • HY-100445A
    αvβ1 integrin-IN-1 TFA

    Integrin Cancer Cardiovascular Disease
    αvβ1 integrin-IN-1 TFA (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC50 of 0.63 nM. Antifibrotic effects.
  • HY-P1328A
    TAT-14 TFA

    Keap1-Nrf2 Others
    TAT-14 TFA is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 TFA has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
  • HY-134130
    Integrin modulator 1

    Integrin Inflammation/Immunology
    Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM.
  • HY-125996
    NR1H4 activator 1

    FXR Inflammation/Immunology
    NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease.
  • HY-110247
    TRAF-STOP inhibitor 6877002

    TNF Receptor NF-κB Inflammation/Immunology Cardiovascular Disease
    TRAF-STOP inhibitor 6877002, is a selective inhibitor of CD40-TRAF6 interaction, compound VII, shows inhibition of NF-κB activation in RAW cells, extracted from patent WO2014033122A1. TRAF-STOP 6877002 prevents the progression of established atherosclerosis in mice, reduces leukocyte recruitment and reduces macrophage activation; reduces macrophage proliferation in atherosclerotic plaques.
  • HY-115677
    ILK-IN-3

    Integrin Cancer
    ILK-IN-3 is an integrin linked kinase inhibitor with antitumor activity.
  • 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-117958
    HJC0197

    Others Cancer Metabolic Disease Cardiovascular Disease
    HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP.
  • HY-15870
    SR 11302

    Others Cancer Inflammation/Immunology
    SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE).
  • HY-130119
    Integrin-IN-2

    Integrin Cancer
    Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC50 values of 7.8, 8.4, 8.4 and 7.4, respectively.
  • HY-100563
    Cyclo(RGDyK) trifluoroacetate

    Integrin Cancer
    Cyclo(RGDyK) trifluoroacetate is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
  • HY-100563A
    Cyclo(RGDyK)

    Integrin Cancer
    Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
  • HY-14857
    Carotegrast

    Integrin Inflammation/Immunology
    Carotegrast is an orally available α4 integrin receptor inhibitor with anti-inflammatories activities.
  • HY-18668
    Integrin Antagonists 27

    Integrin Cancer
    Integrin Antagonists 27 is a small molecule integrin αvβ3 antagonist with binding affinity of 18 nM, as s novel anticancer agent.
  • 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-U00434
    3BDO

    mTOR Autophagy Apoptosis Cancer
    3BDO is a new mTOR activator which can also inhibit autophagy.
  • 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-115576
    P62-mediated mitophagy inducer

    PMI

    Mitophagy Neurological Disease
    P62-mediated mitophagy inducer is a mitophagy regulator which activates mitophagy without recruiting Parkin or collapsing ΔΨm and retains activity in cells devoid of a fully functional PINK1/Parkin pathway.
  • HY-108831
    Natalizumab

    Integrin Inflammation/Immunology
    Natalizumab is a recombinant, humanized monoclonal antibody, binds to α4β1-integrin and blocks its interaction with vascular cell adhesion molecule-1 (VCAM-1). Natalizumab can be used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease. Natalizumab is also the first targeted therapy which blocks an essential mechanism for lymphocyte entry to the CNS and thus prevents acute demyelinating relapses.
  • HY-102011
    BMS-1166

    PD-1/PD-L1 Cancer Inflammation/Immunology
    BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
  • HY-P0078
    TRAP-6

    PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4.
  • HY-17369
    Tirofiban hydrochloride monohydrate

    Integrin Cardiovascular Disease
    Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist IC50 value: Target: integrin IIb/IIIa Tirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation.
  • HY-108434
    Ceapin-A7

    Others Metabolic Disease Neurological Disease
    Ceapin-A7 is a selective blocker of ATF6α signaling in response to ER stress, with an IC50 of 0.59 μM. Ceapin-A7 can be used to explore both the mechanism of activation of ATF6α and its role in pathological settings.
  • 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-P0023
    Cyclo(-RGDfK)

    Integrin Cancer
    Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-111413
    c(phg-isoDGR-(NMe)k)

    Integrin Cancer
    c(phg-isoDGR-(NMe)k) is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM.
  • HY-P0023A
    Cyclo(-RGDfK) TFA

    Integrin Cancer
    Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
  • HY-P1613A
    Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA

    Integrin Cancer
    Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitor of integrin αvβ3, with antitumor activity.
  • 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-111413A
    c(phg-isoDGR-(NMe)k) TFA

    Integrin Cancer
    c(phg-isoDGR-(NMe)k) TFA is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM.
  • HY-15027
    5-Aminosalicylic Acid

    Mesalamine; 5-ASA; Mesalazine

    PPAR PAK NF-κB Endogenous Metabolite Inflammation/Immunology Cancer
    5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-12290A
    Arg-Gly-Asp-Ser (TFA)

    RGDS peptide (TFA); Fibronectin tetrapeptide (TFA)

    Integrin Inflammation/Immunology
    Arg-Gly-Asp-Ser (TFA) is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser (TFA) directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1.
  • HY-17369B
    Tirofiban

    L700462; MK383

    Integrin Cardiovascular Disease
    Tirofiban(L700462;MK383) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist Target: integrin IIb/IIIa Tirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation.
  • HY-19121A
    TCV-309 chloride

    Others Cancer
    TCV-309 chloride is a potent and specific platelet activating factor (PAF) antagonist. TCV-309 chloride specifically inhibits PAF-induced aggregation of rabbit and human platelets, and [3H]PAF binding to rabbit platelet microsomes with IC50 values of 33 nM, 58 nM and 27 nM, respectively. TCV-309 chloride has beneficial effects in anaphylactic shock.
  • 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-101042
    AG-494

    Tyrphostin AG 494

    EGFR CDK Cancer
    AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis.
  • 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-15002
    AST 487

    NVP-AST 487

    RET FLT3 VEGFR c-Kit Bcr-Abl Cancer
    AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
  • HY-N6631
    7-Methoxyisoflavone

    AMPK Metabolic Disease Cancer
    7-Methoxyisoflavone is an isoflavone derivative and also an activator of adenosine monophosphate-activated protein kinase (AMPK).
  • HY-14165
    Veliflapon

    BAY X 1005; DG-031

    FLAP Leukotriene Receptor Inflammation/Immunology Cardiovascular Disease
    Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.
  • HY-13535
    ATN-161

    Integrin Cancer
    ATN-161 is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
  • HY-16143
    Cilengitide TFA

    EMD 121974 TFA

    Integrin Autophagy Cancer
    Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.
  • HY-13535A
    ATN-161 trifluoroacetate salt

    ATN-161 TFA salt

    Integrin Cancer
    ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
  • HY-129453
    BOP sodium

    Integrin Inflammation/Immunology
    BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins.
  • HY-101047
    D-erythro-Sphingosine

    Erythrosphingosine; erythro-C18-Sphingosine; trans-4-Sphingenine

    PKC Phosphatase Endogenous Metabolite Cancer
    D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
  • HY-115497
    BRD5529

    E1/E2/E3 Enzyme Inflammation/Immunology
    BRD5529 is a selective CARD9-E3 ubiquitin ligase TRIM62 protein-protein interaction inhibitor with an IC50 of 8.6 μM. BRD5529 directly and selectively binds CARD9, disrupts TRIM62 recruitment, inhibits TRIM62-mediated ubiquitinylation and activation of CARD9, and demonstrates cellular activity and selectivity in CARD9-dependent pathways.
  • HY-113313
    Aldosterone

    Endogenous Metabolite Cardiovascular Disease
    Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level.
  • HY-W010907
    Pamoic acid disodium

    ERK Neurological Disease
    Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect.
  • 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-100965
    Diphenyleneiodonium chloride

    DPI

    TRP Channel NADPH Oxidase Reactive Oxygen Species Inflammation/Immunology Neurological Disease
    Diphenyleneiodonium chloride is a NADPH oxidase (NOX) inhibitor and also functions as a TRPA1 activator with an EC50 of 1 to 3 μM. Diphenyleneiodonium chloride selectively inhibits intracellular reactive oxygen species.
  • HY-15122
    Sinomenine

    NF-κB Opioid Receptor Autophagy Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Sinomenine, an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.
  • HY-100164
    SDZ-MKS 492

    MKS 492

    Phosphodiesterase (PDE) Inflammation/Immunology
    SDZ-MKS 492 (MKS 492) is a selective inhibitor of cyclic GMP-inhibited phosphodiesterase (type III PDE). SDZ-MKS 492 inhibits antigen- or platelet activating factor (PAF)-induced bronchoconstriction and allergic reactions in guinea pigs and rats.
  • HY-15122A
    Sinomenine hydrochloride

    Cucoline hydrochloride

    NF-κB Opioid Receptor Autophagy Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.
  • HY-13694
    Methionine

    MRX-1024; D-Methionine

    GABA Receptor Cancer Neurological Disease
    Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
  • HY-103349
    PETCM

    Caspase Apoptosis Cancer
    PETCM is an activator of caspase-3 and acts as an cytochrome c (cyto c)-dependent manner. PETCM promotes Apaf-1 oligomerization and induces cell apoptosis in HeLa cells.
  • HY-117917
    (Rac)-MGV354

    Guanylate Cyclase Inflammation/Immunology Cardiovascular Disease
    (Rac)-MGV354 is the racemate of MGV354. MGV354 is a soluble guanylate cyclase (sGC) activator with EC50s of <0.5 nM, and 5 nM in CHO and GTM-3 E cells, respectively.
  • HY-16141
    Cilengitide

    EMD 121974

    Integrin Autophagy Cancer
    Cilengitide (EMD 121974) is a potent and selective inhibitor of the integrins ανβ3 and ανβ5. Cilengitide inhibits binding of isolated ανβ3 and ανβ5 to Vitronectin with an IC50 value of 4 and 79 nM, respectively .
  • HY-13856
    (R)-PS210

    PDK-1 Cancer
    (R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment.
  • HY-16785
    Veledimex

    INXN-1001; RG-115932

    Interleukin Related Cancer Inflammation/Immunology
    Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys.
  • HY-12545
    Brevetoxin-3

    PbTx-3

    Sodium Channel Inflammation/Immunology
    Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na + channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na + channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.
  • HY-13417A
    AICAR phosphate

    Acadesine phosphate; AICA Riboside phosphate

    AMPK Autophagy YAP Mitophagy Cancer
    AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.
  • HY-13417
    AICAR

    Acadesine; AICA Riboside

    AMPK Autophagy YAP Mitophagy Cancer
    AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
  • HY-13650
    Indisulam

    E 7070

    Carbonic Anhydrase Cancer
    Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15.
  • HY-B0167A
    Sodium Salicylate

    Salicylic acid sodium salt; 2-Hydroxybenzoic acid sodium salt

    COX NF-κB Ribosomal S6 Kinase (RSK) Autophagy Apoptosis Inflammation/Immunology Cancer
    Sodium Salicylate (Salicylic acid sodium salt) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation. Sodium Salicylate is also a S6K inhibitor.Sodium Salicylate is a NF-κB inhibitor that decreases inflammatory gene expression and improves repair in aged muscle.
  • HY-W015445
    SD-169

    p38 MAPK Metabolic Disease
    SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.
  • HY-10249
    GSK-690693

    Akt AMPK Autophagy Cancer
    GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation.
  • HY-19700
    trans-Zeatin

    MEK ERK Endogenous Metabolite Others
    trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
  • HY-107589A
    BIO5192 hydrate

    Integrin Inflammation/Immunology
    BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.
  • HY-107589
    BIO5192

    Integrin Inflammation/Immunology
    BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.
  • HY-18935A
    CBL0137 hydrochloride

    Curaxin-137 hydrochloride; CBL-C137 hydrochloride

    MDM-2/p53 NF-κB Cancer
    CBL0137 hydrochloride is an inhibitor of the histone chaperone, FACT. CBL0137 hydrochloride can also activate p53 and inhibits NF-κB with EC50s of 0.37 and 0.47 µM, respectively.
  • 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-19344
    Lifitegrast

    SAR 1118; SHP-606

    Integrin Inflammation/Immunology
    Lifitegrast (SAR 1118) is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
  • HY-N2337
    11beta-Hydroxyprogesterone

    11β-Hydroxyprogesterone

    Endogenous Metabolite Cardiovascular Disease
    11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED50 of 10 nM.
  • HY-131265
    Mesalamine impurity P

    PPAR PAK NF-κB Cancer Inflammation/Immunology
    Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-50730
    Asparagusic acid

    Parasite Infection
    Asparagusic acid is a sulfur-containing flavor component produced by asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
  • HY-13259
    MG-132

    Z-Leu-Leu-Leu-al; MG132

    Proteasome Autophagy Apoptosis Cancer
    MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.
  • HY-14571
    E7820

    ER68203-00

    Integrin Cancer
    E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity.
  • HY-117388
    THI0019

    Integrin Inflammation/Immunology
    THI0019 is a potent integrin α4β1 (VLA-4) agonist with an EC50 range of 1-2 μM. THI0019 induces stem/progenitor cells adhesion. THI0019 also regulates adhesion mediated by α4β7, α5β1 and αLβ2.
  • HY-122203
    PCS1055 dihydrochloride

    mAChR AChE Neurological Disease
    PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively.
  • HY-N0014
    Icariin

    Ieariline

    Phosphodiesterase (PDE) PPAR Autophagy Inflammation/Immunology Cardiovascular Disease Cancer
    Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.
  • HY-118521
    AS-041164

    PI3K Inflammation/Immunology
    AS-041164 is a potent, selective and orally active PI3Kγ isoform inhibitor with an IC50 of 70 nM. AS-041164 shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). AS-041164 has anti-inflammatory effects.
  • HY-115292
    Simvastatin hydroxy acid sodium

    Tenivastatin sodium; Simvastatin Impurity A sodium

    HMG-CoA Reductase (HMGCR) Cancer
    Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
  • HY-N0509
    Astilbin

    Keap1-Nrf2 TNF Receptor NF-κB Inflammation/Immunology Cancer
    Astilbin, a flavonoid compound, is isolated from the rhizome of Smilax glabra. Astilbin enhances NRF2 activation. Astilbin also suppresses TNF-α expression and NF-κB activation.
  • HY-11067
    WHI-P97

    JAK Inflammation/Immunology
    WHI-P97 is a potent and selective JAK-3 inhibitor. WHI-P97 is effective in preventing the development allergic asthma in vivo.
  • HY-P9911
    Vedolizumab

    Anti-Human lymphocyte α4β7 integrin, Humanized Antibody

    Integrin Inflammation/Immunology
    Vedolizumab is a humanized monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.
  • HY-P0278
    RGD

    Integrin Cancer
    RGD is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; binds to integrins.
  • HY-101923B
    LYN-1604 dihydrochloride

    ULK Autophagy Apoptosis Cancer
    LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).
  • HY-101923A
    LYN-1604 hydrochloride

    ULK Autophagy Apoptosis Cancer
    LYN-1604 hydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).
  • HY-101923
    LYN-1604

    ULK Autophagy Apoptosis Cancer
    LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).
  • HY-18711A
    SCR-1481B1

    c-Met inhibitor 2

    c-Met/HGFR VEGFR Cancer
    SCR-1481B1 (c-Met inhibitor 2) is a potent compound that has activity against cancers dependent upon Met activation and also has activity against cancers as a VEGFR inhibitor.
  • HY-N0141
    Parthenolide

    (-)-Parthenolide

    NF-κB Autophagy Mitophagy Apoptosis Cancer
    Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.
  • HY-16592
    Brefeldin A

    BFA; Cyanein; Decumbin

    Autophagy CRISPR/Cas9 Mitophagy HSV Antibiotic Cancer Infection
    Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity.
  • HY-N1504
    Loureirin B

    PAI-1 Potassium Channel ERK JNK Metabolic Disease
    Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
  • HY-17039
    Alcaftadine

    R89674

    Histamine Receptor Inflammation/Immunology Endocrinology
    Alcaftadine (R89674) is a histamine H1 receptor antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis. Alcaftadine is a broad-spectrum antihistamine displaying a high affinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. Alcaftadine also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects.
  • HY-P2267
    LDV

    Integrin
    LDV, a non-fluorescent derivative of LDV FITC, is a α4β1 integrin (VLA-4) ligand (Kd ~ 12 nM).
  • HY-P0278A
    RGD Trifluoroacetate

    Integrin Cancer
    RGD Trifluoroacetate is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; RGD Trifluoroacetate binds to integrins.
  • HY-B1505
    Acefylline

    Theophyllineacetic acid; Theophylline-7-acetic acid

    Adenosine Receptor Protein Arginine Deiminase Phosphodiesterase (PDE) Cancer
    Acefylline (Theophyllineacetic acid), a xanthine derivative, is an adenosine receptor antagonist. Acefylline is a peptidylarginine deiminase (PAD) activator. Acefylline is also a bronchodilator, which inhibits rat lung cAMP phosphodiesterase isoenzymes.
  • HY-124290
    Carotegrast methyl

    AJM300

    Integrin Inflammation/Immunology
    Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of AJM300, is a specific, dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice.
  • 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-N6065
    Praeruptorin A

    NF-κB Inflammation/Immunology
    Praeruptorin A is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin A exerts anti-inflammatory effects in vitro through inhibition of NF-κB activation.
  • HY-N0878
    Bufotalin

    Apoptosis Reactive Oxygen Species Cancer
    Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation.
  • HY-N0139
    Troxerutin

    Trihydroxyethylrutin

    NOD-like Receptor (NLR) Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
    Troxerutin, also known as vitamin P4, is a tri-hydroxyethylated derivative of natural bioflavonoid rutins which can inhibit the production of reactive oxygen species (ROS) and depress ER stress-mediated NOD activation.
  • HY-16031
    AFP464 free base

    NSC710464 free base

    HIF/HIF Prolyl-Hydroxylase Cancer
    AFP464 free base (NSC710464 free base), is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.
  • 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-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-B1546
    Benzamil

    Benzylamiloride

    Sodium Channel Na+/Ca2+ Exchanger Neurological Disease
    Benzamil (Benzylamiloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
  • HY-B1546A
    Benzamil hydrochloride

    Benzylamiloride hydrochloride

    Na+/Ca2+ Exchanger Sodium Channel Neurological Disease
    Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
  • HY-137331
    FAPI-46

    Others Cancer
    FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted radiotracer. FAPI-46 has higher tumor uptake and prolonged tumor accumulation. FAPI-46 can be used for tumor imaging of a multitude of different cancers.
  • HY-N0039
    Ginsenoside Rb1

    Gypenoside III

    Na+/K+ ATPase IRAK NF-κB Autophagy Mitophagy HSV Inflammation/Immunology Cancer
    Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na +, K +-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .
  • HY-10595
    RO-28-1675

    Glucokinase Metabolic Disease
    RO-28-1675 is a potent allosteric glucokinase (GK) activator with an EC50 of 54 nM. RO-28-1675 can be used for the research of type 2 diabetes.
  • HY-P0031
    Cyclo(RADfK)

    Integrin Others
    Cyclo(RADfK) is a selective α(v)β(3) integrin ligand that has been extensively used for research, therapy, and diagnosis of neoangiogenesis.
  • HY-19793
    RS-1

    RAD51 CRISPR/Cas9 Cancer
    RS-1 is a RAD51 activator, and also increases CRISPR/Cas9-mediated knock-in efficiencies.
  • HY-100489
    TBHQ

    tert-Butylhydroquinone

    Keap1-Nrf2 ERK Autophagy Apoptosis Ferroptosis Cancer
    TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2. TBHQ (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma.
  • HY-N0822
    Shikonin

    C.I. 75535; Isoarnebin 4

    Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV Cancer
    Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.
  • HY-B1221
    Flufenamic acid

    COX AMPK Potassium Channel Chloride Channel Calcium Channel Parasite Inflammation/Immunology
    Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
  • HY-P1536
    Thrombin Receptor Activator for Peptide 5 TRAP-5

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Thrombin Receptor Activator for Peptide 5 (TRAP-5) is also called Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), used in the research of coronary heart disease (CHD).
  • HY-19356
    Rocaglamide

    Roc-A

    NF-κB HSP Eukaryotic Initiation Factor (eIF) Cancer
    Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.
  • 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-N0112
    Dihydromyricetin

    Ampelopsin; Ampeloptin

    mTOR Influenza Virus DNA/RNA Synthesis Autophagy Cancer Infection
    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). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 μM.
  • HY-108372
    Boc-C5-O-C5-O-C6-Cl

    PROTAC Linker 2

    PROTAC Linker Cancer
    Boc-C5-O-C5-O-C6-Cl (PROTAC Linker 2) is a PROTAC linker utilized to connect the respective tyrosine kinase inhibitor (TKI) to the E3 recruiting ligand.
  • 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-122727
    STL127705

    DNA-PK Cancer
    STL127705 (Compound L) is a Ku 70/80 heterodimer protein inhibitor, inhibits Ku70/80-DNA interaction, with an IC50 of 3.5 μM. STL127705 also inhibits Ku-dependent activation of DNA-PKCS kinase (IC50, 2.5 μM).
  • HY-16696
    SN 2

    TRP Channel Infection
    SN 2 is a potent activator of TRPML3 ion channel with an EC50 of 1.8 μM. SN 2 also acts as a potent inhibitor of Dengue virus 2 (DENV2) and Zika virus (ZIKV).
  • HY-15394
    (Rac)-Rotigotine hydrochloride

    Dopamine Receptor Adrenergic Receptor 5-HT Receptor Endocrinology Neurological Disease
    (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
  • HY-101180
    C2 Ceramide

    Ceramide 2

    Phosphatase Mitochondrial Metabolism Apoptosis Endocrinology Metabolic Disease
    C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss.
  • 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-18644
    CWHM-12

    Integrin Cancer
    CWHM-12 is a potent inhibitor of αV integrins with IC50s of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1.
  • HY-P2230
    Angstrom6

    A6 Peptide

    PAI-1 Cancer
    Angstrom6 (A6 Peptide) is an 8 amino-acid peptide derived from single-chain urokinase plasminogen activator (scuPA) and interferes with the uPA/uPAR cascade and abrogates downstream effects. Angstrom6 binds to CD44 resulting in the inhibition of migration, invasion, and metastasis of tumor cells, and the modulation of CD44-mediated cell signaling.
  • HY-N6748
    Roquefortine C

