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Results for "

HepG2

" in MCE Product Catalog:

285

Inhibitors & Agonists

4

Fluorescent Dye

1

Biochemical Assay Reagents

4

Peptides

51

Natural
Products

8

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-115962
    Anticancer agent 37

    Others Cancer
    Anticancer agent 37 (compound 18), a sulfonylurea derivative, is a potent anticancer agent. Anticancer agent 37 inhibits HePG2 cell growth with an IC50 of 17.2 µg/mL.
  • HY-146465
    Anticancer agent 60

    Microtubule/Tubulin Cancer
    Anticancer agent 60 (compound 3h) has antiproliferative activity against human HepG2 cells (IC50 = 4.13 μM) and presents antitumor efficacy in a human HepG2 xenograft mouse model.
  • HY-146082
    (Z)-α-Cyanostilbene

    Others Cancer
    (Z)-α-Cyanostilbene (compound 8), a dicyano substituted acrylonitrile, shows selective antiproliferative activity against HeLa and HepG2 cells, with IC50s of 0.33 and 0.52 μM, respectively.
  • HY-147198
    Antimalarial agent 13

    Parasite Infection
    Antimalarial agent 13 (Compound 1) is a potent antimalarial agent. Antimalarial agent 13 shows inhibition with EC50 values of 124 nM and 2.5 μM against P. falciparum parasite and HepG2, respectively.
  • HY-144795
    VEGFR-2-IN-14

    VEGFR Apoptosis Cancer
    VEGFR-2-IN-14 (Compound 5) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-14 arrests the HepG2 cell growth at the Pre-G1 phase and induces apoptosis.
  • HY-143266
    Topoisomerase I inhibitor 3

    Topoisomerase Apoptosis Cancer
    Topoisomerase I inhibitor 3 (Compound ZML-14) is a topoisomerase I inhibitor and can interact with topoisomerase I-DNA complex. Topoisomerase I inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase.
  • HY-N10207
    Penicitide A

    Endogenous Metabolite Cancer Infection
    Penicitide A is a marine secondary metabolite. Penicitide A shows moderate cytotoxicity against pathogen A. brassicae and the human hepatocellular liver carcinoma (HepG2) cell line.
  • HY-145821
    Tubulin inhibitor 15

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 15 is a potent tubulin inhibitor. Tubulin inhibitor 15 shows antiproliferative activity. Tubulin inhibitor 15 shows cytotoxicity in HepG2 cells.
  • HY-145822
    Tubulin inhibitor 16

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 16 is a potent tubulin inhibitor. Tubulin inhibitor 16 shows antiproliferative activity. Tubulin inhibitor 16 shows cytotoxicity in HepG2 cells.
  • HY-116920
    Alyssin

    Reactive Oxygen Species Microtubule/Tubulin Cancer
    Alyssin, found in Cruciferous Vegetables, exerts anticancer activity in HepG2 by increasing intracellular reactive oxygen species and tubulin depolymerization.
  • HY-144796
    VEGFR-2-IN-15

    VEGFR Apoptosis Cancer
    VEGFR-2-IN-15 (Compound 14b) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-15 arrests the HepG2 cell growth at the Pre-G1 phase and induces apoptosis.
  • HY-10332
    (Z)-Semaxanib

    (Z)-SU5416

    c-Met/HGFR Cancer
    (Z)-Semaxanib (compound (z)-1) is a potent tyrosine kinase inhibitor. (Z)-Semaxanib shows cytotoxicity for TAMH and HepG2 cells with IC50s of 6.28 µM and 8.17 µM, respectively.
  • HY-151573
    EGFR/CDK2-IN-1

    EGFR CDK Cancer
    EGFR/CDK2-IN-1 (Compound 3b) is an EGFR/CDK2 inhibitor. EGFR/CDK2-IN-1 shows good cytotoxicity against MCF7 and HepG2 cells. EGFR/CDK2-IN-1 can be used in cancer research.
  • HY-75564
    Cyclo(Ala-Gly)

    Endogenous Metabolite Cancer
    Cyclo(Ala-Gly), a metabolite of a mangrove endophytic fungus, Penicillium thomi, exhibits cytotoxicity against A549, HepG2 and HT29 cells. The IC50 values range from 9.5 to 18.1 μM.
  • HY-146043
    Antiparasitic agent-5

    Parasite Infection
    Antiparasitic agent-5 (compound 8h) has selectively antiparasitic activity against Leishmania infantum (L. infantum) with an IC50 value of 2.50 μM. Antiparasitic agent-5 also has certain cytotoxicity against HepG2 (CC50 = 6.78 μM).
  • HY-146044
    Antiparasitic agent-6

    Parasite Infection
    Antiparasitic agent-6 (compound 5b) has selectively antiparasitic activity against Leishmania infantum (L. infantum) with an IC50 value of 3.89 μM. Antiparasitic agent-6 also has certain cytotoxicity against HepG2 (CC50 = 13.64 μM).
  • HY-146045
    Antiparasitic agent-7

    Parasite Infection
    Antiparasitic agent-7 (compound 5d) has selectively antiparasitic activity against Leishmania infantum (L. infantum) with an IC50 value of 2.85 μM. Antiparasitic agent-7 also has certain cytotoxicity against HepG2 (CC50 = 10.61 μM).
  • HY-147756
    Nampt-IN-7

    NAMPT Cancer
    Nampt-IN-7 (compound GF8) is a potent NAMPT inhibitor, with an IC50 of 7.31 μM. Nampt-IN-7 also displays cytotoxic activity against human HepG2 hepatocellular carcinoma cell line with an IC50 of 24.28 μM.
  • HY-120607
    Chevalone C

    Parasite Cancer Infection
    Chevalone C, a meroterpenoid fungal metabolite, shows antimalarial activity with IC50 value of 25.00 μg/mL. Chevalone C has anti-proliferative activity on colon HCT116, liver HepG2 and melanoma A375 cancer cell lines.
  • HY-115928
    M24

    Bcl-2 Family Cancer
    M24 is a Mcl-1 selective inhibitor. M24 exhibits good binding affinity against Mcl-1 with Ki value of 0.33 μM. M24 exhibits good anti-proliferative activity and induce apoptosis in HepG2 cells.
  • HY-N0069
    Solamargine

    Solamargin; δ-Solanigrine

    P-glycoprotein Apoptosis Cancer
    Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity.
  • HY-137371
    Lactonic sophorolipid

    Bacterial Apoptosis Antibiotic Cancer Infection
    Lactonic sophorolipid is a natural antimicrobial surfactant for oral hygiene. Lactonic sophorolipid, a potential anticancer agent, induces apoptosis in human HepG2 cells through the caspase-3 pathway.
  • HY-W040127
    Peonidin 3-O-glucoside chloride

    Insulin Receptor Metabolic Disease
    Peonidin 3-O-glucoside chloride, an anthocyanin, act as an insulin secretagogue. Peonidin 3-O-glucoside chloride can increase glucose uptake in HepG2 cells. Peonidin 3-O-glucoside chloride has the potential for type-2 diabetes comorbidities research.
  • HY-144754
    VEGFR-2-IN-13

    VEGFR Apoptosis Cancer
    VEGFR-2-IN-13 (Compound 19a) is a potent VEGFR-2 inhibitor with an IC50 of 3.4 nM. VEGFR-2-IN-13 disrupts the HepG2 cell cycle by arresting the G2/M phase and induces apoptosis.
  • HY-N7980
    Rubipodanone A

    NF-κB Cancer
    Rubipodanone A, a naphthohydroquinone dimer, shows cytotoxicity against A549, BEL-7402, HeLa, HepG2, SGC-7901 and U251 cells. Rubipodanone A also shows obvious activating effect at 20 and 40 μM for NF-κB.
  • HY-12841
    KHK-IN-1

    Others Metabolic Disease
    KHK-IN-1 (compound 8) is a selective and cell membrane permeable ketohexokinase (KHK) inhibitor (IC50=12 nM; F=34%). KHK-IN-1 inhibits the production of F1P in HepG2 cell lysates (IC>sub>50=400 nM). KHK-IN-1 has potential for the study of diabetes and obesity.
  • HY-12841A
    KHK-IN-1 hydrochloride

    Others Metabolic Disease
    KHK-IN-1 hydrochloride (compound 8) is a selective and cell membrane permeable ketohexokinase (KHK) inhibitor (IC50=12 nM; F=34%). KHK-IN-1 hydrochloride inhibits the production of F1P in HepG2 cell lysates (IC>sub>50=400 nM). KHK-IN-1 hydrochloride has potential for the study of diabetes and obesity.
  • HY-N0316
    Mollugin

    NF-κB Reactive Oxygen Species Apoptosis VEGFR c-Myc Cancer
    Mollugin is an orally active and potent NF-κB inhibitor. Mollugin induces S-phase arrest of HepG2 cells, and increased intracellular reactive oxygen species (ROS) levels. Mollugin induces DNA damage in HepG2 cells, as well as an increase in the expression of p-H2AX. Mollugin shows anti-cancer effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 (bone morphogenetic protein 2) via the p38-Smad signaling pathway.
  • HY-146467
    Anticancer agent 62

    Others Cancer
    Anticancer agent 62 (compound 4c) is a potent anticancer agent. Anticancer agent 62 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 0.019, 0.060 and 0.016 μM, respectively. Anticancer agent 62 shows effective tumor growth inhibition.
  • HY-N8441
    Neriifolin

    17β-Neriifolin

    Na+/K+ ATPase Apoptosis Cancer Inflammation/Immunology
    Neriifolin, a CNS-penetrating cardiac glycoside, is an inhibitor of the Na +, K +-ATPase. Neriifolin can target beclin 1, inhibits the formation of LC3-associated phagosomes and ameliorates experimental autoimmune encephalomyelitis (EAE) development. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells[2.
  • HY-146729
    ASK1-IN-3

    MAP3K Apoptosis Cancer Inflammation/Immunology
    ASK1-IN-3 is a potent and selective ASK1 kinase inhibitor with IC50 of 33.8 nM, as well as inhibits several cell cycle regulating kinases. ASK1-IN-3 has strong HepG2 cancer cells apoptosis induction and potent cell cycle arrest activities.
  • HY-146240
    ALDH1A1-IN-3

    Aldehyde Dehydrogenase (ALDH) Metabolic Disease
    ALDH1A1-IN-3 (compound 57) is an excellent and selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitor with an IC50 value of 0.379 μM. ALDH1A1-IN-3 can effectively improve glucose consumption in HepG2 cells. ALDH1A1-IN-3 can be used for researching glucose metabolism improvement.
  • HY-146083
    (Z)-p-cyano-α-Cyanostilbene

    Others Cancer
    (Z)-p-cyano-α-Cyanostilbene (compound 11), a phenantrene derivative, has antiproliferative activity. (Z)-p-cyano-α-Cyanostilbene shows significant selectivity against HeLa (IC50=0.21 µM) and HepG2 (IC50=0.230 µM) cells without cytotoxic against normal skin fibroblasts (IC50>100 µM).
  • HY-125254
    LEI110

