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Targets Recommended: Adenylate Cyclase Guanylate Cyclase

Results for "Adenylate cyclase in vivo Inhibitors" in MCE Product Catalog:

937

Inhibitors & Agonists

4

Dye Reagents

1

Biochemical Assay Reagents

42

Peptides

1

Inhibitory Antibodies

52

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-101862
    CB-7921220

    Adenylate Cyclase Neurological Disease Cardiovascular Disease
    CB-7921220 is an adenylate cyclase inhibitor.
  • HY-100396
    SQ22536

    Adenylate Cyclase Metabolic Disease
    SQ22536 is an effective adenylate cyclase (AC) inhibitor.
  • HY-112270
    Glutaminyl Cyclase Inhibitor 2

    Amyloid-β Neurological Disease
    Glutaminyl Cyclase Inhibitor 2 is a glutaminyl cyclase inhibitor with an IC50 of 1.23 μM.
  • HY-112269
    Glutaminyl Cyclase Inhibitor 1

    Amyloid-β Neurological Disease
    Glutaminyl Cyclase Inhibitor 1 is a glutaminyl cyclase inhibitor with an IC50 of 0.5 μM.
  • HY-126331
    Glutaminyl Cyclase Inhibitor 4

    Amyloid-β Neurological Disease
    Glutaminyl Cyclase Inhibitor 4 (compound 90) is a potent, selective glutaminyl cyclase (QC) inhibitor with an IC50 of 6.1 nM. Glutaminyl Cyclase Inhibitor 4 is a potent anti-Alzheimer’s agent.
  • HY-101282
    Glutaminyl Cyclase Inhibitor 3

    Amyloid-β Neurological Disease
    Glutaminyl Cyclase Inhibitor 3 (compound 212 ), a designed anti-Alzheimer’s compound, is a potent human Glutaminyl Cyclase (GC) inhibitor, with an IC50 of 4.5 nM. Glutaminyl Cyclase-IN-1 (compound 212) significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions.
  • HY-127137
    Adenylosuccinic acid

    Adenylosuccinate; Aspartyl Adenylate

    Endogenous Metabolite Metabolic Disease
    Adenylosuccinic acid (Adenylosuccinate; Aspartyl adenylate) is a purine ribonucleoside monophosphate and plays a role in nucleotide cycle metabolite. Adenylosuccinic acid can be converted into fumaric acid through adenylosuccinate lyase. Adenylosuccinic acid has the potential for the study of duchenne muscular dystrophy(DMD).
  • HY-P0004
    Lysipressin

    Lysine vasopressin; [Lys8]-Vasopressin

    Others Others
    Lysipressin is Antidiuretic hormone that have been found in pigs and some marsupial families. Induces contraction of the rabbit urinary bladder smooth muscle, activate adenylate-cyclase.
  • HY-103193
    NKH477

    Colforsin dapropate hydrochloride

    Adenylate Cyclase Cardiovascular Disease
    NKH477 (Colforsin dapropate hydrochloride) is a novel water-soluble forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts.
  • HY-P1495
    Small Cardioactive Peptide B SCPB

    Adenylate Cyclase Neurological Disease Cardiovascular Disease
    Small Cardioactive Peptide B (SCPB), a neurally active peptide, stimulates adenylate cyclase activity in particulate fractions of both heart and gill tissues with EC50s of 0.1 and 1.0 μM, respectively.
  • HY-15371
    Forskolin

    Coleonol; Colforsin

    Adenylate Cyclase FXR Autophagy Cancer Endocrinology Metabolic Disease Inflammation/Immunology
    Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.
  • HY-W010791
    Adenosine 5'-diphosphate sodium salt

    Endogenous Metabolite Others
    Adenosine 5'-diphosphate (ADP) sodium salt is a nucleoside diphosphate, which is the product of ATP dephosphorylation by ATPases. Adenosine 5'-diphosphate sodium salt induces human platelet aggregation and inhibits stimulated adenylate cyclase by an action at P2T-purinoceptors.
  • HY-W010918
    Adenosine 5'-diphosphate

    Adenosine diphosphate; ADP

    Endogenous Metabolite Others
    Adenosine 5'-diphosphate (Adenosine diphosphate) is a nucleoside diphosphate. Adenosine 5'-diphosphate is the product of ATP dephosphorylation by ATPases. Adenosine 5'-diphosphate induces human platelet aggregation and inhibits stimulated adenylate cyclase by an action at P2T-purinoceptors.
  • HY-135878
    2',5'-Dideoxyadenosine

    Adenylate Cyclase Adrenergic Receptor Metabolic Disease
    2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor via binding the P-site with an IC50 of 3 µM . 2',5'-Dideoxyadenosine is a nucleoside analog and exerts a potent antiadrenergic action in heart.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-116175
    BIBB 515

    Others Metabolic Disease
    BIBB 515 is a potent, selective and orally active 2,3-oxidosqualene cyclase (OSC) inhibitor with ED50 values of 0.2-0.5 mg/kg and 0.36-33.3 mg/kg in rats and mice (1-5 hours), respectively. BIBB 515 exerts lipid-lowering effect mainly by inhibiting the production of low-density lipoprotein (LDL).
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-117318
    PDE12-IN-1

    Phosphodiesterase (PDE) Infection
    PDE12-IN-1 is a potent and selective PDE12 inhibitor with a pIC50 value for enzyme inhibition of 9.1. PDE12-IN-1 increases 2′,5′-linked adenylate polymers (2-5A) levels, and the pEC50 value is 7.7. PDE12-IN-1 shows antiviral activity.
  • HY-103195
    NKY80

    Adenylate Cyclase Metabolic Disease
    NKY80 is a potent, selective and non-competitive adenylyl cyclase (AC) type V isoform inhibitor with IC50s of 8.3 µM, 132 µM and 1.7 mM for type V, III and II, respectively. NKY80 is a non-nucleoside quinazolinone and regulates the AC catalytic activity in heart and lung tissues.
  • HY-112461A
    NF449 octasodium

    P2X Receptor Cardiovascular Disease
    NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a G-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs.
  • HY-112860
    Asp-AMS

    Aminoacyl-tRNA Synthetase Mitochondrial Metabolism Metabolic Disease
    Asp-AMS, an analogue of aspartyl-adenylate, is an aspartyl-tRNA synthetase inhibitor and also a strong competitive inhibitor of the mitochondrial enzyme.
  • HY-100524
    LRE1

    Adenylate Cyclase Cancer
    LRE1 is a specific and allosteric inhibitor of soluble adenylyl cyclase.
  • HY-125851
    TGFβRI-IN-2

    ALK Inflammation/Immunology
    TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.
  • HY-12376
    BAY 41-2272

    Guanylate Cyclase Inflammation/Immunology
    BAY 41-2272 is a soluble guanylate cyclases (sGC) activator.
  • HY-100295
    (4-Acetamidocyclohexyl) nitrate

    BM121307

    Guanylate Cyclase Cardiovascular Disease
    (4-Acetamidocyclohexyl) nitrate (BM121307) is a guanylate cyclase activator.
  • HY-18630A
    Ro 48-8071 fumarate

    Others Cancer
    Ro 48-8071 fumarate is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM.
  • HY-16774
    Vericiguat

    BAY1021189

    Guanylate Cyclase Cardiovascular Disease
    Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator.
  • HY-14181
    Cinaciguat

    BAY 58-2667

    Guanylate Cyclase Cardiovascular Disease
    Cinaciguat is an activator of guanylate cyclase (sGC), and used for acute decompensated heart failure.
  • HY-18630
    Ro 48-8071

    Others Cancer
    Ro 48-8071 is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM.
  • HY-14181A
    Cinaciguat hydrochloride

    BAY 58-2667 hydrochloride

    Guanylate Cyclase Cardiovascular Disease
    Cinaciguat hydrochloride is a potent soluble guanylate cyclase (GC) activator with EC50 of 15 nM in platelets.
  • HY-14779
    Riociguat

    BAY 632521

    Guanylate Cyclase Cardiovascular Disease
    Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-P0252
    α-Melanocyte-Stimulating Hormone (MSH), amide

    Adenylate Cyclase Metabolic Disease
    α-Melanocyte-Stimulating Hormone (MSH), amide stimulates melanocortin 1 receptor that results in the activation of adenylyl cyclase.
  • HY-78237
    Nelociguat

    BAY60-4552

    Guanylate Cyclase Cardiovascular Disease
    Nelociguat (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator.
  • HY-101279
    ST034307

    Adenylate Cyclase Neurological Disease
    ST034307 is a potent and selective adenylyl cyclase 1 (AC1) inhibitor, with IC50 of 2.3 μM.
  • HY-14927
    Lificiguat

    YC-1

    Guanylate Cyclase Cancer
    Lificiguat binds to the β subunit of soluble guanylyl cyclase(sGC) with Kd of 0.6-1.1 μM in the presence of CO.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-N6828
    Monocrotaline N-Oxide

    Others Metabolic Disease
    Monocrotaline N-Oxide, a monocrotaline metabolite, leads to DNA adduct formation in vivo.
  • HY-135985
    DCLK1-IN-1

    Others Cancer
    DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1 + pancreatic ductal adenocarcinoma (PDAC).
  • HY-17584
    Linaclotide

    Guanylate Cyclase Others
    Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
  • HY-117962A
    BI 703704

    Guanylate Cyclase Metabolic Disease
    BI 703704 is a potent soluble guanylate cyclase (sGC) activator. BI 703704 inhibits the progression of diabetic nephropathy in the ZSF1 rat.
  • HY-111926
    N6-Methyladenosine 5'-monophosphate disodium salt

    Others Metabolic Disease
    N6-Methyladenosine 5'-monophosphate disodium salt is an activator of glycogen phosphorylase b, with a Ka value of 22 µM. N6-Methyladenosine 5'-monophosphate disodium salt is a non-competitive rat adenylate kinase II inhibitor.
  • HY-32342
    Falecalcitriol

    VD/VDR Metabolic Disease
    Falecalcitriol(Fulstan; Hornel) is an analog of calcitriol; has a higher potency both in vivo and in vitro systems, and longer duration of action in vivo.
  • HY-103410
    Carmoxirole hydrochloride

    EMD 45609 hydrochloride

    Dopamine Receptor Cardiovascular Disease
    Carmoxirole hydrochloride (EMD 45609 hydrochloride) is a selective, peripherally acting dopamine D2 receptor agonist and exhibits antihypertensive activities in vivo.
  • HY-101255
    ODQ

    Guanylate Cyclase Apoptosis Cancer
    ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells.
  • HY-109066
    Olinciguat

    IW-1701

    Guanylate Cyclase Cardiovascular Disease
    Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay.
  • HY-13452
    CID-1067700

    ML282

    Ras Inflammation/Immunology
    CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM.
  • HY-N2843
    α-Amyrin palmitate

    Others Inflammation/Immunology
    α-Amyrin palmitate is isolated from Santalum album (sandalwood). α-Amyrin palmitate can be used for the study of arthritis in vivo.
  • HY-109136
    Runcaciguat

    Guanylate Cyclase Cardiovascular Disease
    Runcaciguat is an orally active stimulator of soluble guanylate cyclase, and is used in the research of cardiovascular and renal diseases combined with selective partial adenosine A1 receptor agonists.
  • HY-N2299
    Morusinol

    Others Cardiovascular Disease
    Morusinol is a flavonoid isolated from Morus alba root bark. Morusinol has an antiplatelet activity and  significantly inhibits arterial thrombosis in vivo.
  • HY-U00160
    SP187

    MON-​DNJ; UV4

    Influenza Virus Infection
    SP187 is a host-targeted iminosugar with activity against filovirus infections in vitro and in vivo. SP187 is active against influenza and dengue in vivo.
  • HY-19373
    RWJ-445167

    3DP-10017

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

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-108741A
    Plecanatide acetate

    Guanylate Cyclase Inflammation/Immunology
    Plecanatide acetate is a guanylate cyclase-C (GC-C) receptor agonist, with an EC50 of 190 nM in T84 cells. Plecanatide acetate shows anti-inflammatory activity in models of murine colitis.
  • HY-115687
    PDE4B-IN-2

    Phosphodiesterase (PDE)
    PDE4B-IN-2 is an orally active and selective PDE4B inhibitor (IC50=15 nM) and exhibits >100-fold selectivity for PDE4B over 4D. PDE4B-IN-2 regulates cAMP in inflammatory cells and inhibits LPS-induced TNF-α production and neutrophil accumulation in mouse lungs. PDE4B-IN-2 reduces microglial and neutrophil activation, and improves behavioral deficits in a traumatic brain injury model in vivo. PDE4B-IN-2 also exhibits antidepressant-like effects.
  • HY-126245
    Keap1–Nrf2-IN-1

    Keap1-Nrf2 Metabolic Disease Inflammation/Immunology
    Keap1–Nrf2 IN-1 (compound35) is a Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) protein-protein interaction inhibitor, and with an IC50 of 43 nM for Keap1 protein. Keap1–Nrf2 IN-1 (compound35) activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models.
  • HY-119173
    PBD-150

    Amyloid-β Neurological Disease
    PBD-150 is a human glutaminyl cyclase (hQC) Y115E-Y117E variant inhibitor, with a Ki value of 490 nM.
  • HY-111516
    MGV354

    Guanylate Cyclase Inflammation/Immunology Cardiovascular Disease
    MGV354 is a soluble guanylate cyclase (sGC) activator with EC50s of <0.5 nM, and 5 nM in CHO and GTM-3 E cells, respectively.
  • HY-U00176
    Org30958

    Aromatase Metabolic Disease
    Org30958 is a potent aromatase inhibitor in vivo.
  • HY-119307
    Apratastat

    MMP TNF Receptor Cancer
    Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) . Apratastat can potently inhibit the release of TNF-α in vitro, ex vivo, and in vivo with IC50s of 144 ng/mL in vitro and 81.7 ng/mL ex vivo, respectively.
  • HY-B1132
    Clidinium bromide

    Ro 2-3773

    mAChR Neurological Disease
    Clidinium bromide is a quaternary amine antimuscarinic agent. Clidinium bromide may help symptoms of cramping and abdominal/stomach pain by decreasing stomach acid, and slowing the intestines in vivo.
  • HY-128366
    Waltonitone

    Apoptosis Cancer
    Waltonitone is a ursane-type pentacyclic triterpene isolated from Gentian waltonii Burkill. Waltonitone significantly inhibits hepatocellular carcinoma cells growth and induces apoptosis in vitro and in vivo.
  • HY-P1067A
    Enterostatin(human,mouse,rat) TFA

    Endogenous Metabolite Metabolic Disease
    Enterostatin (human,mouse,rat) TFA is a pentapeptide mainly formed in the intestine by the cleavage of secreted pancreatic procolipase. Enterostatin  selectively reduces fat intake, bodyweight, and body fat in vivo.
  • HY-126301
    DMT1 blocker 1

    Others Inflammation/Immunology
    DMT1 blocker 1 is a blocker of divalent metal transporter 1 (DMT1) with an IC50 of 0.64 μM, is expected to block iron uptake by enterocytes in vivo.
  • HY-N2542
    Tubeimoside III