    P-glycoprotein Cytochrome P450 Bacterial Cancer Infection
    Roquefortine C, a fungal cyclopeptide isolated from Penicillium roquefortii, activates P-gp and also inhibits P450-3A and other haemoproteins. Roquefortine C has bacteriostatic activities against Gram-positive bacteria.
  • HY-102004
    Rilapladib

    SB 659032

    Phosphatase Inflammation/Immunology Neurological Disease
    Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM. Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist.
  • HY-130822
    K-Ras ligand-Linker Conjugate 4

    Target Protein Ligand-Linker Conjugate Cancer
    K-Ras ligand-Linker Conjugate 4 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 4 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
  • HY-130823
    K-Ras ligand-Linker Conjugate 5

    Target Protein Ligand-Linker Conjugate Cancer
    K-Ras ligand-Linker Conjugate 5 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 5 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
  • HY-130991
    K-Ras ligand-Linker Conjugate 6

    Target Protein Ligand-Linker Conjugate Cancer
    K-Ras ligand-Linker Conjugate 6 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
  • HY-130707
    K-Ras ligand-Linker Conjugate 3

    Target Protein Ligand-Linker Conjugate Cancer
    K-Ras ligand-Linker Conjugate 3 (Compound 001371) incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 3 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
  • HY-124858
    SC99

    STAT JAK Apoptosis Cancer Cardiovascular Disease
    SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities.
  • HY-12736
    GSK143

    Syk PERK Cancer Inflammation/Immunology
    GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC50=7.1). GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.
  • HY-12736A
    GSK143 dihydrochloride

    Syk PERK Cancer Inflammation/Immunology
    GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1). GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.
  • HY-14600
    Rosiglitazone maleate

    BRL 49653C

    PPAR TRP Channel Autophagy Ferroptosis Cancer Metabolic Disease Inflammation/Immunology
    Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
  • HY-103238
    RSVA405

    AMPK STAT Autophagy Metabolic Disease Inflammation/Immunology Neurological Disease
    RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 also can be used for the research of obesity.
  • HY-118628
    N-(p-amylcinnamoyl) Anthranilic Acid

    ACA

    Phospholipase TRP Channel Cardiovascular Disease
    N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker. N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia.
  • HY-15477A
    YS-49 monohydrate

    Akt PI3K Angiotensin Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology
    YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
  • HY-15477
    YS-49

    Akt PI3K Angiotensin Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology
    YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
  • 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-126457
    Thalidomide-propargyl

    Ligand for E3 Ligase Cancer
    Thalidomide-propargyl is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-propargyl can be connected to the ligand for protein by a linker to form the IMiD containing PROTACs.
  • HY-P1187
    HSDVHK-NH2

    Integrin Cancer
    HSDVHK-NH2 is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM).
  • HY-13030
    (+)-JQ-1

    JQ1

    Epigenetic Reader Domain Autophagy Ligand for Target Protein for PROTAC Cancer
    (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.
  • HY-12005
    Fingolimod hydrochloride

    FTY720

    LPL Receptor PAK Inflammation/Immunology Cancer
    Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1 activator.
  • HY-P1187A
    HSDVHK-NH2 TFA

    Integrin Cancer
    HSDVHK-NH2 TFA is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM).
  • HY-120217
    VH032

    Ligand for E3 Ligase Cancer
    VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a Kd
  • HY-N6641
    Monascin

    Others Cancer Inflammation/Immunology
    Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor).
  • HY-N0722
    Neochlorogenic acid

    trans-5-O-Caffeoylquinic acid

    NF-κB Interleukin Related TNF Receptor COX Inflammation/Immunology Cancer
    Neochlorogenic acid is a natural polyphenolic compound found in dried fruits and other plants. Neochlorogenic acid inhibits the production of TNF-α and IL-1β. Neochlorogenic acid suppresses iNOS and COX-2 protein expression. Neochlorogenic acid also inhibits phosphorylated NF-κB p65 and p38 MAPK activation.
  • HY-W009724
    2-Aminoethyl diphenylborinate

    2-APB

    Calcium Channel TRP Channel Infection
    2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R. 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca 2+ (SOC) channel and activates some TRP channels (V1, V2 and V3).
  • 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-15271
    WYE-687

    mTOR PI3K Cancer
    WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
  • HY-100415
    UKI-1

    UKI-1C

    PAI-1 Ser/Thr Protease Infection Cancer
    UKI-1 (UKI-1C) is a potent urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 0.41 μM. UKI-1 is also a low molecular weight serine protease inhibitor. UKI-1 is a potent antimetastatic agent and inhibits the invasive capacity of carcinoma cells.
  • 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-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-117102
    ANI-7

    Aryl Hydrocarbon Receptor Checkpoint Kinase (Chk) Cancer
    ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines.
  • HY-14994
    SCH79797 dihydrochloride

    Protease-Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
  • HY-112257
    S-23

    Androgen Receptor Metabolic Disease
    S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats.
  • HY-108391
    C8-Ceramide

    N-Octanoyl-D-erythro-sphingosine

    Apoptosis PKC Autophagy Cancer Inflammation/Immunology
    C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro.
  • HY-103087
    FIN56

    Ferroptosis Others
    FIN56 is a specific inducer of ferroptosis. FIN56 induces ferroptosis by inducing degradation of GPX4. FIN56 also binds to and activates squalene synthase.
  • HY-15371
    Forskolin

    Coleonol; Colforsin

    Adenylate Cyclase FXR Autophagy Cancer Endocrinology Metabolic Disease Inflammation/Immunology
    Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.
  • HY-101084
    NSC 228155

    EGFR Histone Acetyltransferase Epigenetic Reader Domain Cancer
    NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM.
  • HY-13423
    Tenovin-1

    MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy Cancer
    Tenovin-1, a p53 activator, protects p53 from MDM2-mediated degradation. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a dihydroorotate dehydrogenase (DHODH) inhibitor.
  • HY-12467
    OTS964 hydrochloride

    TOPK CDK Apoptosis Cancer
    OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM. OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.
  • HY-B0808
    Oxaprozin

    Oxaprozinum; Wy21743

    COX NF-κB Inflammation/Immunology Cancer
    Oxaprozin is an inhibitor of both COX-1 and COX-2 with IC50s of 2.2 μM and 36 μM for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB.
  • HY-134205A
    CBR-470-1

    Keap1-Nrf2 Metabolic Disease Neurological Disease
    CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP +-induced cytotoxicity through activation of the Keap1-Nrf2 cascade.
  • HY-B2145
    Ilaprazole sodium

    IY-81149 sodium

    Proton Pump TOPK Cancer Inflammation/Immunology
    Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
  • HY-122808
    (-)-Camphoric acid

    mGluR Metabolic Disease
    (-)-Camphoric acid is the less active enantiomer of Camphoric acid. Camphoric acid stimulates osteoblast differentiation and induces glutamate receptor expression. Camphoric acid also significantly induced the activation of NF-κB and AP-1.
  • HY-B0258
    Gemfibrozil

    CI-719

    PPAR Cytochrome P450 Metabolic Disease Cardiovascular Disease
    Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering drug; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
  • HY-B0764
    Bucladesine sodium

    Dibutyryl cAMP sodium salt; DBcAMP sodium salt

    PKA Phosphodiesterase (PDE) Inflammation/Immunology
    Bucladesine sodium salt (Dibutyryl-cAMP sodium salt) is a stabilized cyclic AMP (cAMP) analog and a selective PKA activator. Bucladesine sodium salt raises the intracellular levels of cAMP. Bucladesine sodium salt is also a phosphodiesterase (PDE) inhibitor. Bucladesine sodium salt has anti-inflammatory activity and can be used for impaired wound healing.
  • HY-106199
    Adenosine A1 receptor activator T62

    Adenosine Receptor Inflammation/Immunology Neurological Disease
    Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor. Adenosine A1 receptor activator T62 produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain.
  • HY-16561
    Resveratrol

    trans-Resveratrol; SRT501

    IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Keap1-Nrf2 Cancer Infection Inflammation/Immunology
    Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
  • HY-118482
    Sauristolactam

    Saurolactam

    Others Neurological Disease
    Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus chinensis, has significant neuroprotective activity against glutamate-induced toxicity in primary cultured rat cortical cells. Sauristolactam also inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation.
  • HY-13757A
    Tamoxifen

    ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. Tamoxifen activates autophagy and induces apoptosis.
  • HY-23095
    Thalidomide-5-OH

    Ligand for E3 Ligase Cancer
    Thalidomide-5-OH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTACs.
  • HY-107212
    Selamectin

    Parasite Chloride Channel P-glycoprotein Infection
    Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM.
  • HY-P1333
    Dynorphin A

    Opioid Receptor Neurological Disease
    Dynorphin A, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A also serve as an agonist for other opioid receptors,  such as mu (MOR) and delta (DOR).
  • HY-103667
    2-HBA

    Caspase Cancer
    2-HBA is a potent inducer of NAD(P)H:quinone acceptor oxidoreductase 1 (NQO1) which can also activate caspase-3 and caspase-10.
  • HY-101664
    Ilaprazole

    IY-81149

    Proton Pump TOPK Cancer Inflammation/Immunology
    Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
  • 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-17363
    Dimethyl fumarate

    DMF

    Keap1-Nrf2 Reactive Oxygen Species HIV Autophagy Endogenous Metabolite Cancer Infection Inflammation/Immunology Neurological Disease
    Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research.
  • HY-100530B
    Sp-cAMPS

    PKA Phosphodiesterase (PDE) Neurological Disease
    Sp-cAMPS, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS binds the PDE10 GAF domain with an EC50 of 40 μM.
  • HY-100530C
    Sp-cAMPS sodium salt

    PKA Phosphodiesterase (PDE) Neurological Disease
    Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM.
  • HY-123109
    (S,R,S)-AHPC-Boc

    VH032-Boc

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC-Boc (VH032-Boc) is a ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Boc is used in PROTAC technology.
  • 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-116364
    AZT triphosphate

    3'-Azido-3'-deoxythymidine-5'-triphosphate

    HIV DNA/RNA Synthesis HBV Reactive Oxygen Species Apoptosis Infection
    AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate also inhibits the DNA polymerase of HBV. AZT triphosphate activates the mitochondria-mediated apoptosis pathway.
  • HY-130604
    DT2216

    PROTAC Apoptosis Cancer
    DT2216 is a potent and selective BCL-XL degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.
  • HY-15271A
    WYE-687 dihydrochloride

    mTOR PI3K Cancer
    WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
  • HY-126020
    Bractoppin

    DNA/RNA Synthesis RAD51 Cancer
    Bractoppin is a potent and selective drug-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem(t) BRCT domain (binding IC50: 74 nM). Bractoppin diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. Bractoppin preferentially inhibits BRCA1 tBRCT-dependent steps in the DNA damage response.
  • HY-13757
    Tamoxifen Citrate

    ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. Tamoxifen Citrate activates autophagy and induces apoptosis.
  • HY-103597
    Thalidomide-O-COOH

    Cereblon ligand 3; E3 ligase Ligand 3

    Ligand for E3 Ligase Others
    Thalidomide-O-COOH (Cereblon ligand 3) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs.
  • HY-P1333A
    Dynorphin A TFA

    Opioid Receptor Neurological Disease
    Dynorphin A TFA, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A TFA also serve as an agonist for other opioid receptors,  such as mu (MOR) and delta (DOR).
  • HY-P1594
    Dynorphin A 1-10

    Opioid Receptor iGluR Neurological Disease
    Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.
  • HY-78263
    MNS

    NSC 170724; 5-(2-Nitrovinyl)benzodioxole

    Src Syk Cancer
    MNS (NSC 170724), the beta-nitrostyrene derivative, is a potent tyrosine kinase inhibitor and a broad-spectrum antiplatelet agent. MNS completely inhibits U46619, ADP-, arachidonic acid-, collagen-, and thrombin-induced platelet aggregation with IC50 values of 2.1, 4.1, 5.8, 7.0, and 12.7 μM, respectively. MNS inhibits Src, Syk, and FAK with IC50 of 27.3, 2.8, and 97.6 μM, respectively.
  • HY-P1098
    Ac2-26

    NF-κB Inflammation/Immunology
    Ac2-26, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue.
  • HY-W058849
    MT 63-78

    AMPK mTOR Apoptosis Cancer
    MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects.
  • HY-B0116
    Stavudine

    d4T

    Reverse Transcriptase HIV Nucleoside Antimetabolite/Analog NOD-like Receptor (NLR) Autophagy Apoptosis Infection
    Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis.
  • HY-B0116A
    Stavudine sodium

    d4T sodium

    Reverse Transcriptase HIV Nucleoside Antimetabolite/Analog NOD-like Receptor (NLR) Autophagy Apoptosis Infection
    Stavudine (d4T) sodium is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine sodium has activity against HIV-1 and HIV-2. Stavudine sodium also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine sodium reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine sodium induces apoptosis.
  • HY-108573
    P-1075

    Potassium Channel Cardiovascular Disease
    P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts.
  • HY-P0122
    iRGD peptide

    c(CRGDKGPDC)

    Integrin Cancer
    iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of drugs by first binding to av integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
  • HY-11063
    Fingolimod

    FTY720 free base

    LPL Receptor PAK Cancer Inflammation/Immunology
    Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant.
  • HY-W020790
    Sialyl-Lewis X

    sLeX

    Others Inflammation/Immunology
    Sialyl-Lewis X (sLeX) is a sialylated fucosylated tetrasaccharide, an endogenous antigen. Sialyl-Lewis X is a high-affinity ligand for selectins (E-, P-, and L-selectin). Sialyl-Lewis X binds to ELAM-1 and CD62 and has the ability to inhibits CD62-mediated neutrophil recruitment to sites of inflammation.
  • HY-10108
    LY294002

    PI3K Casein Kinase DNA-PK Autophagy Apoptosis Cancer Infection
    LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitorr that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an autophagy and apoptosis activator.
  • HY-131159
    Thalidomide-O-C8-Boc

    Ligand for E3 Ligase Cancer
    Thalidomide-O-C8-Boc is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-C8-Boc can be connected to the ligand for protein by a linker to form PROTACs.
  • 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-N2585
    Isodeoxyelephantopin

    Reactive Oxygen Species NF-κB Autophagy Cancer
    Isodeoxyelephantopin is a sesquiterpene lactone isolated from Elephantopus scaber. Isodeoxyelephantopin induces ROS generation, suppresses NF-κB activation. Isodeoxyelephantopin also modulates LncRNA expression and exhibit activities against breast cancer.
  • HY-P1594A
    Dynorphin A (1-10) (TFA)

    Opioid Receptor iGluR Neurological Disease
    Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC50 of 42.0 μM.
  • HY-10220
    SF1126

    PI3K Apoptosis Cancer
    SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis.
  • HY-P1098A
    Ac2-26 TFA

    NF-κB Inflammation/Immunology
    Ac2-26 TFA, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue.
  • HY-P1076
    CALP2

    Calcium Channel Phosphodiesterase (PDE) Inflammation/Immunology
    CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages.
  • HY-116364A
    AZT triphosphate TEA

    3'-Azido-3'-deoxythymidine-5'-triphosphate TEA

    HIV DNA/RNA Synthesis HBV Reactive Oxygen Species Apoptosis Infection
    AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway.
  • HY-13721
    Phenoxodiol

    Idronoxil; Dehydroequol; Haginin E

    Caspase Apoptosis Topoisomerase Cancer
    Phenoxodiol, a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21 WAF1 via a p53 independent manner.
  • HY-107427
    PF-3644022

    MAPKAPK2 (MK2) p38 MAPK Inflammation/Immunology
    PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.
  • HY-12034
    WYE-354

    mTOR Autophagy Apoptosis Cancer
    WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2. WYE-354 induces autophagy activation in vitro.
  • 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-50688
    SB-265610

    CXCR Inflammation/Immunology
    SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively.
  • HY-116767
    BLT-1

    Block lipid transport-1

    HCV Metabolic Disease Inflammation/Immunology
    BLT-1, a thiosemicarbazone copper chelator, is a selective scavenger receptor B, type 1 (SR-BI) inhibitor. BLT-1 inhibits the transfer of lipids between high-density lipoproteins (HDL) and cells mediated by SR-BI. BLT-1 is a potent HCV entry inhibitor.
  • HY-N0277
    Aconine

    Jesaconine

    NF-κB Inflammation/Immunology Cancer
    Aconine inhibits receptor activator of nuclear factor (NF)-κB ligand (RANKL)-induced NF-κB activation.
  • HY-103596
    Thalidomide-4-OH

    Cereblon ligand 2; E3 ligase Ligand 2

    Ligand for E3 Ligase Cancer
    Thalidomide-4-OH (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) can be connected to the ligand for protein by a linker to form PROTACs.
  • HY-133144
    Lenalidomide-OH

    Ligand for E3 Ligase Cancer
    Lenalidomide-OH is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-OH can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BTK degrader SJF620 (HY-133137).
  • HY-15510B
    Tenovin-6 Hydrochloride

    MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy Cancer
    Tenovin-6 Hydrochloride, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 Hydrochloride also inhibits dihydroorotate dehydrogenase (DHODH).
  • HY-15510
    Tenovin-6

    MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy Cancer
    Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH).
  • HY-103000
    HSF1A

    HSP Cancer Cardiovascular Disease
    HSF1A is a cell-permeable activator of heat shock transcription factor 1 (HSF1). HSF1A also acts as a specific inhibitor of TRiC/CCT. Chaperonin TCP-1 ring complex (TRiC)/chaperonin containing TCP-1 (CCT) plays a pivotal role in toxin translocation and/or refolding.
  • HY-12323
    ISX-9

    Isoxazole 9

    Others Neurological Disease
    ISX-9 (Isoxazole 9) is a potent inducer of adult neural stem cell differentiation. ISX-9 activates Ca 2+ influx through both voltage-gated Ca 2+ channels and NMDA receptors and increases neuroD expression. ISX-9 also induces cardiomyogenic differentiation of Notch-activated epicardium-derived cells (NECs).
  • HY-14754
    Salirasib

    S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS

    Ras Autophagy Cancer
    Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
  • HY-44148
    FAK ligand-Linker Conjugate 1

    Target Protein Ligand-Linker Conjugate Cancer
    FAK ligand-Linker Conjugate 1 incorporates a ligand for FAK, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). FAK ligand-Linker Conjugate 1 can be extensively used for PROTAC-mediated protein degradation.
  • HY-130952
    Thalidomide-O-C8-COOH

    Ligand for E3 Ligase Cancer
    Thalidomide-O-C8-COOH is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-C8-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs.
  • HY-114304
    COH000

    E1/E2/E3 Enzyme Cancer
    COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro.
  • HY-P1076A
    CALP2 TFA

    Calcium Channel Phosphodiesterase (PDE) Inflammation/Immunology
    CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages.
  • HY-10037
    Quiflapon

    MK-591

    FLAP Apoptosis Inflammation/Immunology
    Quiflapon (MK-591) is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.6 nM in a FLAP binding assay. Quiflapon is also a potent and orally active Leukotriene biosynthesis (LT) inhibitor, shows IC50 values of 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively. Quiflapon induces cell apoptosis.
  • 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-15424
    5-Iodotubercidin

    NSC 113939; 5-ITu

    Adenosine Kinase Cancer
    5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin.
  • HY-131318
    Lenalidomide-I

    Ligand for E3 Ligase Cancer
    Lenalidomide-I (Compound 72), an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, is used in the recruitment of CRBN protein. Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BET degrader QCA570 (HY-112609).
  • HY-110318
    VUF11207 fumarate

    CXCR Cancer
    VUF11207 fumarate (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7.
  • HY-19635A
    G-5555 hydrochloride

    PAK Cancer
    G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
  • HY-P0295
    Gly-Arg-Gly-Asp-Ser

    Integrin Others
    Gly-Arg-Gly-Asp-Ser is a pentapeptide that forms the cell-binding domain of a glycoprotein, osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin receptors αvβ3 and αvβ5 with estimated IC50 of ∼5 and ∼6.5 μM
  • HY-75385
    Zaurategrast ethyl ester

    CDP323; UCB1184197

    Integrin Inflammation/Immunology
    Zaurategrast ethyl ester (CDP323), the ethyl ester prodrug of CT7758, is a α4β1/α4β7 integrin antagonist used for the treatment of inflammatory and autoimmune disorders.
  • HY-107608
    Leukotriene B4

    LTB4; 5(S),12(R)-DiHETE

    PROTAC Linker Endogenous Metabolite Leukotriene Receptor Cancer Inflammation/Immunology
    Leukotriene B4 (LTB4) is known as one of the most potent chemoattractants and activators of leukocytes and is involved in inflammatory diseases. Leukotriene B4 is also an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-15723A
    NSC 23766 trihydrochloride

    Ras Apoptosis Cancer
    NSC 23766 trihydrochloride is an inhibitor of Rac1 activation.
  • HY-135825
    TFEB activator 1

    Autophagy Neurological Disease
    TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment.
  • HY-108330
    AG126

    Tyrphostin AG126

    ERK Inflammation/Immunology
    AG126 is a tyrosine kinase inhibitor which can prevent the activation of mitogen-activated protein kinase p42MAPK (ERK2).
  • HY-130297
    PROTAC BCR-ABL1 ligand 1

    Bcr-Abl Cancer
    PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1.
  • HY-103371
    DCPIB

    Chloride Channel Potassium Channel Neurological Disease
    DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB voltage-dependently activates potassium channels TREK1 and TRAAK and inhibits TRESK, TASK1 and TASK3 (IC50s of 0.14, 0.95, 50.72 μM, respectively). DCPIB is also a selective blocker of swelling-induced chloride current (ICl,swell), with an IC50 of 4.1 μM in CPAE cells.
  • HY-136251
    BRD0539

    CRISPR/Cas9 Infection
    BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay.
  • HY-136172
    ESI-08

    Ras Cancer Metabolic Disease Cardiovascular Disease
    ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation.
  • HY-P2268
    RAGE antagonist peptide