    Others Infection Metabolic Disease
    LEI110 is a potent, selective and cell-permeable pan-inhibitor of the HRASLS family of thiol hydrolases. LEI110 inhibits PLA2G16, HRASLS2, RARRES3 and iNAT, with pIC50 values of 7.0, 6.8, 6.8, and 7.6, respectively. LEI110 reduces cellular arachidonic acid levels and oleic acid-induced lipolysis in HepG2 cells.
  • HY-146042
    Antiparasitic agent-4

    Parasite Infection
    Antiparasitic agent-4 (compound 4q) has highly antiparasitic activity against Leishmania infantum (L. infantum) and Trypanosoma cruzi (T. cruzi) with IC50s of 8.51 μM and 2.20 μM, respectively. Antiparasitic agent-4 also has certain cytotoxicity against HepG2 (CC50 = 18.97 μM).
  • HY-146395
    HBV-IN-23

    HBV DNA/RNA Synthesis Apoptosis Cancer Infection
    HBV-IN-23 (Compound 5k) is an inhibitor of HBV DNA replication with an IC50 of 0.58 µM. HBV-IN-23 inhibits HBV DNA replication in both drug sensitive and resistant HBV strains. HBV-IN-23 shows anti-hepatocellular carcinoma cell (HCC) activities. HBV-IN-23 induces HepG2 cells apoptosis.
  • HY-146041
    Antiparasitic agent-2

    Parasite Infection
    Antiparasitic agent-2 (compound 8a) has highly antiparasitic activity against Leishmania infantum (L. infantum) and Trypanosoma cruzi (T. cruzi) with IC50s of 7.28 μM and 2.30 μM, respectively. Antiparasitic agent-2 also has certain cytotoxicity against HepG2 (CC50 = 26.79 μM).
  • HY-146114
    Antitumor agent-67

    Others Cancer
    Antitumor agent-67 (compound 3) is a potent antitumor agent. Antitumor agent-67 has highly selective toxicity to cancer cells and lower damage to normal cells. Antitumor agent-67 can be activated by NQO1 and effectively liberate podophyllotoxin and kill tumor cells. Antitumor agent-67 significantly suppresses cancer growth in HepG2 xenograft models without obvious toxicity.
  • HY-146466
    Anticancer agent 61

    Others Cancer
    Anticancer agent 61 (compound 3v) is an orally active and potent anticancer agent. Anticancer agent 61 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 1.12, 1.97 and 1.08 μM, respectively. Anticancer agent 61 shows effective tumor growth inhibition.
  • HY-115947
    Anticancer agent 33

    Others Cancer
    Anticancer agent 33 (compound 3), a Squamocin and Bullatacin derivative, is a potent anticancer agent. Anticancer agent 33 shows high potency to inhibit 4T1 breast cancer cell line (A549, HeLa, HepG2 and MCF-7 cells) growth with IC50s of 1.9-5.4 µM.
  • HY-N0876
    Arenobufagin

    Others Cancer
    Arenobufagin is a natural bufadienolide from toad venom; has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells.
  • HY-143301
    Topoisomerase I inhibitor 4

    Topoisomerase Cancer
    Topoisomerase I inhibitor 4 (compound 7a) is a topoisomerase I inhibitor. Topoisomerase I inhibitor 4 inhibits HepG2, A549, MCF-7 and HeLa cancer cells proliferation with IC50s of 1.20, 2.09, 1.56 and 1.92 μM, respectively. Topoisomerase I inhibitor 4 can be used for the research of cancer.
  • HY-N10447
    Kurzipene D

    Apoptosis Cancer
    Kurzipene D (compound 4) is a potent anticancer agent. Kurzipene D induces the apoptosis and arrested the HepG2 cell cycle at S stage. Kurzipene D shows anti-tumor effects using in vivo zebrafish model. Kurzipene D has the property of inhibiting tumor proliferation and migration.
  • HY-14914
    Azilsartan

    TAK-536

    Angiotensin Receptor Reactive Oxygen Species Apoptosis Cancer Metabolic Disease Neurological Disease Cardiovascular Disease
    Azilsartan (TAK-536) is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research.
  • HY-147853
    B-Raf IN 8

    Raf Cancer
    B-Raf IN 8 (compound 7g) is a potent B-Raf inhibitor, with an IC50 of 70.65 nM. B-Raf IN 8 exhibits antitumor activity against hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland (MCF-7) and human prostate cancer (PC-3) cells, with IC50 values of 9.78, 13.78, 18.52 and 29.85 µM.
  • HY-N10063
    Penispidin A

    Others Metabolic Disease
    Penispidin A inhibits hepatic lipid accumulation in HepG2 cells.
  • HY-B0822
    Fipronil

    GABA Receptor Cytochrome P450 Apoptosis Neurological Disease
    Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes.
  • HY-147852
    B-Raf IN 7

    Raf Cancer
    B-Raf IN 7 (compound 6a) is a potent B-Raf inhibitor, with an IC50 of 110.23 nM. B-Raf IN 7 exhibits antitumor activity against colon carcinoma (HCT-116), mammary gland (MCF-7), hepatocellular carcinoma (HEPG-2), human cervical carcinoma (Hela) and human prostate cancer (PC-3) cells, with IC50 values of 7.50, 9.87, 10.57, 11.63 and 12.83 µM.
  • HY-139987A
    LeuRS-IN-1 hydrochloride

    Bacterial Infection
    LeuRS-IN-1 hydrochloride is a potent, orally active M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS) inhibitor. LeuRS-IN-1 hydrochloride has IC50 and Kd values of 0.06 μM, 0.075 μM for M.tb LeuRS, respectively. LeuRS-IN-1 hydrochloride inhibits human cytoplasmic LeuRS (IC50=38.8 μM), and HepG2 protein synthesis (EC50=19.6 μM).
  • HY-139987
    LeuRS-IN-1

    Bacterial Infection
    LeuRS-IN-1 is a potent, orally active M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS) inhibitor. LeuRS-IN-1 has IC50 and Kd values of 0.06 μM, 0.075 μM for M.tb LeuRS, respectively. LeuRS-IN-1 inhibits human cytoplasmic LeuRS (IC50=38.8 μM), and HepG2 protein synthesis (EC50=19.6 μM).
  • HY-137605
    WSF1-IN-1

    Others Cancer
    WSF1-IN-1 (compound 136), an orally active WSF1 inhibitor, can be used in the study for WSF1 (Wolfram syndrome) related tumors, with IC50 values of 0.33 μM and >27 μM in HepG2 parental and HepG2 WFS1 KO cell lines, respectively.
  • HY-146715
    IDO/Tubulin-IN-2

    Microtubule/Tubulin Apoptosis Cancer
    IDO/Tubulin-IN-2 (HT2) is a potent TDO and tubulin inhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2 cancer cell lines, with IC50 values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity.
  • HY-16558
    Butein

    2’,3,4,4’-tetrahydroxy Chalcone

    EGFR Autophagy Apoptosis Phosphodiesterase (PDE) Cancer
    Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
  • HY-13623A
    Entecavir monohydrate

    BMS200475 monohydrate; SQ34676 monohydrate

    HBV Infection Cancer
    Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
  • HY-13623
    Entecavir

    BMS200475; SQ34676

    HBV Infection Cancer
    Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
  • HY-147839
    Topoisomerase II inhibitor 10

    Topoisomerase Apoptosis Cancer
    Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells.
  • HY-N0125
    Diosmetin

    Cytochrome P450 Cancer
    Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.
  • HY-133667
    Bromoiodoacetamide

    Apoptosis Cancer
    Bromoiodoacetamide is a kind of iodinated haloacetamides (I-HAcAms), with cytotoxicity. Bromoiodoacetamide induces cytotoxicity by via reactive oxygen species (ROS) accumulation and apoptosis in HepG-2 cells.
  • HY-N8882
    Oleoside 11-methyl ester

    Others Cancer
    Oleoside 11-methyl ester is a secoiridoid glucoside and possesses a strong cytotoxic activity against Hep-G2 cells.
  • HY-100303A
    FR194738

    Others Metabolic Disease
    FR194738 is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
  • HY-N0882
    Desacetylcinobufotalin

    Deacetylcinobufotalin

    Apoptosis Cancer
    Desacetylcinobufotalin is a natural compound; apoptosis inducer and shows the marked inhibition effect to HepG2 cells and the IC50 value is 0.0279μmol/ml.
  • HY-N6683
    15-Acetyl-deoxynivalenol

    Drug Metabolite Cancer
    15-Acetyl-deoxynivalenol is a highly toxic trichothecene found in cereals, and a metabolite of deoxynivalenol, exhibits toxicity to HepG2 cells.
  • HY-118224
    BPH-715

    Parasite Infection
    BPH-715 is a bisphosphonate, inhibits Plasmodium liver-stage growth, with an IC50 of 10 μM for Plasmodium exoerythrocytic forms in HepG2 cells.
  • HY-100303
    FR194738 free base

    Others Metabolic Disease
    FR194738 free base is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
  • HY-100249
    XEN723

    Stearoyl-CoA Desaturase (SCD) Metabolic Disease
    XEN723 is a novel and potent thiazolylimidazolidinone inhibitor of Stearoyl-CoA Desaturase (SCD1) with IC50s of 45 and 524 nM in mouse and HepG2 cell, respectively.
  • HY-151453
    Topoisomerase IIα-IN-4

    Topoisomerase Apoptosis Cancer
    Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer.
  • HY-16679
    Helioxanthin derivative 5-4-2

    Helioxanthin 5-4-2

    HBV Infection
    Helioxanthin derivative 5-4-2 is an analogue of helioxanthin, exhibites significant in vitro anti-HBV activity with EC50 of 0.08 uM in HepG2.2.15 cells.
  • HY-11034
    CVT-12012

    Stearoyl-CoA Desaturase (SCD) Metabolic Disease
    CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC50s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively.
  • HY-N0125S
    Diosmetin-d3

    Cytochrome P450 Cancer
    Diosmetin-d3 is the deuterium labeled Diosmetin. Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.
  • HY-N1514
    Ganoderenic acid B

    P-glycoprotein Cancer
    Ganoderenic acid B is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid B exhibits potent reversal effect on ABCB1-mediated multidrug resistance of HepG2/ADM cells to Doxorubicin.
  • HY-N9532
    Isobyakangelicol

    Anhydrobyakangelicin

    Others Cancer
    Isobyakangelicol is a coumarin that can be found in the roots of Angelica dahurica. Isobyakangelicol inhibits the growth of HeLa and HepG2 cells, with IC50s of 70.04 μM and 17.97 μM.
  • HY-19937
    Saroglitazar

    PPAR Metabolic Disease
    Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
  • HY-131710
    PDE5-IN-3