    Others Cancer Inflammation/Immunology
    Tubeimoside III, a triterpenoid saponin isolated from a Chinese folk medicine"Tubeimu", shows anti-inflammatory, anti-tumor, anti-tumorigenic activities, and acute toxicity in vivo.
  • HY-136647
    8-Bromoadenosine 5'-triphosphate tetrasodium

    8-Br-ATP tetrasodium

    Others Others
    8-Bromoadenosine 5'-triphosphate tetrasodium (8-Br-ATP tetrasodium) is an ATP analogue. ATP is a central component of energy storage and metabolism in vivo.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

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

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-N0208
    Kaempferol-3-O-glucorhamnoside

    p38 MAPK NF-κB Inflammation/Immunology
    Kaempferol-3-O-glucorhamnoside, a flavonoid derived from plant Thesium chinense Turcz, inhibits inflammatory responses via MAPK and NF-κB pathways in vitro and in vivo.
  • HY-126302
    DMT1 blocker 2

    Others Inflammation/Immunology
    DMT1 blocker 2, Compound 12f, is a direct inhibitor of divalent metal transporter 1 (DMT1) with an IC50 of 0.83 μM, is expected to block iron uptake by enterocytes in vivo.
  • HY-19095
    TNP-351

    Antifolate Cancer
    TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-135655A
    SPR720

    pVXc-486

    Bacterial Infection
    SPR720 (pVXc-486) is an orally active and potent phosphate prodrug of SPR719 (VXc-486; HY-12930). SPR720 has potent bactericidal activities in vivo.
  • HY-120085
    PFE-360

    PF-06685360

    LRRK2 Neurological Disease
    PFE-360 (PF-06685360) is a potent, selective, brain penetrated and orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor with a mean IC50 of 2.3 nM in vivo.
  • HY-P1418
    DPC-AJ1951

    Thyroid Hormone Receptor Endocrinology
    DPC-AJ1951, a 14 amino acid peptide that acts as a potent agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR) , and characterized its activity in ex vivo and in vivo assays of bone resorption.
  • HY-100080
    A-887826

    Sodium Channel Neurological Disease
    A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo.
  • HY-117962
    (Rac)-BI 703704

    Guanylate Cyclase Metabolic Disease
    (Rac)-BI 703704 is a potent soluble guanylyl cyclase (sGC) activator. (Rac)-BI 703704 reduces progression of renal damage in the ZSF1 rat, and highlight the potential of sGC activation as an effective therapy for diabetic nephropathy.
  • HY-117917
    (Rac)-MGV354

    Guanylate Cyclase Inflammation/Immunology Cardiovascular Disease
    (Rac)-MGV354 is the racemate of MGV354. MGV354 is a soluble guanylate cyclase (sGC) activator with EC50s of <0.5 nM, and 5 nM in CHO and GTM-3 E cells, respectively.
  • HY-P1418A
    DPC-AJ1951 TFA

    Thyroid Hormone Receptor Endocrinology
    DPC-AJ1951 TFA, a 14 amino acid peptide that acts as a potent agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR) , and characterized its activity in ex vivo and in vivo assays of bone resorption.
  • HY-N0212
    Peimine

    Verticine; Dihydroisoimperialine

    Others Inflammation/Immunology
    Peimine(Dihydroisoimperialine; Verticine) is a natural compound with good anti-inflammatory effects in vivo.
  • HY-90003A
    Tianeptine sodium salt

    5-HT Receptor Neurological Disease
    Tianeptine sodium salt is a selective facilitator of 5-HT uptake in vitro and in vivo.
  • HY-90003
    Tianeptine

    5-HT Receptor Neurological Disease
    Tianeptine is a selective facilitator of 5-HT uptake in vitro and in vivo.
  • HY-135655
    SPR720 disodium

    pVXc-486 disodium

    Bacterial Infection
    SPR720 disodium (pVXc-486 disodium) is an orally active and potent phosphate prodrug of SPR719 (VXc-486; HY-12930). SPR720 disodium has potent bactericidal activities in vivo.
  • HY-W012982
    3-Amino-2-oxazolidinone

    AOZ

    Endogenous Metabolite Metabolic Disease
    3-Amino-2-oxazolidinone (AOZ) is the metabolite of Furazolidone (HY-B1336). 3-Amino-2-oxazolidinone is always be detected as a indicator of furazolidone residues in vivo.
  • HY-129997
    Luteolinidin chloride

    Others Inflammation/Immunology
    Luteolinidin is a natural deoxyanthocyanidin, isolated from mosses and ferns. Luteolinidin is a potent CD38 inhibitor which can protect the heart against I/R injury with preservation of eNOS function and prevention of endothelial dysfunction in vivo.
  • HY-76006
    3-Hydroxybenzaldehyde

    Aldehyde Dehydrogenase (ALDH) Cardiovascular Disease
    3-Hydroxybenzaldehyde is a precursor compound for phenolic compounds, such as Protocatechualdehyde (HY-N0295). 3-Hydroxybenzaldehyde is a substrate of aldehyde dehydrogenase (ALDH) in rats and humans (ALDH2). 3-Hydroxybenzaldehyde has vasculoprotective effects in vitro and in vivo.
  • HY-N0511
    Aristolochic acid B

    Others Cancer
    Aristolochic acid B is one of the major components of Aristolochic acids (AA) which are natural products derived from taxa in the Aristolochiaceae. Aristolochic acid is known to be a potent mutagen and carcinogen. Aristolochic acid B showes more carcinogenic risk than Aristolochic acid A in vivo.
  • HY-101277
    Vadadustat

    PG-1016548; AKB-6548

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    Vadadustat (PG-1016548) is a titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor. Vadadustat is an erythropoiesis-stimulating agent and has the potential for anemia treatment in chronic kidney disease in vivo.
  • HY-N0823
    Lithospermic acid

    (+)-Lithospermic acid

    Others Inflammation/Immunology
    Lithospermic acid ((+)-Lithospermic acid) is a plant-derived polycyclic phenolic carboxylic acid isolated from Salvia miltiorrhiza, and has the anti-oxidative and hepatoprotective activity on carbon tetrachloride (CCl4)-induced acute liver damage in vitro and in vivo.
  • HY-B0332
    Menadione

    Vitamin K3

    Endogenous Metabolite Others
    Menadione, a synthetic naphthoquinone, can be converted to active vitamin K2 in vivo.
  • HY-109039
    Praliciguat

    IW-1973

    Guanylate Cyclase Cardiovascular Disease
    Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase stimulator, enhances NO signaling, acts as a vasodilator. Praliciguat (IW-1973) stimulates sGC in HEK-293 cells with an EC50 of 197 nM.
  • HY-108697
    PT2399

    HIF/HIF Prolyl-Hydroxylase Cancer
    PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo.
  • HY-122661
    Mefuparib hydrochloride

    MPH

    PARP Apoptosis Cancer
    Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo.
  • HY-135299
    CH6953755

    Src Cancer
    CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo.
  • HY-103194
    KH7

    Others Others
    KH7 is a soluble adenylyl cyclase (sAC)-specific inhibitor, with IC50s of 3-10 μM toward both recombinant purified human sACt protein and heterologously expressed sACt in cellular assays. KH7 is also a cAMP inhibitor.
  • HY-113926
    BAY 60-2770

    Guanylate Cyclase Cardiovascular Disease
    BAY 60-2770 is a potent, selective, and orally active soluble guanylyl cyclase (sGC) activator. BAY 60-2770 increases the activity of sGC in a nitric oxide-independent manner. BAY 60-2770 shows antifibrotic effect.
  • HY-P1179
    Guanylin(human)

    Guanylate Cyclase Endogenous Metabolite Cancer Endocrinology
    Guanylin(human), a 15-amino acid peptide, is an endogenous intestinal guanylate cyclase activator. Guanylin(human) is mainly found in gastrointestinal tract which regulates electrolytead water transport in intestinal and renal epithelia through cyclic GMP-dependent mechanism.
  • HY-101407
    Nicotinamide N-oxide

    CXCR Drug Metabolite Endogenous Metabolite Inflammation/Immunology Endocrinology
    Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.
  • HY-N6872
    Actein

    JNK Akt Apoptosis Autophagy Cancer
    Actein is a triterpene glycoside isolated from the rhizomes of Cimicifuga foetida. Actein suppresses cell proliferation, induces autophagy and apoptosis through promoting ROS/JNK activation, and blunting AKT pathway in human bladder cancer. Actein has little toxicity in vivo.
  • HY-117832
    Pyripyropene A

    Acyltransferase Infection Inflammation/Immunology Cardiovascular Disease
    Pyripyropene A is a potent and selective sterol O-acyltransferase 2 (SOAT2)/acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2) inhibitor, with an IC50 of 0.07 µM. Pyripyropene A attenuates hypercholesterolemia and atherosclerosis in vivo.
  • HY-112711
    LV-320

    Autophagy Cathepsin Cancer
    LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5 µM and a Kd of 16 µM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo.
  • HY-103460
    IRL 2500

    Endothelin Receptor Cardiovascular Disease
    IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-P1319
    Nociceptin(1-7)

    Opioid Receptor Inflammation/Immunology
    Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo.
  • HY-13055B
    Telotristat

    LP-778902

    Tryptophan Hydroxylase Neurological Disease
    Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM.
  • HY-19147
    BMY-43748

    Bacterial Infection
    BMY-43748 is a promising antibacterial agent, exhibiting great in vitro and in vivo antibacterial activity.
  • HY-P1184
    HNGF6A

    Reactive Oxygen Species Metabolic Disease Neurological Disease Cardiovascular Disease
    HNGF6A is a humanin analogue. HNGF6A increases glucose-stimulated insulin secretion and glucose metabolism, and has the potential for diabetes research. HNGF6A inhibits of ROS production during oxidative stress. HNGF6A can prevent endothelial dysfunction and atherosclerosis in vivo.
  • HY-130243
    RORγt Inverse agonist 6

    ROR Inflammation/Immunology
    RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the treatment of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.
  • HY-W005288
    4-Vinylphenol

    Apoptosis Endogenous Metabolite Cancer
    4-Vinylphenol is found in the medicinal herb Hedyotis diffusa Willd, wild rice and is also the metabolite of p-coumaric and ferulic acid by lactic acid bacteria in wine. 4-Vinylphenol induces apoptosis and inhibits blood vessels formation and suppresses invasive breast tumor growth in vivo.
  • HY-103583
    KDU731

    PI4K Parasite Infection
    KDU731, an orally active C. parvum PI4K inhibitor with an IC50 value of 25 nM, blocks Cryptosporidium infection in vitro and in vivo. KDU731 is a promising drug candidate for the treatment of diarrhea caused by Cryptosporidium and meets a broad range of safety.
  • HY-P1179A
    Guanylin(human) TFA

    Guanylate Cyclase Endogenous Metabolite
    Guanylin(human) TFA, a 15-amino acid peptide, is an endogenous intestinal guanylate cyclase activator. Guanylin(human) TFA is mainly found in gastrointestinal tract which regulates electrolytead water transport in intestinal and renal epithelia through cyclic GMP-dependent mechanism.
  • HY-123820
    LY3020371 hydrochloride

    mGluR Neurological Disease
    LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM. LY3020371 hydrochloride exerts an antidepressant-like signature in vivo.
  • HY-13741
    RH1

    NSC 697726

    Others Cancer
    RH1 (NSC 697726) is a potent bioreductive agent with profound anti-cancer activity in vitro and in vivo.
  • HY-114157
    DO-264

    MAGL Neurological Disease
    DO-264 is a selective and in vivo-active inhibitor of Abhydrolase Domain Containing 12 (ABHD12), with an IC50 of 11 nM.
  • HY-N0189
    Aloe emodin

    Rhabarberone; 3-Hydroxymethylchrysazine

    Autophagy Cancer
    Aloe emodin is a hydroxyanthraquinone present in Aloe vera leaves, has a specific in vitro and in vivo antitumor activity.
  • HY-N0104
    Curcumol

    (-)-Curcumol

    Apoptosis Cancer
    Curcumol is a sesquiterpene originally isolated from curcuma rhizomes; shows anticancer activities both in vitro and in vivo.
  • HY-13965
    Parmodulin 2

    ML161

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.
  • HY-P1319A
    Nociceptin(1-7) TFA

    Opioid Receptor Inflammation/Immunology
    Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo.
  • HY-135368
    8pyDTZ

    Others Others
    8pyDTZ is a pyridyl diphenylterazine (DTZ) analog and an ATP-independent pyridyl substrate of LumiLuc luciferase. 8pyDTZ exhibits spectrally shifted emission and improved water solubility. 8pyDTZ has excellent biocompatibility and superior in vivo sensitivity. 8pyDTZ can be used for in vivo luminescence imaging.
  • HY-P1028
    Hexa-D-arginine

    Furin inhibitor II

    Others Infection
    Hexa-D-arginine (Furin Inhibitor II) is a stable furin inhibitor with Ki values 106 nM, 580 nM and 13.2 μM for furin, PACE4 and prohormone convertase-1 (PC1), respectively. Hexa-D-arginine blocks Pseudomonas exotoxin A and anthrax toxins toxicity in vitro and in vivo.
  • HY-100167
    TAK-778

    Others Cancer
    TAK-778 is a derivative of ipriflavone and has been shown to induce bone growth in in vitro and in vivo models.
  • HY-W010104A
    Methionine sulfoxide

    Endogenous Metabolite Metabolic Disease
    Methionine sulfoxide is an oxidation product of methionine with reactive oxygen species and can be regarded as a biomarker of oxidative stress in vivo.
  • HY-10498
    Lexibulin

    CYT-997

    Microtubule/Tubulin Reactive Oxygen Species Apoptosis Cancer
    Lexibulin (CYT-997) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Lexibulin induces cell apoptosis and induces mitochondrial ROS generation in GC cells.
  • HY-B1751D
    Quinidine sulfate dihydrate

    Cytochrome P450 Cancer
    Quinidine sulfate dihydrate is a potent and selective inhibitor of cytochrome P450db and inhibits amphetamine metabolism in vivo. Quinidine sulfate dihydrate enhances the cytotoxicity of vincristine (VCR) in tumor cells and especially in VCR-resistant sublines of P388 leukemia (P388/VCR) and human myelogenous leukemia.
  • HY-10498A
    Lexibulin dihydrochloride

    CYT-997 dihydrochloride

    Microtubule/Tubulin Reactive Oxygen Species Apoptosis Cancer
    Lexibulin dihydrochloride (CYT-997 dihydrochloride) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Lexibulin dihydrochloride induces cell apoptosis and induces mitochondrial ROS generation in GC cells.
  • HY-111793
    NUCC-390

    CXCR Neurological Disease
    NUCC-390 is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046). NUCC-390 promotes nerve recovery of function after neurodegeneration in vivo.
  • HY-P1184A
    HNGF6A TFA

    Reactive Oxygen Species Metabolic Disease Neurological Disease Cardiovascular Disease
    HNGF6A TFA is a humanin analogue. HNGF6A TFA increases glucose-stimulated insulin secretion and glucose metabolism, and has the potential for diabetes research. HNGF6A TFA inhibits of ROS production during oxidative stress. HNGF6A TFA can prevent endothelial dysfunction and atherosclerosis in vivo.
  • HY-14282
    Lanoconazole