    Amyloid-β
    RAGE antagonist peptide is an antagonist of Receptor for advanced glycation end products (RAGE). RAGE blocks S100P, S100A4 and HMGB-1 mediated RAGE activation. RAGE antagonist peptide inhibits growth and metastasis of rat glioma tumors. RAGE antagonist peptide also reduces cell growth and RAGE-mediated NF-κB activity in human PDAC cell lines.
  • HY-100562
    Flopropione

    5-HT Receptor COMT Neurological Disease
    Flopropione is a 5-HT receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor. Flopropione also as an antispasmodic agent.
  • HY-15336
    AG 555

    Tyrphostin AG 555

    EGFR Reverse Transcriptase Cancer
    AG 555 (Tyrphostin AG 555), a potent antiretroviral drug, is a potent and selective inhibitor of EGFR and blocks Cdk2 activation.
  • HY-10484
    Pevonedistat hydrochloride

    MLN4924 hydrochloride

    NEDD8-activating Enzyme Cancer
    Pevonedistat hydrochloride (MLN4924 hydrochloride) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM.
  • HY-70062
    Pevonedistat

    MLN4924

    NEDD8-activating Enzyme Cancer
    Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM.
  • HY-131717
    Thalidomide-NH-CH2-COOH

    Ligand for E3 Ligase Cancer
    Thalidomide-NH-CH2-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-NH-CH2-COOH can be connected to the ligand for protein by a linker to form PROTACs, such as THAL-SNS-032 (HY-123937).
  • HY-129608
    Lenalidomide-acetylene-C5-COOH

    Cereblon ligand-linker Conjugate

    E3 Ligase Ligand-Linker Conjugate Cancer
    Lenalidomide-acetylene-C5-COOH (compound 43; Cereblon ligand-linker Conjugate) is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-acetylene-C5-COOH can be connected to the ligand for protein by a linker to form PROTAC.
  • HY-14190
    Valategrast

    R-411 free base

    Integrin Inflammation/Immunology
    Valategrast (R-411 free base) is a potent and orally active integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment.
  • HY-75385A
    Zaurategrast ethyl ester sulfate

    CDP323 sulfate; UCB1184197 sulfate

    Integrin Inflammation/Immunology
    Zaurategrast ethyl ester sulfate (CDP323 sulfate), the ethyl ester prodrug of CT7758, is a α4β1/α4β7 integrin antagonist used for the treatment of inflammatory and autoimmune disorders.
  • 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-117656
    ESI-05

    NSC 116966

    Others Others
    ESI-05 (NSC 116966) is a specific antagonist of EPAC2 (exchange protein directly activated by cAMP 2), with an IC50 of 0.4 µM. ESI-05 (NSC 116966) inhibits cAMP-mediated activation of EPAC2 as well as EAPC2 mediated Rap1 activation.
  • HY-17473
    Embelin

    Embelic acid; Emberine; NSC 91874

    IAP NF-κB Apoptosis Autophagy Cancer
    Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells.
  • HY-133121
    WDR5-IN-1

    Histone Methyltransferase Apoptosis Cancer
    WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.
  • HY-122725B
    Lenalidomide-C5-NH2 hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    Lenalidomide-C5-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs, such as MDM2 PROTAC degrader.
  • HY-122725
    Lenalidomide-C5-NH2

    Cereblon Ligand-Linker Conjugates 19; E3 ligase Ligand-Linker Conjugates 31

    E3 Ligase Ligand-Linker Conjugate Cancer
    Lenalidomide-C5-NH2 is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTAC, such as MDM2 PROTAC degrader.
  • HY-123931
    ZLDI-8

    Notch Phosphatase Apoptosis Cancer
    ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM.
  • HY-P0295A
    Gly-Arg-Gly-Asp-Ser (TFA)

    Integrin Inflammation/Immunology
    Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide that forms the cell-binding domain of a glycoprotein, osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin receptors αvβ3 and αvβ5 with estimated IC50 of ∼5 and ∼6.5 μM.
  • HY-17386
    Rosiglitazone

    BRL 49653

    PPAR TRP Channel Autophagy Ferroptosis Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
    Rosiglitazone (BRL 49653) is a selective, orally active PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone is also an activator of TRPC5 (EC50=~30 μM) and an inhibitor of TRPM3.
  • HY-17386A
    Rosiglitazone hydrochloride

    BRL 49653 hydrochloride

    PPAR TRP Channel Autophagy Ferroptosis Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
    Rosiglitazone hydrochloride (BRL 49653 hydrochloride) is a selective, orally active PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone hydrochloride binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone hydrochloride is also an activator of TRPC5 (EC50=~30 μM) and an inhibitor of TRPM3.
  • HY-B0167
    Salicylic acid

    2-Hydroxybenzoic acid

    COX Autophagy Mitophagy Apoptosis Endogenous Metabolite Inflammation/Immunology Cancer
    Salicylic acid (2-Hydroxybenzoic acid) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation.
  • HY-15542A
    FRAX597

    PAK Cancer
    FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC50 of 8, 13 and 19 nM for PAK1, 2 and 3.
  • HY-12364
    C75

    Fatty Acid Synthase (FASN) Cancer
    C75 is a synthetic fatty-acid synthase (FASN) inhibitor; inhibits prostate cancer cells PC3 with an IC50 of 35 μM. C75 is a potent CPT1A activator.
  • HY-100472
    ZYZ-488

    Caspase Cancer
    ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor. ZYZ-488 inhibits the activation of binding protein procaspase-9 and procaspase-3.
  • HY-101796
    NSC-70220

    Others Cancer
    NSC-70220 is a selective and allosteric SOS1 inhibitor. NSC-70220 inhibits allosteric site activation, and partially inhibited catalytic site activation. NSC-70220 has an anticancer effect.
  • HY-136190
    TRPC6-PAM-C20

    TRP Channel
    TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator. TRPC6-PAM-C20 selectively activates TRPC6 over other TRP channels and also activates TRPA1. TRPC6-PAM-C20 induces transient increase in intracellular Ca 2+ in HEK cells expressing TRPC6 (EC50=2.37 μM).
  • HY-N0221
    Daurisoline

    (R,R)-Daurisoline

    Autophagy Potassium Channel Cancer
    Daurisoline is a hERG inhibitor and also an autophagy blocker.
  • HY-41547
    Thalidomide 4-fluoride

    Cereblon ligand 4; E3 ligase Ligand 4

    Ligand for E3 Ligase Cancer
    Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966).
  • HY-B1197
    Amcinonide

    CL-34699

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    Amcinonide inhibit NO release from activated microglia with IC50 3.38 nM.
  • HY-12028
    PD98059

    MEK ERK Aryl Hydrocarbon Receptor Autophagy Cancer
    PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits autophagy.
  • HY-15542B
    FRAX486

    PAK Cancer
    FRAX486 is a p21-activated kinase (PAK) inhibitor with IC50s of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively.
  • HY-N4182
    Licochalcone E

    Akt p38 MAPK Autophagy Inflammation/Immunology
    Licochalcone E, a flavonoid compound isolated from Glycyrrhiza inflate, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPK activation.
  • HY-19635
    G-5555

    PAK Cancer
    G-5555 is a potent p21-activated kinase 1 (PAK1) inhibitor with Kis of 3.7 nM and 11 nM for PAK1 and PAK2, respectively.
  • HY-126214
    JH-RE-06

    DNA/RNA Synthesis Cancer
    JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Kd=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 improves chemotherapy.
  • HY-14252
    Milrinone

    Win 47203

    Phosphodiesterase (PDE) Cardiovascular Disease
    Milrinone is a PDE3 inhibitor, and also an inotrope and vasodilator.
  • HY-P1260
    FSLLRY-NH2

    Protease-Activated Receptor (PAR) Neurological Disease
    FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.
  • HY-10255A
    Sunitinib

    SU 11248

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-W006230
    Anthraflavic acid

    Others Cancer
    Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens.
  • 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-10943
    GNF-7

    Bcr-Abl Ack1 Cancer
    GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-Abl WT and Bcr-Abl T315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies.
  • HY-101676
    RG-12525

    NID 525

    Leukotriene Receptor PPAR Cytochrome P450 Metabolic Disease
    RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.
  • HY-107406
    Antimycin A1

    Mitochondrial Metabolism Cancer
    Antimycin A1 is a specific electron transfer inhibitor of ubiquinol-cytochrome c oxidoreductase. Antimycin A1 inhibits angiogenesis through decrease in VEGF production caused by inhibition of HIF-1α activation.
  • HY-N6688
    Verruculogen

    Potassium Channel Bacterial Antibiotic Infection
    Verruculogen is a toxin produced mainly by Penicillium and Aspergillus spp. and causes severe tremors in affected animals. Verruculogen inhibits Ca 2+-activated K + channels. Verruculogen is an M phase inhibitor of the mammalian cell cycle.
  • HY-W008859
    Tetrac

    Tetraiodothyroacetic acid; 3,3',5,5'-Tetraiodothyroacetic acid

    Integrin Endogenous Metabolite Cancer
    Tetrac (Tetraiodothyroacetic acid), a derivative of L-thyroxine (T4), is a thyrointegrin receptor antagonist. Tetrac blocks the actions of T4 and 3,5,3'-triiodo-L-thyronine (T3) at the cell surface receptor for thyroid hormone on integrin αvβ3. Tetra has anti-angiogenic and anti-tumor activities.
  • HY-14951
    Firategrast

    SB 683699

    Integrin Neurological Disease
    Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.
  • HY-14452
    Fatostatin

    125B11

    Fatty Acid Synthase (FASN) Cancer
    Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
  • HY-B0289
    Erdosteine

    RV 144

    NF-κB Bacterial Infection Metabolic Disease Inflammation/Immunology
    Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation. Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects.
  • HY-N1380
    Guaiacol

    2-Methoxyphenol

    COX NF-κB Endogenous Metabolite Inflammation/Immunology
    Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity.
  • HY-13764
    Tetrandrine

    NSC-77037; d-Tetrandrine

    Calcium Channel Potassium Channel Cancer Inflammation/Immunology
    Tetrandrine (NSC-77037; d-Tetrandrine) is a bis-benzyl-isoquinoline alkaloid, which inhibits voltage-gated Ca 2+ current (ICa) and Ca 2+-activated K + current.
  • HY-101932
    TNP-470

    AGM-1470

    Aminopeptidase Cancer Cardiovascular Disease
    TNP-470 is a methionine aminopeptidase-2 inhibitor and also an angiogenesis inhibitor.
  • HY-13434
    Ionomycin

    SQ23377

    Calcium Channel PKC Bacterial Apoptosis Antibiotic Cancer Infection
    Ionomycin (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin (SQ23377) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin also induces the activation of protein kinase C (PKC).
  • HY-19638A
    Cangrelor tetrasodium

    P2Y Receptor Inflammation/Immunology Cardiovascular Disease
    Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor tetrasodium is also a nonspecific GPR17 antagonist.
  • HY-100602
    HJC0152 hydrochloride

    STAT Apoptosis Cancer
    HJC0152 hydrochloride is a signal transducers and activators of transcription 3 (STAT3) inhibitor.
  • HY-N0441
    Neferine

    (-)-Neferine

    NF-κB Autophagy Apoptosis Metabolic Disease Cancer
    Neferine is a major bisbenzylisoquinline alkaloid. Neferine strongly inhibits NF-κB activation.
  • HY-101214
    UK-371804

    PAI-1 Inflammation/Immunology
    UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
  • HY-P1260A
    FSLLRY-NH2 TFA

    Protease-Activated Receptor (PAR) Neurological Disease
    FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.
  • HY-18965
    TAS-301

    PKC Cardiovascular Disease
    TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.
  • HY-123844
    dBET57

    PROTAC Epigenetic Reader Domain Cancer
    dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4 CRBN E3 ubiquitin ligase, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2.
  • HY-130492
    ARCC-4

    PROTAC Androgen Receptor Cancer
    ARCC-4 is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy.
  • HY-P1102
    TC14012

    CXCR HIV Cancer Infection
    TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity.
  • HY-125845A
    (S,S,S)-AHPC hydrochloride

    (S,S,S)-VH032-NH2 hydrochloride

    Ligand for E3 Ligase Cancer
    (S,S,S)-AHPC hydrochloride is a von Hippel-Lindau (VHL) amino building block. (S,S,S)-AHPC (Compound 27) is a ligand used as a negative control for (S,R,S)-AHPC. (S,R,S)-AHPC is the VH032-based VHL ligand used in the recruitment of the VHL protein.
  • HY-10255
    Sunitinib Malate

    SU 11248 Malate

    PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-116699
    CP-868388 free base

    PPAR Metabolic Disease Inflammation/Immunology Neurological Disease
    CP-868388 free base is a potent, selective and orally active PPARα agonist with a Ki value of 10.8 nM. CP-868388 free base has little or no affinity for PPARβ (Ki of 3.47 μM) and PPARγ. CP-868388 free base has hypolipidemic and anti-inflammatory actions.
  • HY-135388
    ent-Ezetimibe

    ent-SCH 58235

    Drug Metabolite Cardiovascular Disease
    ent-Ezetimibe (ent-SCH 58235) is the RRS-enantiomer of Ezetimibe. Ezetimibe is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
  • 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-136059
    Desfluoro-ezetimibe

    Keap1-Nrf2 Autophagy Cancer Cardiovascular Disease
    Desfluoro-ezetimibe is a desfluoro impurity of Ezetimibe. Ezetimibe is a potent, metabolically stable cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
  • HY-B2099
    Buformin

    1-Butylbiguanide

    AMPK Cancer Metabolic Disease
    Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).
  • HY-B2099A
    Buformin hydrochloride

    1-Butylbiguanide hydrochloride

    AMPK Cancer
    Buformin hydrochloride (1-Butylbiguanide hydrochloride), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin hydrochloride decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin hydrochloride also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).
  • HY-N0424
    Cycloastragenol

    Cyclogalagenin; Cyclogalegenin; Cyclogalegigenin

    Telomerase Others
    Cycloastragenol is a natural tetracyclic triterpenoid, is identified when screening Astragalus membranaceus extracts for active ingredients with antiaging properties. Cycloastragenol is a potent telomerase activator in neuronal cells. Cycloastragenol also has other pharmacological effects, including anti-inflammatory and anti-oxidative properties.
  • HY-100973A
    Adenosine 5′-diphosphoribose sodium

    ADP ribose sodium

    TRP Channel Autophagy Endocrinology Metabolic Disease
    Adenosine 5′-diphosphoribose sodium (ADP ribose sodium) is a nicotinamide adenine nucleotide (NAD +) metabolite. Adenosine 5′-diphosphoribose sodium is the most potent and primary intracellular Ca 2+-permeable cation TRPM2 channel activator. Adenosine 5′-diphosphoribose sodium also can enhance autophagy.
  • HY-110105
    NS8593 hydrochloride

    Potassium Channel Neurological Disease
    NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively).
  • HY-18749
    SC79

    Akt Cancer Inflammation/Immunology Neurological Disease
    SC79, a unique specific and BBB permeable Akt activator, activates Akt in the cytosol and inhibits Akt membrane translocation. SC79 specifically binds to the PH domain of Akt.
  • HY-18234A
    Leupeptin hemisulfate

    Cathepsin Inflammation/Immunology
    Leupeptin hemisulfate is a membrane-permeable thiol protease inhibitor that inhibits Cathepsin B, Cathepsin H and Cathepsin L, and also impairs amphisome-lysosome fusion. Leupeptin hemisulfate also exhibits anti-inflammatory effect.
  • HY-15300
    Skepinone-L

    CBS3830

    p38 MAPK Autophagy Inflammation/Immunology
    Skepinone-L (CBS3830) is a selective p38 mitogen-activated protein kinase inhibitor.
  • HY-W011109
    CKI-7

    Casein Kinase CDK SGK Ribosomal S6 Kinase (RSK) Cancer
    CKI-7 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 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.
  • HY-103666
    CY-09

    NOD-like Receptor (NLR) Inflammation/Immunology
    CY-09 is a selective and direct NLRP3 inhibitor. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation.
  • HY-14452A
    Fatostatin hydrobromide

    125B11 hydrobromide

    Fatty Acid Synthase (FASN) Cancer
    Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
  • HY-B1521
    Aluminum Hydroxide

    Others Inflammation/Immunology
    Aluminum Hydroxide is an orally active main form of aluminum used as adjuvant. Aluminum hydroxide-based adjuvant researches include the repository effect, pro-phagocytic effect, and activation of the pro-inflammatory NLRP3 pathway. Aluminum Hydroxide also acts as adjuvant to compensate low inherent immunogenicity of subunit vaccines.
  • HY-103319
    Calmidazolium chloride

    R 24571

    CaMK Autophagy Cancer Neurological Disease
    Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively. Also in anti-cancer research. Calmidazolium binds to CaMK with a Kd of 3 nM.
  • HY-B1074
    Ethamsylate

    Prostaglandin Receptor Cardiovascular Disease Endocrinology
    Ethamsylate is a haemostatic drug, also inhibits biosynthesis and action of those prostaglandins.
  • HY-B1664
    Iopanoic acid

    Others Endocrinology
    Iopanoic acid is an inhibitor of 5'-Deiodinase and also an iodinated contrast medium.
  • HY-108601A
    Ro 32-0432 hydrochloride

    PKC Inflammation/Immunology Neurological Disease
    Ro 32-0432 hydrochloride is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of Ro 32-0432 hydrochloride for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. Ro 32-0432 hydrochloride is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. Ro 32-0432 hydrochloride prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research.
  • HY-N2117
    Isoginkgetin

    MMP Cancer
    Isoginkgetin is a MMP-9 inhibitor, also a Pre-mRNA Splicing Inhibitor with IC 50 of 30 uM.
  • HY-100447
    TM5275 sodium

    PAI-1 Cancer Cardiovascular Disease
    TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM.
  • HY-B0809
    Theophylline

    1,3-Dimethylxanthine; Theo-24

    Adenosine Receptor Phosphodiesterase (PDE) Autophagy Endogenous Metabolite Cancer
    Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
  • HY-128642
    FAPI-2

    Others Cancer
    FAPI-2 is a fibroblast activation protein (FAP) inhibitor for cancer research.
  • HY-15253
    Tiplaxtinin

    PAI-039; Tiplasinin

    PAI-1 Apoptosis Metabolic Disease Cancer
    Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM.
  • HY-13736A
    Quinagolide hydrochloride

    CV205-502 hydrochloride

    Dopamine Receptor Neurological Disease
    Quinagolide hydrochloride is a selective dopamine D2 receptor agonist, also is a prolactin inhibitor.
  • 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-118165
    Phenthoate

    AChE Neurological Disease
    Phenthoate is an organophosphorus pesticide having low toxicity in animals. Phenthoate is also a AChE inhibitor.
  • HY-103593A
    LCL521 dihydrochloride

    Phospholipase Cancer
    LCL521 dihydrochloride is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
  • HY-103593
    LCL521

    Phospholipase Cancer
    LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
  • HY-N6258
    Kahweol

    AMPK Apoptosis Metabolic Disease
    Kahweol is one of the consituents of the coffee from Coffea Arabica with anti-inflammatory anti-angiogenic, and anti-cancerous activities. Kahweol inhibits adipogenesis and increase glucose uptake by AMP-activated protein kinase (AMPK) activation. Kahweol induces apoptosis.
  • HY-10162
    Olaparib

    AZD2281; KU0059436

    PARP Autophagy Mitophagy Cancer
    Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
  • HY-135897
    Urolithin C

    Calcium Channel Reactive Oxygen Species Apoptosis Endogenous Metabolite Metabolic Disease
    Urolithin C, a gut-microbial metabolite of Ellagic acid, is a glucose-dependent activator of insulin secretion. Urolithin C is a L-type Ca 2+ channel opener and enhances Ca 2+ influx. Urolithin C induces cell apoptosis through a mitochondria-mediated pathway and also stimulates reactive oxygen species (ROS) formation.
  • HY-131231
    Thalidomide-NH-PEG3-CH2CHO

    Ligand for E3 Ligase Cancer
    Thalidomide-NH-PEG3-CH2CHO is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-NH-PEG3-CH2CHO can be connected to the ligand for protein by a linker to form PROTAC BCL-XL degrader XZ739 (HY-133557).
  • HY-125834
    GMB-475

    PROTAC Bcr-Abl Apoptosis Cancer
    GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
  • HY-130256
    β-NF-JQ1

    PROTAC Epigenetic Reader Domain Cancer
    β-NF-JQ1 is a PROTAC that recruits AhR E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity.
  • HY-120793
    CMC2.24

    TRB-N0224

    Ras Apoptosis MMP Cancer Inflammation/Immunology
    CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis.
  • HY-112473
    NAV-2729

    Others Cancer
    NAV-2729 is a dual Arf1/Arf6 activation inhibitor.
  • HY-128643
    FAPI-4

    Others Cancer
    FAPI-4 is a fibroblast activation protein (FAP) inhibitor used in cancer research.
  • HY-15840
    YLF-466D

    C24

    AMPK Cancer
    YLF-466D is a newly developed AMPK activator, which inhibits platelet aggregation.
  • HY-12496
    NS-1619

    Potassium Channel Cardiovascular Disease
    NS-1619 is a selective large conductance Ca2+-activated K+-channel activator.
  • HY-136427
    KRM-III

    Others Inflammation/Immunology
    KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity.
  • HY-B0099S
    Edaravone D5

    MCI-186 D5

    MMP Apoptosis Neurological Disease
    Edaravone D5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator.
  • HY-13502
    Mitoxantrone

    mitozantrone

    Topoisomerase PKC Cancer
    Mitoxantrone is a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM.
  • HY-107994
    Aminooxyacetic acid hemihydrochloride

    Carboxymethoxylamine Hemihydrochloride

    GABA Receptor Cancer
    Aminooxyacetic acid hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
  • HY-112860
    Asp-AMS

    Aminoacyl-tRNA Synthetase Mitochondrial Metabolism Metabolic Disease
    Asp-AMS, an analogue of aspartyl-adenylate, is an aspartyl-tRNA synthetase inhibitor and also a strong competitive inhibitor of the mitochondrial enzyme.
  • HY-13502A
    Mitoxantrone dihydrochloride

    mitozantrone dihydrochloride

    Topoisomerase PKC Cancer
    Mitoxantrone dihydrochloride is a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM.
  • HY-B0004
    Doxofylline