    Phosphodiesterase (PDE) EGFR Wnt Apoptosis Cancer
    PDE5-IN-3 (compound 11j) is a potent PDE5 inhibitor with an IC50 of 1.57 nM. PDE5-IN-3 shows moderate EGFR inhibition with IC50 of 5.827 µM. PDE5-IN-3 significantly inhibits the Wnt/β-catenin pathway (IC50=1286.96 ng/mL). PDE5-IN-3 induces the intrinsic apoptotic mitochondrial pathway in HepG2 cells. PDE5-IN-3 has strong antitumor activity.
  • HY-N0907
    Ginsenoside Rg6

    NF-κB Apoptosis Cancer Inflammation/Immunology
    Ginsenoside Rg6 inhibits TNF-α-induced NF-κB transcriptional activity with an IC50 of 29.34 μM in HepG2 cells. Ginsenoside Rg6 also exhibits apoptosis-inducing effect.
  • HY-19937A
    Saroglitazar magnesium

    PPAR Metabolic Disease
    Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
  • HY-N7605
    11-epi-mogroside V

    Others Metabolic Disease
    11-epi-mogroside V is a mogroside in the fruit of Siraitia grosvenori. 11-epi-mogroside V exhibits considerable bioactivity in promoting glucose uptake in human HepG2 cells in vitro.
  • HY-N9339
    Norglaucine

    (+)-Norglaucine

    Others Cancer
    Norglaucine ((+)-Norglaucine), a cytotoxic alkaloid, exhibits cytotoxicity towards the tumor cell lines B16-F10, HepG2, K562 and HL-60 cells.
  • HY-N8934
    6β-Hydroxytomentosin

    Others Cancer
    6β-Hydroxytomentosin, a sesquiterpenoid, can be found in flowers of Inula japonica. 6β-Hydroxytomentosin exhibits weak cytotoxicities against A549, SK-OV-3, HepG-2 and HT-29 cell lines.
  • HY-N3121
    Pachypodol

    Others Cancer
    Pachypodol exerts antioxidant and cytoprotective effects in HepG2 cells.Pachypodol inhibits the growth of CaCo 2 colon cancer cell line in vitro(IC50 = 185.6 mM).
  • HY-N7273
    Soyasaponin III

    Apoptosis Cancer
    Soyasaponin III, a monodesmodic oleanane triterpenoid, is one of the main potentially bioactive saponins found in soy (Glycine max) and related products. Soyasaponin III can induce apoptosis in Hep-G2 cells.
  • HY-N0906
    Ginsenoside Rk3

    NF-κB Inflammation/Immunology Cardiovascular Disease
    Ginsenoside Rk3 is present in the roots Panax ginseng herbs. Ginsenoside Rk3 significantly inhibits TNF-α-induced NF-κB transcriptional activity, with an IC50 of 14.24±1.30 μM in HepG2 cells.
  • HY-13623S
    Entecavir-d2

    BMS200475-d2; SQ34676-d2

    HBV Infection
    Entecavir-d2 (BMS200475-d2) is the deuterium labeled Entecavir. Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
  • HY-135383B
    (Z)-Pitavastatin calcium

    Others Metabolic Disease
    (Z)-Pitavastatin calcium is the Z-Isomer of Pitavastatin hemicacium. Pitavastatin calcium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin calcium inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells.
  • HY-19937S
    Saroglitazar-d5

    PPAR Metabolic Disease
    Saroglitazar-d5 is the deuterium labeled Saroglitazar. Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
  • HY-N2078
    Yamogenin

    Neodiosgenin

    LXR Metabolic Disease
    Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin (Neodiosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin (Neodiosgenin) inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes.
  • HY-147682
    NF-κB-IN-5

    NF-κB Apoptosis Cancer
    NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase.
  • HY-146374
    Antibacterial agent 96

    Bacterial Infection
    Antibacterial agent 96 (compound 4k) is a potent antibacterial agent. Antibacterial agent 96 shows antitubercular activity against drug-susceptible and multidrug-resistantMycobacterium tuberculosis (M. tuberculosis) strains. Antibacterial agent 96 shows toxicity to HepG2 and Vero cells.
  • HY-126970
    HBF-0259

    HBV Infection
    HBF-0259 is a potent and selective inhibitor of hepatitis B virus (HBV) surface antigen (HBsAg) secretion, with an EC50 of 1.5 μM in HepG2.2.15 cells. HBF-0259 has no effect on HBV DNA synthesis.
  • HY-147501
    TRβ agonist 3

    Thyroid Hormone Receptor Metabolic Disease
    TRβ agonist 3 (Compound 3) is a potent agonist of TRβ. TRβ agonist 3 reduces lipid accumulation in HepG2 and promote lipolysis with comparable effects. TRβ agonist 3 is a new potential TRβ-selective thyromimetics.
  • HY-147500
    TRβ agonist 2

    Thyroid Hormone Receptor Metabolic Disease
    TRβ agonist 2 (Compound 1) is a potent agonist of TRβ. TRβ agonist 2 reduces lipid accumulation in HepG2 and promote lipolysis with comparable effects. TRβ agonist 2 is a new potential TRβ-selective thyromimetics.
  • HY-145052
    HBV-IN-9

    HBV Infection
    HBV-IN-9 is a potent HBsAg (HBV Surface antigen) inhibitor (IC50=10 nM) and HBV DNA production inhibitor (IC50=0.15 nM in HepG2.2.15 cells). From patent WO2018001952A1, example 20.
  • HY-N3761
    Dimethylmatairesinol

    (-)-Maculatin; Methylarctigenin

    Others Others
    Dimethylmatairesinol (compound 8) is a lignan compound isolated from the seed of Hernandia nymphaeifolia. Dimethylmatairesinol shows cytotoxicity against the KKU-M156 and HepG2 cell line with IC50s of 5.4 μM (Emax 59%) and 5.2 μM (Emax 78%), respectively.
  • HY-N0854
    Alisol F

    HBV Infection
    Alisol F is a triterpene isolated from Alisma orinentale, has immunosuppressive and anti-virus functions. Alisol F exhibits inhibitory activity in vitro on hepatitis B virus (HBV) surface antigen (HBsAg) secretion of the HepG2.2.15 cell line with an IC50 of 0.6 μM.
  • HY-145908
    Antitumor agent-49

    Others Cancer
    Antitumor agent-49 (Compound 10) is a Harmine derivative-furoxan hybrids containing NO donor, with antitumor activities. Antitumor agent-49 shows cytotoxic activity against HepG2 cells with an IC50 of 1.79 µM. Antitumor agent-49 produces high levels of NO in vitro.
  • HY-114196
    Aclimostat

    ZGN-1061

    Others Metabolic Disease
    Aclimostat (ZGN-1061) is a potent inhibitor of the MetAP2 enzyme and displays favorable efficacy and safety in preclinical studies. ZGN-1061 produced similar efficacy as beloranib for weight loss, improvements in metabolic parameters in a mouse model of obesity and insulin resistance, and concordant changes in gene transcription in HepG2 cells.
  • HY-146148
    KDM4C-IN-1

    Histone Demethylase Cancer
    KDM4C-IN-1 (Compound 4d) is a potent KDM4C inhibitor with an IC50 of 8 nM. KDM4C-IN-1 inhibits the growth of HepG2 and A549 cells with IC50s of 0.8 µM and 1.1 µM, respectively.
  • HY-146350
    TrxR-IN-4

    TrxR Cancer
    TrxR-IN-4 (Compound 1b) is a potent inhibitor of TrxR. TrxR-IN-4 induces HepG2 cells apoptosis by activating the endoplasmic reticulum stress (ERS). TrxR-IN-4 improves the CCl4-induced liver damage in vivo by down-regulation of TrxR expression and inflammation level.
  • HY-146819
    CAIX/CAXII-IN-1

    Carbonic Anhydrase Cancer
    Compound 9 is the most effective against tumor specific Ca ix/ca XII (ki=29.1 and 8.8 nm), so it is possible to evaluate its cytotoxicity and selectivity to HepG-2, HCT-116 and MCF-7 cancer cell lines in vitro, and its IC50 values to tumor cells are 1.78, 1.94 and 3.07, respectively μ M. It showed that it had obvious cytotoxicity.
  • HY-147913
    PI3K/Akt/mTOR-IN-3

    PI3K Akt mTOR Apoptosis Cancer
    PI3K/Akt/mTOR-IN-3 (compound 3d) is a potent PI3K/AKT/mTOR inhibitor. PI3K/Akt/mTOR-IN-3 displays the inhibitory activity in MCF-7, HeLa and HepG2 cells, with IC50 values of 0.77, 1.23, and 4.57μM, respectively. PI3K/Akt/mTOR-IN-3 inhibits the migration of MCF-7 and HeLa cells at the concentration of 4 μM. PI3K/Akt/mTOR-IN-3 induces cell apoptosis and S phase arrest.
  • HY-N8214
    Isorhamnetin 3-O-β-D-glucose-7-O-β-D-gentiobioside

    Others Cardiovascular Disease
    Isorhamnetin 3-O-β-D-glucose-7-O-β-D-gentiobioside is a bioactive constituent that can be found in the seeds of Lepidium apetalum Willd. Isorhamnetin 3-O-β-D-glucose-7-O-β-D-gentiobioside exhibits significant triglyceride (TG)-lowering effects in HepG2 cells.
  • HY-B1826
    Adefovir

    GS-0393; PMEA

    HBV Reverse Transcriptase Infection
    Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses.
  • HY-112338
    C188

    CPD188

    STAT Cancer
    C188 is a STAT3 inhibitor that inhibits IL-6-stimulated STAT3 phosphorylation and nuclear translocation in HepG2 cells by targeting STAT3 SH2 domain peptide-binding pocket. C188, in particular, was highly active in inducing apoptosis of the breast cancer cell line MB-MDA-468 in vitro (EC50= 0.7 μM).
  • HY-B0144AS1
    Pitavastatin-d5 sodium

    NK-104-d5 sodium

    Mitophagy HMG-CoA Reductase (HMGCR) Apoptosis Autophagy Cancer Metabolic Disease
    Pitavastatin-d5 sodium (NK-104-d5 sodium) is the deuterium labeled Pitavastatin sodium. Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.
  • HY-115950
    Antitumor agent-48

    Others Cancer
    Antitumor agent-48 (Compound 4a) is a 2,3-dehydrosilybin derivative with an antitumor activity. Antitumor agent-48 shows cytotoxic activity against MCF-7, NCI-H1299, HepG2 and HT29 cells with IC50 values of 8.06 µM, 13.1 µM, 16.51 µM and 12.44 µM, respectively.
  • HY-B0144A
    Pitavastatin

    NK-104

    HMG-CoA Reductase (HMGCR) Autophagy Mitophagy Apoptosis Cancer Metabolic Disease Neurological Disease Cardiovascular Disease
    Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects.
  • HY-B0144B
    Pitavastatin sodium

    NK-104 sodium

    HMG-CoA Reductase (HMGCR) Autophagy Mitophagy Apoptosis Cancer Metabolic Disease Neurological Disease Cardiovascular Disease
    Pitavastatin (NK-104) sodium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin sodium inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin sodium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin sodium also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects.
  • HY-146006
    Tubulin/MMP-IN-1