    Fungal Infection Inflammation/Immunology
    Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo. Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis.
  • HY-50514
    AT9283

    JAK Aurora Kinase Bcr-Abl FLT3 Apoptosis Autophagy Cancer
    AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo.
  • HY-103430
    SKF-83566 hydrobromide

    Dopamine Receptor Neurological Disease
    SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active dopamine D1/D5 receptor antagonist. SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM and attenuates cocaine effects in vivo.
  • HY-103355
    YM022

    CCR Metabolic Disease
    YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo.
  • HY-111793A
    NUCC-390 dihydrochloride

    CXCR Neurological Disease
    NUCC-390 dihydrochloride is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 dihydrochloride induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046). NUCC-390 dihydrochloride promotes nerve recovery of function after neurodegeneration in vivo.
  • HY-111551
    FT113

    Fatty Acid Synthase (FASN) Cancer
    FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC50 of 213 nM for full-length recombinant human FASN enzyme. In cell-based assay, FT113 blocks FASN activity in BT474 cells (IC50, 90 nM). FT113 shows anti-proliferative activity, and exhibits anti-cancer activity both in vitro and in vivo.
  • HY-101918
    DS-1040 Tosylate

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

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-A0024
    Tolterodine

    (R)-(+)-Tolterodine; (+)-Tolterodine; (R)-Tolterodine; PNU-200583

    mAChR Neurological Disease
    Tolterodine(PNU-200583) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo.
  • HY-18754
    FR 167653 free base

    p38 MAPK Autophagy Endocrinology
    FR 167653 free base, an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 free base is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo.
  • HY-129491
    O-Desmethyl Midostaurin

    CGP62221; O-Desmethyl PKC412

    PKC Cancer
    O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo. Midostaurin is a multi-targeted protein kinase inhibitor with IC50 ranging from 22-500 nM.
  • HY-18619
    YL-109

    Others Cancer
    YL-109 is a novel anticancer agent which has ability to inhibit breast cancer cell growth and invasiveness in vitro and in vivo.
  • HY-B2176
    ATP

    Adenosine 5'-triphosphate

    Endogenous Metabolite Inflammation/Immunology
    ATP is a central component of energy storage and metabolism in vivo, provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells.
  • HY-123522
    PAT-048

    Phosphodiesterase (PDE) Inflammation/Immunology
    PAT-048 is a potent, selective and orally active autotaxin inhibitor, inhibits IL-6 mRNA expression, but shows no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in lung fibrosis model. PAT-048 shows an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma. PAT-048 reduces dermal fibrosis in vivo.
  • HY-12680
    PRN694

    Itk Inflammation/Immunology
    PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo.
  • HY-18754A
    FR 167653

    FR 167653 sulfate

    p38 MAPK Autophagy Endocrinology
    FR 167653 (FR 167653 sulfate), an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 (FR 167653 sulfate) is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo.
  • HY-N7395
    Cyclic ADP-​ribose

    cADPR

    Calcium Channel TRP Channel Endogenous Metabolite Infection Endocrinology Inflammation/Immunology Neurological Disease Cardiovascular Disease
    Cyclic ADP-ribose (cADPR) is a potent second messenger for calcium mobilization that is synthesized from NAD + by a ADP-ribosyl cyclase. Cyclic ADP-ribose increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels.
  • HY-P1852
    TIP 39, Tuberoinfundibular Neuropeptide

    Adenylate Cyclase Neurological Disease
    TIP 39, Tuberoinfundibular Neuropeptide is a neuropeptide and parathyroid hormone 2 receptor (PTH2R) agonist. TIP 39 is highly conserved among species. TIP39 from all species activates adenylyl cyclase and elevates intracellular calcium levels through parathyroid hormone 2 receptor (PTH2R).
  • HY-W010735
    ATP disodium salt hydrate

    Adenosine 5'-triphosphate disodium salt hydrate

    Endogenous Metabolite Inflammation/Immunology
    ATP disodium salt hydrate is a central component of energy storage and metabolism in vivo, provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells.
  • HY-101757
    NO-prednisolone

    NCX-1015

    Interleukin Related Inflammation/Immunology
    NO-prednisolone is a nitric oxide (NO)-releasing derivative of Prednisolone. NO-prednisolone potently stimulates IL-10 production in vivo.
  • HY-10294
    Relacatib

    SB-462795

    Cathepsin Cancer Metabolic Disease
    Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo.
  • HY-B1339
    Dicyclomine hydrochloride

    Dicycloverine hydrochloride

    mAChR Neurological Disease
    Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo.
  • HY-16312
    MDL-29951

    iGluR Neurological Disease
    MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [ 3H]glycine binding in vitro and in vivo.
  • HY-16672
    AVX 13616

    Bacterial Infection
    AVX 13616 shows the potent in vivo antibacterial activity of Avexa’s lead antibacterial candidate; particularly against drug-resistant Staphylococcus pathogens.
  • HY-101727
    Nexopamil racemate

    Calcium Channel 5-HT Receptor Cardiovascular Disease
    Nexopamil racemate is the racemate of Nexopamil. Nexopamil is a combined Ca 2+/5-HT2 antagonist on thrombus formation in vivo and on platelet aggregation in vitro.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-106994
    Nebentan free base

    YM598 free base

    Endothelin Receptor Inflammation/Immunology Cardiovascular Disease
    Nebentan (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.
  • HY-19331
    WZB117

    GLUT Cancer
    WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.
  • HY-12379
    NS-2028

    Guanylate Cyclase Inflammation/Immunology
    NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor with IC50 values of 30 nM and 200 nM for basal and NO-stimulated enzyme activity. NS-2028 inhibits soluble Guanylyl Cyclase activity in homogenates of mouse cerebellum and neuronal NO synthase with IC50 values of 17 nM and 20 nM. NS-2028 inhibits 3-morpholino-sydnonimine (SIN-1)-elicited formation of cyclic GMP in human cultured umbilical vein endothelial cells with an IC50 of 30 nM. NS-2028 is commonly used in the research of nitric oxide signaling pathways, it inhibits NO-dependent relaxant responses in non-vascular smooth muscle completely (1 μM). NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability.
  • HY-14350
    AC-55541

    Protease-Activated Receptor (PAR) Others
    AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation. AC-55541 has pEC50 values of 5.9 and 6.6 in PI hydrolysis assays and Ca 2+ mobilization assays and exhibits pronociceptive activity in vivo.
  • HY-15708
    LY2795050

    Opioid Receptor Neurological Disease
    LY2795050 is a novel selective κ-opioid Receptor (KOR) antagonist (IC50=0.72 nM) and has the potential as a PET tracer to image KOR in vivo.
  • HY-112129
    AGI-25696

    Others Cancer
    AGI-25696 is a methionine adenosyltransferase 2A (MATA2 ) inhibitors useful for treatment of cancer. AGI-25696 blocks growth of MTAP-deleted tumors in vivo.
  • HY-104047
    LM22B-10

    Trk Receptor Akt ERK Neurological Disease
    LM22B-10 is an activator of TrkB/TrkC neurotrophin receptor, and can induce TrkB, TrkC, AKT and ERK activation in vitro and in vivo.
  • HY-19947
    PF-06291874

    Glucagon receptor antagonists-4

    Glucagon Receptor Metabolic Disease
    PF-06291874 (Glucagon receptor antagonists-4) is a highly potent and orally active glucagon receptor antagonist. It displays low in vivo clearance in both rats and dogs.
  • HY-14536
    Methylene Blue

    Basic Blue 9; Methylthioninium chloride; CI-52015

    Guanylate Cyclase Monoamine Oxidase NO Synthase Parasite Cancer Infection Neurological Disease
    Methylene blue (Basic Blue 9) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue has antinociception, antimalarial, antidepressant and anxiolytic activity effects. Methylene Blue has the potential for methemoglobinemias, neurodegenerative disorders and ifosfamide-induced encephalopathytreatment.
  • HY-108584
    Flindokalner

    BMS-204352

    Potassium Channel Neurological Disease
    Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
  • HY-N6690
    Destruxin B

    Bcl-2 Family Caspase Apoptosis Cancer Infection
    Destruxin B, isolated from entomopathogenic fungus Metarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B induces apoptosis via a Bcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lung cancer cells. Destruxin B significantly activates caspase-3 and reduces tumor cell proliferation through caspase-mediated apoptosis, not only in vitro but also in vivo.
  • HY-P1208
    PG-931

    Melanocortin Receptor Inflammation/Immunology
    PG-931, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R (IC50=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo.
  • HY-B1454
    Clindamycin palmitate hydrochloride

    Bacterial Antibiotic Infection
    Clindamycin palmitate hydrochloride is a water soluble hydrochloride salt of the ester of clindamycin and palmitic acid and it is an antibacterial drug. Clindamycin palmitate hydrochloride is inactive in vitro, rapid in vivo hydrolysis converts this compound to the antibacterially active clindamycin.
  • HY-101414
    L-DABA

    L-2,4-Diaminobutyric acid

    GABA Receptor Endogenous Metabolite Neurological Disease Cancer
    L-DABA (L-2,4-Diaminobutyric acid) is a week GABA transaminase inhibitor with an IC50 of larger than 500 μM; exhibits antitumor activity in vivo and in vitro.
  • HY-90010
    Tolterodine tartrate

    Kabi-2234; PNU-200583E

    mAChR Neurological Disease
    Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
  • HY-P2108
    Lysobactin

    Antibiotic Bacterial Infection
    Lysobactin, produced by several genera of Gram-negative gliding bacteria found in soil, is a potent antibiotic with in vivo efficacy against Staphylococcus aureus and Streptococcus pneumoniae.
  • HY-15893
    DMOG

    Dimethyloxallyl Glycine

    HIF/HIF Prolyl-Hydroxylase Autophagy Cancer
    DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy.
  • HY-112610
    CF53

    Epigenetic Reader Domain Histone Acetyltransferase Cancer
    CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
  • HY-Y0265
    Isatin

    indoline-2,3-dione

    Monoamine Oxidase Apoptosis Cancer Neurological Disease Cardiovascular Disease
    Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM). Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity. Shows effect on the serotonergic system.
  • HY-18227
    B-Raf IN 1

    Raf Cancer
    B-Raf IN 1 is a potent and selective B-Raf kinase inhibitor with an IC50 of 24 nM.
  • HY-D0227
    Trometamol

    Tromethamine

    Others Metabolic Disease
    Trometamol is a biologically inert amino alcohol of low toxicity, which buffers carbon dioxide and acids in vitro and in vivo. Trometamol is an effective amine compound for pH control in the physiological range.
  • HY-133558
    VII-31

    E1/E2/E3 Enzyme Apoptosis Cancer
    VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways.
  • HY-16339
    N3PT

    N3-pyridyl thiamine

    Others Cancer
    N3PT(N3-pyridyl thiamine) is a potent and selective transketolase(TK) inhibitor (IC50= 22 nM for Apo-TK) both in vitro and in vivo.
  • HY-108045
    Lodenafil carbonate

    Phosphodiesterase (PDE) Endocrinology
    Lodenafil carbonate, a dimer that acts as a prodrug delivering Lodenafil in vivo, is an orally active phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).
  • HY-101692
    AZ-1355

    Prostaglandin Receptor Metabolic Disease Endocrinology
    AZ-1355 is an effctive lipid-lowering compound, which also inhibits platelet aggregation in vivo and elevates the prostaglandin I2/thromboxane A2 ratio in vitro.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-P1208A
    PG-931 TFA

    Melanocortin Receptor Inflammation/Immunology
    PG-931 TFA, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R(IC50=2.4 nM). PG-931 TFA can reverse haemorrhagic shock and prevent multiple organ damage in vivo.
  • HY-114414
    HDACs/mTOR Inhibitor 1

    HDAC mTOR Apoptosis Cancer
    HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM and >500 nM for HDAC1, HDAC6, mTOR and PI3Kα, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induce tumor cell apoptosis with low toxicity in vivo.
  • HY-18758
    IN-1130

    TGF-β Receptor Cancer Inflammation/Immunology
    IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis.
  • HY-D0227A
    Trometamol hydrochloride

    Tromethamine hydrochloride

    Others Metabolic Disease
    Trometamol hydrochloride (Tromethamine hydrochloride) is a biologically inert amino alcohol of low toxicity, which buffers carbon dioxide and acids in vitro and in vivo. Trometamol hydrochloride is an effective amine compound for pH control in the physiological range.
  • HY-14907
    Verubulin

    MPC 6827

    Microtubule/Tubulin Apoptosis Cancer
    Verubulin (MPC-6827) is a microtubule-disrupting agent with potent and broad-spectrum in vitro and in vivo cytotoxic activities, and acts as a promising candidate for the treatment of multiple cancer types.
  • HY-14221
    Siramesine

    Lu 28-179

    Sigma Receptor Ferroptosis Cancer
    Siramesine(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.
  • HY-P1156
    Insulin(cattle)

    insulin from bovine pancreas

    Insulin Receptor Metabolic Disease Endocrinology
    Insulin cattle (Insulin from bovine pancreas) is a two-chain polypeptide hormone produced in vivo in the pancreatic β cells. Insulin cattle has often been used as growth supplement in culturing cells.
  • HY-14532
    Brincidofovir

    CMX001; HDP-CDV

    CMV Infection
    Brincidofovir (CMX001; HDP-CDV) is an orally active, lipophilic form of cidofovir (CDV); has enhanced activity in vitro and in vivo compared to CDV against certain herpesviruses, adenoviruses and orthopoxviruses.
  • HY-14221A
    Siramesine hydrochloride

    Lu 28-179 hydrochloride

    Sigma Receptor Ferroptosis Cancer
    Siramesine hydrochloride (Lu 28-179 hydrochloride) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.
  • HY-B0834
    Indoxacarb

    (±)-indoxacarb

    Sodium Channel
    Indoxacarb ((±)-Indoxacarb) is a broad-spectrum oxadiazine insecticide. Indoxacarb is metabolized in vivo to its active N-decarbomethoxyllated metabolite DCJW. Indoxacarb suppresses voltage-gated sodium channel currents in rat dorsal root ganglion neurons.
  • HY-W042039
    Methyl homoveratrate

    Calcium Channel Cardiovascular Disease
    Methyl homoveratrate, a metabolite of RWJ-26240 in vivo, can be identified in plasma, urine and faecal extract. McN5691 (RWJ-26240) is a voltage-sensitive calcium channel blocker.
  • HY-126328
    PKC-theta inhibitor 1

    PKC Inflammation/Immunology
    PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM. PKC-theta inhibitor 1 demonstrates a reduction of symptoms in a mouse model of multiple sclerosis.
  • HY-13410
    Xanomeline oxalate

    LY246708 oxalate

    mAChR Neurological Disease
    Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease.
  • HY-12246
    XEN445

    Others Cardiovascular Disease
    XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.
  • HY-N0376
    Liquiritin

    Reactive Oxygen Species Cancer Inflammation/Immunology Neurological Disease
    Liquiritin, a flavonoid isolated from Glycyrrhiza, is a potent and competitive AKR1C1 inhibitor with IC50s of 0.62 μM, 0.61 μM, and 3.72μM for AKR1C1, AKR1C2 and AKR1C3, respectively. Liquiritin efficiently inhibits progesterone metabolism mediated by AKR1C1 in vivo. Liquiritin acts as an antioxidant and has neuroprotective, anti-cancer and anti-inflammatory activity.
  • HY-B1359
    Methylene blue trihydrate