    Adenosine Receptor Phosphodiesterase (PDE) Inflammation/Immunology
    Doxofylline is an antagonist of adenosine A1 receptor which also inhibits phosphodiesterase IV.
  • HY-100615A
    R 80123

    Phosphodiesterase (PDE) Cardiovascular Disease
    R 80123 is the Z-isomer of R 79595, is also a highly selective phosphodiesterase inhibitor.
  • HY-N2587
    Irigenin

    Integrin Cancer
    Irigenin is a is a lead compound, and mediates its anti-metastatic effect by specifically and selectively blocking α9β1 and α4β1 integrins binding sites on C-C loop of Extra Domain A (EDA). Irigenin shows anti-cancer properties. It sensitizes TRAIL-induced apoptosis via enhancing pro-apoptotic molecules in gastric cancer cells.
  • 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-B0845
    Prochloraz

    BTS 40542

    Fungal Estrogen Receptor/ERR Androgen Receptor Aryl Hydrocarbon Receptor Infection
    Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Prochloraz inhibits human placenta microsomal aromatase in vitro (IC50=40 nM). Prochloraz also acts as an antagonist of the estrogen receptor (ER) and androgen receptor (AR) (IC50s=25 μM and 4 μM, respectively) as well as activates the aryl hydrocarbon receptor (AhR; EC50=1 μM).
  • HY-15342
    Timapiprant

    OC000459

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Timapiprant (OC000459) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant (OC000459) potently displaces [ 3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant (OC000459) inhibits mast cell activation of Th2 lymphocytes and eosinophils.
  • HY-15342A
    Timapiprant sodium

    OC000459 sodium

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [ 3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils.
  • HY-13285
    Ki16425

    Debio 0719

    LPL Receptor Neurological Disease Cancer
    Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK. Ki16425 also can inhibits LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells.
  • HY-129619
    SNIPER(ER)-87

    SNIPER Estrogen Receptor/ERR Cancer
    SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation.
  • HY-12884
    OAC2

    Oct3/4 Others
    OAC2 is an Oct4-activating compound which activates expression through the Oct4 gene promoter.
  • HY-122760
    Bax activator-1

    Bcl-2 Family Apoptosis Cancer
    Bax activator-1 (compound 106) is a Bax activator that induces Bax-dependent tumor cell apoptosis.
  • HY-19734
    NK-252

    Keap1-Nrf2 Cancer
    NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.
  • HY-U00458
    K-80003

    TX-803

    Akt Cancer
    K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
  • HY-15252
    Reparixin L-lysine salt

    Repertaxin L-lysine salt

    CXCR Cancer Inflammation/Immunology Endocrinology
    Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation.
  • HY-N0896
    Inulicin

    1-O-Acetylbritannilactone

    NF-κB COX Cancer Inflammation/Immunology
    Inulicin (1-O-Acetylbritannilactone) is an active compound isolated from Inula Britannica L. Inulicin (1-O-Acetylbritannilactone) inhibits VEGF-mediated activation of Src and FAK. Inulicin (1-O-Acetylbritannilactone) inhibits LPS-induced PGE2 production and COX-2 expression, and NF-κB activation and translocation.
  • HY-108741A
    Plecanatide acetate

    Guanylate Cyclase Inflammation/Immunology
    Plecanatide acetate, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide acetate activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide acetate can be used for the research of chronic idiopathic constipation, and it also shows anti-inflammatory activity in models of murine colitis.
  • HY-B1794A
    Thiethylperazine dimaleate

    Dopamine Receptor Histamine Receptor Bacterial Infection Neurological Disease
    Thiethylperazine dimaleate is a phenothiazine derivate, and an orally active dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a slective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects.
  • HY-13606
    Dacinostat

    NVP-LAQ824; LAQ824

    HDAC Autophagy Cancer
    Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.
  • HY-B0830
    Isoprocarb

    AChE Neurological Disease
    Isoprocarb is carbamate insecticide that widely used to control rice paddy lice and leafhopper. Isoprocarb is also an AChE inhibitor.
  • HY-12420
    JNJ-47117096 hydrochloride

    MELK-T1 hydrochloride

    MELK FLT3 Cancer
    JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC50 of 23 nM, also effectively inhibits Flt3, with an IC50 of 18 nM.
  • HY-12357
    Bempedoic acid

    ETC-1002; ESP-55016

    ATP Citrate Lyase AMPK Metabolic Disease
    Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor. Bempedoic acid (ETC-1002) activates AMPK.
  • HY-N7452
    Coumermycin A1

    JAK Bacterial Metabolic Disease
    Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.
  • 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-W018781
    Benzamidine hydrochloride

    Ser/Thr Protease Cancer
    Benzamidine hydrochloride is an reversible competitive inhibitor of trypsin-like serine proteases, with Kis of 97 µM, 21 µM, 20 µM and 110 µM for uPA, trypsin, tryptase and factor Xa, respectively.
  • HY-B2119
    Sodium tauroglycocholate

    Tauroglycocholic acid sodium salt

    Others Endocrinology
    Sodium tauroglycocholate is an inhibitor of the biliary acid transporting system of the hepatocyte and also a surfactant used as a chemical permeation enhancer.
  • HY-N3807
    Enniatin B1

    Acyltransferase ERK NF-κB Cancer Infection Cardiovascular Disease
    Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes. Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.
  • 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-12831
    Ampkinone

    AMPK Metabolic Disease
    Ampkinone is an indirect AMP-activated protein kinase (AMPK) activator.
  • HY-107301
    Dehydrosoyasaponin I

    Soyasaponin Be; DHS-I

    Potassium Channel Neurological Disease
    Dehydrosoyasaponin I (Soyasaponin Be;DHS-I), a triterpene glycoside, is a potent and reversible calcium-activated potassium (maxi-K) channels activator.
  • HY-N0897
    Corylifol A

    Corylifol-A; Corylinin

    STAT Others
    Corylifol A inhibits IL-6-induced STAT3 activation and phosphorylation, with an IC50 of 0.81 μM.
  • HY-15530
    CID-2858522

    NF-κB Inflammation/Immunology Cancer
    CID-2858522 is a highly potent and selective antigen receptor-mediated NF-κB activation inhibitor with an IC50 of 70 nM.
  • HY-50703
    MK-2461

    c-Met/HGFR Cancer
    MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met with a mean IC50 of 2.5 nM.
  • HY-B0167S
    Salicylic acid-D6

    2-Hydroxybenzoic acid-D6

    COX Autophagy Mitophagy Apoptosis Cancer Inflammation/Immunology
    Salicylic acid-D6 (2-Hydroxybenzoic acid-D6) is a deuterium labeled Salicylic acid. Salicylic acid inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation.
  • HY-12399
    MKC9989

    IRE1 Cancer
    MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
  • HY-108941
    Salicyl-AMS

    Bacterial Infection
    Salicyl-AMS is a mycobactin biosynthesis inhibitor which can also inhibit M. tuberculosis growth in vitro under iron-limited conditions.
  • HY-13420
    Zebularine

    NSC309132; 4-Deoxyuridine

    DNA Methyltransferase Autophagy Cancer
    Zebularine (NSC309132; 4-Deoxyuridine) is a DNA methyltransferase inhibitor. Zebularine also inhibits cytidine deaminase with a Ki of 0.95 μM.
  • HY-B1863
    Iprobenfos

    Fungal Infection
    Iprobenfos is an organophosphorus fungicide and is widely used to control the rice blast fungus. Iprobenfos is also a choline biosynthesis inhibitor.
  • 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-N2033
    Chebulinic acid

    DNA/RNA Synthesis TGF-beta/Smad Proton Pump Infection
    Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.
  • HY-100463
    TPI-1

    Phosphatase Inflammation/Immunology Cancer
    TPI-1, also known as Tyrosine Phosphatase Inhibitor 1, is a SHP-1 inhibitor; inhibits recombinant SHP-1 with an IC50 of 40 nM.
  • HY-134477
    NF-κΒ activator 2

    NF-κB Neurological Disease
    NF-κΒ activator 2 is a potent and orally active NF-ҡB activator, with an EC50 of 1.58 μM. NF-κΒ activator 2 induces SOD2 through increasing NF-ҡB expression and activation. NF-κΒ activator 2 can be used for the research of amyotrophic lateral sclerosis (ALS).
  • HY-19339
    Tenovin-3

    MDM-2/p53 Cancer
    Tenovin-3 is a p53 activator.
  • HY-101788
    Glucokinase activator 1

    Glucokinase Metabolic Disease
    Glucokinase activator 1 is a liver-directed glucokinase activator with an EC50 of 34 nM.
  • HY-13434A
    Ionomycin calcium

    SQ23377 calcium

    Calcium Channel PKC Bacterial Apoptosis Antibiotic Cancer Infection
    Ionomycin calcium (SQ23377 calcium) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin calcium (SQ23377 calcium) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin calcium (SQ23377 calcium) also induces the activation of protein kinase C (PKC).
  • HY-B0413S
    Fenbendazole-d3

    Parasite HIF/HIF Prolyl-Hydroxylase Antibiotic Infection
    Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole is a benzimidazole anthelmintic. Fenbendazole is active against Giardia in vitro (IC50 = 0.3 μM). Fenbendazole (20 mg/kg) prevents infiltration of parasites into the brain in a rabbit model of E. cuniculi infection. Fenbendazole also activates HIF-1α and prevents oxidative stress-induced death in primary neurons in vitro.
  • HY-G0021
    N-Desmethylclozapine

    Norclozapine; Desmethylclozapine; Normethylclozapine

    mAChR Opioid Receptor Drug Metabolite Virus Protease Infection
    N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic drug Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.
  • HY-19556
    (+)-SJ733

    SJ000557733

    Na+/K+ ATPase Parasite Infection
    (+)-SJ733 is an anti-malaria agent which can also inhibit Na +-ATPase PfATP4.
  • HY-B1436
    Nifuroxazide

    STAT Bacterial Cancer Infection
    Nifuroxazide is an effective inhibitor of STAT3, also exerts potent anti-tumor and anti-metastasis activity.
  • HY-B1371A
    Spiperone hydrochloride

    Spiroperidol hydrochloride

    Dopamine Receptor 5-HT Receptor Adrenergic Receptor Chloride Channel Inflammation/Immunology Neurological Disease
    Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) and 5-HT2A/5-HT1A receptor (Kis of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities.
  • HY-136173
    TNO155

    Phosphatase Cancer
    TNO155 is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). TNO155 has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors.
  • HY-100508
    ITSA-1

    HDAC Cancer
    ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation.
  • HY-13103
    NS 11021

    Potassium Channel Others
    NS 11021 is a potent and specific Ca 2+-activated big-conductance K + Channels (KCa1.1 channels) activator. NS 11021 at concentrations above 0.3 μM activates KCa1.1 in a concentration-dependent manner by parallelshifting the channel activation curves to more negative potentials.
  • HY-16511
    Upamostat

    WX-671

    Ser/Thr Protease PAI-1 Cancer
    Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
  • HY-50714
    Quiflapon sodium

    MK-591 sodium

    FLAP Apoptosis Inflammation/Immunology
    Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
  • HY-N0516
    Casticin

    Vitexicarpin

    STAT Inflammation/Immunology
    Casticin is a methyoxylated flavonol isolated from Viticis Fructus, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.
  • HY-13719
    Oleandrin

    Na+/K+ ATPase Apoptosis Cancer
    Oleandrin inhibits the Na +, K +-ATPase activity with an IC50 of 620 nM. Oleandrin induces apoptosis via activating endoplasmic reticulum stress.
  • 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-14645A
    (+)-DHMEQ

    (1R,2R,6R)-Dehydroxymethylepoxyquinomicin; (1R,2R,6R)-DHMEQ

    Keap1-Nrf2 Inflammation/Immunology
    (+)-DHMEQ is an activator of antioxidant transcription factor Nrf2. (+)-DHMEQ is the enantiomer of (-)-DHMEQ. (-)-DHMEQ inhibits NF-kB than its enantiomer (+)-DHMEQ.
  • HY-112125A
    KRN2 bromide

    Others Inflammation/Immunology
    KRN2 (bromide) is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 0.1 μM.
  • HY-77251
    TAK1/MAP4K2 inhibitor 1

    MAP4K MAP3K Cancer
    TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
  • HY-N0518
    Toddalolactone

    PAI-1 Cardiovascular Disease
    Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM.
  • HY-15770
    TR-14035

    Integrin Inflammation/Immunology
    TR-14035 is a orally active dual α4β74β1 integrin antagonist, with IC50 s of 7 nM and 87 nM for α4β7 and α4β1, respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases.
  • 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-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-15416
    NS309

    Potassium Channel Neurological Disease Cardiovascular Disease
    NS309 is a potent and selective activator of the Ca 2+-activated SK/IK potassium channels, but displays no activity at BK channels.
  • HY-131012
    GoSlo-SR-5-69

    Potassium Channel Others
    GoSlo-SR-5-69 is a potent activator of large conductance Ca 2+-activated K + (BK) channels, with an EC50 of 251 nM.
  • HY-P0190
    Iberiotoxin

    Potassium Channel Cardiovascular Disease
    Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels.
  • HY-12326
    c-di-AMP

    Cyclic diadenylate; Cyclic-di-AMP

    STING Bacterial Endogenous Metabolite 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-N0336
    3-Butylidenephthalide

    Butylidenephthalide

    Parasite Infection
    3-Butylidenephthalide (Butylidenephthalide) is a phthalic anhydride derivative identified in Ligusticum chuanxiong Hort, and has larvicidal activity (LC50 of 1.56 mg/g for Spodoptera litura larvae).
  • HY-B1235
    Acetohydroxamic acid

    AHA

    Bacterial Infection
    Acetohydroxamic acid is a potent and irreversible inhibitor of bacterial and plant urease and also used as adjunctive therapy in chronic urinary infection.
  • HY-N0143
    Phlorizin

    Floridzin; NSC 2833

    SGLT Na+/K+ ATPase Metabolic Disease
    Phlorizin is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na +/K +-ATPase inhibitor.
  • HY-15457
    Triciribine

    API-2; NSC 154020; TCN

    DNA/RNA Synthesis Akt HIV Cancer
    Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1/2 with IC50 of 130 nM, and 0.02-0.46 μM, respectively.
  • HY-130499
    ERRα Ligand-Linker Conjugates 1

    Target Protein Ligand-Linker Conjugate Cancer
    ERRα Ligand-Linker Conjugates 1 incorporates a ligand for estrogen-related receptor alpha (ERRα), and a PROTAC linker, which recruit E3 ligases MDM2. ERRα Ligand-Linker Conjugates 1 can be used in the synthesis of a series of PROTACs, such as PROTAC ERRalpha Degrader-1 (HY-128838). PROTAC ERRalpha Degrader-1 is an ERRα degrader.
  • HY-114363A
    SRI 31215 TFA

    c-Met/HGFR Cancer
    SRI 31215 (TFA), a triplex inhibitor of matriptase, hepsin and hepatocyte growth factor activator (HGFA) with IC50s of 0.69 μM, 0.65 μM, 0.3 μM, blocks pro-HGF activation and thus mimics the activity of HAI-1/2.
  • HY-103697
    Gardiquimod

    Toll-like Receptor (TLR) HIV Cancer Infection
    Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10 μM.
  • HY-12689
    Mitapivat

    Pyruvate Kinase Cancer
    Mitapivat is a pyruvate kinase isoenzyme M2 (PKM2) activator.
  • HY-N0761
    Isoferulic acid

    3-Hydroxy-4-methoxycinnamic acid

    Adrenergic Receptor Influenza Virus Infection Endocrinology Metabolic Disease
    Isoferulic acid (3-Hydroxy-4-methoxycinnamic acid) is a cinnamic acid derivative that has antidiabetic activity. Isoferulic acid binds to and activates α1-adrenergic receptors (IC50=1.4 µM) to enhance secretion of β-endorphin (EC50=52.2 nM) and increase glucose use. Isoferulic acid also has anti-influenza virus activities.
  • HY-128586A
    TAS4464 hydrochloride

    NEDD8-activating Enzyme Cancer
    TAS4464 (hydrochloride) is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM.
  • HY-N2506
    Ginsenoside Ra1

    Others Cardiovascular Disease
    Ginsenoside Ra1 is a component from ginseng, inhibits protein tyrosine kinase (PTK) activation induced by hypoxia/reoxygenation.
  • HY-15869
    Inauhzin

    INZ

    Sirtuin MDM-2/p53 Cancer
    Inauhzin is a dual SirT1/IMPDH2 inhibitor, and acts as an activator p53, used in the research of cancer.
  • HY-128586
    TAS4464

    NEDD8-activating Enzyme Cancer
    TAS4464 is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM.
  • HY-78131B
    (R)-(-)-Ibuprofen

    (R)-Ibuprofen

    NF-κB Inflammation/Immunology Cancer
    (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
  • HY-100407
    JNJ16259685

    mGluR Neurological Disease
    JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
  • HY-131334
    AMPK activator 4

    AMPK Metabolic Disease
    AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect.
  • HY-10162S2
    Olaparib D4

    AZD2281 D4; KU0059436 D4

    Autophagy Mitophagy PARP Cancer
    Olaparib D4 (AZD2281 D4) is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
  • HY-10162S1
    Olaparib D8

    AZD2281 D8; KU0059436 D8

    PARP Autophagy Mitophagy Cancer
    Olaparib D8 (AZD2281 D8) is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
  • HY-14266
    Dapivirine

    TMC120; R147681

    HIV Reverse Transcriptase Apoptosis Autophagy Infection
    Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.
  • HY-13971
    GPR40 Activator 1

    GPR40 Metabolic Disease
    GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes.
  • HY-119692
    Curvulin

    Microtubule/Tubulin Others
    Curvulin, isolated from Curvularia lunata, is a phytotoxin. Curvularin is reported to inhibit microtubule assembly and has also been shown to inhibit iNOS expression.
  • HY-12056
    BIX02189

    MEK ERK Cancer
    BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM.
  • HY-12589
    ZM39923 hydrochloride

    JAK Cancer Neurological Disease
    ZM39923 hydrochloride is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 hydrochloride also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.
  • HY-15417
    ML-7 hydrochloride

    Myosin YAP Cancer
    ML-7 hydrochloride is a naphthalene sulphonamide derivative, potently inhibits MLCK (IC50=300 nM). ML-7 hydrochloride also inhibits YAP/TAZ.
  • HY-12589A
    ZM39923

    JAK Cancer Neurological Disease
    ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.
  • HY-B1902
    Diaveridine

    EGIS-5645

    Antifolate Bacterial Infection
    Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.
  • 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-U00206
    D2343

    Adrenergic Receptor Endocrinology
    D2343 is a β2-adrenoceptor agonist and also is an α1- adrenoceptor inhibitor.
  • HY-17024
    Cyclopamine

    11-Deoxojervine

    Hedgehog Smo Endogenous Metabolite Cancer
    Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay. Cyclopamine is also a selective Smo inhibitor.
  • HY-15004
    AUZ 454

    K03861

    CDK Cancer
    AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
  • HY-136065
    bpV(phen)

    PTEN Phosphatase Parasite Apoptosis Cancer Infection Metabolic Disease Inflammation/Immunology
    bpV(phen), a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
  • HY-B0112
    Minoxidil

    U10858

    Potassium Channel Cardiovascular Disease
    Minoxidil (U10858) is an ATP-sensitive potassium (KATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. Minoxidil is also a potent inhibitor of soybean lipoxygenaseare with an IC50 of 20 μM.
  • HY-N1990
    Gypenoside XLIX

    PPAR Inflammation/Immunology Cardiovascular Disease
    Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells.
  • HY-19354
    Aglafoline

    Aglafolin; Rocaglamide U; (-)-Methyl rocaglate

    Others Cardiovascular Disease
    Aglafoline inhibits in a selective and concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor).
  • HY-15251
    Reparixin

    Repertaxin; DF 1681Y

    CXCR Inflammation/Immunology Endocrinology Cancer
    Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
  • HY-N2283
    Deltonin

    ERK Akt Endogenous Metabolite Cancer
    Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis Wright, with antitumor activity; Deltonin inhibits ERK1/2 and AKT activation.
  • HY-32735
    Triptolide

    PG490

    NF-κB Apoptosis Cancer
    Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory and antiproliferative effects. Triptolide is a NF-κB activation inhibitor.
  • HY-136352
    Adenosine 5'-succinate

    Others Others
    Adenosine 5'-succinate is a chemically AMP-related compound and potently inhibits Denatonium benzoate/taste receptor activation of transducin.
  • HY-50910
    Temsirolimus

    CCI-779

    mTOR Autophagy Apoptosis Cancer
    Temsirolimus is an inhibitor of mTOR with an IC50 of 1.76 μM. Temsirolimus activates autophagy and prevents deterioration of cardiac function in animal model.
  • 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-N6946
    Mitraphylline

    Others Inflammation/Immunology
    Mitraphylline is the major pentacyclic oxindolic alkaloid presented in Uncaria tomentosa. Mitraphylline inhibits lipopolysaccharide-mediated activation of primary human neutrophils.
  • HY-101790A
    ZM223 hydrochloride

    NEDD8-activating Enzyme Cancer
    ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity.
  • HY-131035
    Lys-CoA TFA

    Histone Acetyltransferase Cancer
    Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC50=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC50=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation.
  • HY-129775
    K-Ras ligand-Linker Conjugate 1

    Target Protein Ligand-Linker Conjugate Cancer
    K-Ras ligand-Linker Conjugate 1 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 1 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
  • HY-107988
    MK-3903

    AMPK Metabolic Disease
    MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM.
  • HY-112705
    VU0529331

    Potassium Channel Neurological Disease
    VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 µM and 5.2 µM for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.
  • HY-134476
    NF-κΒ activator 1

    NF-κB Inflammation/Immunology
    NF-κΒ activator 1 is a potent NF-κΒ activator with an EC50 of 0.9 μM. NF-κΒ activator 1 induces superoxide dismutase (SOD)2 mRNA expression.
  • 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-16657
    TAPI-1

    MMP Cancer Inflammation/Immunology
    TAPI-1 is a TACE (ADAM17) inhibitor and blocks the shedding of several cell surface proteins. TAPI-1 is also a metalloproteinase (MMP) inhibitor.
  • HY-100737
    ML349