    Microtubule/Tubulin MMP Cancer
    Tubulin/MMP-IN-1 (compound 15g) is a potent inhibitor of tubulin and MMP. Tubulin/MMP-IN-1 has the potential for the research of cancer diseases. Tubulin/MMP-IN-1 suppresses tubulin polymerization, induces cell cycle arrest at the G2/M phase, leads to reactive oxidative stress (ROS) generation of HepG2 cells, and results in apoptosis by the mitochondrial-dependent apoptotic pathway.
  • HY-B1826S1
    Adefovir-d4 diphosphate triethylamine

    HBV Reverse Transcriptase Infection
    Adefovir-d4 diphosphate triethylamine is the deuterium labeled Adefovir. Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses.
  • HY-15823
    CAY10566

    Stearoyl-CoA Desaturase (SCD) Cancer
    CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM).
  • HY-B1826S
    Adefovir-d4 phosphate triethylamine

    HBV Reverse Transcriptase Infection
    Adefovir-d4 phosphate triethylamine is the deuterium labeled Adefovir. Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses.
  • HY-144389
    hAChE/Aβ1-42-IN-1

    Cholinesterase (ChE) Amyloid-β Neurological Disease
    hAChE/Aβ1-42-IN-1 (Compound 16) is a potent inhibitor of hAChE and Aβ1-42 aggregation. hAChE/Aβ1-42-IN-1 shows acceptable relative safety upon hepG2 cell line and excellent BBB penetration with wide safety margin. hAChE/Aβ1-42-IN-1 has the potential for the research of Alzheimer disease (AD).
  • HY-147552
    HIV-1 inhibitor-35

    HIV Infection
    HIV-1 inhibitor-35 (compound 74) is a potent HIV-1 inhibitor with EC50s of 80 nM and 70 nM for LTR and CMV in HEK293 cells, respectively. HIV-1 inhibitor-35 has inhibitory activity against liver cancer cell HepG2 with a CC50 of 40 nM. HIV-1 inhibitor-35 can be used as HIV-1 latency reversing agent.
  • HY-N0385
    Gomisin J

    AMPK Calcium Channel Metabolic Disease Cardiovascular Disease
    Gomisin J is a small molecular weight lignan found in Schisandra chinensis and has been demonstrated to have vasodilatory activity. Gomisin J suppresses lipid accumulation by regulating the expression of lipogenic and lipolytic enzymes and inflammatory molecules through activation of AMPK, LKB1 and Ca 2+/calmodulin-dependent protein kinase II and inhibition of fetuin-A in HepG2 cells. gomisin J has potential benefits in treating nonalcoholic fatty liver disease.
  • HY-B0144S
    Pitavastatin-d4 hemicalcium

    NK-104-d4 hemicalcium; Pitavastatin-d4 hemicalcium

    HMG-CoA Reductase (HMGCR) Autophagy Mitophagy Apoptosis Metabolic Disease Cancer
    Pitavastatin-d4 (hemicalcium) is deuterium labeled Pitavastatin (Calcium). Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.
  • HY-146398
    AMPK activator 6

    AMPK Metabolic Disease
    AMPK activator 6 (Compound GC) reduces lipid content and activates the AMPK pathway in HepG2 and 3T3-L1 cells. AMPK activator 6 significantly suppresses the increase in triglyceride (TG) , total cholesterol (TC), low-density lipoprotein-C (LDL-C), and other biochemical indices in blood serum. AMPK activator 6 can be used for the research of non-alcoholic fatty liver disease (NAFLD) and metabolic syndrome.
  • HY-146172
    Antioxidant agent-3

    Reactive Oxygen Species Cancer Inflammation/Immunology
    Antioxidant agent-3 (Compound 14q), an potent antioxidant, displays potent DPPH radicals scavenging activity and ABTS + scavenging activity with IC50s of 26.58 and 30.31 μM, respectively. Antioxidant agent-3 (Compound 14q) increases reactive oxygen species (ROS), superoxide dismutase (SOD) and glutathione (GSH), and reduced lactate dehydrogenase (LDH) in H2O2-treated HepG2 cells.
  • HY-151486
    GLUT1-IN-1

    GLUT Cancer
    GLUT1-IN-1 is a glucose transporter 1 (GLUT1) inhibitor and has a GLUT1-specific inactivation ability. GLUT1-IN-1 exhibits concentration-dependent cytotoxicity for HeLa, A549 and HepG2 cells with IC50 values of 5.49 μM, 11.14 μM, and 8.73 μM, respectively. GLUT1-IN-1 can be used for the research of photodynamic therapy (PDT) and severals cancer.
  • HY-B1826S2
    Adefovir-d4

    GS-0393-d4; PMEA-d4

    HBV Reverse Transcriptase Infection
    Adefovir-d4 (GS-0393-d4) is the deuterium labeled Adefovir. Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses.
  • HY-B0144
    Pitavastatin Calcium

    NK-104 hemicalcium; Pitavastatin hemicalcium

    HMG-CoA Reductase (HMGCR) Autophagy Mitophagy Apoptosis Cancer Metabolic Disease Neurological Disease Cardiovascular Disease
    Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin Calcium also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects.
  • HY-146366
    Tubulin inhibitor 26

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight.
  • HY-151459
    VEGFR-2/DHFR-IN-2

    VEGFR Bacterial Dihydrofolate reductase (DHFR) Fungal Cancer Infection
    VEGFR-2/DHFR-IN-2 (compound 5b) is an inhibitor of VEGFR-2 and DHFR with IC50s of 0.623 and 9.085 μM, respectively. VEGFR-2/DHFR-IN-2 exhibits good cytotoxic activities against C26, HepG2, and MCF7 cancer cell lines with IC50 values of 3.59-8.38 μM. VEGFR-2/DHFR-IN-2 can be used for the research of cancer.
  • HY-125990
    SLC13A5-IN-1

    Sodium Channel Metabolic Disease Cardiovascular Disease
    SLC13A5-IN-1 is a selective sodium-citrate co-transporter (SLC13A5) inhibitor. SLC13A5-IN-1 completely blocks the uptake of  14C-citrate with an IC50 value of 0.022 μM in HepG2 cells. SLC13A5-IN-1 has the potential for the treatment of metabolic and/or cardiovascular diseases. SLC13A5-IN-1 is extracted from patent WO2018104220A1, Compound I-5.
  • HY-N7676
    Marein

    AMPK HDAC Metabolic Disease Neurological Disease Cardiovascular Disease
    Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects.
  • HY-N0043
    Ginsenoside Rd

    Gypenoside VIII

    NF-κB COX Calcium Channel Cytochrome P450 Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease Cancer
    Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
  • HY-124346
    T-3364366

    Others Metabolic Disease
    T-3364366 is a reversible, slow-binding, thienopyrimidinone delta-5 desaturase (D5D) inhibitor with IC50s of 1.9 nM and 2.1 nM in HepG2 and RLN-10 cells, respectively. T-3364366 exhibits potent D5D (IC500=19 nM) inhibitory activity and excellent selectivity away from delta-6 desaturase (D6D, IC50=6200 nM) and delta-9 desaturase (stearoyl-CoA desaturase, SCD,50 >10000 nM) in the enzymatic activity assay.
  • HY-147901
    KDM1/CDK1-IN-1

    Histone Demethylase CDK Apoptosis Caspase Cancer
    KDM1/CDK1-IN-1 (compound 4) is a potent KDM1 and CDK1 inhibitor, with IC50 values of 0.096 and 0.078 μM, respectively.KDM1/CDK1-IN-1 induces cell cycle arrest at G2/M phase and apoptosis in HOP-92 cells. KDM1/CDK1-IN-1 exhibits potent cytotoxic activity against the CCRF-CEM, HOP-92 and Hep-G2 cells, with IC50 values of 16.34, 3.45 and 7.79 μM, respectively.
  • HY-144791
    Bcl-2-IN-6

    Bcl-2 Family MDM-2/p53 Caspase Apoptosis Cancer
    Bcl-2-IN-6 (compound 10) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.91, 22.30, 42.29, and 48.00 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively.
  • HY-144792
    Bcl-2-IN-7

    Bcl-2 Family MDM-2/p53 Caspase Apoptosis Cancer
    Bcl-2-IN-7 (compound 6) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.17, 22.64, 45.57, and 51.50 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively.
  • HY-151458
    VEGFR-2/DHFR-IN-1

    VEGFR Bacterial Dihydrofolate reductase (DHFR) Fungal Cancer Infection
    VEGFR-2/DHFR-IN-1 (compound 8b) is an inhibitor of VEGFR-2 and DHFR with IC50s of 0.384 and 7.881 μM, respectively. VEGFR-2/DHFR-IN-1 shows good antibacterial activities against Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA and MRSA with MIC values of 16, 16, 16, 8, and 16 μg/mL, respectively. VEGFR-2/DHFR-IN-1 exhibits good cytotoxic activities against C26, HepG2, and MCF7 cancer cell lines with IC50 values of 2.97-7.12 μM. VEGFR-2/DHFR-IN-1 can be used for the research of cancer.
  • HY-P2276
    Pep2-8

    Ser/Thr Protease Cancer
    Pep2-8 is a PCSK9 inhibitor with a binding KD of 0.7 μM and an IC50 of 1.4 μM.
  • HY-P3455
    Ac-SVVVRT-NH2

    PGC-1α Cancer Metabolic Disease
    Ac-SVVVRT-NH2 is a PGC-1α modulator that modulates the activity of the human PGC-1α promoter (114%). Ac-SVVVRT-NH2 increases PGC-1α mRNA (125%) and accumulation of intracellular lipids (128%) in subcutaneous human adipocytes. Ac-SVVVRT-NH2 can be used in the research of diseases which is modulated by PGC-1α.
  • HY-146728
    STAT3-IN-10

    STAT Apoptosis Cancer
    STAT3-IN-10 is a STAT3 inhibitor with an IC50 value of 5.18 µM. STAT3-IN-10 directly binds to STAT3 SH2 domain, induces cancer cells apoptosis.
  • HY-146040
    Anticancer agent 47

    Apoptosis Cancer
    Anticancer agent 47 (compound 4j) is a potent anticancer agent. Anticancer agent 47 shows antiproliferative activities. Anticancer agent 47 induces apoptosis and cell cycle arrest at G0/G1 phase. Anticancer agent 47 shows shows antitumor activities in vivo.
  • HY-147800
    VEGFR-2-IN-21

    VEGFR Cancer
    VEGFR-2-IN-21 (Compound 5d) is a potent VEGFR-2 inhibitor with an IC50 of 0.10 μM. VEGFR-2-IN-21 shows anticancer activity.
  • HY-151570
    Anticancer agent 87

    Others Cancer
    Anticancer agent 87 is a potent anticancer agent. Anticancer agent 87 can be used in the research of breast adenocarcinoma and liver cancer.
  • HY-144804
    VEGFR-2-IN-17

    VEGFR Cancer
    VEGFR-2-IN-17 (Compound 15a) is a potent VEGFR-2 inhibitor with an IC50 of 67.25 nM. VEGFR-2-IN-17 shows antitumor activities.
  • HY-144760
    EGFR-IN-3