    C.I. Basic Blue 9 trihydrate

    Guanylate Cyclase Monoamine Oxidase NO Synthase Parasite Cancer Infection Neurological Disease
    Methylene blue trihydrate (C.I. Basic Blue 9 trihydrate) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue trihydrate is a vasopressor and is often used as a dye in several medical procedures. Methylene blue trihydrate has antinociception, antimalarial, antidepressant and anxiolytic activity effects. Methylene Blue trihydrate has the potential for methemoglobinemias, neurodegenerative disorders and ifosfamide-induced encephalopathytreatment.
  • HY-13735A
    Quinacrine dihydrochloride

    Mepacrine dihydrochloride; SN-390 dihydrochloride

    Parasite Apoptosis Autophagy Mitophagy Cancer Infection
    Quinacrine dihydrochloride (Mepacrine dihydrochloride) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis.
  • HY-18353
    mTOR inhibitor-3

    mTOR Cancer
    mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
  • HY-N7095
    Ceftezole

    CTZ

    Bacterial Antibiotic Infection
    Ceftezole (CTZ) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole (CTZ) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity.
  • HY-15641
    FG-2216

    IOX3; YM311

    HIF/HIF Prolyl-Hydroxylase Others
    FG-2216 (IOX3; YM311) is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme; orally bioavailable and induced significant and reversible Epo induction in vivo.
  • HY-N7096
    Ceftezole sodium

    CTZ sodium

    Bacterial Antibiotic Infection
    Ceftezole sodium (CTZ sodium) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole sodium (CTZ sodium) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity.
  • HY-13735B
    Quinacrine hydrochloride hydrate

    Mepacrine hydrochloride hydrate; SN-390 hydrochloride hydrate

    Parasite Apoptosis Autophagy Mitophagy Cancer Infection
    Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis.
  • HY-116649
    CB1 antagonist 2

    Cannabinoid Receptor Neurological Disease
    CB1 antagonist 2 is caimabinoid 1 (CB1) antagonist extracted from patent WO2016184310A1, compound 3, inhibits CB1 in vivo with an IC50 of 25.5 nM.
  • HY-103261
    SCH28080

    Proton Pump Endocrinology
    SCH28080 is a reversible, K +-competitive inhibitor of the gastric (H +/K +)-ATPase, with a Ki of 0.12 μM. SCH28080 is an effective inhibitor of acid secretion in vivo and with anti-gastric ulcer activity.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-B1057
    Nefopam hydrochloride

    Fenazoxine hydrochloride

    β-catenin Neurological Disease
    Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo.
  • HY-100876
    GGTI298

    Ras Apoptosis Cancer
    GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
  • HY-15975
    GNF179

    Parasite Infection
    GNF179 is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.
  • HY-108649A
    MRS2768 tetrasodium salt

    P2Y Receptor Cardiovascular Disease
    MRS2768 tetrasodium salt is a moderately potent and selective P2Y2 receptor agonist. MRS2768 tetrasodium salt has a protective effect on cardiomyocytes from ischemic damage in vivo and in vitro.
  • HY-16561
    Resveratrol

    trans-Resveratrol; SRT501

    IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Cancer Infection Inflammation/Immunology
    Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor.
  • HY-16659
    EHT 1864

    Ras Neurological Disease Cancer
    EHT 1864 is an inhibitor of Rac family small GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 also potently inhibits other Rac-dependent transformation processes, Tiam1- and Ras-mediated growth transformation. EHT 1864 prevents Aβ 40 and Aβ 42 production in vivo.
  • HY-103129
    SB-200646A

    5-HT Receptor Neurological Disease
    SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.
  • HY-103129A
    SB-200646

    5-HT Receptor Neurological Disease
    SB-200646 is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646 is orally active and has electrophysiological and anxiolytic properties in vivo.
  • HY-111434
    UAA crosslinker 1

    Others Cancer
    UAA crosslinker 1 hydrochloride is an amber codon used for non-canonical amino acids (ncAAs) incorporation. The ncAAs can be incorporated into proteins in vivo by making use of the promiscuous activity of certain wildtype and engineered aminoacyl-tRNA synthetases.
  • HY-18006
    NKP608

    Neurokinin Receptor Neurological Disease Endocrinology
    NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo.
  • HY-111434A
    UAA crosslinker 1 hydrochloride

    Others Cancer
    UAA crosslinker 1 hydrochloride is an amber codon used for non-canonical amino acids (ncAAs) incorporation. The ncAAs can be incorporated into proteins in vivo by making use of the promiscuous activity of certain wildtype and engineered aminoacyl-tRNA synthetases.
  • HY-15427
    GDC-0834

    Btk Inflammation/Immunology
    GDC-0834 is a potent and selective BTK inhibitor. GDC-0834 inhibits BTK with an in vitro IC50 of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC50 of 1.1 and 5.6 μM in mouse and rat, respectively.
  • HY-15858
    AP-III-a4

    ENOblock

    Enolase Cancer
    ENOblock(AP-III-a4) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.
  • HY-P2281
    Atrial natriuretic factor (1-28) (human, porcine)

    Atrial natriuretic peptide (1-28)

    Endogenous Metabolite
    Atrial natriuretic factor (1-28) (human, porcine) (Atrial natriuretic peptide (1-28)) is an endogenous peptide produced by the heart, involved in blood pressure regulation. Atrial natriuretic factor (1-28) (human, porcine) produces natriuresis, diuresis and vasorelaxation in vivo.
  • HY-P1252
    Parathyroid Hormone (1-34), bovine

    Thyroid Hormone Receptor Metabolic Disease
    Parathyroid Hormone (1-34), bovine is a potent parathyroid hormone (PTH) receptor agonist. Parathyroid Hormone (1-34), bovine increases calcium and inorganic phosphate levels in vivo. Parathyroid Hormone (1-34), bovine can be used for th reseach of osteoporosis.
  • HY-112038A
    GSK2983559

    RIP kinase Inflammation/Immunology
    GSK2983559 (compound 3) is a potent, specific and oral bioavailable receptor interacting protein 2 (RIP2) kinase inhibitor, which has excellent activity in blocking many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples.
  • HY-15858A
    AP-III-a4 hydrochloride

    ENOblock hydrochloride

    Enolase Cancer
    AP-III-a4 hydrochloride (ENOblock hydrochloride) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.
  • HY-106993
    Cipralisant

    GT-2331

    Histamine Receptor Neurological Disease Endocrinology
    Cipralisant is a potent and selective histamine H3 receptor antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor; Cipralisant has the potential for attention-deficit hyperactivity disorder treatment.
  • HY-18296
    AKT-IN-1

    Akt Cancer
    AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.
  • HY-102059
    MOZ-IN-2

    Histone Acetyltransferase Cancer
    MOZ-IN-2 is an inhibitor of protein MOZ, a member of histone acetyltransferases, with an IC50 of 125 μM.
  • HY-17499
    EGFR-IN-12

    EGFR Apoptosis Cancer
    EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFR L858R and EGFR L861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity.
  • HY-130119
    Integrin-IN-2

    Integrin Cancer
    Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC50 values of 7.8, 8.4, 8.4 and 7.4, respectively.
  • HY-128523
    Kgp-IN-1

    Others Inflammation/Immunology
    Kgp-IN-1 is an arginine-specific gingipain (Rgp) inhibitor extracted from patent WO2017201322A1, compound 13-R.
  • HY-115688
    TXNIP-IN-1

    Others Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    TXNIP-IN-1 is TXNIP-TRX (thioredoxin-interacting protein- thioredoxin) complex inhibitor extracted from patent US20200085800A1, Compound 1. TXNIP-IN-1 can be used in the research of TXNIP-TRX complex associated metabolic disorder (diabetes), cardiovascular disease, or inflammatory disease.
  • HY-101509
    HSL-IN-1

    Others Metabolic Disease
    HSL-IN-1 (compound 24b) is a potent and orally active hormone sensitive lipase (HSL) inhibitor (IC50=2 nM) with a significantly reduced reactive metabolite liability.
  • HY-111538
    MAGL-IN-1

    MAGL Metabolic Disease
    MAGL-IN-1 is a potent and selective monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 80 nM.
  • HY-136393
    IKK-IN-4

    IKK Inflammation/Immunology
    IKK-IN-4 is a potent and selective IkappaB kinase 2 (IKKβ orIKK2) inhibitor, with IC50s of 45 and 650 nM for IKKβ and IKKα, respectively.
  • HY-18564
    HCV-IN-3

    HCV Infection
    HCV-IN-3 is a hepatitis C virus (HCV) NS3/4a protein inhibitor, with an IC50 of 20 μM, a Kd of 29 μM.
  • HY-112829
    FASN-IN-2

    Fatty Acid Synthase (FASN) Others
    FASN-IN-2 is a Fatty Acid Synthase (FASN) inhibitor extracted from patent WO2012122391A1, compound 152, has an IC50 of 0.052 μM and an EC50 of 0.072 μM.
  • HY-16903
    PKC-IN-1

    PKC Inflammation/Immunology
    PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
  • HY-135666
    DHODH-IN-8

    Parasite Dihydroorotate Dehydrogenase DNA/RNA Synthesis Infection
    DHODH-IN-8 (Compound 27) is an inhibitor of human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) with IC50s of 0.13 μM and 47.4 μM, and Kis of 0.016 μM and 5.6 μM, respectively. DHODH-IN-8 has antimalarial activity.
  • HY-100857
    PrPSc-IN-1

    Others Neurological Disease
    PrPSc-IN-1 is a fluorescent probe, binds to the misfolded protein PrP Sc, inhibits its accumulation, with an IC50 of 1.6 μM. Anti-prion activity.
  • HY-133018
    HCV-IN-7

    HCV Infection
    HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity.
  • HY-U00318
    JAK-IN-11

    JAK Inflammation/Immunology
    JAK-IN-11 is a potent and selective JAK inhibitor extracted from patent WO2012122452A1, Compound II, has the potential for the skin disorders (such as cutaneous lupus) treatment.
  • HY-U00351
    ROCK-IN-1

    ROCK Inflammation/Immunology Cardiovascular Disease
    ROCK-IN-1 is a potent inhibitor of ROCK, with an IC50 of 1.2 nM for ROCK2.
  • HY-130839
    LolCDE-IN-1

    Bacterial Infection
    LolCDE-IN-1 is an inhibitor of the Lol proteins (LolCDE) complex, with antibacterial activity.
  • HY-13827
    JAK-IN-1

    JAK Inflammation/Immunology
    JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.
  • HY-23524
    HSL-IN-3

    Others Others
    HSL-IN-3 (example 42), a boronic acid ester derivative, is an inhibitor of hormone-sensitive lipase (HSL).
  • HY-133553
    RET-IN-3

    RET Cancer
    RET-IN-3 (compound 34) is a selective RETV804M kinase inhibitor, with an IC50 of 19 nM.
  • HY-135664
    DHODH-IN-7

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Cancer
    DHODH-IN-7 is a human dihydroorotate dehydrogenase (DHODH) inhibitor, with an IC50 of 0.91 μM. DHODH-IN-7 induces differentiation in acute myeloid leukemia.
  • HY-115677
    ILK-IN-3

    Integrin Cancer
    ILK-IN-3 is an integrin linked kinase inhibitor with antitumor activity.
  • HY-136282
    OGT-IN-2

    Others
    OGT-IN-2 is a O-GlcNAc transferase (OGT) inhibitor with an IC50 of 53 μM. OGT-IN-2 reduces proliferation and viability of prostate cancer cells in vitro. OGT-IN-2 depletes intracellular alanine and decreases glucose consumption by cancer cells. OGT-IN-2 decreases markers of ER stress and apoptosis in pregnant diabetic mice and reduces neural tube defects in embryos from diabetic mice.
  • HY-111472
    Porcn-IN-1

    Porcupine Cancer
    Porcn-IN-1 is potent porcupine inhibitor with an IC50 of 0.5±0.2 nM.
  • HY-16987
    IDO-IN-3

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO-IN-3 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 290 nM.
  • HY-108944
    LYP-IN-1

    Phosphatase Inflammation/Immunology
    LYP-IN-1 is a potent, selective and specific LYP inhibitor with a Ki and an IC50 of 110 nM and 0.259 μM, respectively. LYP-IN-1 also has selectivity for a large panel of PTPs, such as SHP1 (IC50=5 μM) and SHP2 (IC50=2.5 μM). LYP-IN-1 exhibits highly efficacious cellular activity in T- and mast cells. LYP-IN-1 can be used for the study of autoimmune disorders.
  • HY-100520
    EGFR-IN-2

    EGFR Cancer
    EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.
  • HY-126248
    Tankyrase-IN-2

    PARP Cancer
    Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model.
  • HY-135618
    DHODH-IN-3

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Infection
    DHODH-IN-3 (compound 3) is a potent inhibitor of Human Dihydroorotate Dehydrogenases (HsDHODH) with an IC50 value of 261 nM. DHODH-IN-3 binds to the the ubiquinone binding cavities in DHODH with a Ki app of 32 nM. DHODH-IN-3 has the potential for malaria treatment.
  • HY-U00054
    LDL-IN-3

    Others Metabolic Disease Cardiovascular Disease
    LDL-IN-3 is an anti-atherosclerotic compound extracted from patent WO/2005/039596A1, example C25 and patent US 6133467, example 3.
  • HY-19815
    EGFR-IN-3

    EGFR Cancer
    EGFR-IN-3 is an epidermal growth factor receptor (EGFR) inhibitor.
  • HY-130840
    LolCDE-IN-2

    Bacterial Cancer
    LolCDE-IN-2 is a potent Lol protein (LolCDE) inhibitor. LolCDE-IN-2 inhibits E. coli MG1655 with a MIC of 2 μg/ml. Antibacterial activity.
  • HY-128569
    ALK-IN-5

    ALK Neurological Disease
    ALK-IN-5 is a potent, selective, and brain-penetrant inhibitor of anaplastic lymphoma kinase (ALK), with an IC50 of 2.9 nM.
  • HY-135676
    DHODH-IN-12

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    DHODH-IN-12 (Compound 12b) is a Leflunomide derivative and a weak dihydroorotate dehydrogenase (DHODH) inhibitor with a pKa of 5.07.
  • HY-50736
    DUB-IN-1

    Deubiquitinase Cancer
    DUB-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC50 of 0.24 μM for USP8.
  • HY-100172
    Proteasome-IN-1

    Proteasome Cancer
    Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1.
  • HY-126257
    AKT-IN-3

    Akt Apoptosis Cancer
    AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells.
  • HY-128889
    FXIa-IN-1

    Factor Xa Cardiovascular Disease
    FXIa-IN-1 (compound EP-7041) is a potent β-lactam covalent heparin-derived factor XIa (fXIa) inhibitor.
  • HY-18671
    BoNT-IN-1

    Others Neurological Disease
    BoNT-IN-1 is a potent inhibitor of Botulinum neurotoxin A light chain (BoNTA LC) with IC50 of 0.9 uM.
  • HY-135678
    DHODH-IN-14