    Phospholipase Cancer
    ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.
  • HY-103334
    MAFP

    Methyl Arachidonyl Fluorophosphonate

    Phospholipase Metabolic Disease Neurological Disease Cardiovascular Disease
    MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.
  • HY-B0069
    Fludarabine

    F-ara-A; NSC 118218

    Nucleoside Antimetabolite/Analog DNA/RNA Synthesis STAT Apoptosis Cancer
    Fludarabine (NSC 118218) is a DNA synthesis inhibitor, which also inhibits phosphorylation of STAT1. Fludarabine, a pro-drug, is converted metabolically by dephosphorylation to the antimetabolite, F-ara-A.
  • HY-N3266
    Methyl rosmarinate

    Tyrosinase Cancer
    Methyl rosmarinate is a noncompetitive tyrosinase inhibitor which is isolated from Rabdosia serra, with an IC50 of 0.28 mM for mushroom tyrosinase, and also inhibits a-glucosidase.
  • HY-101587
    PGS-IN-1

    KME-4

    PGE synthase Lipoxygenase Inflammation/Immunology
    PGS-IN-1 is a potent inhibitor of prostaglandin synthetase (PGS) with an IC50 of 0.28 μM; also inhibits 5-lipoxygenase with an IC50 of 1.05 μM.
  • HY-125567
    Antileukinate

    CXCR Inflammation/Immunology
    Antileukinate, a hexapeptide, is a potent inhibitor of CXC-chemokine receptor (CXCR). Antileukinate inhibits neutrophil chemotaxis and activation. Antileukinate can be used for the research of acute inflammation and injury.
  • HY-124873
    SERCA2a activator 1

    Calcium Channel Cardiovascular Disease
    SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca 2+-dependent ATPase 2a (SERCA2a) activator. SERCA2a activator 1 attenuates phospholamban inhibition and enhances the systolic and diastolic functions of the heart. SERCA2a activator 1 can be used for heart failure.
  • HY-114398
    BAY-293

    Ras Cancer
    BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM. BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1). SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS.
  • HY-103697A
    Gardiquimod diTFA

    Toll-like Receptor (TLR) HIV Cancer Infection
    Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM.
  • HY-10119
    Vorapaxar

    SCH 530348

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
  • HY-B0939
    Etebenecid

    Others Metabolic Disease
    Etebenecid is a uricosuric agents, lower uric acid levels in the body by increasing the elimination of uric acid by the kidneys, also inhibits penicillin tubular secretion.
  • HY-101445
    Trolox

    Reactive Oxygen Species Ferroptosis Apoptosis Cancer
    Trolox is an analogue of vitamin E with a powerful antioxidant effect. Trolox is also a powerful inhibitor of membrane damage.
  • HY-14149
    Cisapride

    R 51619; (±)-Cisaprid

    5-HT Receptor Neurological Disease
    Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.
  • HY-B1305
    Chloropyramine hydrochloride

    FAK Histamine Receptor VEGFR Cancer Endocrinology
    Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.
  • HY-15102
    MK-0429

    L-000845704

    Integrin Inflammation/Immunology Cancer
    MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively.
  • HY-100671
    L002

    Histone Acetyltransferase STAT Cancer Inflammation/Immunology
    L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment.
  • HY-111789
    Subasumstat

    TAK-981

    E1/E2/E3 Enzyme Cancer Inflammation/Immunology
    Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.
  • HY-15707
    NS6180

    Potassium Channel Inflammation/Immunology
    NS6180 is a novel potent and selective KCa3.1 channel inhibitor(IC50= 9 nM) prevents T-cell activation and inflammation.
  • HY-N0708
    Vanillic acid

    NF-κB Bacterial Endogenous Metabolite Infection Inflammation/Immunology
    Vanillic acid is a flavoring agent found in edible plants and fruits. Vanillic acid inhibits NF-κB activation. Anti-inflammatory, antibacterial, and chemopreventive effects.
  • HY-B0099
    Edaravone

    MCI-186

    MMP Apoptosis Neurological Disease
    Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator.
  • HY-N0492
    α-Lipoic Acid

    Thioctic acid; (±)-α-Lipoic acid; DL-α-Lipoic acid

    NF-κB HIV Mitochondrial Metabolism Endogenous Metabolite Apoptosis Cancer Infection Inflammation/Immunology
    α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells.
  • HY-136477
    Pentagamavunon-1

    PGV-1

    Apoptosis COX VEGFR NF-κB Cancer
    Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation.
  • HY-10119A
    Vorapaxar sulfate

    SCH 530348 sulfate

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
  • HY-101297
    Z-IETD-FMK

    Z-IE(OMe)TD(OMe)-FMK

    Caspase Cancer
    Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.
  • HY-126382
    Hesperidin methylchalcone

    NF-κB Inflammation/Immunology
    Hesperidin methylchalcone (Hesperidin methyl chalcone) inhibits oxidative stress, cytokine production and NF-κB activation. Hesperidin methylchalcone inhibits inflammation and pain. Hesperidin methylchalcone exhibits vasoprotective activity.
  • HY-17376
    Ezetimibe

    SCH 58235

    Keap1-Nrf2 Autophagy Cardiovascular Disease Cancer
    Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
  • HY-N2065
    Withaferin A

    NF-κB Ferroptosis Cancer Inflammation/Immunology
    Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
  • HY-103097
    ST271

    Phospholipase Others
    ST271 is a potent inhibitor of protein tyrosine kinase (PTK), inhibits phospholipase D activation stimulated by fMet-Leu-Phe and PAF, with IC50s of 6.7 and 9 μM, respectively.
  • HY-50866
    NVP-AEW541

    AEW541

    IGF-1R Insulin Receptor Autophagy Cancer Endocrinology
    NVP-AEW541 is a potent inhibitor of IGF-1R with IC50 of 0.15 μM, also inhibits InsR, with IC50 of 0.14 μM.
  • HY-19696A
    Tauroursodeoxycholate Sodium

    Sodium tauroursodeoxycholate; Tauroursodeoxycholic acid sodium salt

    ERK Caspase Apoptosis Cancer
    Tauroursodeoxycholate Sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
  • HY-15881
    TCS JNK 5a

    JNK Inhibitor IX

    JNK Apoptosis Cancer
    TCS JNK 5a is a potent JNK3 inhibitor with a pIC50 of 6.7. TCS JNK 5a also inhibits JNK2 with a pIC50 of 6.5.
  • HY-14682
    GSK319347A

    IKK Inflammation/Immunology
    GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. GSK319347A also inhibits IKK2 with an IC50 of 790 nM.
  • HY-15192
    GSK 650394

    SGK Influenza Virus Cancer Infection
    GSK 650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively. GSK 650394 also inhibits influenza virus replication.
  • HY-15719
    NU 7026

    LY293646

    DNA-PK Apoptosis Cancer
    NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM.
  • HY-B0869A
    Bispyribac sodium

    Others Others
    Bispyribac sodium is a selective, systemic and post emergent herbicide used to eradicate grasses and broad leaf weeds. Bispyribac sodium is also an acetolactate synthase (ALS or known as AHAS) inhibitor.
  • HY-100223
    Calpeptin

    Cathepsin Proteasome Apoptosis Inflammation/Immunology
    Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.
  • HY-115446A
    Lenalidomide-C4-NH2 hydrochloride

    Cereblon ligand 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 32 hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    Lenalidomide-C4-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC (Compound 24), which has IC50s of 0.98 nM and 13.7 nM in inhibition of RS4;11 and MOLM-13 acute leukemia cell lines growth, respectively.
  • HY-D0843
    N-Ethylmaleimide

    NEM

    Cathepsin Deubiquitinase Others
    N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor.
  • HY-N1446B
    Sodium oleate

    Oleic acid sodium; 9-cis-Octadecenoic acid sodium; 9Z-Octadecenoic acid sodium

    Na+/K+ ATPase Apoptosis Cancer Metabolic Disease
    Sodium oleate (Oleic acid sodium) is an abundant monounsaturated fatty acid sodium. Sodium oleate is a Na +/K + ATPase activator.
  • HY-104038
    Gcase activator 1

    Glucosidase Neurological Disease
    Gcase activator 1 is an activator of glucocerebrosidase (Gcase) extracted from patent WO 2017192841 A1.
  • HY-12404
    Diminazene aceturate

    Diminazene diaceturate

    Parasite Angiotensin-converting Enzyme (ACE) Infection Inflammation/Immunology
    Diminazene aceturate (Diminazene diaceturate) is an anti-trypanosome agent for livestock. The main biochemical mechanism of the trypanocidal actions of Diminazene aceturate is by binding to trypanosomal kinetoplast DNA (kDNA) in a non-intercalative manner through specific interaction with sites rich in adenine-thymine base pairs. Diminazene aceturate is also an angiotensin-converting enzyme 2 (ACE2) activator and has strong and potent anti-inflammatory properties.
  • 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-12987
    Pimozide

    R6238

    Dopamine Receptor Adrenergic Receptor STAT Cancer Neurological Disease Endocrinology
    Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-B0831
    Buprofezin

    Reactive Oxygen Species Others
    Buprofezin is an insecticide that acts by inhibiting chitin synthesis. Buprofezin also dose-dependently increases the production of reactive oxygen species (ROS) in vitro.
  • HY-17390
    Loxapine

    5-HT Receptor Neurological Disease
    Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
  • HY-15595
    360A

    G-quadruplex Telomerase Cancer
    360A is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
  • HY-17390A
    Loxapine succinate

    5-HT Receptor Neurological Disease
    Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
  • HY-100548
    GSK621

    AMPK Autophagy Apoptosis Cancer
    GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation.
  • 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-15847
    HS38

    DAPK Cardiovascular Disease
    HS38 is a potent, selective, and ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK, also called DAPK3), with Kds of 300 nM and 280 nM, respectively. HS38 is also a PIM3 inhibitor with an IC50 of 200 nM. HS38 can be used for the research of smooth muscle related disorders.
  • HY-122818
    bpV(phen) trihydrate

    PTEN Phosphatase Parasite Apoptosis Cancer Infection Metabolic Disease Inflammation/Immunology
    bpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
  • HY-115687
    PDE4B-IN-2

    Phosphodiesterase (PDE)
    PDE4B-IN-2 is an orally active and selective PDE4B inhibitor (IC50=15 nM) and exhibits >100-fold selectivity for PDE4B over 4D. PDE4B-IN-2 regulates cAMP in inflammatory cells and inhibits LPS-induced TNF-α production and neutrophil accumulation in mouse lungs. PDE4B-IN-2 reduces microglial and neutrophil activation, and improves behavioral deficits in a traumatic brain injury model in vivo. PDE4B-IN-2 also exhibits antidepressant-like effects.
  • HY-108635
    C16-PAF

    PAF (C16)

    p38 MAPK MEK ERK Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease
    C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability.
  • HY-120859A
    Zidebactam sodium salt

    WCK-5107 sodium salt

    Bacterial Infection
    Zidebactam sodium salt (WCK-5107 sodium salt) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
  • HY-120859
    Zidebactam

    WCK-5107

    Bacterial Infection
    Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
  • HY-15718A
    Istaroxime hydrochloride

    PST2744 hydrochloride

    Na+/K+ ATPase Calcium Channel Cardiovascular Disease
    Istaroxime hydrochloride is a Na +/K +-ATPase inhibitor (IC50=0.11 μM) and a sarcoplasmic/endoplasmic reticulum calcium ATPase 2 (SERCA 2) activator.
  • HY-19205A
    CMI-392

    Lipoxygenase Inflammation/Immunology
    CMI-392 is a dual 5-lipoxygenese inhibitor and platelet-activating factor (PAF) receptor antagonist with IC50s of 100 and 10 nM, respectively.
  • HY-108634
    Apafant

    WEB 2086

    Others Inflammation/Immunology
    Apafant (WEB 2086), a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM.
  • HY-100611
    CaCCinh-A01

    Chloride Channel Cancer Inflammation/Immunology
    CaCCinh-A01 is an inhibitor of both TMEM16A and calcium-activated chloride channel (CaCC) with IC50s of 2.1 and 10 μM, respectively.
  • HY-19306
    SB-267268

    Integrin Cancer
    SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression.
  • HY-N0773
    Isovitexin

    Saponaretin; Homovitexin

    JNK NF-κB Inflammation/Immunology
    Isovitexin is a flavonoid isolated from rice hulls of Oryza sativa, possesses anti-inflammatory and anti-oxidant activities; Isovitexin acts like a JNK1/2 inhibitor and inhibits the activation of NF-κB.
  • HY-100221
    AM-2394

    Glucokinase Metabolic Disease
    AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC50 of 60 nM.
  • HY-16712
    LDN-214117

    TGF-β Receptor Cancer
    LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).
  • HY-114166
    2-D08

    E1/E2/E3 Enzyme TAM Receptor Cancer
    2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 also inhibits Axl with an IC50 of 0.49 nM.
  • HY-101840
    EIPA

    L593754; MH 12-43

    TRP Channel Sodium Channel Cancer Inflammation/Immunology
    EIPA (L593754) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na +/H +-exchanger (NHE) and macropinocytosis.
  • HY-101840A
    EIPA hydrochloride

    L593754 hydrochloride; MH 12-43 hydrochloride

    TRP Channel Sodium Channel Cancer Inflammation/Immunology
    EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also inhibits Na +/H +-exchanger (NHE) and macropinocytosis.
  • HY-13020
    GSK1838705A

    ALK IGF-1R Insulin Receptor Cancer Endocrinology
    GSK1838705A is a potent and reversible IGF-IR and the insulin receptor inhibitor with IC50s of 2.0 and 1.6 nM, respectively. It also inhibits ALK with an IC50 of 0.5 nM.
  • HY-B1816
    Zaprinast

    M&B 22948

    Phosphodiesterase (PDE) Neurological Disease Cardiovascular Disease Endocrinology
    Zaprinast (M&B 22948) is an inhibitor of cGMP-selective Phosphodiesterases(PDEs). Zaprinast is a G protein-coupled receptor (GPR) 35 agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects.
  • HY-108586
    NS3623

    Potassium Channel Neurological Disease
    NS3623 is an activator of human ether-a-go-go-related gene (hERG1/KV11.1) potassium channels. NS3623 activates the IKr and Ito currents and has antiarrhythmic effect. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels.
  • HY-50694
    Senicapoc

    ICA-17043

    Potassium Channel Others
    Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca 2+-activated K + channel; KCa3.1) blocker with an IC50 of 11 nM. Senicapoc blocks Ca 2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
  • HY-B0853
    Paclobutrazol

    Fungal Infection
    Paclobutrazol is a triazole-containing plant growth retardant that is known to inhibit the biosynthesis of gibberellins. Paclobutrazol also has antifungal activities. Paclobutrazol, transported acropetally in plants, can also suppress the synthesis of abscisic acid and induce chilling tolerance in plants. Paclobutrazol is typically used to support research on the role of gibberellins in plant biology.
  • HY-113960
    ERRα antagonist-1

    Estrogen Receptor/ERR Cancer
    ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.
  • HY-103490
    Takinib

    MAP3K Apoptosis Cancer
    Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, which inhibits autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation.
  • HY-105118A
    Zaldaride maleate

    CGS-9343B; KW 5617

    nAChR Metabolic Disease Inflammation/Immunology Neurological Disease
    Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate (CGS-9343B) inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM. Zaldaride maleate (CGS-9343B) prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR.
  • HY-105917
    Endovion

    NS3728

    Chloride Channel Others
    Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
  • HY-10326
    GW788388

    TGF-β Receptor Cancer
    GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
  • HY-13228
    YM-201636

    PIKfyve PI3K Autophagy Influenza Virus Cancer Infection
    YM-201636 is a potent and selective PIKfyve inhibitor with an IC50 of 33 nM. YM-201636 also inhibits p110α with an IC50 of 3.3 μM. YM-201636 inhibits retroviral replication.
  • HY-B0545
    Probenecid

    TRP Channel Bacterial HIV Metabolic Disease
    Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels.
  • HY-15595A
    360A iodide

    360 A iodide

    G-quadruplex Telomerase Cancer
    360A iodide is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
  • HY-123056
    EAD1

    Autophagy Apoptosis Cancer
    EAD1 is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 also induces apoptosis.
  • HY-19341
    Compound 401

    DNA-PK Cancer
    Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM) that also targets mTOR but not PI3K in vitro.
  • HY-19900
    ITX5061

    p38 MAPK Autophagy HCV Infection
    ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1).
  • HY-N0835
    (20S)-Protopanaxatriol

    20(S)-APPT; g-PPT

    Glucocorticoid Receptor Estrogen Receptor/ERR LXR Apoptosis Cardiovascular Disease Endocrinology
    (20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor.
  • HY-B1425
    Ethoxyquin

    HSP Reactive Oxygen Species Cancer
    Ethoxyquin is an antioxidant which has been used in animal feed for many years and also an inhibitor of heat shock protein 90 (Hsp90).
  • HY-15096
    MKT-077

    FJ-776

    HSP Cancer
    MKT-077 is a rhodacyanine dye and also a heat shock protein 70 (Hsp70) inhibitor which exhibits significant antitumor activity.
  • HY-N0625A
    Alpinetin

    PPAR Inflammation/Immunology Cancer
    Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity.
  • HY-12070
    DPH

    Bcr-Abl Cancer
    DPH is a potent cell permeable c-Abl activator, which displays potent enzymatic and cellular activity in stimulating c-Abl activation.  
  • HY-100381
    Nigericin sodium salt

    Potassium Channel NOD-like Receptor (NLR) Bacterial Antibiotic Cancer Infection
    Nigericin sodium salt is an antibiotic from Streptomyces hygroscopicus that works by acting as an H +, K +, and Pb 2+ ionophore, a NLRP3 activator.
  • HY-B0493
    Niflumic acid

    Chloride Channel Inflammation/Immunology
    Niflumic acid, a Ca2+-activated Cl- channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.
  • HY-N2787
    8-​Prenylnaringenin

    Apoptosis Cancer
    8-prenylnaringenin is a prenylflavonoid isolated from hop cones (Humulus lupulus), with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice .
  • HY-N6690
    Destruxin B

    Bcl-2 Family Caspase Apoptosis Cancer Infection
    Destruxin B, isolated from entomopathogenic fungus Metarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B induces apoptosis via a Bcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lung cancer cells. Destruxin B significantly activates caspase-3 and reduces tumor cell proliferation through caspase-mediated apoptosis, not only in vitro but also in vivo.
  • HY-107436
    LE135

    RAR/RXR TRP Channel Cancer Neurological Disease
    LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC50s of 2.5 μM and 20 μM, respectively.
  • HY-135483A
    AR-R17779 hydrochloride

    nAChR Neurological Disease
    AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis of 92 and 16000 nM for α7 and α4β2 subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways.
  • HY-15098
    Apoptozole

    Apoptosis Activator VII

    HSP Apoptosis Cancer
    Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.
  • HY-138558
    PAR-2-IN-1

    Protease-Activated Receptor (PAR) Cancer Inflammation/Immunology
    PAR-2-IN-1 is a protease-activated receptor-2 (PAR2) signaling pathway inhibitor with anti-inflammatory and anticancer effects.
  • 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-13296
    PYR-41

    E1/E2/E3 Enzyme Apoptosis Cancer
    PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
  • HY-19084
    Ro-24-0238

    Others Inflammation/Immunology
    Ro-24-0238 is an antagonist of platelet activating factor (PAF) and inhibitor of thromboxane synthesis, used for lessening the inflammation and damage resulting from a local release of PAF.
  • HY-N0629
    Maslinic acid

    Crategolic acid; 2α-Hydroxyoleanolic acid

    NF-κB Bacterial HIV Inflammation/Immunology Cancer
    Maslinic acid can inhibit the DNA-binding activity of NF-κB p65 and abolish the phosphorylation of IκB-α, which is required for p65 activation.
  • HY-U00444
    DDR1-IN-2

    Discoidin Domain Receptor Inflammation/Immunology
    DDR1-IN-2 is a potent inhibitor of discoidin domain receptor 1 (DDR1), with an IC50 of 13.1 nM, and also less potently inhibits DDR2, with an IC50 of 203 nM.
  • HY-16736
    Centanafadine

    EB-1020

    Adrenergic Receptor Dopamine Transporter Serotonin Transporter Neurological Disease Endocrinology
    Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
  • HY-16736A
    Centanafadine hydrochloride

    EB-1020 hydrochloride

    Adrenergic Receptor Dopamine Transporter Serotonin Transporter Neurological Disease Endocrinology
    Centanafadine (hydrochloride) is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
  • HY-100695
    DDR-TRK-1

    Discoidin Domain Receptor Cancer
    DDR-TRK-1 is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR-TRK-1 also inhibits TRK family.
  • HY-100625
    BVT948

    Phosphatase Cytochrome P450 Histone Methyltransferase Cancer
    BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8 (KMT5A).
  • HY-P1291
    PKI 14-22 amide,myristoylated

    PKA Cancer
    PKI 14-22 amide,myristoylated is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
  • HY-17362
    Vancomycin hydrochloride

    Bacterial Autophagy Antibiotic Infection Cancer
    Vancomycin hydrochloride is an antibiotic for the treatment of bacterial infections. It acts by inhibiting the second stage of cell wall synthesis of susceptible bacteria. Vancomycin also alters the permeability of the cell membrane and selectively inhibits ribonucleic acid synthesis.
  • HY-12063
    PHT-427

    Akt Apoptosis Cancer
    PHT-247 is an inhibitor of the pleckstrin homology (PH) domain of Akt, and it is also an inhibitor of PDPK1 with Kis of 2.7 µM and 5.2 µM and for Akt and PDPK1, respectively.
  • HY-100395
    F16

    Apoptosis Cancer
    F16 is a potent growth inhibitor of the neu-overexpressing cells and also selectively inhibits proliferation of mammary epithelial as well as a variety of mouse mammary tumor and human breast cancer cell lines.
  • HY-110153
    NS19504

    Potassium Channel Neurological Disease
    NS19504 is a Ca 2+-activated K + channel (BK channel, KCa1.1 channel) activator (EC50=11.0 µM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions.
  • HY-100227
    E 64c