    EGFR Apoptosis Cancer
    EGFR-IN-3 (Compound 4c) is a potent EGFR inhibitor with an IC50 of 0.32 µM against EGFRwt-TK. EGFR-IN-3 shows cytotoxic activity against cancer cell lines and induces apoptosis.
  • HY-N2253
    Neoruscogenin

    ROR Infection Neurological Disease
    Neoruscogenin, a member of the steroidal sapogenin family, is a bioavailable, potent, and high-affinity agonist of the nuclear receptor RORα (NR1F1).
  • HY-144803
    VEGFR-2-IN-16

    VEGFR Cancer
    VEGFR-2-IN-16 (Compound 15b) is a potent VEGFR-2 inhibitor with an IC50 of 86.36 nM. VEGFR-2-IN-16 shows antitumor activities.
  • HY-146474
    EGFR-IN-54

    EGFR Cancer
    EGFR-IN-54 (Compound 3c) is a potent EGFR inhibitor with an IC50 of 1.623 µM. EGFR-IN-54 shows cytotoxic activity against cancer cell lines.
  • HY-146473
    EGFR-IN-53

    EGFR Cancer
    EGFR-IN-53 (Compound 7) is a potent EGFR inhibitor with an IC50 of 8.264 µM. EGFR-IN-53 shows cytotoxic activity against cancer cell lines.
  • HY-151572
    Anticancer agent 88

    Others Cancer
    Anticancer agent 88 is a potent anticancer agent. Anticancer agent 88 can be used in the research of breast adenocarcinoma and liver cancer.
  • HY-150538
    STAT3-IN-12

    STAT Apoptosis Cancer
    STAT3-IN-12 is a potent STAT3 signal inhibitor that can inhibit IL-6 induced JAK/STAT3 signalling pathway activation. STAT3-IN-12 inhibits cancer cell growth, migration, and induce cell apoptosis as well as cycle arrest. STAT3-IN-12 can be used in cancer-related research, such as hepatocellular carcinoma (HCC) and oesophageal carcinoma.
  • HY-N0324B
    Cholic acid sodium hydrate

    Endogenous Metabolite Metabolic Disease
    Cholic acid sodium hydrate is a major primary bile acid produced in the liver and usually conjugated with glycine or taurine. Cholic acid sodium hydrate facilitates fat absorption and cholesterol excretion. Cholic acid sodium hydrate is orally active.
  • HY-144381
    Glutamate-5-kinase-IN-1

    Others Infection
    Glutamate-5-kinase-IN-1 (compound 50) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.1 µM. Glutamate-5-kinase-IN-1 shows G5K inhibition by alters the ATP binding site architecture for enzyme recognition. Glutamate-5-kinase-IN-1 has the potential for the research of anti-TB agents.
  • HY-144382
    Glutamate-5-kinase-IN-2

    Others Infection
    Glutamate-5-kinase-IN-2 (compound 54) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.2 µM. Glutamate-5-kinase-IN-2 shows G5K inhibition by promotes conformational changes at the L-glutamate binding site. Glutamate-5-kinase-IN-2 has the potential for the research of anti-TB agents.
  • HY-N0324A
    Cholic acid sodium

    Endogenous Metabolite Metabolic Disease
    Cholic acid sodium is a major primary bile acid produced in the liver and usually conjugated with glycine or taurine. It facilitates fat absorption and cholesterol excretion. Cholic acid sodium is orally active.
  • HY-B1978
    Iprodione

    Fungal Reactive Oxygen Species Infection
    Iprodione, a dicarboximide fungicide, has a highly specific action, with a capacity to cause oxidative damage through production of free oxygen radicals (ROS). Iprodione does not appear to be species selective.
  • HY-146725
    FBPase-IN-1

    FBPase Metabolic Disease
    FBPase-IN-1 is a potent FBPase (Fructose-1,6-bisphosphatase) inhibitor for Type 2 diabetes (T2D) study with an IC50 of 0.22 μM. FBPase-IN-1 can reduce blood glucose levels and ameliorate glucose tolerance. FBPase-IN-1 modifies the C128 site, regulates the N125-S124-S123 allosteric pathway of FBPase and affects the catalytic activity of FBPase.
  • HY-146792
    PLK1-IN-4

    Polo-like Kinase (PLK) Cancer
    PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma.
  • HY-103118
    PU02

    5-HT Receptor Apoptosis Cancer Neurological Disease
    PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively.
  • HY-146094
    Antitumor agent-63

    Topoisomerase Cancer
    Antitumor agent-63 (Compound 40), a 20 (S)-O-linked camptothecin (CPT) glycoconjugate, is an antitumor agent without toxicity towards normal cells. Antitumor agent-63 shows high stability and very weak direct topoisomerase I (Topo I) inhibition.
  • HY-146142
    AChE/BuChE-IN-2

    Cholinesterase (ChE) Amyloid-β Neurological Disease
    AChE/BuChE-IN-2 (Compound 5f) is an orally active AChE and BuChE inhibitor with IC50 values of 0.72 μM and 0.16 μM, respectively. AChE/BuChE-IN-2 shows a non-competitive inhibition with AChE and shows potent self-induced β-amyloid (Aβ) aggregation inhibition with an IC50 of 62.52 μM. AChE/BuChE-IN-2 can cross the BBB.
  • HY-N0324
    Cholic acid

    Endogenous Metabolite Metabolic Disease
    Cholic acid is a major primary bile acid produced in the liver and usually conjugated with glycine or taurine. It facilitates fat absorption and cholesterol excretion. Cholic acid is orally active.
  • HY-151575
    PfGSK3/PfPK6-IN-2

    GSK-3 Infection
    PfGSK3/PfPK6-IN-2 is a potent dual PfGSK3/PfPK6 (Plasmodium falciparum GSK3/PK6) inhibitor (IC50: 172 nM and 11 nM respectively). PfGSK3/PfPK6-IN-2 can be used in the research of Malaria.
  • HY-N10641
    Epinodosinol

    Others Cancer
    Epinodosinol is a diterpenoid derived from plant Rabdosia angustifolia. Epinodosinol has inhibitory activity against certain cancer cells.
  • HY-146997
    TRβ agonist 1

    Thyroid Hormone Receptor Metabolic Disease
    TRβ agonist 1 is a selective and mutation-sensitive thyroid hormone receptor β (TRβ) agonist, with an EC50 value of 21 nM. TRβ agonist 1 can be used for researching dyslipidemia, nonalcoholic steatohepatitis (NASH), and resistance to thyroid hormone (RTH).
  • HY-147983
    PI3Kα-IN-8

    PI3K Reactive Oxygen Species Apoptosis Cancer
    PI3Kα-IN-8 (Compound 9g) is a selective PI3Kα inhibitor with an IC50 of 0.012 μM. PI3Kα-IN-8 increases intracellular reactive oxygen species level, decreases mitochondrial membrane potential and induces apoptosis.
  • HY-141714
    SBC-115337

    Ser/Thr Protease Cancer
    SBC-115337, as a potent benzofuran compound, is a PCSK9 inhibitor with an IC50 value of 0.5 μM.
  • HY-151565
    Anticancer agent 86

    Others Cancer
    Anticancer agent 86 (compound 6i) shows potential activity against breast adenocarcinoma.
  • HY-146197
    Apoptotic agent-1

    Apoptosis Cancer
    Apoptotic agent-1 (Compound 8a) is an apoptotic agent with high antiproliferative activity against cancer cells and low cytotoxic effect. Apoptotic agent-1 induces over-expression of Fas receptor and Cyto C genes.
  • HY-146472
    EGFR-IN-52

    EGFR Apoptosis Cancer
    EGFR-IN-52 (Compound 4) is a potent EGFR inhibitor with IC50 values of 0.358, 86.02 and 432.67 µM against EGFR, EGFR L858R-TK and EGFR T790M-TK, respectively. EGFR-IN-52 shows cytotoxic activity against cancer cell lines and induces apoptosis.
  • HY-147971
    Anticancer agent 75

    Parasite Topoisomerase Cancer Infection
    Anticancer agent 75 is a potent anticancer agent. Anticancer agent 75 shows cytotoxicity and selectivity in cancer cell lines. Anticancer agent 75 shows cytotoxicity to normal human kidney cell lines is at least 35 times lower than that of the Doxorubicin standard. Anticancer agent 75 shows good activity of antiplasmodial.
  • HY-123091
    Ivangustin

    Others Cancer
    Ivangustin is a sesquiterpene isolated from the flower heads of the medicinal plant Inula britannica.
  • HY-147698
    ZLHQ-5f

    CDK Topoisomerase Apoptosis Cancer
    ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile.
  • HY-146048
    Antitumor agent-57

    Apoptosis Reactive Oxygen Species Cancer
    Antitumor agent-57 (Compound 3o) is an NQO1-directed antitumor agent. Antitumor agent-57 inhibits tumor cell growth, triggers ROS generation and induces cell apoptosis.
  • HY-N6617
    Norswertianolin

    Others Cardiovascular Disease
    Norswertianolin acts as a CSE activator and is isolated from G. acuta. Norswertianolin may be a potential agent for cardiovascular diseases.
  • HY-16196
    ENMD-1198

    IRC-110160

    Microtubule/Tubulin HIF/HIF Prolyl-Hydroxylase STAT Cancer
    ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
  • HY-146092
    Apoptosis inducer 4

    Apoptosis Cancer
    Apoptosis inducer 4 (Compound 12b) is an apoptosis inducer with anticancer activities.
  • HY-146471
    EGFR-IN-51

    EGFR Apoptosis Cancer
    EGFR-IN-51 (Compound 6) is a potent EGFR inhibitor with IC50 values of 0.493, 102.60 and 461.63 µM against EGFR, EGFR L858R-TK and EGFR T790M-TK, respectively. EGFR-IN-51 shows cytotoxic activity against cancer cell lines and induces apoptosis.
  • HY-101568
    Roblitinib

    FGF-401

    FGFR Cancer
    Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity.
  • HY-147895
    PCAF-IN-2

    Histone Acetyltransferase Apoptosis Cancer
    PCAF-IN-2 (compound 17) is a potent PCAF inhibitor with an IC50 value of 5.31 µM. PCAF-IN-2 shows anti-tumour activity. CAF-IN-2 induces apoptosis and arrest the cell cycle at the G2/M phase.
  • HY-144259
    Metallo-β-lactamase-IN-2

    Bacterial Infection
    Metallo-β-lactamase-IN-4 (compound 40) is a potent metallo-β-lactamases (MBL) inhibitor, with IC50 values of 0.1 μM (VIM-1), 1.3 μM (NDM-1), and 5.0 μM (IMP-7), respectively.
  • HY-N1912
    Andropanolide

    Others Cancer
    Andropanolide is a natural product that exerts cytotoxicity toward carcinoma cells and significantly inhibits the overproduction of nitric oxide (NO) in Lipopolysaccharides (HY-D1056) (LPS)-stimulated RAW264.7 macrophages.
  • HY-143250
    Tubulin inhibitor 12