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    DHODH-IN-14 (Compound 7l) is a hydroxyfurazan analog of A771726. DHODH-IN-14 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 0.49 μM for rat liver DHODH. DHODH-IN-14 can be used for rheumatoid arthritis.
  • HY-112534
    GSTO-IN-2

    Gutathione S-transferase Cancer
    GSTO-IN-2 is a glutathione S-transferase inhibitor with IC50s of 3.6, 16.3, and 1.4 μM for GSTA2, GSTM1, and GSTP1-1.
  • HY-111916
    BET-IN-4

    Epigenetic Reader Domain Cancer
    BET-IN-4 is a potent BET bromodomain protein (BRD4) inhibitor, with an IC50 of ≤ 1 μM.
  • HY-128597
    BRD-IN-3

    Epigenetic Reader Domain Cancer
    BRD-IN-3 ((R,R)-36n) is a highly potent PCAF bromodomain (BRD) inhibitor, with an IC50 of 7 nM. BRD-IN-3 also exhibits activity against GCN5 and FALZ.
  • HY-102054
    Acetylhydrolase-IN-1

    FAAH Cardiovascular Disease
    Acetylhydrolase-IN-1 is a 1-Alkyl-2-acetylglycerophosphocholine esterase (Alkylacetyl-GPC: acetylhydrolase) inhibtor.
  • HY-130680
    Syk-IN-3

    Syk Cancer
    Syk-IN-3, a potent spleen tyrosine kinase (Syk) inhibitor, extracted from patent WO2011075515A1, compound example 152, has an IC50 of 1 nM.
  • HY-111389
    FAAH-IN-1

    FAAH Autophagy Metabolic Disease
    FAAH-IN-1 is a fatty acid amide hydrolase (FAAH) inhibitor, with IC50s of 145 nM and 650 nM for rat and human FAAH, respectively.
  • HY-110387
    IDO-IN-9

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO-IN-9 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50s of 0.011 μM (Kinase) and 0.0018 μM (Hela Cell), extracted from patent WO 2016041489 A1, compound 6.
  • HY-126130
    LysRs-IN-2

    Aminoacyl-tRNA Synthetase Infection
    LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC50s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) and Cryptosporidium parvum lysyl-tRNA synthetase (CpKRS), respectively.
  • HY-18769
    IDO-IN-4

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO-IN-4 is an indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor, extracted from patent WO2014150677A1, Compound example 1 enantiomer 1.
  • HY-135659
    BSH-IN-1

    Bacterial Infection
    BSH-IN-1 is a potent and covalent inhibitor of gut bacterial recombinant bile salt hydrolases (BSHs) with IC50s of 108 nM and 427 nM for B. longum BSH (Gram positive) and B. theta BSH (Gram negative), respectively.
  • HY-79531
    IDO-IN-1

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 59 nM.
  • HY-135670B
    Glycosidase-IN-2

    Others Metabolic Disease
    Glycosidase-IN-2 (Compound 20) is an azasugar class of glycosidase inhibitor. Glycosidase-IN-2 has hypoglycemic activity.
  • HY-128862
    EGFR-IN-7

    EGFR Cancer
    EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity.
  • HY-136266
    HCV-IN-29

    HCV Cancer
    HCV-IN-29 is a hepatitis C virus (HCV) inhibitor exacted from patent US8329159B2, compound 1e.
  • HY-135654
    hDHODH-IN-2

    Lactate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    hDHODH-IN-2 is an analogue of the active metabolite of Leflunomide. hDHODH-IN-2 is a human dihydroorotate dehydrogenase (hDHODH) inhibitor. hDHODH-IN-1 has anti-inflammatory activity.
  • HY-16615
    SIRT-IN-1

    Sirtuin Metabolic Disease Neurological Disease Cancer Inflammation/Immunology
    SIRT-IN-1 is a potent inhibitor of SIRT1/2/3, with IC50s of 15, 10, 33 μM, respectively.
  • HY-U00345
    CHK-IN-1

    Checkpoint Kinase (Chk) Cancer
    CHK-IN-1 is an inhibitor of CHK1 and CHK2, with anti-proliferative activities.
  • HY-50737
    DUB-IN-3

    Deubiquitinase Cancer
    DUB-IN-3 is a potent deubiquitinase (USP) enzyme inhibitor extracted from reference compound 22c with an IC50 of 0.56 μM for USP8.
  • HY-12791
    hPGDS-IN-1

    PGE synthase Inflammation/Immunology
    hPGDS-IN-1 is a hPGDS inhibitor ,with IC50 of 12 nM in the Fluorescence Polarization Assay or the EIA assay.
  • HY-102044
    BET-IN-2

    Epigenetic Reader Domain Cancer
    BET-IN-2 is a BET inhibitor with an IC50 of 52 nM for BRD4-BD1.
  • HY-124699
    MMSET-IN-1

    Others Cancer
    MMSET-IN-1 is a multiple myeloma SET domain (MMSET, aka NSD2/WHSC1) inhibitor against SETD2 and MMSET with IC50s of 0.49 and 3.3 μM, respectively. MMSET-IN-1 has a Kd of 1.6 μM for MMSET.
  • HY-114192
    TGFβRI-IN-1

    TGF-β Receptor Cancer
    TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively .
  • HY-103478
    KHK-IN-2

    Hexokinase Metabolic Disease
    KHK-IN-2 is a potent and selective ketohexokinase (KHK) inhibitor with an IC50 of 0.45 μM.
  • HY-135677
    DHODH-IN-13

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    DHODH-IN-13 (Compound 7a) is a hydroxyfurazan analog of A771726. DHODH-IN-13 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 4.3 μM for rat liver DHODH. DHODH-IN-13 can be used for rheumatoid arthritis.
  • HY-130813
    BET-IN-6

    Ligand for Target Protein for PROTAC Epigenetic Reader Domain Cancer
    BET-IN-6 is a potent and high affnity BRD2/BRD4 inhibitor. BET-IN-6 is the ligand for target protein BRD2/4, and is used for the systhesis of PROTAC BRD2/BRD4 degrader-1 (HY-130612).
  • HY-103479
    GOAT-IN-1

    Acyltransferase Cancer Metabolic Disease Neurological Disease Cardiovascular Disease
    GOAT-IN-1 is an inhibitor of ghrelin O-acyltransferase (GOAT), which could be useful for the prophylaxis or treatment of obesity, diabetes, hyperlipidemia, metabolic, non-alcoholic fatty liver, steatohepatitis, sarcopenia, appetite control, alcohol/narcotic dependence, Alzheimer’s disease, Parkinson’s disease, cerebrovascular dementia, cerebral apoplexy, cerebral infarction, cardic disease, some kind of tumors.
  • HY-U00436
    FASN-IN-3

    Fatty Acid Synthase (FASN) Cancer
    FASN-IN-3 is a fatty acid synthase (FASN) inhibitor extracted from patent US20170119786A1, compound 242A.
  • HY-101628
    KDR-in-4

    VEGFR Cardiovascular Disease
    KDR-in-4 is a potent kinase insert domain-containing receptor (KDR/VEGFR2) inhibitor with an IC50 of 7 nM.
  • HY-129749
    IDO-IN-13

    Indoleamine 2,3-Dioxygenase (IDO) Inflammation/Immunology
    IDO-IN-13 is a potent indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an EC50 of 17 nM, extracted from patent WO2019040102A1, example 43.
  • HY-112950
    RET-IN-1

    RET Cancer
    RET-IN-1 is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 552, has IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively .
  • HY-12426
    mAChR-IN-1

    mAChR Neurological Disease
    mAChR-IN-1 is a potent muscarinic cholinergic receptor(mAChR) antagonist with IC50 of 17 nM.
  • HY-126482
    Telomerase-IN-2

    Telomerase Cancer
    Telomerase-IN-2 is a telomerase inhibitor, and inhibits telomerase activity by decreasing expression of dyskerin, with an IC50 of 0.89 µM. Anti-cancer activity.
  • HY-U00294
    NEP-In-1

    Neprilysin Neurological Disease
    NEP-IN-1 is a neutral endopeptidase (NEP) inhibitor with IC50 of 2 nM for dNEP.
  • HY-100771
    IDO-IN-2

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO-IN-2 is an IDO inhibitor extracted from patent WO/2015031295 A1, compound example 1, has IC50 values of 0.068 μM in HeLa cell and 0.16 μM in HEK293 cell.
  • HY-123637
    Autotaxin-IN-1

    Phosphodiesterase (PDE) Inflammation/Immunology
    Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK/PD relationship. Autotaxin-IN-1 is used in treatment of osteoarthritis pain.
  • HY-U00312
    MEK-IN-1

    MEK Cancer
    MEK-IN-1 is a MEK inhibitor extracted from patent WO2008076415A1.
  • HY-135220
    PERK-IN-2

    PERK Cancer
    PERK-IN-2 is a potent PERK inhibitor with an IC50 of 0.2 nM.
  • HY-111234
    IDO-IN-11

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO-IN-11 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50s of 0.18 μM (Kinase) and 0.014 μM (Hela Cell), extracted from patent WO 2016041489 A1, compound 13.
  • HY-135658
    hDHODH-IN-1

    Lactate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    hDHODH-IN-1 is a human dihydroorotate dehydrogenase (hDHODH) inhibitor. hDHODH-IN-1 has anti-inflammatory effect.
  • HY-U00015
    MAO-IN-1

    Monoamine Oxidase Neurological Disease
    MAO-IN-1 is a monoamine oxidase B (MAO B) inhibitor with an IC50 of 20 nM.
  • HY-128338
    CETP-IN-3

    CETP Cardiovascular Disease
    CETP-IN-3 (Compound 13) is an small molecule inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP. CETP-IN-3 for the CETP inhibitory activity in the scintillation proximity (SPA) and whole plasma assay (WPA) with IC50s of 0.002 μM and 0.06 μM, respectively.
  • HY-12962
    NMDA-IN-1

    iGluR Neurological Disease
    NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.
  • HY-128596
    ALK-IN-6

    ALK Cancer
    ALK-IN-6 (compound 11) is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK), with IC50 values of 71 nM, 18.72 nM and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L, respectively.
  • HY-111351
    MLK-IN-1

    Mixed Lineage Kinase Neurological Disease
    MLK-IN-1 is a potent, brain penetrant and specific mixed lineage kinase 3 (MLK-3) inhibitor, compound 68, extracted from patent US20140256733A1.
  • HY-12841
    KHK-IN-1

    Others Metabolic Disease
    KHK-IN-1 is a potent ketohexokinase (KHK) inhibitor with IC50 of 12 nM; interacts with Asp-27B in the ATP-binding region of KHK.
  • HY-101933
    MARK-IN-1

    Others Neurological Disease
    MARK-IN-1 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of <0.25 nM.
  • HY-111777
    FASN-IN-1

    Fatty Acid Synthase (FASN) Cancer
    FASN-IN-1 is a fatty acid synthase (FASN) inhibitor extracted from patent WO2015134790A1, compound 56.
  • HY-135088
    Autotaxin-IN-4

    Phosphodiesterase (PDE) Inflammation/Immunology
    Autotaxin-IN-4 (compound 51), extracted from patent WO2018212534A1, is an Autotaxin inhibitor. Autotaxin-IN-4 has the potential to treat idiopathic pulmonary fibrosis.
  • HY-128787
    DHODH-IN-5

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Influenza Virus Infection
    DHODH-IN-5 is a potent human dihydroorotate dehydrogenase (DHODH) inhibitor, with a pIC50 of 7.8 for human recombinant DHODH. DHODH-IN-5 inhibits measles virus replication, with a pMIC50 of 8.8.
  • HY-101934
    MARK-IN-2

    Others Neurological Disease
    MARK-IN-2 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 5 nM.
  • HY-136579
    ERK-IN-3

    ERK Cancer
    ERK-IN-3 is a potent and oral inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.
  • HY-125965
    BioA-IN-13

    Bacterial Infection
    BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme.
  • HY-128758
    DYRKs-IN-1

    DYRK Cancer
    DYRKs-IN-1 (Example 183) is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 9 nM and 5 nM for DYRK1B and DYRK1A, respectively. DYRKs-IN-1 has antitumor activity.
  • HY-126320
    EGFR-IN-8

    EGFR c-Met/HGFR Cancer
    EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC.
  • HY-125028
    Hck-IN-1

    Src HIV Infection
    Hck-IN-1 (compound B9), a diphenylpyrazolo compound, is a selective Nef-dependent Hck inhibitor with IC50s of 2.8 μM, >20 μM for Nef:Hck complex and Hck, respectively. Hck-IN-1 is a direct and wide HIV-1 Nef antagonists with an IC50 of 100-300 nM for wild-type HIV-1 replication. Hck-IN-1 binds pocket residue Asn126 and has anti-retroviral activity.
  • HY-112094
    WNK-IN-11

    Others Others
    WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor, with an IC50 of 4 nM for WNK1.
  • HY-135648
    PfDHODH-IN-1

    Parasite Lactate Dehydrogenase DNA/RNA Synthesis Infection
    PfDHODH-IN-1 is an analogue of the active metabolite of Leflunomide. PfDHODH-IN-1 is a Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor. PfDHODH-IN-1 has antimalarial activity.
  • HY-130606
    Nampt-IN-5

    Nampt Cancer
    Nampt-IN-5 is a potent and orally active nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively.
  • HY-U00287
    BACE-IN-1

    Beta-secretase Neurological Disease
    BACE-IN-1 (Compound 13) is a substituted lmidazo[1 ,2-a]pyridine derivative which can inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease.
  • HY-135675
    DHODH-IN-11

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    DHODH-IN-11 (Compound 14b) is a Leflunomide derivative and a weak dihydroorotate dehydrogenase (DHODH) inhibitor with a pKa of 5.03.
  • HY-111756
    BLM-IN-1

    Apoptosis Cancer
    BLM-IN-1 (compound 29) is an effective Bloom syndrome protein (BLM) inhibitor, with a strong BLM binding KD of 1.81 μM and an IC50 of 0.95 μM for BLM. Induces DNA damage response, as well as apoptosis and proliferation arrest in cancer cells.
  • HY-111749
    JAK-IN-4

    JAK Inflammation/Immunology
    JAK-IN-4 is a prodrug of a JAK inhibitor, effective in murine collagen induced arthritis model.
  • HY-103280
    LysRs-IN-1

    Others Others
    LysRs-IN-1 is a Lysyl-tRNA synthetase (LysRs) inhibitor.
  • HY-111108
    LDH-IN-1

    Lactate Dehydrogenase Cancer
    LDH-IN-1 is a novel pyrazole-based inhibitor of human lactate dehydrogenase (LDH) with IC50s of 32 and 27 nM for LDHA and LDHB, respectively.
  • HY-13873
    IKK-IN-1

    IKK Inflammation/Immunology
    IKK-IN-1 is an inhibitor of IKK extracted from patent WO2002024679A1, compound example 18-13.
  • HY-19702
    PKR-IN-2

    Others Cancer
    PKR-IN-2 is a pyruvate kinase (PKR) activator, extracted from patent WO2014139144A1, compound 160, has an IC50 of <100 nM for. PKR (R510Q), PKR (R532W), PKR (WT), and PKR (WT Cell Based).
  • HY-114491
    ERK-IN-1