    Cathepsin SARS-CoV Metabolic Disease
    E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
  • 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-114372
    Lycopodine

    Lipoxygenase Caspase Apoptosis Cancer
    Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.
  • HY-124822
    COH-SR4

    AMPK Cancer Metabolic Disease
    COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation. COH-SR4 can be used for the research of obesity and related metabolic disorders.
  • 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-N1446
    Oleic acid

    9-cis-Octadecenoic acid; 9Z-Octadecenoic acid

    Na+/K+ ATPase Endogenous Metabolite Apoptosis Cancer Metabolic Disease
    Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid. Oleic acid is a Na +/K + ATPase activator.
  • HY-70002
    Enzalutamide

    MDV3100

    Androgen Receptor Autophagy Cancer
    Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator.
  • HY-135884
    PKR activator 2

    Pyruvate Kinase Cardiovascular Disease
    PKR activator 2 is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035863A1, compound 385.
  • HY-102052
    DCEBIO

    Potassium Channel Inflammation/Immunology
    DCEBIO, a derivative of 1-EBIO, is an extremely potent activator of Cl - secretion in T84 colonic cells. DCEBIO stimulates Cl - secretion via the activation of hIK1 K + channels and the activation of an apical membrane Cl - conductance.
  • HY-B0211
    Riluzole

    PK 26124

    Sodium Channel GABA Receptor Neurological Disease
    Riluzole is an anticonvulsant drug and belongs to the family of use-dependent Na + channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
  • HY-B0211A
    Riluzole hydrochloride

    PK 26124 hydrochloride

    Sodium Channel GABA Receptor Neurological Disease
    Riluzole hydrochloride is an anticonvulsant drug and belongs to the family of use-dependent Na + channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
  • HY-10999
    Trametinib

    GSK1120212; JTP-74057

    MEK Autophagy Apoptosis Cancer
    Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
  • HY-N2119
    Sciadopitysin

    NF-κB Inflammation/Immunology
    Sciadopitysin is a type of biflavonoids in leaves from ginkgo biloba. Sciadopitysi inhibits RANKL-induced osteoclastogenesis and bone loss by inhibiting NF-κB activation and reducing the expression of c-Fos and NFATc1.
  • HY-N4171
    Dihydrocucurbitacin B

    Others Inflammation/Immunology
    Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activated T cells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity.
  • HY-13865
    P 22077

    Deubiquitinase Cancer
    P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. P 22077 also inhibits USP47 with an EC50 of 8.74 μM.
  • HY-112182
    UM-164

    DAS-DFGO-II

    Src p38 MAPK Autophagy Cancer
    UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
  • HY-19502
    Artemisone

    Artemifone; BAY 44-9585

    Parasite CMV Infection
    Artemisone (Artemifone) is a potent and semi-synthetic antimalarial, inhibits P. falciparum strains, with a mean IC50 of 0.83 nM. Artemisone is also a potent inhibitor of human CMV.
  • HY-B0114
    Oxcarbazepine

    GP 47680

    Sodium Channel Neurological Disease
    Oxcarbazepine (GP 47680) inhibits the binding of [3H]BTX to sodium channels with IC50 of 160 μM and also inhibits the influx of 22Na+ into rat brain synaptosomes with IC50 about 100 μM.
  • HY-14622
    Necrostatin 2

    RIP kinase Cancer
    Necrostatin 2 is a potent necroptosis inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM. Necrostatin 2 is also a RIPK1 inhibitor.
  • HY-108940
    GlyRS-IN-1

    Aminoacyl-tRNA Synthetase Bacterial Cancer Infection
    GlyRS-IN-1 is a glycyl-tRNA synthase (GlyRS) inhibitor extracted from patent WO 2017066459 A1. GlyRS-IN-1 can also inhibit the growth of bacteria.
  • HY-123962
    G6PD activator AG1

    Others Metabolic Disease
    G6PD activator AG1 is a potent and selective glucose-6-phosphate dehydrogenase (G6PD) activator with an EC50 of 3 µΜ. G6PD activator AG1 reduces hemolysis of human erythrocytes.
  • HY-N6781
    Ophiobolin A

    Phosphodiesterase (PDE) Cancer Infection
    Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase, with an IC50 value of 9 μM. Ophiobolin A antimicrobial and anticancer activity.
  • HY-N0177
    Diosgenin

    STAT Metabolic Disease
    Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway. Diosgenin is an exogenous activator of Pdia3/ERp57.
  • HY-13772
    Valrubicin

    AD-32

    PKC Cancer Inflammation/Immunology
    Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively, and has antitumor and antiinflammatory activity.
  • HY-N0754
    Eupalinolide A

    HSP Inflammation/Immunology
    Eupalinolide A, isolated from Eupatorium lindleyanum, induces the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90.
  • HY-120261
    GB-88

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca 2+ release with an IC50 of 2 µM.
  • HY-B0649
    Propofol

    2,6-Diisopropylphenol

    GABA Receptor Endogenous Metabolite Neurological Disease
    Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic.
  • HY-N6046
    Kamebakaurin

    NF-κB Cancer Inflammation/Immunology
    Kamebakaurin is a natural compound isolated from Isodon japonicus. Kamebakaurin is a potent inhibitor of NF-κB activation by directly targeting DNA-binding activity of p50.
  • HY-B0795
    MHY1485

    mTOR Autophagy Cancer
    MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.
  • HY-101763A
    (S,R,S)-AHPC hydrochloride

    VH032-NH2 hydrochloride; VHL ligand 1 hydrochloride

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC hydrochloride can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
  • HY-10201
    Sorafenib

    Bay 43-9006

    Raf VEGFR FLT3 Autophagy Apoptosis Ferroptosis Cancer
    Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator.
  • 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-10201A
    Sorafenib Tosylate

    Bay 43-9006 tosylate

    Raf VEGFR FLT3 Autophagy Ferroptosis Apoptosis Cancer
    Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosis activator.
  • HY-13454
    CID 2011756

    PKD Cancer
    CID 2011756 is an ATP competitive PKD inhibitor, with an IC50 of 3.2 µM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC50, 0.6 and 0.7 µM, respectively). CID 2011756 also has antitumor activity.
  • HY-13636
    Fulvestrant

    ICI 182780; ZD 9238; ZM 182780

    Estrogen Receptor/ERR Autophagy Apoptosis Cancer
    Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
  • 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-108593
    BMS-191011

    BMS-A

    Potassium Channel Neurological Disease
    BMS-191011 (BMS-A) is an opener of the large-conductance, Ca 2+-activated potassium (maxi-K) channel, effective in stroke models.
  • HY-124793A
    GAK inhibitor 49 hydrochloride

    Others Infection
    GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 hydrochloride also shows binding to RIPK2.
  • HY-124793
    GAK inhibitor 49

    Others Infection
    GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2.
  • HY-101202
    SNC80

    NIH 10815

    Opioid Receptor Neurological Disease
    SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.
  • HY-108584
    Flindokalner

    BMS-204352

    Potassium Channel Neurological Disease
    Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
  • HY-17366A
    Clozapine N-oxide dihydrochloride

    mAChR Dopamine Receptor Drug Metabolite Neurological Disease
    Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
  • HY-17366
    Clozapine N-oxide

    mAChR Dopamine Receptor Drug Metabolite Neurological Disease
    Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
  • HY-131445
    RJW100

    MicroRNA Cancer Endocrinology
    RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC50s of 6.6 and 7.5, respectively. RJW100 also causes strong activation of the miR-200c (miRNA-200c, microRNA-200c) promoter.
  • HY-130354
    Dibutyryl-cGMP sodium

    Bt2cGMP sodium

    Potassium Channel Cardiovascular Disease
    Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [ 3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K + channels.
  • HY-18307
    SYN1143

    c-Met/HGFR Cancer
    SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively. SYN1143 has weak inhibitory activity on Lck, Tie2, Src, and BTK with IC50s ranging from 160 to 710 nM. SYN1143 can be used for the research of cancers that RON and c-Met are activated.
  • HY-15760
    Necrostatin-1

    Nec-1

    RIP kinase Autophagy Indoleamine 2,3-Dioxygenase (IDO) Ferroptosis Cancer
    Necrostatin-1 (Nec-1) is a potent necroptosis inhibitor with an EC50 of 490 nM in Jurkat cells. Necrostatin-1 inhibits RIP1 kinase (EC50=182 nM). Necrostatin-1 is also an IDO inhibitor.
  • HY-15295
    Vonoprazan Fumarate

    TAK-438

    Proton Pump Metabolic Disease
    Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
  • HY-N2006
    Ganoderic acid B

    HIV Protease Infection
    Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease.
  • HY-18253
    Udenafil

    DA8159

    Phosphodiesterase (PDE) Endocrinology Others
    Udenafil (DA8159) is a potent, selective and orally active phosphodiesterase type 5 (PDE5) inhibitor. Udenafil also inhibits cGMP hydrolysis and can be used for erectile dysfunction research.
  • HY-D0145
    7-Ethoxyresorufin

    Resorufin ethyl ether

    Cytochrome P450 NO Synthase Others
    7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase.
  • HY-13785
    ZM 306416

    CB 676475

    VEGFR Cancer
    ZM-306416 (CB 676475) is a potent inhibitor of VEGFR with IC50s of 0.1 and 2 μM for KDR and Flt, respectively. ZM-306416 is also a EGFR inhibitor with an IC50 of <10 nM.
  • HY-19696
    Tauroursodeoxycholate

    TUDCA; UR 906; Taurolite

    ERK Caspase Endogenous Metabolite Apoptosis Cancer
    Tauroursodeoxycholate (TUDCA; UR 906; Taurolite) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
  • HY-B0250
    Lamivudine

    BCH-189

    HIV Reverse Transcriptase Infection
    Lamivudine (BCH-189) is a nucleoside reverse transcriptase inhibitors (NRTIs). Lamivudine (BCH-189) can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus.
  • HY-10321
    PD173074

    FGFR VEGFR Apoptosis Cancer
    PD173074 is a potent FGFR1 inhibitor with an IC50 of 25 nM and also inhibits VEGFR2 with an IC50 of 100-200 nM, showing 1000-fold selectivity for FGFR1 over PDGFR and c-Src.
  • HY-P1291A
    PKI 14-22 amide,myristoylated TFA

    PKA Cancer
    PKI 14-22 amide,myristoylated TFA is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated TFA reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
  • 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-N0054
    Osthole

    Osthol; NSC 31868

    Histamine Receptor Apoptosis Parasite HBV Cancer Infection Endocrinology Inflammation/Immunology Cardiovascular Disease
    Osthole (Osthol) 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-N2192
    Swertianolin

    AChE HBV Bacterial Infection Inflammation/Immunology
    Swertianolin, a xanthone isolated from Gentianella Acuta, inhibits acetylcholinesterase (AChE). Swertianolin also exhibits anti-HBV and anti-bacterial activity.
  • HY-13895
    WHI-P154

    EGFR JAK Apoptosis Cancer
    WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively.
  • HY-102003
    Rucaparib Camsylate

    PARP Cancer
    Rucaparib Camsylate is an inhibitor of PARP with a Ki of 1.4 nM for PARP1. Rucaparib Camsylate also shows binding affinity to eight other PARP domains.
  • HY-12303
    OAC1

    Oct3/4 Others
    OAC1 is a Octamer-binding transcription factor 4 (Oct4)-activating compound; enhances the iPSC reprogramming efficiency and accelerated the reprogramming process.
  • HY-131018
    Jedi2

    Others Inflammation/Immunology Neurological Disease
    Jedi2 is a Piezo1 activator, but not a specific Piezo2 activator. Jedi2 binds to the mouse Piezo1 proteins with a Kd of 2770  μM.
  • HY-14714
    NSC-207895

    XI-006

    MDM-2/p53 Cancer
    NSC-207895 (XI-006), a DNA damaging agent, is an anticancer agent and p53 activator.
  • HY-N2632
    Uvarigrin

    Apoptosis Cancer
    Uvarigrin, isolated from the roots of Uvaria calamistrata, induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation.
  • HY-100007
    Vonoprazan

    TAK-438 free base

    Proton Pump Endocrinology
    Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
  • 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-101255
    ODQ

    Guanylate Cyclase Apoptosis Cancer
    ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells.
  • HY-133558
    VII-31

    E1/E2/E3 Enzyme Apoptosis Cancer
    VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways.
  • HY-N0168A
    (Rac)-Hesperetin

    p38 MAPK Apoptosis Autophagy Cancer Neurological Disease
    (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
  • HY-16677A
    Mofegiline hydrochloride

    MDL72974A

    Monoamine Oxidase Neurological Disease
    Mofegiline hydrochloride (MDL72974A) is a potent and selective enzyme-activated irreversible inhibitor of MAO-B; shows marked selectivity for the B form (IC50 = 680 and 3.6 nM for MAO-A and MAO-B).
  • HY-19770
    GSK2981278

    ROR Inflammation/Immunology
    GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.
  • HY-13595
    Chrysophanol

    Chrysophanic acid

    EGFR Cancer
    Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.
  • 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-10257
    BAY 11-7085

    BAY 11-7083

    NF-κB Ferroptosis Apoptosis Cancer
    BAY 11-7085 (BAY 11-7083) is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC50 of 10 μM.
  • HY-112816
    MA242

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    MA242 is a dual inhibitor of murine double minute 2 (MDM2) and nuclear factor of activated T cells 1 (NFAT1) for Pancreatic Cancer Therapy.
  • HY-18286
    NCGC00229600

    TSH Receptor Endocrinology
    NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease.
  • 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-N1483
    Guanfu base A

    Potassium Channel Cardiovascular Disease
    Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes. Guanfu base A also inhibits HERG channel current.
  • HY-B0520A
    Benztropine mesylate

    Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate

    Dopamine Receptor mAChR Histamine Receptor Cancer Neurological Disease
    Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
  • HY-103269
    BAI1

    Bcl-2 Family Apoptosis Cancer
    BAI1 is a selective and allosteric inhibitor of BAX, an apoptosis regulator. BAI1 directly binds to BAX and allosterically inhibits BAX activation. BAI1 has the potential for the research of diseases mediated by BAX-dependent cell death.
  • HY-135883
    PKR activator 1

    Pyruvate Kinase Cardiovascular Disease
    PKR activator 1 is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035865A1, compound E7-93.
  • HY-12647
    GPR40 Activator 2

    GPR40 Metabolic Disease
    GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.
  • HY-103368
    Eact

    Chloride Channel Neurological Disease
    Eact is a selective and potent activator of TMEM16A, directly activates the TRPV1 channels in sensory nociceptors and produces itch, acute nociception and thermal hypersensitivity.
  • HY-17538
    ZLN005

    PGC-1α Autophagy Metabolic Disease
    ZLN005 is a potent activator of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α).
  • HY-104047
    LM22B-10

    Trk Receptor Akt ERK Neurological Disease
    LM22B-10 is an activator of TrkB/TrkC neurotrophin receptor, and can induce TrkB, TrkC, AKT and ERK activation in vitro and in vivo.
  • HY-16670
    Dafadine-A

    Cytochrome P450 Others
    Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1).
  • HY-50752
    LY-411575

    γ-secretase Notch Apoptosis Neurological Disease
    LY-411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), and also inhibits Notch S3 cleavage with IC50 of 0.39 nM.
  • HY-76383
    LR-90

    Others Metabolic Disease Inflammation/Immunology
    LR-90 is an advanced glycation end product (AGE) inhibitor, inhibits inflammatory responses in human monocytes. LR-90 is also used in the research of diabetic animal model.
  • HY-100957
    Dilazep dihydrochloride

    Others Cardiovascular Disease
    Dilazep dihydrochloride is an inhibitor of adenosine uptake. Dilazep dihydrochloride has cerebral and coronary vasodilating action through enhancement of effect of adenosine. Dilazep dihydrochloride also inhibits the ischemic damage, platelet aggregation, and membrane transport of nucleosides.
  • HY-129571
    BioE-1115

    Ser/Thr Protease Casein Kinase Metabolic Disease
    BioE-1115 is a highly selective and potent PAS kinase (PASK) inhibitor with an IC50 of ~4 nM. BioE-1115 is also a potent casein kinase 2α inhibitor with an IC50 of ~10 μM.
  • HY-13438
    AZD3839 free base

    Beta-secretase Cancer
    AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor.
  • HY-B0579
    Cyclosporin A

    Cyclosporine; Ciclosporin; CsA

    Phosphatase Complement System Antibiotic Inflammation/Immunology Cancer
    Cyclosporin A is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC50 of 5 nM. Cyclosporin A also inhibits CD11a/CD18 adhesion.
  • HY-12659
    LX7101

    ROCK Others
    LX7101 is a potent inhibitor of LIMK and ROCK2 with IC50 values of 24, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2, respectively; also inhibits PKA with an IC50 less than 1 nM.
  • HY-N2019
    Chaetocin

    Histone Methyltransferase Bacterial Antibiotic Cancer Infection
    Chaetocin is a specific inhibitor of the histone methyltransferase (HMT) SU(VAR)3-9 with an IC50 of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 μM.
  • HY-N7018
    20-Hydroxyganoderic Acid G

    Others Inflammation/Immunology
    20-Hydroxyganoderic Acid G is a lanostane triterpenoid obtained from the EtOH extract of fruiting bodies of the Ganoderma curtisii. 20-Hydroxyganoderic Acid G inhibits BV-2 microglia cells activated by LPS with an IC50 of 21.33 μM. 20-Hydroxyganoderic Acid G has therapeutic potential in the drug discovery of nerve inflammation diseases associated with microglia activated by LPS.
  • 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-N4116
    Xanthyletin

    Fungal Cancer Infection
    Xanthyletin is a coumarin isolated from Citrus, with anti-tumor and anti-bacterial activities. Xanthyletin also inhibits symbiotic fungus cultivated by leaf-cutting ants.
  • HY-B1478
    Dimaprit dihydrochloride

    Histamine Receptor NO Synthase Endocrinology
    Dimaprit dihydrochloride is a selective histamine H2 receptor agonist, it also inhibits nNOS with an IC50 of 49 μM. Dimaprit dihydrochloride can stimulate gastric acid secretion.
  • HY-N0765
    Isoliquiritin

    Fungal Infection Inflammation/Immunology Neurological Disease
    Isoliquiritin, isolated from Licorice Root, inhibits angiogenesis and tube formation. Isoliquiritin also exhibits antidepressant-like effects and antifungal activity.
  • HY-15589
    GW9508

    GPR40 Potassium Channel Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.
  • HY-15701
    Leukadherin-1

    Integrin Complement System Inflammation/Immunology
    Leukadherin-1, a specific agonist of the leukocyte surface integrin CD11b/CD18, increases CD11b/CD18-dependent cell adhesion to fibrinogen with an EC50 of 4 μM. Leukadherin-1 enhances leukocyte adhesion to ligands (such as ICAM-1) and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites. Leukadherin-1 suppresses innate inflammatory signaling.
  • HY-101860
    GIBH-130

    Interleukin Related Neurological Disease
    GIBH-130 is an effective inhibitor of neuroinflammation. GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50=3.4 nM).
  • HY-P2228
    Chlamydocin

    HDAC Apoptosis Cancer
    Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3.
  • HY-114481
    Imidazole ketone erastin

    IKE

    Ferroptosis Cancer
    Imidazole ketone erastin is a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system xc - and an activator of ferroptosis. Imidazole ketone erastin has anti-tumor activity.
  • HY-14290A
    Pinacidil monohydrate

    Potassium Channel Others
    Pinacidil monohydrate, an antihypertensive drug, is a potassium channel activator.
  • HY-133114
    Ezetimibe ketone

    EZM-K

    Keap1-Nrf2 Autophagy Cancer Cardiovascular Disease
    Ezetimibe ketone (EZM-K) is a phase-I metabolite of Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe is a potent cholesterol absorption inhibitor.
  • HY-112800
    cyt-PTPε Inhibitor-1

    Phosphatase Metabolic Disease
    cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity.
  • HY-118532
    Tyrphostin AG30

    AG30

    EGFR Cancer
    Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.
  • 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-U00292
    AMPK activator 1

    AMPK Metabolic Disease
    AMPK activator 1 is an AMPK activator extracted from patent WO2013116491A1, compound No.1-75, has an EC50 of <0.1μM.
  • HY-128574
    GLUT4 activator 1

    GLUT Metabolic Disease
    GLUT4 activator 1 (Compound 26b) is a potent glucose transporter type 4 (GLUT4) translocation activator with an EC50 of 0.14 μM.
  • HY-119931
    2-Hydroxychalcone

    Bcl-2 Family Apoptosis NF-κB Cancer Metabolic Disease
    2-hydroxychalcone, a natural flavonoid, is a potent antioxidant, inhibiting lipid peroxidation. 2-Hydroxychalcone induces apoptosis by Bcl-2 downregulation. 2-Hydroxychalcone inhibits the activation of NF-kB.
  • 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-127002A
    Squarunkin A hydrochloride

    Src Cancer
    Squarunkin A hydrochloride is a potent and selective UNC119-cargo interaction inhibitor (IC50 of 10 nM for inhibiting the UNC119A-myristoylated Src N-terminal peptide interaction). Squarunkin A hydrochloride interferes with the activation of Src kinase in cells.
  • 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-15198
    KG5

    Raf PDGFR FLT3 c-Kit Cancer
    KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.
  • HY-123390
    DB07107

    Bcr-Abl Akt Cancer
    DB07107 is a potent drug resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM.
  • HY-80013A
    THZ1 Hydrochloride

    CDK Cancer
    THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
  • HY-104074
    Pocapavir

    SCH-48973; V-073

    Enterovirus Infection
    Pocapavir (SCH-48973) is an orally active capsid inhibitor. Pocapavir prevents virion uncoating upon entry into the cell. Pocapavir has antiviral activity against polioviruses. Pocapavir also inhibits enterovirus infections.
  • HY-12338
    ON 146040

    PI3K Bcr-Abl Cancer
    ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).
  • HY-80013
    THZ1

    CDK Cancer
    THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
  • HY-12054
    Hesperadin

    Aurora Kinase Autophagy Influenza Virus Parasite Cancer
    Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.
  • HY-101499
    GKT136901