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 12 (Hit 9) is a novel tubulin inhibitor (IC50=25.3 μM). Tubulin inhibitor 12 shows anti-tumor activity and anti-proliferative activity.
  • HY-144261
    Metallo-β-lactamase-IN-3

    Bacterial Infection
    Metallo-β-lactamase-IN-3 (compound 35) is a potent metallo-β-lactamases (MBL) inhibitor. Metallo-β-lactamase-IN-3 shows high activity against VIM-1 and NDM-1, with IC50 of 0.6 and 1.0 μM, respectively. Metallo-β-lactamase-IN-3 does not show inhibition of IMP-7.
  • HY-111489
    LMPTP inhibitor 1

    Phosphatase Metabolic Disease
    LMPTP inhibitor 1 is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
  • HY-15353
    Emivirine

    MKC-442

    HIV Infection Inflammation/Immunology
    Emivirine (MKC-442) is a non-nucleoside reverse transcriptase inhibitors (NNRTIs) with Ki values of 0.20 and 0.01 μM for dTTP- and dGTP-dependent DNA or RNA polymerase activity, respectively. Emivirine displays potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity.
  • HY-148201
    Oleana-2,12-dien-28-oic acid

    HBV Infection
    Oleana-2,12-dien-28-oic acid is an HBV-DNA inhibitor, HBsAg and HBeAg inhibitor. Oleana-2,12-dien-28-oic acid can be used in hepatitis B virus infection disease research.
  • HY-151433
    Antiparasitic agent-10

    Parasite Infection
    Antiparasitic agent-10 (Compound 94) is an anti-parasitic agent, shows anti-schistosomal activity. Antiparasitic agent-10 shows activity against adults of Schistosoma mansoni, and can be used in Schistosomiasis research.
  • HY-122614
    S29434

    NMDPEF

    Autophagy Neurological Disease
    S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1. S29434 induces autophagy and inhibits QR2-mediated ROS production.
  • HY-W104368
    Nicotinic acid riboside

    Endogenous Metabolite Cancer Metabolic Disease
    Nicotinic acid riboside is a NAD + precursor in human cells. Nicotinic acid riboside is an authentic intermediate of human NAD + metabolism.
  • HY-147872
    VEGFR-2-IN-22

    VEGFR Microtubule/Tubulin Apoptosis Cancer
    VEGFR-2-IN-22 (Compound 25) is a dual VEGFR-2 and β-tubulin polymerization inhibitor with an IC50 of 19.82 nM against VEGFR-2. VEGFR-2-IN-22 induces apoptosis.
  • HY-144262
    Metallo-β-lactamase-IN-4

    Bacterial Infection
    Metallo-β-lactamase-IN-4 (compound 40) is a potent metallo-β-lactamases (MBL) inhibitor, with IC50 values of 0.5 μM (VIM-1), 2.1 μM (NDM-1), and 3.3 μM (IMP-7), respectively.
  • HY-146138
    EGFR-IN-57

    EGFR VEGFR Casein Kinase Topoisomerase Microtubule/Tubulin Apoptosis Cancer
    EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis.
  • HY-100028
    AT-130

    HBV DNA/RNA Synthesis Cancer Infection
    AT-130, a phenylpropenamide derivative, is a potent hepatitis B virus (HBV) replication non-nucleoside inhibitor. AT-130 inhibits the viral DNA synthesis with an EC50 of 0.13 μM. AT-130 inhibits both wt and mutant HBVs. AT-130 has anti-HBV activity in hepatoma cells.
  • HY-146093
    Antitumor agent-62

    Apoptosis Cancer
    Antitumor agent-62 (Compound 47) is a NO-releasing antitumor agent. Antitumor agent-62 shows antiproliferative activity against four cancer cell lines. Antitumor agent-62 activates mitochondrial apoptosis pathway and arrests cell cycle at G2/M phase.
  • HY-144292
    HDAC-IN-30

    HDAC Cancer
    HDAC-IN-30 is a novel multi-target HDAC inhibitor, including HDAC1 (IC50=13.4 nM),HDAC2 (IC50=28.0 nM), HDAC3 (IC50=9.18 nM), HDAC6 (IC50=42.7 nM), HDAC8 (IC50=131 nM). HDAC-IN-30 exhibits potent antitumor efficacy.
  • HY-147877
    Topoisomerase II inhibitor 12

    Topoisomerase Cancer
    Topoisomerase II inhibitor 12 (Compound 8c) is a topoisomerase II (topo II) inhibitor, working as a DNA non-intercalator. Topoisomerase II inhibitor 12 shows antineoplastic activity.
  • HY-W028393
    Indole-3-pyruvic acid

    Endogenous Metabolite Aryl Hydrocarbon Receptor Inflammation/Immunology Neurological Disease
    Indole-3-pyruvic acid, a keto analogue of tryptophan, is an orally active AHR agonist. Indole-3-pyruvic acid has antioxidant properties, and can be used in the research of inflammation, anxiety.
  • HY-151461
    CHNQD-01255

    Others Cancer
    CHNQD-01255 is an orally active Arf-GEFs inhibitor with potent anti-hepatocellular carcinoma (HCC) efficacy.
  • HY-N10436
    Anti-inflammatory agent 30

    Others Metabolic Disease Inflammation/Immunology
    Anti-inflammatory agent 30 (Compound 5) is an anti-inflammatory agent with hepatoprotective activity.
  • HY-151162
    HER2-IN-12

    EGFR Cancer
    HER2-IN-12 is a HER2 inhibitor (IC50: 121 nM). HER2-IN-12 can be used in the research of cancers, such as breast cancer.
  • HY-147981
    Tubulin polymerization-IN-31

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin polymerization-IN-31 (Compound 4c) is a tubulin polymerization inhibitor with an IC50 of 3.64 μM. Tubulin polymerization-IN-31 induces cancer cell apoptosis and shows antitumor activity.
  • HY-144805
    VEGFR-2-IN-18

    VEGFR Apoptosis Cancer
    VEGFR-2-IN-18 (Compound 15d) is a potent VEGFR-2 inhibitor with an IC50 of 60 nM. VEGFR-2-IN-18 induces cell apoptosis. VEGFR-2-IN-18 shows antitumor activities.
  • HY-N1039A
    Manool

    Others Cancer
    Manool is a diterpene from Salvia officinalis. Manool induces selective cytotoxicity in cancer cells. Manool arrests the cancer cells at the G(2)/M phase of the cell cycle.
  • HY-N10435
    Anti-inflammatory agent 29

    Others Metabolic Disease Inflammation/Immunology
    Anti-inflammatory agent 29 (Compound 7) is an anti-inflammatory agent with hepatoprotective activity.
  • HY-N10434
    Anti-inflammatory agent 28

    Others Metabolic Disease Inflammation/Immunology
    Anti-inflammatory agent 28 (Compound 9) is an anti-inflammatory agent with hepatoprotective activity.
  • HY-N1082
    Visnagin

    Others Inflammation/Immunology Neurological Disease Cardiovascular Disease
    Visnagin, an antioxidant furanocoumarin derivative, possess anti-inflammatory and analgesic properties. Visnagin has substantial potential to prevent Cerulein induced acute pancreatitis (AP). Visnagin possess promising vasodilator effects in vascular smooth muscles.
  • HY-147916
    RNA polymerase II-IN-1

    DNA/RNA Synthesis Cancer
    RNA polymerase II-IN-1 (compound 19iv) is a amatoxin, inhibiting RNA polymerase II (Pol II) with an IC50 value of 36.66 nM. RNA polymerase II-IN-1 has higher cytotoxicity against cancer cells and less toxic in normal cells than α-Amanitin.
  • HY-146210
    EGFR-IN-50

    EGFR Cancer
    EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells.
  • HY-147102
    tri-GalNAc biotin

    LYTACs Cancer
    tri-GalNAc biotin is a small molecule lysosome targeting degrader. tri-GalNAc is a ligand of ASGPR (asialoglycoprotein receptor). tri-GalNAc biotin can facilitate the uptake of NeutrAvidin (NA) through ASGPR in liver cells. tri-GalNAc biotin delivers NeutrAvidin to lysosome for degradation. tri-GalNAc biotin can be used for research of LYsosome TArgeting Chimera (LYTAC).
  • HY-103490
    Takinib

    EDHS-206

    MAP3K Apoptosis Cancer Infection Inflammation/Immunology
    Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM).
  • HY-144254
    PI3Kδ-IN-10

    PI3K Akt Apoptosis Cancer
    PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor with IC50 of 2 nM. PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models.
  • HY-151285
    JAK-2/3-IN-3

    Apoptosis JAK Cancer Inflammation/Immunology
    JAK-2-/3-IN-3 (compound ST4j) is a potent JAK2/3 inhibitor with IC50s of 13.00 and 14.86 nM for JAK2 and JAK3, respectively. JAK-2-/3-IN-3 inhibits autophosphorylation of JAK2 and induces apoptosis in a dose- and time-dependent manner. JAK-2-/3-IN-3 can be used in studies of lymph derived diseases and leukemia.
  • HY-146863
    Tubulin polymerization-IN-10

    Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-10 is a potent tubulin polymerization inhibitor with an IC50 of 4.25±0.75 μM. Tubulin polymerization-IN-10 has anti-tumor effects.
  • HY-B1334
    Perhexiline

    Mitochondrial Metabolism Apoptosis Cancer Cardiovascular Disease
    Perhexiline is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline can be used in the research of cancers, and cardiovascular disease like angina.
  • HY-145655
    CDK7-IN-11

    CDK Cancer
    CDK7-IN-11 is an orally active CDK7 inhibitor. CDK7-IN-11 exhibits high CDK7 inhibitory activity with IC50 value of 4.2 nM. CDK7-IN-11 can be effectively used for the research of diseases associated with CDK7.
  • HY-B1334A
    Perhexiline maleate

    Mitochondrial Metabolism Apoptosis Cancer Cardiovascular Disease
    Perhexiline maleate is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline maleate induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline maleate can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline maleate can be used in the research of cancers, and cardiovascular disease like angina.
  • HY-123402
    GSK3987

    LXR Metabolic Disease
    GSK3987 is a pan LXRα/β agonist with EC50s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellular cholesterol efflux and triglyceride accumulation.
  • HY-17502
    Simvastatin

    MK 733

    HMG-CoA Reductase (HMGCR) Autophagy Mitophagy Apoptosis Ferroptosis Cardiovascular Disease Cancer
    Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
  • HY-151159
    DHFR-IN-4

    Dihydrofolate reductase (DHFR) EGFR Cancer
    DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with an IC50 value of 123 nM. DHFR-IN-4 also has inhibitory activity against EGFR and HER2 with IC50s of 246 nM and 357 nM, respectively. DHFR-IN-4 has remarkable broad spectrum cytotoxic potency against cancer cells.
  • HY-143260
    GSK-3β inhibitor 6