    Raf ERK Cancer
    ERK-IN-1 (compound B) is a RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC (non-small celllung cancer), BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovanan cancer.
  • HY-12648
    FASN-IN-4

    Fatty Acid Synthase (FASN) Metabolic Disease
    FASN-IN-4 is a potent inhibitor of fatty acid synthase (FASN) extracted from patent WO 2012064642 A1, compound 29; has an IC50 of 10 nM.
  • HY-135089
    Autotaxin-IN-5

    Phosphodiesterase (PDE) Inflammation/Immunology
    Autotaxin-IN-5 (compound 63), extracted from patent WO2018212534A1, is an Autotaxin inhibitor. Autotaxin-IN-5 has the potential to treat idiopathic pulmonary fibrosis.
  • HY-135667
    DHODH-IN-9

    Influenza Virus Dihydroorotate Dehydrogenase DNA/RNA Synthesis Infection
    DHODH-IN-9 (Compound 10k) is an azine-bearing analogue and is a human dihydroorotate dehydrogenase inhibitor. DHODH-IN-9 has antiviral effect with a pMIC50 of 7.4.
  • HY-P0162
    HCV-IN-4

    HCV Infection
    HCV-IN-4 is a potent and orally active HCV NS5A inhibitor, shows great potency against GT1a, GT2b, GT3a, GT1a Y93H and GT1a L31V, with EC90s of 3 pM, 0.3 nM, 0.01 nM, 0.5 nM and 0.02 nM, respectively.
  • HY-114439
    MtbHU-IN-1

    Bacterial Infection
    MtbHU-IN-1 is an inhibitor of Mycobacterium tuberculosis nucleoid-associated protein HU (MtbHU), with a Kd of 98 nM for binding to WT MtbHU.
  • HY-U00327
    Prenyl-IN-1

    Farnesyl Transferase Neurological Disease
    Prenyl-IN-1 is a protein prenylation inhibitor, especially a geranylgeranyltransferase (GGT) or a farnesyltransferase (FT) inhibitor, exhibiting potent activity against oxidative stress, and particularly in the treatment of Parkinson's Disease.
  • HY-114331
    DLK-IN-1

    MAP3K Neurological Disease
    DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM. DLK-IN-1 retains excellent CNS penetration and is well tolerated following multiple days of dosing at concentrations that exceed those required for DLK inhibition in the brain. DLK-IN-1 has activity in a model of Alzheimer’s Disease.
  • HY-18362
    HDAC-IN-5

    HDAC Cancer
    HDAC-IN-5 is a histone deacetylase (HDAC) inhibitor.
  • HY-129911
    FABP-IN-1

    FABP Inflammation/Immunology
    FABP-IN-1 (Compounds 4b) is a high affinity fatty acid binding protein (FABP) inhibitor. FABP-IN-1 inhibits FABP3, FABP5, and FABP7 with Ki values of 0.69 μM, 0.55 μM and 0.67 μM, respectively. FABP-IN-1 displays potent antinociceptive effects.
  • HY-128570
    FD-IN-1

    Complement System Inflammation/Immunology
    FD-IN-1 (Compound 12) is a factor D (FD) inhibitor with an IC50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5µM, respectively.
  • HY-129634
    TrkA-IN-1

    Trk Receptor Neurological Disease
    TrkA-IN-1 is a potent and selective Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 of 99 nM in a cell-based assay. TrkA-IN-1 has analgesic activity.
  • HY-16616
    SIRT-IN-2

    Sirtuin Metabolic Disease Neurological Disease Cancer Inflammation/Immunology
    SIRT-IN-2 is a potent inhibitor of SIRT1/2/3, with IC50s of 4, 4, 7 μM, respectively.
  • HY-U00282
    Chymase-IN-2

    Others Inflammation/Immunology
    Chymase-IN-2 is a chymase modulator which is useful in the treatment of inflammatory and serine protease mediated disorders.
  • HY-18213
    EGFR-IN-9

    EGFR Cancer
    EGFR-IN-9 (Compound 8) is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity.
  • HY-123984
    LTβR-IN-1

    Others Metabolic Disease
    LTβR-IN-1 is a potent, selective lymphotoxin β receptor (LTβR) inhibitor with an IC50 of 10 μM. LTβR-IN-1 is potent in TWEAK-stimulated p52 translocation assays with an IC50 of 10 μM and did not alter TNF-α–induced p65 nuclear translocation.
  • HY-135679
    DHODH-IN-15

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    DHODH-IN-15 (Compound 7b) is a hydroxyfurazan analog of A771726. DHODH-IN-15 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 11 μM for rat liver DHODH. DHODH-IN-15 can be used for rheumatoid arthritis.
  • HY-111750
    JAK-IN-3

    JAK Inflammation/Immunology
    JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively.
  • HY-19772
    HDAC-IN-3

    HDAC Cancer
    HDAC-IN-3 is a histone deacetylase (HDAC) inhibitor, extracted from patent WO/2008040934 A1.
  • HY-128759
    DYRKs-IN-2

    DYRK Cancer
    DYRKs-IN-2 (Example 132) is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively. DYRKs-IN-2 has antitumor activity.
  • HY-129651
    SHMT-IN-1

    Others Cancer
    SHMT-IN-1 (compound (±)-46) is a potent inhibitor of plasmodial serine hydroxymethyltransferase (SHMT). SHMT-IN-1 has antitumor activity.
  • HY-126216
    TAM-IN-2

    TAM Receptor Cancer
    TAM-IN-2 is a TAM inhibitor extracted from patent US 20170275290 A1, pyrrolotriazine compound 0904.
  • HY-U00336
    NEP-IN-2

    Neprilysin Cardiovascular Disease
    NEP-IN-2 is an inhibitor of neutral endopeptidase, used in the research of proliferation in atherosclerosis, restenosis.
  • HY-100269
    Chymase-IN-1

    Others Inflammation/Immunology
    Chymase-IN-1 is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC50 of 29 nM.
  • HY-19760
    BET-IN-1

    Epigenetic Reader Domain Inflammation/Immunology
    BET-IN-1 is a bromodomain inhibitor extracted from patent WO/2013024104A1, compound example 2, has a plC50 in the range 6.0 - 7.0.
  • HY-101931
    hVEGF-IN-1

    VEGFR Cancer
    hVEGF-IN-1 represses human VEGF-A translation and shows antitumor activity.
  • HY-108701
    Nampt-IN-3

    Nampt HDAC Autophagy Apoptosis Cancer
    Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC50s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death.
  • HY-101515
    MELK-IN-1

    MELK Cancer
    MELK-IN-1 is a potent inhibitor of maternal embryonic leucine zipper kinase (MELK) with an IC50 and a Ki of 3 nM and 0.39 nM, respectively.
  • HY-133084
    ERK-IN-2

    ERK Cancer
    ERK-IN-2 is a potent, highly seletive and orally active ERK2 inhibitor probe with an IC50 value of 1.8 nM. ERK-IN-2 might lead to off-target toxicity and/or off-target activity at dose >10 μM.
  • HY-112148
    AKT-IN-2

    Akt Cancer
    AKT-IN-2 is a potent, selective and orally bioavailable AKT inhibitor with an IC50 of 5 nM for AKT1.
  • HY-19617
    EGFR-IN-1

    EGFR Cancer
    EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-18271
    CaMKII-IN-1

    CaMK Autophagy Inflammation/Immunology
    CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor with IC50 of 63 nM; significantly high selectivity against CaMKIV, MLCK, p38a, Akt1, and PKC.
  • HY-130616
    EGFR-IN-11

    EGFR Cancer
    EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.
  • HY-135619
    DHODH-IN-4

    Parasite Dihydroorotate Dehydrogenase DNA/RNA Synthesis Infection Inflammation/Immunology
    DHODH-IN-4 (compound 17) is a human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) inhibitor, with IC50 values of 4 μM and 0.18 μM for PfDHODH and HsDHODH, respectively. DHODH-IN-4 (compound 17) possess antimalarial activity.
  • HY-135199
    Ubiquitination-IN-1

    E1/E2/E3 Enzyme Cancer
    Ubiquitination-IN-1 (compound 24) is a ubiquitination and Cksl-Skp2 protein-protein interaction (IC50=0.17 μM) inhibitor. Ubiquitination-IN-1 increases levels of p27. Ubiquitination-IN-1 has the potential for treatment disease by blocking the degradation of tumor suppressors.
  • HY-126140
    MDRTB-IN-1

    Bacterial Infection
    MDRTB-IN-1 (5aα) is an antibiotic which is against Mycobacterium tuberculosis H37Rv with a MIC90 value of 10.5 μM.
  • HY-130643
    PERK-IN-3

    PERK Cancer
    PERK-IN-3 is a potent PERK inhibitor with an IC50 of 7.4 nM.
  • HY-18599
    Chitinase-IN-2

    Others Others
    Chitinase-IN-2 is a insect chitinase and N- acetyl hexosaminidase inhibitor and pesticide; 50 uM/20uM compound concentration's inhibitory percentage are 98%/92% for chitinase/N- acetyl-hexosaminidase respectively.
  • HY-126483
    Telomerase-IN-3

    Telomerase Cancer
    Telomerase-IN-3 is a telomerase inhibitor, which directly targets hTERT promoter activity. hTERT is the key component for maintenance of telomerase activity.
  • HY-112673
    RSV-IN-1

    RSV Infection
    RSV-IN-1 is a human respiratory syncytical virus (hRSV) inhibitor, with an IC50 of 0.11 μM.
  • HY-135570
    DHODH-IN-2

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Influenza Virus Infection
    DHODH-IN-2 (compound 21d) is a human dihydroorotate dehydrogenase (HsDHODH) inhibitor, inhibits measles virus replication with a pMIC50 value of 8.6.
  • HY-111471
    JAK-IN-5

    JAK Inflammation/Immunology
    JAK-IN-5 is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283.
  • HY-135053
    Autotaxin-IN-3

    Phosphodiesterase (PDE) Inflammation/Immunology
    Autotaxin-IN-3 is a Autotaxin(ATX) inhibitor with an IC50 of 2.4 nM, compound 33, sourced from patent WO2018212534A1.
  • HY-108940
    GlyRS-IN-1

    Aminoacyl-tRNA Synthetase Bacterial Cancer Infection
    GlyRS-IN-1 is a glycyl-tRNA synthase (GlyRS) inhibitor extracted from patent WO 2017066459 A1. GlyRS-IN-1 can also inhibit the growth of bacteria.
  • HY-13319
    JNK-IN-8

    JNK Cancer
    JNK-IN-8 is a potent JNK inhibitor with IC50s of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively.
  • HY-103669
    HAT-IN-1

    Histone Acetyltransferase Cancer
    HAT-IN-1 is an inhibitor of HAT, used in the research of cancer.
  • HY-U00268
    Telomerase-IN-1

    Telomerase Cancer
    Telomerase-IN-1 is a Telomerase inhibitor with an IC50 of 0.19 μM.
  • HY-107978
    RIPK-IN-4

    RIP kinase Inflammation/Immunology
    RIPK-IN-4 is a potent and selective RIPK2 inhibitor with excellent oral bioavailability, and has an IC50 of 3 nM.
  • HY-116349
    Bromodomain IN-1

    Epigenetic Reader Domain Cancer
    Bromodomain IN-1 is a Bromodomain inhibitor extracted from patent WO2016069578A1, compound 4 .
  • HY-135282
    DHODH-IN-1

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Infection
    DHODH-IN-1 (compound 18d) is a potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 25 nM. DHODH-IN-1 is an inhibitor of pyrimidine biosynthesis pathway.
  • HY-100691
    NOD-IN-1

    NOD-like Receptor (NLR) Inflammation/Immunology
    NOD-IN-1 is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors, NOD1 and NOD2, with IC50 of 5.74 μM and 6.45 μM, respectively.
  • HY-10836
    Cruzain-IN-1

    Others Others
    Cruzain-IN-1 is a covalent and reversible Cruzain inhibitor, with an IC50 of 10 nM.
  • HY-135670
    Glycosidase-IN-1

    Others Metabolic Disease
    Glycosidase-IN-1 (Compound 9) is a glycosidase inhibitor synthesized from D-mannose. Glycosidase-IN-1 be used to synthesize some immunosuppressive agents and β-glucosidase inhibitors. Glycosidase-IN-1 has hypoglycemic activity.
  • HY-115486
    MPO-IN-28

    Glutathione Peroxidase Cardiovascular Disease
    MPO-IN-28 (Compound 28) is a myeloperoxidase (MPO) inhibitor with an IC50 of 44 nM.
  • HY-136392
    IKK-IN-3

    IKK Inflammation/Immunology
    IKK-IN-3 is a potent and selective IkappaB kinase 2 (IKK2 or IKKβ) inhibitor, with IC50s of 19 and 400 nM for IKK2 and IKK1 (or IKKα), respectively.
  • HY-18598
    Chitinase-IN-1

    Parasite Infection
    Chitinase-IN-1 is a insect chitinase and N- acetyl hexosaminidase inhibitor and pesticide; 50 uM/20 uM compound concentration's inhibitory percentage are 75%/67% for chitinase/N- acetyl-hexosaminidase respectively.
  • HY-115122
    IDO-IN-12

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO-IN-12 is an indoleamine 2,3-dioxygenase (IDO) inhibitor extracted from patent WO 2017181849 A1.
  • HY-128763
    HDAC-IN-4

    HDAC Cancer
    HDAC-IN-4 is a selective HDAC6 and HDAC10 inhibitor with pIC50s of 7.2 and 6.8 in BRET assay, respectively. Antitumoral activity.
  • HY-50737A
    DUB-IN-2

    Deubiquitinase Cancer
    DUB-IN-2 is a potent deubiquitinase inhibitor with an IC50 of 0.28 μM for USP8.
  • HY-18551
    DAGLβ-IN-1

    Others Inflammation/Immunology
    DAGLβ-IN-1 is an inhibitor of diacylglycerol lipase-β (DAGLβ), serves as a versatile intermediate for the design of DAGL-tailored activity-based probes.
  • HY-111784
    CBP-IN-1

    Epigenetic Reader Domain Cancer
    CBP-IN-1 is a potent p300/CBP bromodomain inhibitor.
  • HY-111415
    EGFR-IN-5

    EGFR Cancer
    EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFR L858R, EGFR L858R/T790M, and EGFR L858R/T790M/C797S, respectively.
  • HY-U00277
    JAK-IN-10

    JAK Others
    JAK-IN-10 is a useful composition for treating and/or preventing dry eye disorders.
  • HY-136535
    hTrkA-IN-1

    Trk Receptor Inflammation/Immunology
    hTrkA-IN-1 is a potent and orally active inhibitor of TrkA kinase with an IC50 of 1.3 nM, compound 2. extracted from patent WO2015175788. hTrkA-IN-1 can be used for the study of inflammatory disease, such as prostatitis, pelvic, et al.
  • HY-136267
    HCV-IN-30

    HCV Infection
    HCV-IN-30 (compound 48) is a HCV NS5A replication complex inhibitor, with IC50s of 901 and 102 nM for genotypes 1a and 1b replicons, respectively.
  • HY-131244
    ALK-IN-9