    NADPH Oxidase Metabolic Disease Inflammation/Immunology Neurological Disease
    GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 is also a selective and direct scavenger of peroxynitrite. GKT136901 can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 also has anti-inflammatory activity.
  • HY-125845
    (S,R,S)-AHPC

    VH032-NH2; VHL ligand 1

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
  • HY-42424
    (S,R,S)-AHPC-Me hydrochloride

    VHL ligand 2 hydrochloride; E3 ligase Ligand 1

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
  • HY-42424A
    (S,R,S)-AHPC-Me dihydrochloride

    VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
  • HY-137516
    LC-2

    PROTAC Ras Cancer
    LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines.
  • HY-130269
    β-Naphthoflavone-CH2-OH

    β-NF-CH2-OH

    Ligand for E3 Ligase Cancer
    β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) is a ligand for arylhydrocarbon receptor (AhR) E3 ligase. β-Naphthoflavone-CH2-OH can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1) that recruit the AhR E3 ligase complex by incorporating AhR ligands into chimeric molecules. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
  • HY-112078
    (S,R,S)-AHPC-Me

    VHL ligand 2; E3 ligase Ligand 1A

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
  • 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-133615
    8(14)-Abietenic acid

    Others Others
    8(14)-Abietenic acid is an abietane diterpenoid. Abietenic acid is racemic of 8(14)-Abietenic acid. Abietenic acid acts as a PPARα/γ dual activator.
  • HY-101069
    Y-26763

    Potassium Channel Cardiovascular Disease
    Y-26763 is a K + channel opener and active metabolite of Y-27152. Y-26763 is an ATP-sensitive K + (KATP) channel activator.
  • HY-N2432
    Paederoside

    HBV Cancer Infection
    Paederoside is a monoterpene S-methyl thiocarbonate isolated from Paederia pertomentosa. Paederoside shows a high anti-tumor promoting activity against the Epstein-Barr virus activation.
  • HY-18175
    CCT244747

    Checkpoint Kinase (Chk) Cancer
    CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
  • HY-13424
    RITA

    NSC 652287

    MDM-2/p53 Autophagy DNA Alkylator/Crosslinker Cancer
    RITA is an inhibitor of p53-HDM-2 interaction, binds to p53dN, with a Kd of 1.5 nM, and also induces DNA-DNA cross-links.
  • HY-15489
    Scriptaid

    Scriptide; GCK1026

    HDAC Autophagy Apoptosis Influenza Virus Cancer
    Scriptaid is a potent histone deacetylase (HDAC) inhibitor, used in cancer research. Scriptaid is also a sensitizer to antivirals and has potential for epstein-barr virus (EBV)-associated lymphomas treatment.
  • HY-B1473
    Serotonin hydrochloride

    5-Hydroxytryptamine hydrochloride; 5-HT hydrochloride

    5-HT Receptor COMT Endogenous Metabolite Neurological Disease
    Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
  • HY-15312
    WP1066

    STAT JAK Apoptosis Cancer
    WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.
  • HY-U00170
    Bunaprolast

    U66858

    Leukotriene Receptor Prostaglandin Receptor Lipoxygenase Inflammation/Immunology Endocrinology
    Bunaprolast (U66858) is a potent inhibitor of LTB4 production in human whole blood. Bunaprolast (U66858) also exhibits significant inhibition of lipoxygenase and TXB2 release.
  • HY-18629
    SU9516

    CDK Autophagy Apoptosis Cancer
    SU9516 is a potent CDK2 inhibitor, with an IC50 of 22 nM, and also shows inhibitory effects on CDK1 and CDK4, with IC50s of 40, 200 nM, respectively.
  • HY-B0941
    6-Benzylaminopurine

    Benzyladenine; 6-BAP; N6-Benzyladenine

    Others Others
    6-Benzylaminopurine is a first-generation synthetic cytokinin that elicits plant growth and development, also is an inhibitor of respiratory kinase in plants, increases post-harvest life of green vegetables.
  • 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-B0527A
    Amitriptyline hydrochloride

    Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor Neurological Disease
    Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity.
  • HY-13324
    Bardoxolone methyl

    RTA 402; NSC 713200; CDDO Methyl ester

    Keap1-Nrf2 Autophagy Apoptosis Ferroptosis Cancer
    Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester) is a synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities, acting as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway.
  • HY-13255A
    TAME hydrochloride

    APC Cancer
    TAME hydrochloride is an inhibitor of anaphase-promoting complex/cyclosome (APC/C or APC), which binds to APC/C and prevents its activation by Cdc20 and Cdh1, produces mitotic arrest.
  • 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-13255
    TAME

    APC Cancer
    TAME is an inhibitor of anaphase-promoting complex/cyclosome (APC/C or APC), which binds to APC/C and prevents its activation by Cdc20 and Cdh1, produces mitotic arrest.
  • HY-17471A
    Metformin hydrochloride

    1,1-Dimethylbiguanide hydrochloride

    AMPK Autophagy Mitophagy Metabolic Disease Cardiovascular Disease
    Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy.
  • HY-13520
    Nocodazole

    Oncodazole; R17934

    Microtubule/Tubulin Bcr-Abl CRISPR/Cas9 Autophagy Apoptosis Cancer
    Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
  • HY-N0447
    8-Gingerol

    TRP Channel Infection Inflammation/Immunology Cancer
    8-Gingerol, found in the rhizomes of ginger (Z. officinale) with oral bioavailability, activates TRPV1, with an EC50 of 5.0 µM. 8-Gingerol inhibits COX-2, and inhibits the growth of H. pylori in vitro.
  • HY-10219
    Rapamycin

    Sirolimus; AY-22989

    mTOR FKBP Fungal Autophagy Endogenous Metabolite Antibiotic Cancer
    Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
  • 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-N0170
    Indole-3-carbinol

    I3C; 3-Indolemethanol

    NF-κB Aryl Hydrocarbon Receptor E1/E2/E3 Enzyme Endogenous Metabolite Cancer
    Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).
  • HY-13034
    Gandotinib

    LY2784544

    JAK FLT3 FGFR VEGFR Cancer
    Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM.
  • HY-32718
    Pelitinib

    EKB-569; WAY-EKB 569

    EGFR Src Cancer
    Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.
  • HY-111947
    c-Fms-IN-6

    c-Fms Inflammation/Immunology
    c-Fms-IN-6 is a potent inhibitor of c-FMS, with an IC50 of ≤10 nM for unphosphorylated c-FMS, also weakly inhibits unphosphorylated c-KIT and PDGFR (IC50, > 1 μM). Used in the research of autoimmune diseases.
  • HY-16026
    Ricolinostat

    ACY-1215; Rocilinostat

    HDAC Apoptosis Cancer
    Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.
  • HY-N2000
    Bellidifolin

    HIV Cancer Infection Inflammation/Immunology
    Bellidifolin is a xanthone isolated from the stems of Swertia punicea, with hepatoprotective, hypoglycemic, anti-oxidation, anti-inflammatory and antitumor activities. Bellidifolin also acts as a viral protein R (Vpr) inhibitor.
  • HY-N1926
    Dihydrocoumarin

    Hydrocoumarin; Chroman-2-one

    Sirtuin Cancer
    Dihydrocoumarin is a compound found in Melilotus officinalis. Dihydrocoumarin is a yeast Sir2p inhibitor. Dihydrocoumarin also inhibits human SIRT1 and SIRT2 with IC50s of 208 μM and 295 μM, respectively.
  • HY-P0240
    Tuftsin

    Endogenous Metabolite Inflammation/Immunology
    Tuftsin is a tetrapeptide. Tuftsin is a macrophage/microglial activator.
  • HY-101594
    Tulopafant

    RP 59227

    Others Cardiovascular Disease
    Tulopafant is a platelet activating factor (PAF) antagonist.
  • HY-101675
    Setipafant

    BN-50727; LAU-0901

    Others Cardiovascular Disease
    Setipafant is a platelet-activating factor (PAF) antagonist.
  • 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-133614
    Dihydroisopimaric acid

    Potassium Channel Others
    Dihydroisopimaric acid activates large conductance Ca 2+ activated K + (BK) channels alphabeta1 in the direct measurement of BKalphabeta1 opening under whole-cell voltage clamp.
  • HY-N6892
    3'-​O-​Acetylhamaudol

    Others Cancer
    3'-O-Acetylhamaudol, isolated from Angelica japonica roots, exhibits anti-tumor activity through dual actions, anti-angiogenesis and intestinal intraepithelial lymphocyte activation.
  • HY-12041
    SP600125

    JNK Autophagy Apoptosis Ferroptosis Cancer
    SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 inhibits autophagy and activates apoptosis.
  • 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-70083
    SPK-601

    LMV-601

    Phospholipase Reverse Transcriptase Infection
    SPK-601 (LMV-601) is an inhibitor of the phosphatidylcholine-specific phospholipase C (PC-PLC). SPK-601 also can be used as an antimicrobial agent.
  • HY-13777
    Zoledronic Acid

    Zoledronate; CGP 42446; CGP42446A; ZOL 446

    Apoptosis Autophagy Cancer Metabolic Disease
    Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects.
  • HY-100351
    BI-7273

    Epigenetic Reader Domain Cancer
    BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.
  • HY-W016349
    Chelidamic acid

    Others Others
    Chelidamic acid is a heterocyclic organic acid with a pyran skeleton. Chelidamic acid has good coordination ability with noble metal ions. Chelidamic acid is also one of the most potent inhibitors of glutamate decarboxylase, with a Ki of 33 μM.
  • HY-13777A
    Zoledronic acid monohydrate

    Zoledronate monohydrate; CGP 42446 monohydrate; CGP42446A monohydrate; ZOL 446 monohydrate

    Apoptosis Autophagy Cancer Metabolic Disease
    Zoledronic acid monohydrate (Zoledronate monohydrate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic acid monohydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic acid monohydrate also has anti-cancer effects.
  • HY-111445
    CeMMEC1

    Epigenetic Reader Domain DNA/RNA Synthesis Cancer
    CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 μM for TAF1, and a Kd of 1.8 μM for TAF1 (2).
  • HY-100760
    Toxoflavin

    Xanthothricin; toxoflavine; PKF-118-310

    β-catenin Cancer
    Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity.
  • HY-N1490
    14-Deoxy-11,12-didehydroandrographolide

    14-dehydro Andrographolide; AP10

    NF-κB Inflammation/Immunology Cancer
    14-Deoxy-11,12-didehydroandrographolide is an analogue of Andrographolide that can be isolated from A. paniculata. 14-Deoxy-11,12-didehydroandrographolide inhibits NF-κB activation.
  • HY-B1218
    Sulfaphenazole

    Bacterial Infection
    Sulfaphenazole is a specific inhibitor of CYP2C9 which blocks atherogenic and pro-inflammatory effects of linoleic acid (increase in oxidative stress and activation of AP-1) mediated by CYP2C9.
  • HY-114330A
    ZK824859 hydrochloride

    PAI-1 Inflammation/Immunology
    ZK824859 hydrochloride is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively.
  • HY-126361
    ZK824190

    Ser/Thr Protease PAI-1 Inflammation/Immunology
    ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.
  • HY-123963
    C-178

    STING Inflammation/Immunology
    C-178 is a potent and selective covalent inhibitor of STING. C-178 binds to Cys91 and suppresses the STING responses elicited by distinct bona fide activators in mouse but not human.
  • HY-114330
    ZK824859

    PAI-1 Ser/Thr Protease Inflammation/Immunology
    ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively.
  • HY-U00441
    DPBQ

    MDM-2/p53 Apoptosis Cancer
    DPBQ activates p53 and triggers apoptosis in a polyploid-specific manner, but does not inhibit topoisomerase or bind DNA. DPBQ elicits expression and phosphorylation of p53 and this effect is specific to tetraploid cells.
  • HY-78869
    Mutated EGFR-IN-1

    Osimertinib analog

    EGFR Cancer
    Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
  • 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-B0166
    L-Ascorbic acid

    L-Ascorbate; Vitamin C

    Calcium Channel Reactive Oxygen Species Apoptosis Metabolic Disease
    L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor.
  • 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 IC50s of 10.9, 12 and 12.1 nM, respectively; also inhibits Notch signaling with IC50 of 14.1 nM.
  • HY-Y0445A
    Sodium dichloroacetate

    PDHK Reactive Oxygen Species NKCC Apoptosis Cancer
    Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.
  • HY-13512
    Camostat mesylate

    Camostat mesilate; FOY305; FOY-S980

    Ser/Thr Protease SARS-CoV Infection Inflammation/Immunology
    Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase.
  • HY-16594
    Lactacystin

    Proteasome Neurological Disease
    Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC50 of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces neurite outgrowth.
  • HY-B0166A
    L-Ascorbic acid sodium salt

    Sodium L-ascorbate; Vitamin C sodium salt

    Calcium Channel Reactive Oxygen Species Apoptosis Cancer
    L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.
  • HY-124151
    Adenosine-2'-monophosphate

    2'-AMP; Adenosine 2'-phosphate; AMP 2'-phosphate

    Adenosine Receptor Endogenous Metabolite Neurological Disease
    Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation.
  • HY-100669
    Mycro 3

    c-Myc Autophagy Cancer
    Mycro 3 is a potent and selective inhibitor of Myc-associated factor X (MAX) dimerization. Mycro 3 also inhibit DNA binding of c-Myc. Mycro 3 could be used for the research of pancreatic cancer.
  • HY-B1488
    Tacrine hydrochloride

    AChE iGluR Neurological Disease
    Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease.
  • HY-B2174
    Ethacridine lactate

    Acrinol

    Bacterial Infection
    Ethacridine lactate (Acrinol) is a widely used antiseptic and abortifacient. Ethacridine lactate is effective against Staphylococcus aureus and other gram-positive cocci. Ethacridine lactate is also a poly(ADP-ribose) glycohydrolase (PARG) inhibitor.
  • HY-14403
    ERK5-IN-1

    ERK Cancer
    ERK5-IN-1 is a potent ERK5 inhibitor with an IC50 of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC50 of 26 nM.
  • HY-125130
    Hesperetin 7-O-glucoside

    HMG-CoA Reductase (HMGCR) Bacterial Infection Metabolic Disease
    Hesperetin 7-O-glucoside is produced by the enzymatic conversion of Hesperidin. Hesperetin 7-O-glucoside is a potent human HMG-CoA reductase inhibitor and also effectively inhibits the growth of Helicobacter pylori. Antihypertensive effect.
  • HY-15647
    BRD9539

    Histone Methyltransferase Cancer
    BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1.
  • HY-19327
    ACY-738

    HDAC Cancer
    ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50 of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM.
  • HY-18317
    JNJ-38158471

    VEGFR RET c-Kit Cancer
    JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively.
  • HY-B0889
    Ethacridine lactate monohydrate

    Acrinol monohydrate

    Bacterial Infection
    Ethacridine lactate (Acrinol) monohydrate is a widely used antiseptic and abortifacient. Ethacridine lactate monohydrate is effective against Staphylococcus aureus and other gram-positive cocci. Ethacridine lactate monohydrate is also a poly(ADP-ribose) glycohydrolase (PARG) inhibitor.
  • HY-10440
    Vismodegib

    GDC-0449

    Hedgehog Autophagy Cancer
    Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively.
  • HY-123879
    BAA473

    Others Inflammation/Immunology
    BAA473 is a bile acid analog and is a potent activator of the pyrin inflammasome that induces the secretion of interleukin 18 (IL-18) through activation of the inflammasome in both myeloid and intestinal epithelial cells.
  • HY-N0831
    Jaceosidin

    Bcl-2 Family COX Apoptosis Cancer Inflammation/Immunology
    Jaceosidin is a flavonoid isolated from Artemisia vestita, induces apoptosis in cancer cells, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin exhibits anti-cancer, anti-inflammatory activities, decreases leves of inflammatory markers, and suppresses COX-2 expression and NF-κB activation.
  • HY-111363
    MK8722

    AMPK Metabolic Disease
    MK8722 is a potent and systemic pan-AMPK activator.
  • HY-112483
    QX77

    Autophagy Cancer
    QX77 is a chaperone-mediated autophagy (CMA) activator.
  • HY-112878
    CL656

    c-[2’FdAMP(S)-2’FdIMP(S)]

    STING Inflammation/Immunology
    CL656 is an activator of stimulator of interferon genes (STING).
  • HY-N0019
    Daidzein

    PPAR Endogenous Metabolite Endocrinology Cancer
    Daidzein is a soy isoflavone, which acts as a PPAR activator.
  • HY-15964
    Tirasemtiv

    CK-2017357

    Others Neurological Disease
    Tirasemtiv is an activator of the fast skeletal muscle troponin complex.
  • HY-N0865
    Ingenol

    (-)-Ingenol

    PKC Cancer
    Ingenol is a PKC activator, with a Ki of 30 μM, with antitumor activity.
  • HY-103194
    KH7

    Others Others
    KH7 is a soluble adenylyl cyclase (sAC)-specific inhibitor, with IC50s of 3-10 μM toward both recombinant purified human sACt protein and heterologously expressed sACt in cellular assays. KH7 is also a cAMP inhibitor.
  • HY-112062
    POL1-IN-1

    DNA/RNA Synthesis Cancer
    POL1-IN-1 is a RNA polymerase 1 (POL1, also known as Pol I) inhibitor with an IC50 of less than 0.5 uM. POL1-IN-1 inhibits ribosome biogenesis by inhibiting POL1 transcription.
  • HY-11001
    PHA-793887

    CDK Apoptosis Cancer
    PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC50 of 79 nM.
  • HY-100783A
    (-)-Bicuculline methochloride

    l-Bicuculline methochloride

    GABA Receptor Neurological Disease
    (-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
  • HY-100783
    (-)-Bicuculline methobromide

    l-Bicuculline methobromide

    GABA Receptor Neurological Disease
    (-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
  • HY-18633
    MDK83190

    Apoptosis Cancer
    MDK83190 is a potent apoptosis activator, induces Apaf-1 oligomerization, increases procaspase-9 processing and subsequent caspase-3 activation in a cyto c-dependent Manner.
  • HY-N0540
    Cynaroside

    Luteolin 7-glucoside; Luteolin 7-O-β-D-glucoside

    Influenza Virus DNA/RNA Synthesis Cancer Infection
    Cynaroside (Luteolin 7-glucoside) is a flavone, a flavonoid-like chemical compound. Cynaroside is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 32 nM.
  • HY-13263
    CHIR-124

    Checkpoint Kinase (Chk) FLT3 PDGFR Apoptosis Cancer
    CHIR-124 is a potent and selective Chk1 inhibitor with IC50 of 0.3 nM, and also potently targets PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM.
  • HY-18719B
    Endoxifen hydrochloride

    Estrogen Receptor/ERR Drug Metabolite Parasite Aromatase Cancer
    Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study.
  • HY-14462
    NP118809

    39-1B4

    Calcium Channel Cardiovascular Disease
    NP118809 is a potent N-type calcium channel blocker, with an IC50 of 0.11 μM; also less potently inhibits L-type calcium channel with an IC50 of 12.2 μM.
  • HY-101692
    AZ-1355

    Prostaglandin Receptor Metabolic Disease Endocrinology
    AZ-1355 is an effctive lipid-lowering compound, which also inhibits platelet aggregation in vivo and elevates the prostaglandin I2/thromboxane A2 ratio in vitro.
  • HY-121450
    Lavoltidine

    Loxtidine; AH-234844

    Histamine Receptor Cancer
    Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia.
  • HY-15484
    Pifithrin-α hydrobromide

    Pifithrin hydrobromide; PFTα hydrobromide

    MDM-2/p53 Aryl Hydrocarbon Receptor Ferroptosis Cancer
    Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.
  • HY-18719E
    Endoxifen

    Estrogen Receptor/ERR Aromatase Drug Metabolite Parasite Cancer
    Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study.
  • HY-N6681
    15-Acetoxyscirpenol

    Caspase Bacterial Apoptosis Antibiotic Infection
    15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat T cell growth in a dose-dependent manner by activating other caspases independent of caspase-3.
  • HY-110228
    Metformin D6 hydrochloride

    1,1-Dimethylbiguanide D6 hydrochloride

    AMPK Autophagy Mitophagy Metabolic Disease Cardiovascular Disease
    Metformin D6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy.
  • HY-N6261
    Epimagnolin B

    Others Inflammation/Immunology
    Epimagnolin B is a bisepoxylignan isolated from Magnolia fargesii, with anti-inflammatory activity and antiallergic effects. Epimagnolin B inhibits NO production in LPS-activated microglia. Epimagnolin B exhibited antiallergic effects.
  • HY-18937
    WEHI-345

    RIP kinase Cancer
    WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation.
  • HY-16785B
    Veledimex (S enantiomer)

    INXN-1001 (S enantiomer); RG-115932 (S enantiomer)

    Interleukin Related Cytochrome P450 Cancer
    Veledimex S enantiomer (INXN-1001 S enantiomer) is the S enantiomer of veledimex. Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
  • HY-112125
    KRN2

    Others Inflammation/Immunology
    KRN2 is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 100 nM. KRN2 has potential to treat NFAT5-mediated Chronic Arthritis.
  • HY-N0826
    Corynoline

    AChE Keap1-Nrf2 Inflammation/Immunology Neurological Disease Cancer
    Corynoline, isolated from Corydalis incise (Papaveraceae), is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM. Corynoline exhibits anti-inflammatory activity by activating Nrf2.
  • HY-13812
    QNZ

    EVP4593

    NF-κB TNF Receptor Inflammation/Immunology Neurological Disease
    QNZ (EVP4593) shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. QNZ (EVP4593) is a neuroprotective inhibitor of SOC channel.
  • HY-137552
    MKI-1

    MASTL Kinase Inhibitor-1

    Others Cancer
    MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer.
  • HY-N3085
    Phellamurin

    P-glycoprotein Apoptosis Cancer Metabolic Disease
    Phellamurin is a plant flavonone glycoside from the leaves of Phellodendron amurense and inhibits intestinal P-glycoprotein. Phellamurin also inhibits egg laying by Papilio protenor. Phellamurin induces cells apoptosis and has anti-tumor activity.
  • HY-B0486
    Lonidamine