    GSK-3 Cancer Metabolic Disease Inflammation/Immunology
    GSK-3β inhibitor 6 is a potent GSK-3β inhibitor with an IC50 value of 24.4 μM. GSK-3β inhibitor 6 shows high hepatocyte glucose uptake (38%). GSK-3β inhibitor 6 can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.
  • HY-143261
    GSK-3β inhibitor 7

    GSK-3 Cancer Metabolic Disease Inflammation/Immunology
    GSK-3β inhibitor 7 is a GSK-3β inhibitor with an IC50 value of 5.25 μM. GSK-3β inhibitor 7 is inserted into the ATP-binding binding pocket of GSK-3β and forms hydrogen-bond. GSK-3β inhibitor 7 shows high hepatocyte glucose uptake (83.5%), and can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.
  • HY-146315
    AChE/BChE-IN-6

    Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    AChE/BChE-IN-6 (compound 22) is a potent dual AChE/BChE inhibitor with IC50 values of 0.809 µM, 2.248 µM and > 100 µM for hBChE, hAChE and hMAO-B, respectively. AChE/BChE-IN-6 penetrates the blood-brain barrier (BBB). AChE/BChE-IN-6 can be used for Alzheimer’s disease (AD) research.
  • HY-116999
    IR415

    HBV Infection
    IR415 is a potent anti-HBV agent and inhibits HBV replication by blocking the HBx activity. IR415 selectively interacts with HBx (Kd=2 nM) and blocks HBV-mediated RNAi suppression, reverses the inhibitory effect of HBx protein on the activity of the dicer endoribonuclease. HBx: hepatitis B virus X protein.
  • HY-151109
    IR-990

    Others Others
    IR-990 is an activatable NIR-II fluorescent probe with an acceptor-π-acceptor (A-π-A) skeleton for real-time detection of H2O2 in vivo. IR-990 is a powerful diagnosis of drug-induced liver injury (DILI).
  • HY-115463
    EB-3D

    AMPK Apoptosis Cancer
    EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.
  • HY-151471
    Anticancer agent 84

    c-Myc Cancer
    Anticancer agent 84 is an anticancer agent. Anticancer agent 84 represses the transcription of c-MYC by stabilizing the G-quadruplex (G4) structure. Anticancer agent 84 can be used for the research of cancer.
  • HY-147722
    hCAIX-IN-8

    Carbonic Anhydrase Cancer
    hCAIX-IN-8 (compound 7i) is a potent and selective hCAIX inhibitor with IC50s of 1.99, 0.024, 1.10 µM for CAII, CAIX, CAVA respectively. hCAIX-IN-8 shows anti-proliferation activity with low toxicity. hCAIX-IN-8 decreases the epithelial to mesenchymal transitions and induces apoptosis. hCAIX-IN-8 inhibits cell migration and colonization potential.
  • 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-N0779A
    Silybin

    Apoptosis Cancer Inflammation/Immunology
    Silybin is a flavonolignan isolated from milk thistle (Silybum marianum) seeds. Silybin induces apoptosis and exhibits hepatoprotective, antioxidant, anti-inflammatory, anti-cancer activity.
  • HY-113066A
    Guanosine 5'-diphosphate disodium salt

    GDP disodium salt

    Endogenous Metabolite Potassium Channel Inflammation/Immunology
    Guanosine 5'-diphosphate (GDP) disodium salt is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate disodium salt is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate disodium salt can be used in the research of inflammation, such as anemia of inflammation (AI).
  • HY-120349
    LL-Z1640-4

    p38 MAPK JNK Apoptosis Reactive Oxygen Species Cancer
    LL-Z1640-4 is a potent p38/JNK signaling inhibitor. LL-Z1640-4 significantly diminishes p38 and JNK activation in HCC cells transfected with MLK4 siRNA. LL-Z1640-4 markedly attenuates ROS production induced by MLK4 knockdown. LL-Z1640-4 significantly reduces the apoptotic cells in HCC cells transfected with siMLK4.
  • HY-146288
    LXR agonist 2

    LXR Metabolic Disease
    LXR agonist 2 (compound 18rr) is a potent LXR (liver X receptor) agonist. LXR agonist 2 can stabilize NCOA1 (co-activator), leading to LXR agonism.
  • HY-117469
    Triptohypol C

    Others Inflammation/Immunology
    Triptohypol C, a Tripterin (HY-13067) derivative, is a potent Nur77-targeting anti-inflammatory agent with an Kd value of 0.87 μM. Triptohypol C inhibits inflammatory response by promoting the interactions of Nur77 with TRAF2 and p62/SQSTM1.
  • HY-139576B
    Larsucosterol (trimethylamine)

    DUR-928 (trimethylamine)

    LXR Endogenous Metabolite Metabolic Disease
    Larsucosterol (DUR-928) trimethylamine, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol trimethylamine as a potent endogenous regulator decreases lipogenesis. Larsucosterol trimethylamine inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.
  • HY-113066
    Guanosine 5'-diphosphate

    GDP

    Endogenous Metabolite Potassium Channel Inflammation/Immunology
    Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
  • HY-150655
    Hsp90-IN-15

    HSP Cancer
    Hsp90-IN-15 is an Hsp90 inhibitor with anticancer activity. Hsp90-IN-15 induces cell apoptosis, arrests the cell cycle at S phase and decreases the expression level of Hsp90 in Hela cell.
  • HY-113066C
    Guanosine 5'-diphosphate sodium

    GDP sodium

    Endogenous Metabolite Potassium Channel Inflammation/Immunology
    Guanosine 5'-diphosphate (GDP) sodium is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate sodium is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate sodium can be used in the research of inflammation, such as anemia of inflammation (AI).
  • HY-139576
    Larsucosterol

    DUR-928

    Endogenous Metabolite Metabolic Disease
    Larsucosterol (DUR-928), a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol as a potent endogenous regulator decreases lipogenesis. Larsucosterol inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.
  • HY-P2282
    APTSTAT3-9R

    STAT Cancer
    APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity.
  • HY-139576A
    Larsucosterol sodium

    DUR-928 sodium

    Endogenous Metabolite Metabolic Disease
    Larsucosterol (DUR-928) sodium, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol sodium as a potent endogenous regulator decreases lipogenesis. Larsucosterol sodium inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.
  • HY-144395
    HDAC6-IN-4

    HDAC Apoptosis Cancer Inflammation/Immunology
    HDAC6-IN-4 (C10) is a potent, orally active and highly selective HDAC6 inhibitor with an IC50 value of 23 nM. HDAC6-IN-4 induces cancer cells apoptosis and shows significant antitumor efficacy, without obvious toxicity.
  • HY-110381
    JNJ-DGAT2-A

    Acyltransferase Metabolic Disease
    JNJ-DGAT2-A is a selective diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 value of 0.14 μM in human DGAT2-expressing Sf9 insect cell membranes. JNJ-DGAT2-A can be used for the research of triglyceride (TG) synthesis.
  • HY-151443
    HDAC-IN-47

    HDAC Cancer
    HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo.
  • 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-18964
    MG-101

    Calpain inhibitor I; Ac-LLnL-CHO; ALLN

    Proteasome Apoptosis Cancer
    MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer.
  • HY-151432
    URAT1 inhibitor 3

    URAT1 Inflammation/Immunology
    URAT1 inhibitor 3 is a potent, orally active, selective URAT1 inhibitor with an IC50 value of 0.8 nM. URAT1 inhibitor 3 has urate-lowering efficacy. URAT1 inhibitor 3 can be used in research of gout and hyperuricemi.
  • HY-W009731
    Dibenzoylmethane

    Keap1-Nrf2 Cancer Metabolic Disease
    Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2.
  • HY-137005
    CS1

    Topoisomerase Apoptosis Cancer
    CS1 is a potent DNA Topo II α inhibitor. CS1 displays broad-spectrum in vitro antitumor effects, low toxicity in vivo and potential anti-multidrug resistance capabilities. CS1 leads to DNA damage, cell cycle arrest at G2/M phase and apoptosis.
  • HY-147854
    B-Raf IN 9

    Raf Apoptosis Cancer
    B-Raf IN 9 (compound 8b) is a potent B-Raf inhibitor, with an IC50 of 24.79 nM. B-Raf IN 9 induces apoptosis and shows cell cycle arrest at G2/M phase. B-Raf IN 9 exhibits potent antitumor activity against human prostate cancer PC-3 cell line, with an IC50 of 7.83 µM.
  • HY-151799
    Antitumor agent-81

    E1/E2/E3 Enzyme Cancer
    Antitumor agent-81 (compound 5a) is a low cytotoxic P62-RNF168 agonist that promotes the interaction of P62 with RNF168. Antitumor agent-81 induces a decrease in RNF168-mediated H2A ubiquitination and impairs homologous recombination-mediated DNA repair. Antitumor agent-81 also inhibits mice xenograft tumor growth in a dose-dependent manner.
  • HY-144829
    PI3Kα-IN-5

    PI3K mTOR Cancer
    PI3Kα-IN-5 (Compound 6ab) is a potent PI3Kα inhibitor with an IC50 of 0.7 nM. PI3Kα-IN-5 shows antitumor activity with good metabolic stabilities and safety profiles.
  • HY-15259
    CP-640186

    Acetyl-CoA Carboxylase Metabolic Disease
    CP-640186 is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 can also stimulate muscle fatty acid oxidation.
  • HY-146289
    LXR antagonist 2

    LXR Metabolic Disease
    LXR antagonist 2 (compound 10rr) is a potent LXR (liver X receptor) inverse agonist, with IC50 values of 0.36 and 2.25 μM for LXRβ and LXRα, respectively. LXR antagonist 2 is a lipogenesis inhibitor through down-regulating LXR target genes SREBP-1c, ACC, FAS and SCD-1. LXR antagonist 2 shows lipid-lowering effects in mice with Triton WR-1339-induced hyperlipidemia.
  • HY-W011434
    Triglycidyl isocyanurate

    TGIC; Teroxirone

    MDM-2/p53 Apoptosis Cancer Inflammation/Immunology
    Triglycidyl isocyanurate (TGIC; Teroxirone) is a triazene triepoxide with antiangiogenic and antineoplastic activities. Triglycidyl isocyanurate inhibits the growth of non-small-cell-lung cancer cells via p53 activation. Triglycidyl isocyanurate induces cell apoptosis. Triglycidyl isocyanurate can be used for cancer research.
  • HY-143265
    Topoisomerase I inhibitor 2

    Topoisomerase Apoptosis Caspase Cancer
    Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect.
  • HY-146046
    Antitumor agent-56

    Apoptosis Cancer Inflammation/Immunology
    Antitumor agent-56 (Compound 33) is a triptolide derivative with antitumor, anti-inflammatory and NO release activities. Antitumor agent-56 significantly inhibits the growth of melanoma. Antitumor agent-56 is orally active.
  • HY-151156
    EGFR/HER2-IN-6

    EGFR Apoptosis Cancer
    EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer.
  • HY-14913
    Apricitabine

    SPD754; AVX754

    Nucleoside Antimetabolite/Analog HIV DNA/RNA Synthesis Infection
    Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection[2].
  • HY-146548
    Anticancer agent 43