    ALK Cancer
    ALK-IN-9 (compound 40) is a potent ALK inhibitor. ALK-IN-9 inhibits cell proliferation with IC50s of <0.2 nM, <0.2 nM, 0.2 nM for Ba/F3-EML4-ALK, KM 12 (TPM3-TRKA), KG-l cell (OP2-FGFR1), respectively.
  • HY-10895
    SB-334867

    SB 334867A

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
  • HY-19589
    JTS-653

    TRP Channel Inflammation/Immunology Neurological Disease
    JTS-653 is a highly potent and selective transient receptor potential vanilloid 1 (TRPV1) antagonist in vitro and in vivo. JTS-653 attenuates chronic pain refractory to non-steroidal anti-inflammatory agents.
  • HY-101981
    Uridine 5'-monophosphate

    5'-​Uridylic acid

    Endogenous Metabolite Others
    Uridine 5'-monophosphate (5'-​Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk.
  • HY-P1252A
    Parathyroid Hormone (1-34), bovine TFA

    Thyroid Hormone Receptor Metabolic Disease
    Parathyroid Hormone (1-34), bovine TFA is a potent parathyroid hormone (PTH) receptor agonist. Parathyroid Hormone (1-34), bovine increases calcium and inorganic phosphate levels in vivo. Parathyroid Hormone (1-34), bovine can be used for th reseach of osteoporosis.
  • HY-12838
    Mirk-IN-1

    Dyrk1B/A-in-1

    DYRK Cancer
    Mirk-IN-1 is a potent inhibitor of Dyrk1B(Mirk kianse) and Dyrk1A with IC50 of 68±48 nM and 22±8 nM respectively.
  • HY-100513A
    Dehydroaltenusin

    Apoptosis DNA/RNA Synthesis Cancer
    Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM). Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis. Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo.
  • HY-10895A
    SB-334867 free base

    SB334867A free base

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
  • HY-103406A
    PNU-177864 hydrochloride

    Dopamine Receptor Neurological Disease
    PNU-177864 hydrochloride is a potent, selective and orally active dopamine D3 receptor antagonist. PNU-177864 hydrochloride is structurally consistent with a cationic amphiphilic drug (CAD) and induces phospholipidosis in vivo. PNU-177864 hydrochloride antischizophrenic activity.
  • HY-130603
    DCZ0415

    NF-κB Apoptosis Cancer
    DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients.
  • HY-Y1620
    3-(3,4-Dimethoxyphenyl)propanoic acid

    Others Cardiovascular Disease
    3-(3,4-Dimethoxyphenyl)propanoic acid is an orally active short-chain fatty acids (SCFAs). 3-(3,4-Dimethoxyphenyl)propanoic acid stimulates γ globin gene expression, erythropoiesis in vivo and is used for the β hemoglobinopathies and other anemias.
  • HY-15980
    GNF179 Metabolite

    Parasite Infection
    GNF179 metabolite is the metabolite of GNF179, which is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.
  • HY-N0705
    Curculigoside

    JAK STAT NF-κB Inflammation/Immunology Neurological Disease Cancer
    Curculigoside is the main saponin in C. orchioide, exerts significant antioxidant, anti-osteoporosis, antidepressant and neuroprotection effects. Curculigoside possesses significant anti-arthritic effects in vivo and in vitro via regulation of the JAK/STAT/NF-κB signaling pathway.
  • HY-112038
    GSK2983559 free acid

    RIP kinase Inflammation/Immunology
    GSK2983559 free acid (compound 3) is a potent, specific and oral bioavailable receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 free acid has excellent activity in blocking many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples.
  • HY-120394
    TVB-3166

    Fatty Acid Synthase (FASN) Apoptosis Cancer
    TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.
  • HY-133115
    N-Desmethylnefopam

    β-catenin Neurological Disease
    N-Desmethylnefopam is the main metabolite of Nefopam. N-Desmethylnefopam is a centrally-acting but non-opioid analgesic agent, for the relief of moderate to severe pain. Nefopam targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo.
  • HY-15584A
    Taltobulin trifluoroacetate

    HTI-286 trifluoroacetate; SPA-110 trifluoroacetate

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Taltobulin trifluoroacetate (HTI-286 trifluoroacetate), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin trifluoroacetate inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
  • HY-128774
    AM-6494

    Beta-secretase Neurological Disease
    AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM).
  • HY-N2177
    3-Dehydrotrametenolic acid

    Lactate Dehydrogenase Apoptosis Cancer
    3-​Dehydrotrametenolic acid, isolated from the sclerotium of Poria cocos, is a lactate dehydrogenase (LDH) inhibitor. 3-​Dehydrotrametenolic acid promotes adipocyte differentiation in vitro and acts as an insulin sensitizer in vivo. 3-​Dehydrotrametenolic acid induces apoptosis and has anticancer activity.
  • HY-15584B
    Taltobulin hydrochloride

    HTI-286 hydrochloride; SPA-110 hydrochloride

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Taltobulin hydrochloride (HTI-286 hydrochloride), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin hydrochloride inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
  • HY-15584
    Taltobulin

    HTI-286; SPA-110

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Taltobulin (HTI-286), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
  • HY-15473
    MLN120B

    ML120B

    IKK Cancer
    MLN120B (ML120B) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis.
  • HY-B0761
    (R,R)-Glycopyrrolate

    (R,R)-Glycopyrronium bromide; (R,R)-Glycopyrrolate bromide

    mAChR Neurological Disease
    (R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) is an anticholinergic agent. (R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) has the ability to reduce the frequency of drooling in vivo with developmental disabilities.
  • HY-15473A
    MLN120B dihydrochloride

    ML120B dihydrochloride

    IKK Cancer Inflammation/Immunology
    MLN120B dihydrochloride (ML120B dihydrochloride) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis.
  • HY-76915
    24, 25-Dihydroxy VD3

    VD/VDR Endogenous Metabolite Metabolic Disease
    24, 25-Dihydroxy VD3 is a compound which is closely related to 1,25-dihydroxyvitamin D3, the active form of vitamin D3, but like vitamin D3 itself and 25-hydroxyvitamin D3 is inactive as a hormone both in vitro and in vivo.
  • HY-107222
    Lysionotin

    Others Inflammation/Immunology
    Lysionotin is a flavonoid isolated from few flower lysionotus herbs. Lysionotin efficiently inhibit α-Toxin (a pore-forming protein) expression and shows significant protection against S. aureus in vitro and in vivo. Lysionotin has the potential for the treatment of S. aureus induced pneumonia.
  • HY-12648A
    FASN-IN-4 tosylate

    Fatty Acid Synthase (FASN) Cancer
    FASN-IN-4 tosylate is a potent inhibitor of fatty acid synthase (FASN) extracted from patent WO 2012064642 A1, compound 29; has an IC50 of 10 nM.
  • HY-130836
    LpxH-IN-AZ1

    Bacterial Infection
    LpxH-IN-AZ1, a sulfonyl piperazine compound, is a potent UDP-2,3-diacylglucosamine pyrophosphate hydrolase LpxH inhibitor. LpxH-IN-AZ1 is a potent inhibitor of Klebsiella pneumoniae LpxH with IC50 of 0.36 μM .
  • HY-122615
    SPOP-IN-6b

    Others Cancer
    SPOP-IN-6b is a speckle-type POZ protein (SPOP) inhibitor extracted from patent CN 107141287, SPOP-B-88.
  • HY-114181
    IRAK4-IN-4

    IRAK Inflammation/Immunology
    IRAK4-IN-4 is an interleukin-1 receptor–associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM. IRAK4-IN-4 also inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM.
  • HY-18709
    Tyk2-IN-3

    JAK Inflammation/Immunology
    Tyk2-IN-3 is a Tyk2 pseudokinase inhibitor, with an IC50 of 485 nM.
  • HY-122627
    Mcl1-IN-8

    Bcl-2 Family Cancer
    Mcl1-IN-8 (Comp8) is a Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. Mcl1-IN-8 (Comp8) exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells.
  • HY-U00444
    DDR1-IN-2

    Discoidin Domain Receptor Inflammation/Immunology
    DDR1-IN-2 is a potent inhibitor of discoidin domain receptor 1 (DDR1), with an IC50 of 13.1 nM, and also less potently inhibits DDR2, with an IC50 of 203 nM.
  • HY-136301
    Acid secretion-IN-1

    Others Inflammation/Immunology
    Acid secretion-IN-1 is a polycyclic compound extracted from patent WO2018024188A1, Compound Example 17.4. Acid secretion-IN-1 is synthesized and used in the IDO inhibitor synthetic experiment.
  • HY-116505
    JAK1-IN-4

    JAK Cancer
    JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM).
  • HY-101805
    SK1-IN-1

    SPHK Inflammation/Immunology Cancer
    SK1-IN-1 is a potent sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 58 nM.
  • HY-111778
    EHMT2-IN-1

    Histone Methyltransferase Cancer
    EHMT2-IN-1 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disorder or cancer.
  • HY-112275
    TNF-α-IN-1

    TNF Receptor Cancer Inflammation/Immunology
    TNF-α-IN-1 is a TNF-α inhibitor extracted from patent US20030096841A1, compound example I-7.
  • HY-100182
    BACE1-IN-1

    Beta-secretase Neurological Disease
    BACE1-IN-1 is a potent and highly brain penetrant BACE1 inhibitor with IC50s of 32 and 47 nM for human BACE1 and BACE2, respectively.
  • HY-130684
    MDM2-IN-1

    MDM-2/p53 Cancer
    MDM2-IN-1 (Compound 30) is a synthetic MDM2-p53 interaction (MDM2) inhibitor and contains the trans (D-)configuration.
  • HY-128343
    KDM4-IN-2

    Histone Demethylase Cancer
    KDM4-IN-2 (Compound 19a) is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively.
  • HY-101523
    Cdc7-IN-1

    CDK Cancer
    Cdc7-IN-1 (Compound 13) is a highly potent, selective and ATP competitive inhibitor of Cdc7 kinase, with an IC50 value of 0.6 nM at 1 mM ATP and with slow off-rate characteristics. Cdc7-IN-1 potently inhibits Cdc7 activity in cancer cells, and effectively induces cell death.
  • HY-18787
    c-Fms-IN-2

    c-Fms Inflammation/Immunology
    c-Fms-IN-2 is a FMS kinase inhibitor with an IC50 of 0.024 μM.
  • HY-130518
    Cdc7-IN-6

    CDK Cancer
    Cdc7-IN-6 (compound I-D) is a potent Cdc7 kinase inhibitor (IC50=4 nM), extracted from patent WO2019165473A1, compound I- D, has anti-tumor activity.
  • HY-101098
    PD-1-IN-18

    PD-1/PD-L1 Inflammation/Immunology
    PD-1-IN-18 is a PD1 signaling pathway inhibitor, which acts as an immunomodulator.
  • HY-135967
    MTH1-IN-2

    DNA/RNA Synthesis Cancer
    MTH1-IN-2 is a MutT homolog 1 (MTH1) inhibitor extracted from patent WO2016135138A1, Compound (6), MTH1-IN-2 can be used for the research of cancer. Anti-tumor activity.
  • HY-16434
    DGAT1-IN-3

    Acyltransferase Metabolic Disease
    DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with the IC50s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome.
  • HY-100859
    LSD1-IN-5

    Histone Demethylase Cancer
    LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
  • HY-13994
    Mps1-IN-2

    Mps1 Polo-like Kinase (PLK) Cancer
    Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.
  • HY-U00346
    DPP-IV-IN-1

    Dipeptidyl Peptidase Metabolic Disease
    DPP-IV-IN-1 is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV), a highly specific serine protease, with an IC50 of 4.6 nM.
  • HY-136464
    β-catenin-IN-2

    β-catenin Cancer
    β-catenin-IN-2 is a potent β-catenin inhibitor, compound H1B1, extracted from patent US20150374662A1. β-catenin-IN-2 can be used for the study of colorectal cancer.
  • HY-18791
    c-Fms-IN-1

    c-Fms Inflammation/Immunology
    c-Fms-IN-1 is a FMS kinase inhibitor with an IC50 of 0.0008 μM.
  • HY-18744
    FLT3-IN-2

    FLT3 Cancer
    FLT3-IN-2 is a FLT3 inhibitor with IC50 of < 1 μM, detailed information refer to WO 2012158957 A2 and WO 2007013896.
  • HY-128607
    Mcl1-IN-9

    Bcl-2 Family Cancer
    Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM.
  • HY-111905
    BRD7-IN-1

    Epigenetic Reader Domain Cancer
    BRD7-IN-1, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively).
  • HY-101031
    c-met-IN-1

    c-Met/HGFR Cancer
    c-met-IN-1 (compound 16) is a potent and selective c-Met inhibitor, with IC50 of 1.1 nM, with antitumor activity..
  • HY-103033
    T.cruzi-IN-1

    Parasite Infection
    T.cruzi-IN-1 is a potent Trypanosoma cruzi inhibitor with an IC50 of 8 nM. T.cruzi-IN-1, a 4-trifluoromethyl substituted analog, has the potential for both the acute and chronic stages of Chagas disease.
  • HY-110347
    Mps1-IN-1 dihydrochloride

    Mps1 Cancer
    Mps1-IN-1 dihydrochloride is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM.
  • HY-136339
    Cbl-b-IN-1

    E1/E2/E3 Enzyme Inflammation/Immunology
    Cbl-b-IN-1 (example 519) is a Cbl-b inhibitor, extracted from patent WO2019148005A1, with an IC50 <100 nM.
  • HY-111887
    RAD51-IN-2

    RAD51 Cancer
    RAD51-IN-2 (compound example 67A) is a RAD51 inhibitor extracted from patent WO2019/051465A1.
  • HY-129168
    USP7-IN-5

    Deubiquitinase Cancer
    USP7-IN-5 is a potent ubiquitin specific protease 7 (USP7) inhibitor extracted from patent WO2017212012A1, example 40, has an IC50 of 49.9 nM.
  • HY-130608
    Mutated EGFR-IN-3

    EGFR Cancer
    Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively.
  • HY-100004
    Fumarate hydratase-IN-1

    Mitochondrial Metabolism Cancer
    Fumarate hydratase-IN-1 (compound 2) is a cell-permeable fumarate hydratase inhibitor. Fumarate hydratase-IN-1 has antiproliferative activity against several cancer cell lines with a mean IC50 of 2.2 μM.
  • HY-135642
    SMS1-IN-1

    Others Inflammation/Immunology
    SMS1-IN-1, compound SAPA 1j, is a novel and the most potent sphingomyelin synthase 1 (SMS1) inhibitor with an IC50 value of 2.1 μM. SMS1-IN-1 has the potential for the treatment of atherosclerosis.
  • HY-U00352
    PDE IV-IN-1

    Phosphodiesterase (PDE) Inflammation/Immunology
    PDE IV-IN-1 is an inhibitor of phosphodiesterase IV, used for the research of asthma, COPD or other inflammatory diseases.
  • HY-117535
    CDK2-IN-4

    CDK Cancer
    CDK2-IN-4 is a potent and selective CDK2 inhibitor with an IC50 of 44 nM for CDK2/cyclin A, shows 2,000-fold selectivity over CDK1/cyclin B (IC50=86 uM).
  • HY-101922
    IRAK4-IN-1