    AF-1890; Diclondazolic Acid; DICA

    Hexokinase Mitochondrial Metabolism Apoptosis Cancer
    Lonidamine (AF-1890), an antitumor agent, is a hexokinase, mitochondrial pyruvate carrier (Ki 2.5 μM in isolated rat liver mitochondria) and plasma membrane monocarboxylate transporters inhibitor, which also inhibits mitochondrial complex II.
  • HY-15999
    Cerdulatinib

    PRT062070; PRT2070

    JAK Syk Cancer
    Cerdulatinib (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.
  • HY-100184
    DSM265

    Dihydroorotate Dehydrogenase Parasite Infection
    DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 of 8.9 nM. DSM265 can also inhibit the growth of Pf3D7 parasites with an EC50 of 4.3 nM.
  • HY-N0285
    Imperatorin

    Ammidin

    AChE TRP Channel Neurological Disease
    Imperatorin is an effective of NO synthesis inhibitor (IC50=9.2 μmol), which also is a BChE inhibitor (IC50=31.4 μmol). Imperatorin is a weak agonist of TRPV1 with EC50 of 12.6±3.2 μM.
  • 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-B1228
    Ribostamycin sulfate

    Vistamycin sulfate

    Bacterial Antibiotic Infection
    Ribostamycin sulfate (Vistamycin sulfate) is a broad-spectrum antimicrobial, inhibits bacterial protein synthesis at the level of 30S and 50S ribosomal subunit binding, also inhibits the chaperone activity of protein disulfide isomerase (PDI), used in pharmacokinetic and nephrotoxicity studies
  • HY-17009
    Iguratimod

    T614

    COX Inflammation/Immunology
    Iguratimod is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC50 of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod also inhibits macrophage migration inhibitory factor (MIF) with an IC50 of 6.81 μM.
  • HY-Y0265
    Isatin

    Indoline-2,3-dione

    Monoamine Oxidase Apoptosis Cancer Neurological Disease Cardiovascular Disease
    Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM). Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity. Shows effect on the serotonergic system.
  • HY-12033
    2-Methoxyestradiol

    2-ME2; NSC-659853

    Microtubule/Tubulin Reactive Oxygen Species Apoptosis Autophagy Endogenous Metabolite Cancer
    2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa.
  • 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-102011A
    BMS-1166 hydrochloride

    PD-1/PD-L1 Cancer Inflammation/Immunology
    BMS-1166 hydrochloride is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 hydrochloride induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 hydrochloride antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
  • 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-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-110402
    (S,R,S)-AHPC TFA

    VH032-NH2 TFA; VHL ligand 1 TFA

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC TFA (VH032-NH2 TFA) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC TFA can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
  • 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-N0052A
    Sanguinarine chloride

    Sanguinarin chloride; Sanguinarium chloride; Pseudochelerythrine chloride

    Apoptosis Autophagy Bacterial Parasite Cancer
    Sanguinarine (Sanguinarin) chloride, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
  • HY-N0052
    Sanguinarine

    Sanguinarin; Sanguinarium; Pseudochelerythrine

    Apoptosis Autophagy Cancer
    Sanguinarine (Sanguinarin), a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
  • HY-100886
    BAY1082439

    PI3K Apoptosis Cancer
    BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.
  • HY-111549
    Bragsin1

    Others Cancer
    Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity.
  • HY-108900
    Leu-AMS

    Aminoacyl-tRNA Synthetase Bacterial Cancer Infection
    Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation. Leu-AMS shows cytotoxicity in cancer cells and normal cells, and inhibits the growth of bacteria.
  • HY-114421
    FKBP12 PROTAC dTAG-13

    dTAG-13

    PROTAC FKBP Epigenetic Reader Domain Cancer
    FKBP12 PROTAC dTAG-13 (dTAG-13) is a PROTAC-based heterobifunctional degrader. FKBP12 PROTAC dTAG-13 (dTAG-13) is a degrader of FKBP12 F36V with expression of FKBP12 F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 (dTAG-13) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN.
  • HY-123941
    FKBP12 PROTAC dTAG-7

    dTAG-7

    PROTAC FKBP Epigenetic Reader Domain Cancer
    FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12 F36V with expression of FKBP12 F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN.
  • HY-124798
    Rheb inhibitor NR1

    mTOR Cancer Inflammation/Immunology Neurological Disease
    Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 also is a selective mTORC1 inhibitor. NR1 inhibits the phosphorylation of T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner.
  • HY-B0725
    Doxepin Hydrochloride

    Histamine Receptor Cytochrome P450 Neurological Disease
    Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2.
  • HY-10163
    Dabigatran

    BIBR 953; BIBR 953ZW

    Thrombin Cardiovascular Disease
    Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM).
  • HY-10329
    JNJ-7706621

    Aurora Kinase CDK Apoptosis Cancer
    JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2, with IC50s of 9 nM, 3 nM, 11 nM, and 15 nM for CDK1, CDK2, aurora-A and aurora-B, respectively.
  • HY-108435
    GNE-049

    Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively.
  • HY-N1255
    Scoulerine

    (-)-Scoulerine; Discretamine

    Microtubule/Tubulin Beta-secretase Apoptosis Cancer
    Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (ß-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.
  • HY-B0429
    Pancuronium dibromide

    nAChR Neurological Disease
    Pancuronium dibromide, a bis-quaternary steroid, is a neuromuscular relaxant. Pancuronium dibromide inhibits neuromuscular transmission by competing with acetylcholine for binding sites on nACh receptors. Pancuronium dibromide also inhibits cardiac muscarinic receptors and has a sympathomimetic action.
  • 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-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-15272
    WAY-600

    mTOR Cancer Inflammation/Immunology
    WAY-600 is a potent, ATP-competitive, and selective mTOR inhibitor with an IC50 of 9 nM for recombinant mTOR enzyme. WAY-600 blocks mTOR complex 1/2 (mTORC1/2) assemble and activation.
  • HY-P0318
    Hemorphin-7

    Opioid Receptor Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Hemorphin-7 is a hemorphin peptide, an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemorphin peptides exhibits antinociceptive and antihypertensive activities, activating opioid receptors and inhibiting angiotensin-converting enzyme (ACE).
  • HY-135145
    CB-103

    Notch Cancer
    CB-103 is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. CB-103 has anti-tumor activity.
  • HY-B0190A
    Nafamostat mesylate

    FUT-175

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease Cancer
    Nafamostat mesylate, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat mesylate supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat mesylate blocks activation of SARS-CoV-2..
  • HY-B0190
    Nafamostat

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease
    Nafamostat, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat blocks activation of SARS-CoV-2.
  • HY-B0190B
    Nafamostat hydrochloride

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease
    Nafamostat hydrochloride, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat hydrochloride supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat hydrochloride blocks activation of SARS-CoV-2..
  • HY-124108
    Eicosatetraynoic acid

    ETYA

    COX PPAR Others
    Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively). Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 µM.
  • HY-N0250
    Saikosaponin D

    STAT NF-κB Estrogen Receptor/ERR Bacterial Cancer Infection Inflammation/Immunology
    Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.
  • HY-17376S
    Ezetimibe D4

    SCH 58235 D4

    Others Cardiovascular Disease Cancer
    Ezetimibe D4 (SCH 58235 D4) is the deuterium labeled Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
  • HY-133651
    2,2-Dibromopropanoic acid

    Fungal Infection
    2,2-Dibromopropanoic acid is a dibromo product based on propionic acid. Propionic acid is a short chain fatty acid and acts as chemical intermediate. Propionic acid is also a mold inhibitor and widely used in food preservative.
  • HY-107795
    Benorilate

    Salipran

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Benorylate (Salipran) is the esterification product of paracetamol and acetylsalicylic acid. Benorylate has anti-inflammatory, analgesic and antipyretic properties. Benorylate could also inhibit prostaglandin (PG) synthesis.
  • HY-125974
    HM03

    HSP Cancer
    HM03 is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 has anticancer activity.
  • HY-125974A
    HM03 trihydrochloride

    HSP Cancer
    HM03 trihydrochloride is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 trihydrochloride has anticancer activity.
  • HY-B0745
    Ramatroban

    BAY u3405

    Prostaglandin Receptor Inflammation/Immunology Endocrinology Cancer
    Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.
  • HY-N1482
    Methyl palmitate

    Others Inflammation/Immunology
    Methyl palmitate, an acaricidal compound occurring in green walnut husks, inhibits phagocytic activity and immune response. Methyl palmitate also posseses anti-inflammatory and antifibrotic effects.
  • HY-10256A
    SB 203580 hydrochloride

    RWJ 64809 hydrochloride

    p38 MAPK Autophagy Mitophagy Inflammation/Immunology Cancer
    SB 203580 hydrochloride (RWJ 64809 hydrochloride) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 hydrochloride is an autophagy and mitophagy activator.
  • HY-14255
    Levcromakalim

    (-)-Cromakalim; BRL 38227

    Potassium Channel Cardiovascular Disease
    Levcromakalim ((-)-Cromakalim) is an ATP-sensitive K + channel (KATP) activator.
  • HY-112060
    Saccharin 1-methylimidazole

    DNA/RNA Synthesis Cancer
    Saccharin 1-methylimidazole is an activator for DNA/RNA Synthesis.
  • HY-12376
    BAY 41-2272

    Guanylate Cyclase Inflammation/Immunology
    BAY 41-2272 is a soluble guanylate cyclases (sGC) activator.
  • HY-13529
    Globalagliatin

    LY2608204

    Glucokinase Metabolic Disease
    Globalagliatin (LY2608204) is a activator of glucokinase (GK) with EC50 of 42 nM.
  • HY-12987S
    Pimozide D4

    R6238 D4

    Dopamine Receptor Adrenergic Receptor STAT Cancer Endocrinology Neurological Disease
    Pimozide D4 (R6238 D4) is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-17537
    APY29

    IRE1 Cancer
    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
  • HY-13297
    PYZD-4409

    E1/E2/E3 Enzyme Cancer
    PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells.
  • HY-N0592
    Demethyleneberberine

    NF-κB AMPK Metabolic Disease Inflammation/Immunology
    Demethyleneberberine is a natural mitochondria-targeted antioxidant. Demethyleneberberine alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine could serve as a AMPK activator for treating non-alcoholic fatty liver disease (NAFLD).
  • HY-112671
    CDDO-dhTFEA

    RTA dh404

    Keap1-Nrf2 NF-κB Inflammation/Immunology
    CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB. CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats.
  • 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-13634B
    TLK117

    TER117

    Gutathione S-transferase Cancer Inflammation/Immunology
    TLK117, the active metabolite of TLK199, selective inhibits Glutathione S-transferase P1–1 (GSTP1-1) with a Ki of 0.4 μM for GSTP. TLK117 also competitively inhibits glyoxalase I with a Ki of 0.56 μM.
  • HY-114200
    Imrecoxib

    BAP-909

    COX Inflammation/Immunology
    Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with an IC50 value of 18 nM, it also inhibits COX1- activity with an IC50 value of 115 nM. Imrecoxib (BAP-909) has anti-inflammatory effect.
  • HY-19696B
    Tauroursodeoxycholate dihydrate

    TUDCA dihydrate; UR 906 dihydrate; Taurolite dihydrate

    ERK Caspase Apoptosis Cancer
    Tauroursodeoxycholate dihydrate (TUDCA dihydrate; UR 906 dihydrate; Taurolite dihydrate) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
  • HY-100898
    OGT 2115

    Others Cancer
    OGT 2115 is a potent, cell-permeable and orally active heparanase inhibitor with an IC50 of 0.4 μM. OGT 2115 has anti-angiogenic properties (IC50 of 1 μM). OGT 2115 also inhibits heparan sulfate degradation activity.
  • HY-19718
    OTS964

    TOPK CDK Apoptosis Cancer
    OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.
  • HY-131247
    Bcl-2-IN-2

    Bcl-2 Family Cancer Inflammation/Immunology
    Bcl-2-IN-2 is a potent and selective Bcl-2 inhibitor with an IC50 of 0.034 nM and also inhibits Bcl-xL with an IC50 of 43 nM, showing >1000-fold selectivity for Bcl-2 over Bcl-xL.
  • HY-10528
    Tasquinimod

    ABR-215050

    HDAC Cancer
    Tasquinimod is an oral antiangiogenic agent, which has the potential for castration-resistant prostate cancer treatment. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor.
  • HY-P0256
    Apamin

    Apamine

    Potassium Channel Inflammation/Immunology Neurological Disease
    Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca 2+-activated K + (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.
  • HY-117962
    (Rac)-BI 703704

    Guanylate Cyclase Metabolic Disease
    (Rac)-BI 703704 is a potent soluble guanylyl cyclase (sGC) activator. (Rac)-BI 703704 reduces progression of renal damage in the ZSF1 rat, and highlight the potential of sGC activation as an effective therapy for diabetic nephropathy.
  • 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-12754
    ML228

    CID-46742353

    HIF/HIF Prolyl-Hydroxylase Cancer
    ML228 (CID-46742353) is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM. ML228 potently activates HIF in vitro as well as its downstream target VEGF.
  • HY-111343
    ONC212

    Apoptosis Cancer Endocrinology
    ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer agent and also a selective agonist of GPR132. ONC212 also induces apoptosis.
  • HY-N0802
    Tenuigenin

    Senegenin

    NF-κB Infection Inflammation/Immunology
    Tenuigenin is a major active component isolated from the root of the Chinese herb Polygala tenuifolia. Tenuigenin protects against S.aureus-induced pneumonia by inhibiting NF-κB activation. Tenuigenin has anti-inflammatory effect.
  • HY-N0220
    Dauricine

    NF-κB Apoptosis Cancer Inflammation/Immunology
    Dauricine, a bisbenzylisoquinoline alkaloid in Asiatic Moonseed Rhizome, possesses anti-inflammatory activity. Dauricine inhibits cell proliferation and invasion, and induces apoptosis by suppressing NF-κB activation in a dose- and time-dependent manner in colon cancer.
  • 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-15880
    CCT007093

    Phosphatase Apoptosis Autophagy Cancer
    CCT007093 is an effective protein phosphatase 1D (PPM1D Wip1) inhibitor. Wip1 inhibition can activate the mTORC1 pathway and enhance hepatocyte proliferation after hepatectomy.
  • HY-B0789
    SU6656

    Src FAK Akt Cancer
    SU6656 is a Src family kinases inhibitor with IC50s of 280, 20, 130, 170 nM for Src, Yes, Lyn, and Fyn, respectively. SU6656 inhibits FAK phosphorylation at Y576/577, Y925, Y861 sites. SU6656 also inhibits p-AKT.
  • HY-19743
    Triazavirin

    Nucleoside Antimetabolite/Analog Influenza Virus DNA/RNA Synthesis Infection
    Triazavirin is a nucleoside analogue of nucleic acid and an antiviral agent. Triazavirin works by inhibiting the synthesis of viral RNA and DNA and replication of genomic fragments. Triazavirin is also an effective protective agent on the transmission stage of influenza.
  • HY-N4096
    Tsugaric acid A

    Others Inflammation/Immunology
    Tsugaric acid A can significantly inhibit superoxide anion formation. Tsugaric acid A also protects human keratinocytes against damage induced by ultraviolet B (UV B) light. Tsugaric acid A can protect keratinocytes from photodamage.
  • HY-N0602
    Ginsenoside Rg2

    Chikusetsusaponin I; Panaxoside Rg2; Prosapogenin C2

    NF-κB Amyloid-β Neurological Disease Cardiovascular Disease Cancer
    Ginsenoside Rg2 is one of the major active components of ginseng. Ginsenoside Rg2 acts as a NF-κB inhibitor. Ginsenoside Rg2 also reduces 1-42 accumulation.
  • 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-11035
    WAY-262611

    β-catenin Cancer
    WAY-262611 is a wingless β-Catenin agonist that increases bone formation rate with an EC50 of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also a Dkk1 inhibitor.
  • HY-19095
    TNP-351

    Antifolate Cancer
    TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.
  • HY-18570
    1-Naphthaleneacetic acid

    1-Naphthylacetic acid

    Phospholipase Others
    1-Naphthaleneacetic acid (1-Naphthylacetic acid), a synthetic auxin, can promote plant growth. 1-Naphthaleneacetic acid is also an inhibitor of PLA2, with an IC50 of 13.16 μM.
  • HY-18570A
    1-Naphthaleneacetic acid potassium salt

    Potassium 1-Naphthaleneacetate

    Phospholipase Others
    1-Naphthaleneacetic acid potassium salt (Potassium 1-Naphthaleneacetate), a synthetic auxin, can promote plant growth. 1-Naphthaleneacetic acid potassium salt is also an inhibitor of PLA2, with an IC50 of 13.16 μM.
  • HY-W009732
    Sinapinic acid

    Sinapic acid

    HDAC Angiotensin-converting Enzyme (ACE) Reactive Oxygen Species Apoptosis Cancer Metabolic Disease
    Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM, and also inhibits ACE-I activity. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells. Sinapinic acid shows antioxidant and antidiabetic activities. Sinapinic acid reduces total cholesterol, triglyceride, and HOMA-IR index, and also normalizes some serum parameters of antioxidative abilities and oxidative damage in ovariectomized rats.
  • HY-136179
    ZAP-180013

    Tyrosinase Inflammation/Immunology
    ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs).
  • HY-N0191
    Andrographolide

    Andrographis

    NF-κB SARS-CoV Influenza Virus Autophagy Cancer Infection Inflammation/Immunology
    Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.
  • HY-111926
    N6-Methyladenosine 5'-monophosphate disodium salt

    Others Metabolic Disease
    N6-Methyladenosine 5'-monophosphate disodium salt is an activator of glycogen phosphorylase b, with a Ka value of 22 µM. N6-Methyladenosine 5'-monophosphate disodium salt is a non-competitive rat adenylate kinase II inhibitor.
  • HY-10999A
    Trametinib (DMSO solvate)

    GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)

    MEK Apoptosis Cancer
    Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis.
  • HY-P1382
    Rac1 Inhibitor W56

    Ras Cancer
    Rac1 Inhibitor W56 is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.
  • HY-14233
    Omecamtiv mecarbil

    CK-1827452

    Myosin Cardiovascular Disease
    Omecamtiv mecarbil (CK-1827452) is a selective cardiac myosin activator.
  • HY-14909
    Bardoxolone

    CDDO; RTA 401

    Keap1-Nrf2 Cancer
    Bardoxolone is a novel nuclear regulator factor (Nrf-2) activator.
  • HY-59047
    Tolimidone

    MLR-1023

    Src Metabolic Disease
    Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.
  • HY-P0136
    SAMS

    AMPK Metabolic Disease
    SAMS peptide is a specific substrate for the AMP-activated protein kinase (AMPK).
  • HY-14256
    BMS-191095

    Potassium Channel Metabolic Disease
    BMS-191095 is an activators of mitochondrial ATP-sensitive potassium (mitoKATP) channels.
  • HY-10164
    E-​6123

    Others Inflammation/Immunology
    E-​6123 is a platelet-activating factor (PAF) receptor antagonist.
  • HY-100295
    (4-Acetamidocyclohexyl) nitrate

    BM121307

    Guanylate Cyclase Cardiovascular Disease
    (4-Acetamidocyclohexyl) nitrate (BM121307) is a guanylate cyclase activator.
  • HY-U00040
    PAF-AN-1

    Others Inflammation/Immunology Cardiovascular Disease
    PAF-AN-1 is a platelet activating factor receptor (PAF) antagonist.
  • HY-P1847
    IKKγ NBD Inhibitory Peptide

    NF-κB Cancer
    IKKγ NBD Inhibitory Peptide is a NEMO-binding domain peptide (NBD peptide) corresponding to the NEMO amino-terminal alpha-helical region, which is shown to block TNF-alpha-induced NF-kB activation.
  • HY-N0699
    Daphnoretin

    Dephnoretin; Thymelol

    PKC Influenza Virus Infection
    Daphnoretin (Dephnoretin), isolated from Wikstroemia indica, possesses antiviral activity. Daphnoretin likes PMA, may direct activation of protein kinase C which in turn activated NADPH oxidase and elicited respiratory burst.
  • HY-128591
    DIPQUO

    Others Metabolic Disease
    DIPQUO is an activator of the bone marker alkaline phosphatase (ALP), with an EC50 of 6.27 μM in C2C12 cells. DIPQUO promotes mouse and human osteoblast differentiation via activation of p38 MAPK-β.
  • HY-100194
    FKK

    Others Inflammation/Immunology Cardiovascular Disease
    FKK is an indazole derivative and also a novel bronchodilator.
  • HY-18990
    GSK180736A

    ROCK Cardiovascular Disease
    GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
  • HY-N0720
    Neobavaisoflavone

    Apoptosis DNA/RNA Synthesis Cancer
    Neobavaisoflavone, a flavonoid, is isolated from the seeds of Psoralea corylifolia. Neobavaisoflavone exhibits anti-inflammatory, anti-cancer and anti-oxidation activities. Neobavaisoflavone inhibits DNA polymerase at moderate to high concentrations. Neobavaisoflavone also inhibits platelet aggregation.
  • HY-18780
    RR6

    Others Cancer
    RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540 nM for recombinant vanin-1. RR6 also potently inhibits human, bovine and rat serum pantetheinase with IC50 values of 40 nM, 41 nM and 87 nM, respectively.
  • HY-12046
    PIK-93

    PI4K PI3K Virus Protease Cancer
    PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively.
  • HY-10579
    Pluripotin

    SC1

    Ribosomal S6 Kinase (RSK) ERK Cancer
    Pluripotin is a dual inhibitor of ERK1 and RasGAP with KDs of 98 nM and 212 nM, respectively. Pluripotin also inhibits RSK1, RSK2, RSK3, and RSK4 with IC50s of 0.5, 2.5, 3.3, and 10.0 µM, respectively.
  • HY-W009783
    1-Deoxymannojirimycin hydrochloride

    HIV Influenza Virus Infection
    1-Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC50 of 20 μM. 1-Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor and inhibits HIV‐1 strains. 1-Deoxymannojirimycin hydrochloride has antiviral activity.
  • HY-101920
    Autophinib

    Autophagy Cancer Neurological Disease
    Autophinib is a potent, selective autophagy inhibitor with IC50s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC50 of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34.
  • HY-15874A
    Fiboflapon sodium

    GSK2190915 sodium salt; AM-803 sodium

    FLAP Leukotriene Receptor Inflammation/Immunology
    Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
  • HY-109011