    Apoptosis Bcl-2 Family Caspase PARP Cancer
    Anticancer Agent 43 is a potent anticancer agent. Anticancer Agent 43 induces apoptosis by caspase 3, PARP1, and Bax dependent mechanisms. Anticancer Agent 43 induces DNA damage.
  • HY-150026
    Multi-kinase-IN-2

    VEGFR PDGFR FGFR c-Kit Akt Src Apoptosis Cancer
    Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity.
  • HY-15259A
    CP-640186 hydrochloride

    Acetyl-CoA Carboxylase Metabolic Disease
    CP-640186 hydrochloride is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 hydrochloride can also stimulate muscle fatty acid oxidation.
  • HY-150027
    Multi-kinase-IN-3

    VEGFR PDGFR Cancer
    Multi-kinase-IN-3 (compound 2) is a potent angiokinase inhibitor. Multi-kinase-IN-3 shows inhibition activity against VEGFR-2 and PDGFRβ, with IC50 values of 58.3 and 55 nM, respectively.
  • HY-101021
    Ascochlorin

    Ilicicolin D

    STAT Apoptosis Antibiotic Cancer Inflammation/Immunology
    Ascochlorin (Ilicicolin D), an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. Ascochlorin induces apoptosis. Anti-inflammatory activity.
  • HY-145820
    Tubulin inhibitor 14

    Apoptosis Microtubule/Tubulin Cancer
    Tubulin inhibitor 14 is a potent NQO2 (quinone oxidoreductase 2) inhibitor with an IC50 of 1.0 μM. Tubulin inhibitor 14 also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. Tubulin inhibitor 14 is a microtubule-destabilizing agent with potential tumor-selectivity and antiangiogenic and vascular disrupting features.
  • HY-143241
    HDAC-IN-34

    HDAC MDM-2/p53 Apoptosis Cancer
    HDAC-IN-34 (compound 27) is a potent HDAC inhibitor, with IC50 values of 0.022 and 0.45 μM for HDAC1 and HDAC6, respectively. HDAC-IN-34 can bind to DNA and cause DNA damage. HDAC-IN-34 causes cells apoptosis through p53 signaling pathway. HDAC-IN-34 exhibits significant anti-proliferation effect against HCT-116 cells, with an IC50 of 1.41 μM.
  • HY-151161
    EGFR/HER2-IN-8

    EGFR Cancer
    EGFR/HER2-IN-8 (compound 34) is a EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-8 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.45, 0.244 and 5.669 μM, respectively. EGFR/HER2-IN-8 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer.
  • HY-147187
    MNK8

    STAT Apoptosis Bcl-2 Family Survivin Cancer
    MNK8 is a potent STAT3 (signal transducer and activator of transcription 3) inhibitor. MNK8 inhibits STAT3 activation and reduced its DNA binding ability. MNK8 shows good growth inhibition against hepatocellular carcinoma (HCC) cells. MNK8 induces apoptosis in HCC cells. MNK8 reduces prosurvival proteins expression and migration/invasion of HCC cells.
  • HY-150044
    Type II topoisomerase inhibitor 1

    DNA/RNA Synthesis Topoisomerase Bacterial Infection
    Type II topoisomerase inhibitor 1 is a potent and selective E. coli DNA gyrase inhibitor (IC50: 1.7 nM), and forms hydrogen bonds with Asp73 residue. Type II topoisomerase inhibitor 1 inhibits topoisomerase IV activity (IC50: 0.98 μM). Type II topoisomerase inhibitor 1 can be used in the research of antibacterial area.
  • HY-136348
    ML338

    Bacterial Infection
    ML338 is a selective small molecule inhibitor probe of non-replicating Mycobacterium tuberculosis bacilli and is against the non-replicating M. tuberculosis with IC90 and IC99 values of 1 μM and 4 μM, respectively by CFU. ML338 is a invaluable tool for identifying both essential functions and vulnerabilities of the M. tuberculosis bacilli in the nutrient deprivation states. ML338 can be used for the study of M. tuberculosis chemotherapy.
  • HY-133180
    YW1128

    Wnt β-catenin Metabolic Disease
    YW1128 (compound 3a) is a potent Wnt/β-Catenin inhibitor. YW1128 induces the proteasome degradation of β-catenin and subsequent inhibits the Wnt/β-catenin signaling in cells. YW1128 significantly decreases hepatic lipid accumulation. YW1128 improves glucose tolerance of high fat diet-fed mice without noticeable toxicity. YW1128 down regulates the genes involved in the glucose and fatty acid anabolism.
  • HY-14414
    GSK4112

    SR6452

    Apoptosis Metabolic Disease
    GSK4112 (SR6452) is a Rev-erbα agonist with an EC50 value of 0.4 μM. GSK4112 can be used as a chemical tool to probe the function of Rev-erbα in transcriptional repression, regulation of circadian biology, and metabolic pathways.
  • HY-146403
    Antibacterial agent 98

    Bacterial Infection
    Antibacterial agent 98 (compound g37) is a potent and orally active antibacterial agent. Antibacterial agent 98 inhibits the ATPase activity of Gyrase B and impairs Staphylococcus aureus (S. aureus ) DNA supercoiling. Antibacterial agent 98 shows antibacterial activity and not induce resistance development of MRSA (methicillin-resistant S. aureus).
  • HY-137506
    XST-14

    ULK p38 MAPK TGF-β Receptor Anaplastic lymphoma kinase (ALK) CaMK Apoptosis Cancer
    XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects.
  • HY-146314
    MAO-B-IN-9

    Monoamine Oxidase Amyloid-β Neurological Disease
    MAO-B-IN-9 (compound 16) is a potent, selective, BBB-penetrated, irreversible and time-dependent MAO-B (monoamine oxidase B) inhibitor, with an IC50 of 0.18 μM. MAO-B-IN-9 prevents Aβ1-42-induced neuronal cell death. MAO-B-IN-9 shows neuroprotective effects, which may be the result of its Aβ1-42 anti-aggregation effects.
  • HY-112764
    DMG-PEG 2000

    Others Metabolic Disease
    DMG-PEG 2000 is used for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG 2000 is also used for the lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles.
  • HY-151425
    TDO-IN-1

    Others Cancer
    TDO-IN-1 is an orally active and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), shows excellent selectivity over indoleamine-2,3-dioxygenase (IDO), with an IC50 value of 0.62 μM (IDO). TDO-IN-1 reverse the local immune tolerance of tumor tissue to inhibit tumor growth in vivo.
  • HY-147803
    TrxR-IN-5

    Reactive Oxygen Species Cancer
    TrxR-IN-5 (compound 4f) is a potent TrxR (thioredoxin reductase) inhibitor, with an IC50 of 0.16 μM. TrxR-IN-5 increases the levels of ROS, thus leading to potent antiproliferative effects. TrxR-IN-5 exhibits prominent anticacer and anti-metastasis effects.
  • HY-144725
    HDAC1/6-IN-1

    HDAC Apoptosis Cancer
    HDAC1/6-IN-1 (compound D7) is a potent multitarget inhibitor of GLP, HDAC6 and HDAC1, with IC50 values of 1.3, 13, and 89 nM, respectively. HDAC1/6-IN-1 can inhibit the methylation and deacetylation of H3K9 on protein level. HDAC1/6-IN-1 induces cancer cell apoptosis, G0/G1 cell cycle arrest, and blocks migration and invasion.
  • HY-146313
    BChE-IN-7

    Cholinesterase (ChE) Neurological Disease
    BChE-IN-7 (compound 13) is a potent, selective, BBB-penetrated and reversible AChE and BChE inhibitor, with an IC50 of 0.06 μM (BChE). BChE-IN-7 can protect neuronal-like cells from toxic Aβ-species.
  • HY-123611
    Supinoxin

    RX-5902

    DNA/RNA Synthesis Apoptosis Cancer
    Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM.
  • HY-143302
    Anticancer agent 31

    Others Cancer
    Anticancer agent 31 is a 1,3-diphenylurea quinoxaline derivative, and a anticancer agent. Anticancer agent 31 exhibits antitumor acitvity by arresting cell cycle at S phase and inducing apoptosis.
  • HY-14454
    TPh A

    Triphenyl Compound A

    Others Cancer
    TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells.
  • HY-111329
    JGB1741

    ILS-JGB-1741

    Sirtuin Apoptosis Cancer
    JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research.
  • HY-132302A
    Hu7691 free base

    Akt PKA PKC ROCK Ribosomal S6 Kinase (RSK) SGK Cancer
    Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
  • HY-132302
    Hu7691

    Akt PKA PKC ROCK Ribosomal S6 Kinase (RSK) SGK Cancer
    Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
  • HY-151257
    IHMT-MST1-58

    Hippo (MST) Metabolic Disease
    IHMT-MST1-58 is a potent, selective mammalian and orally active STE20-like protein 1 kinase (MST1) inhibitor with IC50 value of 23 nM. IHMT-MST1-58 can be used for the research of Type 1/2 diabetes.
  • HY-N0214A
    Peimisine hydrochloride

    Ebeiensine hydrochloride

    mAChR Angiotensin-converting Enzyme (ACE) Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Peimisine (Ebeiensine) hydrochloride is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine hydrochloride shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research.
  • HY-N0214
    Peimisine

    Ebeiensine

    mAChR Angiotensin-converting Enzyme (ACE) Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Peimisine (Ebeiensine) is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research.
  • HY-B0402A
    Amantadine hydrochloride

    1-Adamantanamine hydrochloride; 1-Adamantylamine hydrochloride; 1-Aminoadamantane hydrochloride

    Influenza Virus Orthopoxvirus SARS-CoV Apoptosis Bcl-2 Family CDK Cancer Infection Neurological Disease
    Amantadine (1-Adamantanamine) hydrochloride is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine hydrochloride inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine hydrochloride also has anti-orthopoxvirus and anticancer activity. Amantadine hydrochloride can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.
  • HY-B0402
    Amantadine

    1-Adamantanamine; 1-Aminoadamantane

    Influenza Virus Orthopoxvirus SARS-CoV Apoptosis CDK Bcl-2 Family Cancer Infection Neurological Disease
    Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.
  • HY-B0402B
    Amantadine sulfate

    1-Adamantanamine sulfate; 1-Aminoadamantane sulfate

    Influenza Virus Orthopoxvirus SARS-CoV Apoptosis CDK Bcl-2 Family Cancer Infection Neurological Disease
    Amantadine (1-Adamantanamine) sulfate is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine sulfate inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine sulfate also has anti-orthopoxvirus and anticancer activity. Amantadine sulfate can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.
  • HY-14543
    Sertindole

    Lu 23-174

    5-HT Receptor Dopamine Receptor Adrenergic Receptor Autophagy Neurological Disease Cancer
    Sertindole (Lu 23-174) is an orally active 5-HT2A, 5-HT2C, dopamine D2, and αl-adrenergic receptors antagonist. Sertindole shows antipsychotic activity and anti-proliferative activity to multiple cancer cells.