    IRAK Inflammation/Immunology
    IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.
  • HY-130001
    CDK9-IN-9

    CDK Cancer
    CDK9-IN-9 (example 2) is a potent and selective CDK9 inhibitor with an IC50 of 1.8 nM. CDK9-IN-9 inhibits CDK2 with an IC50 of 155 nM. CDK9-IN-9 has anti-cancer activity.
  • HY-130852
    CDK9-IN-11

    CDK Ligand for Target Protein for PROTAC Cancer
    CDK9-IN-11 is a potent CDK9 inhibitor. CDK9-IN-11 is the ligand for the PROTAC CDK9 Degrader-1 (HY-103628).
  • HY-129169
    USP7-IN-6

    Deubiquitinase Cancer
    USP7-IN-6 is a potent ubiquitin specific protease 7 (USP7) inhibitor, extracted from patent WO2017212010A1, example 25, has an IC50 of 6.8 nM.
  • HY-131064
    RIPK3-IN-1

    RIP kinase Inflammation/Immunology
    RIPK3-IN-1 is a RIPK3 type II DFG-out inhibitor with an IC50 of 9.1 nM. RIPK3-IN-1 inhibits RIPK1 and RIPK2 with IC50s of 5.5 and >10 μM. RIPK3-IN-1 is also a c-Met kinase inhibitor with an IC50 of 1.1 μM.
  • HY-128523A
    Kgp-IN-1 hydrochloride

    Others Inflammation/Immunology
    Kgp-IN-1 hydrochloride is an arginine-specific gingipain (Rgp) inhibitor extracted from patent WO2017201322A1, compound 13-R.
  • HY-111820
    CK1-IN-1

    Casein Kinase Inflammation/Immunology
    CK1-IN-1 is a casein kinase 1 (CK1) inhibitor extracted from patent WO2015119579A1, compound 1c, has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively.
  • HY-101516
    CYP17-IN-1

    Cytochrome P450 Cancer
    CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC50s of 15.8 and 20.1 nM.
  • HY-135232
    MMP-9-IN-1

    MMP Cancer
    MMP-9-IN-1 is a specific matrix metalloproteinase-9 (MMP-9) inhibitor, which selectively target the hemopexin (PEX) domain of MMP-9, but not other MMPs.
  • HY-15240
    c-Kit-IN-1

    c-Kit c-Met/HGFR Cancer
    c-Kit-IN-1 is a potent inhibitor of c-Kit and c-Met with IC50s of <200 nM.
  • HY-12826
    Mcl1-IN-2

    Bcl-2 Family Cancer
    Mcl1-IN-2 is an inhibitor of myeloid cell factor 1 (Mcl-1).
  • HY-16462
    CDK9-IN-2

    CDK Infection
    CDK9-IN-2 is a special cyclin-dependent kinase 9 (CDK9) inhibitor, extracted from patent WO/2012131594A1, compound CDKI(8), has an IC50 of 5 nM and 7 nM in H929 multiple myeloma(MM) cell line (72 hours) and A2058 skin cell line (72 hours), respectively.
  • HY-121832
    DDX3-IN-1

    HIV HCV Infection
    DDX3-IN-1 (Compound 16f) is a DEAD-box polypeptide 3 (DDX3) inhibitor with CC50s of 50 and 36 μM for HIV and HCV, respectively. Antiviral activity.
  • HY-12795
    Vps34-IN-1

    PI3K Autophagy Cancer
    Vps34-IN-1 is an inhibitor of Vps34 extracted from patent WO2012085815A1, compound example 16a, with an IC50 of 4 nM. Vps34-IN-1 modulates autophagy.
  • HY-128341
    ERK5-IN-2

    ERK Cancer Cardiovascular Disease
    ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis.
  • HY-136556
    Factor B-IN-1

    Others Inflammation/Immunology
    Factor B-IN-1 is a Factor B inhibitor extracted from patent WO2013164802A1, Example 24.
  • HY-101547
    TRPC6-IN-1

    TRP Channel Cancer
    TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM.
  • HY-13075
    c-Fms-IN-3

    c-Fms Inflammation/Immunology
    c-Fms-IN-3 is a novel c-Fms kinase inhibitor with a potential as anti-inflammatory agent and antirheumatic agent.
  • HY-119933
    RIPK1-IN-7

    RIP kinase Cancer
    RIPK1-IN-7 is a potent and selective RIPK1 inhibitor with a Kd of 4 nM and an enzymatic IC50 of 11 nM. RIPK1-IN-7 exhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model.
  • HY-103483
    MD2-IN-1

    Toll-like Receptor (TLR) Inflammation/Immunology
    MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD of 189  μM for the recombinant human MD2 (rhMD2).
  • HY-124029
    MMP13-IN-3

    MMP Inflammation/Immunology
    MMP13-IN-3 is a potent, selective, and orally active MMP-13 inhibitor (IC50=1 nM) for the potential treatment of osteoarthritis. MMP13-IN-3 is >1000 selective over other MMPs.
  • HY-126294
    JAK1-IN-7

    JAK Inflammation/Immunology
    JAK1-IN-7 is a Janus-associated kinase 1 (JAK1) inhibitor extracted from patent WO2018134213A1, Example 63, has an anti-inflammatory effect.
  • HY-100864
    mPGES1-IN-3

    PGE synthase Inflammation/Immunology
    mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM).
  • HY-114460
    SHP2 IN-1

    Phosphatase Others
    SHP2 IN-1 (compound 13) is an allergic inhibitor of SHP2 (PTPN11), with an IC50 of 3 nM.
  • HY-U00275
    COX-2-IN-1

    COX Inflammation/Immunology
    COX-2-IN-1 is potent and slective COX-2 inhibitor with an IC50 of 3.9 μM.
  • HY-101853
    STAT5-IN-1

    STAT Cancer
    STAT5-IN-1 is a STAT5 inhibitor with an IC50 of 47 μM for STAT5β isoform.
  • HY-126137
    PDE9-IN-1

    Phosphodiesterase (PDE) Neurological Disease
    PDE9-IN-1 is a potent, selective, and orally bioavailable phosphodiesterase-9A (PDE9A) Inhibitor with an IC50 of 8.7 nM.
  • HY-112165
    PRMT5-IN-2

    Histone Methyltransferase Cancer
    PRMT5-IN-2 is a rotein arginine methyltransferase 5 (PRMT5) inhibitor extracted from patent WO2018130840A1, compound 3.
  • HY-126251
    CDK9-IN-7

    CDK Apoptosis Cancer
    CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC.
  • HY-100759
    JAK2-IN-4

    JAK Cancer
    JAK2-IN-4 (compound 16h) is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively.
  • HY-135273
    BCL2-IN-1

    Bcl-2 Family Cancer
    BCL2-IN-1 is a potent Bcl-2 inhibitor. BCL2-IN-1 binds Bcl-2 with a Ki of <0.01 nM.
  • HY-12426A
    mAChR-IN-1 hydrochloride

    mAChR Neurological Disease
    mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM.
  • HY-12473
    Vps34-IN-2

    PI3K Cancer
    Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively.
  • HY-101025
    Nrf2-IN-1

    Keap1-Nrf2 Cancer
    Nrf2-IN-1 is an inhibitor of nuclear factor-erythroid 2-related factor 2 (Nrf2). Nrf2-IN-1 is developed for the research of acute myeloid leukemia (AML).
  • HY-130240
    GCN2-IN-6

    Eukaryotic Initiation Factor (eIF) Cancer
    GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells).
  • HY-U00390
    JAK3-IN-7

    JAK Cancer
    JAK3-IN-7 is a potent and selective JAK3 inhibitor extracted from patent WO2011013785A1, has an IC50 of <0.01 μM.
  • HY-111467
    Mcl1-IN-4

    Bcl-2 Family Cancer
    Mcl1-IN-4 is an inhibitor of Mcl1 with an IC50 of 0.2 μM.
  • HY-112815
    ALK2-IN-2

    TGF-β Receptor Cancer
    ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3.
  • HY-U00430
    MGAT2-IN-2

    Acyltransferase Metabolic Disease
    MGAT2-IN-2 is a potent and selective acyl CoA:monoacylglycerol acyltransferase 2 (MGAT2) inhibitor with an IC50 of 3.4 nM.
  • HY-126290A
    Tyk2-IN-9

    JAK Inflammation/Immunology
    Tyk2-IN-9 is a potent,selective and specific inhibitor of JAK kinases, inhibits Tyk2, JAK1 and JAK2 with IC50 values of 6 nM, 21nM and 6nM, respectively. Tyk2-IN-9, example 19, is extracted from patent US2017240552A1.
  • HY-128352
    SMYD3-IN-1

    Histone Methyltransferase Cancer
    SMYD3-IN-1 (compound 29) is an irreversible and selective inhibitor of SMYD3 (SET and MYND domain containing 3), with an IC50 of 11.7 nM.
  • HY-100860
    LSD1-IN-6

    Histone Demethylase Cancer
    LSD1-IN-6 (Compound 4m) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 123 nM. LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
  • HY-136526
    BCR-ABL-IN-3

    Bcr-Abl Cancer
    BCR-ABL-IN-3 is a potent and irreversible Bcr-Abl inhibitor with an IC50 of ≤100 nM for Ba/F3Bcr-Abl T3151. BCR-ABL-IN-3 has anti-cancer activity.
  • HY-103082
    CLK1-IN-1

    CDK Others
    CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 (CLK1) inhibitor, with an IC50 of 2 nM.
  • HY-133018A
    HCV-IN-7 hydrochloride

    HCV Cancer
    HCV-IN-7 hydrochloride is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 hydrochloride shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 hydrochloride has anti-viral activity.
  • HY-109585
    IRAK4-IN-7

    IRAK Cancer Inflammation/Immunology
    IRAK4-IN-7 is a selective, potent and orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor, extracted from patent WO2015104688 (example 1). IRAK4-IN-7 has the potential for cancer and inflammatory diseases treatment.
  • HY-103492
    CDK8-IN-1

    CDK Cancer
    CDK8-IN-1 is a potent and selective CDK8 inhibitor with an IC50 of 3 nM.
  • HY-102035
    PARP-2-IN-1

    PARP Cancer
    PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC50 of 11.5 nM.
  • HY-108319
    DPP-IV-IN-2

    Dipeptidyl Peptidase Inflammation/Immunology Neurological Disease
    DPP-IV-IN-2 is an inhibitor of both dipeptidyl peptidase IV (DPIV) and DP8/9 with IC50s of 0.1 and 0.95 μM, respectively.
  • HY-129171
    TGFBR1-IN-1

    TGF-β Receptor Cancer Inflammation/Immunology
    TGFBR1-IN-1 is an ALK5 inhibitor extracted from patent WO2018004290A1, Compound 33, has an IC50 of 10-100 nM.
  • HY-18967
    Aldose reductase-IN-1

    Aldose Reductase Metabolic Disease
    Aldose reductase-IN-1 is a inhibitor of aldose reductase with IC50 of 28.9 pM.
  • HY-136604
    RAD51-IN-3

    RAD51 Cancer
    RAD51-IN-3 is a Rad51 inhibitor extracted from patent WO2019051465A1, compound Example 66A.
  • HY-128860
    Mutated EGFR-IN-2

    EGFR Cancer
    Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=<1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity.
  • HY-18819
    BCR-ABL-IN-2

    Bcr-Abl Cancer
    BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1 native and ABL1 T315I, respectively.
  • HY-135893
    SGK1-IN-2

    SGK Inflammation/Immunology
    SGK1-IN-2 (14h) is a selective SGK1 (serum and glucocorticoid regulated kinase 1) inhibitor, with an IC50 of 5 nM at 10 μM ATP concentration.
  • HY-128355
    IDO/TDO-IN-1

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO/TDO-IN-1 (compound 25) is a highly potent and orally active dual indoleamine-2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO) inhibitor with IC50s of 9.7 and 47 nM, respectively .
  • HY-130516
    Cdc7-IN-4

    CDK Cancer
    Cdc7-IN-4 (compound I-C) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-C. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
  • HY-133554
    ASK1-IN-1

    p38 MAPK Inflammation/Immunology
    ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC50=138 nM; Biochemical IC50=21 nM).
  • HY-133669
    DDR1-IN-5

    Discoidin Domain Receptor Cancer
    DDR1-IN-5 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC50 of 7.36 nM. DDR1-IN-5 inhibits auto-phosphorylation DDR1b (Y513) with an IC50 of 4.1 nM. DDR1-IN-5 has anti-cancer activity.
  • HY-100862
    BRCA1-IN-2

    PARP Cancer
    BRCA1-IN-2 (compound 15) is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1 with an IC50 of 0.31 μM and a Kd of 0.3 μM, which shows antitumor activities via the disruption of BRCA1 (BRCT)2/protein interactions.
  • HY-133126
    hDDAH-1-IN-1

    Others Cancer Inflammation/Immunology
    hDDAH-1-IN-1 (compound 8a) is a potent and selective non-amino acid catalytic site inhibitor of human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1), with a Ki of 18 µM.
  • HY-123834
    FEN1-IN-1

    Others Cancer
    FEN1-IN-1 (compound 1) is a flap endonuclease 1 (FEN1) inhibitor. FEN1-IN-1 binds to the active site of FEN1 and partly achieves inhibition by the co-ordination of Mg 2+ ions.
  • HY-102041
    SMS2-IN-1

    Others Inflammation/Immunology
    SMS2-IN-1 is a highly selective sphingomyelin synthase 2 (SMS2) inhibitor with an IC50 of 6.5 nM.
  • HY-101430
    PGD2-IN-1

    Others Inflammation/Immunology
    PGD2-IN-1 is an antagonist of DP extracted from patent WO 2006044732 A2, example 15 (d); has an IC50 of 0.3 nM.
  • HY-103695
    CD73-IN-1

    CD73 Cancer
    CD73-IN-1 is an inhibitor of CD73 which can be used in the treatment of cancer extracted from patent WO 2017153952 A1, example 80.
  • HY-16669
    Mcl1-IN-1

    Bcl-2 Family Cancer
    Mcl1-IN-1 is an inhibitor of myeloid cell factor 1 (Mcl-1) (IC50=2.4 µM).
  • HY-136484
    FEN1-IN-3

    Others Cancer
    FEN1-IN-3 (Compound 4) is a human flap endonuclease-1 (hFEN1) inhibitor. FEN1-IN-3 stabilizes hFEN1 with an EC50 of 6.8 μM.
  • HY-130244
    BACE1-IN-5

    Beta-secretase Neurological Disease
    BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux.
  • HY-12834
    MK2-IN-1

    MAPKAPK2 (MK2) Cancer
    MK2-IN-1 is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.
  • HY-128682
    PGAM1-IN-2

    Phosphatase Cancer
    PGAM1-IN-2 is a phosphoglycerate mutase 1 (PGAM1) inhibitor with an IC50 of 2.1 μM.
  • HY-111753
    WDR5-IN-4

    Histone Methyltransferase Cancer
    WDR5-IN-4 is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity.
  • HY-12622
    HSP70-IN-1

    HSP Cancer
    HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
  • HY-14403
    ERK5-IN-1

    ERK Cancer
    ERK5-IN-1 is a potent ERK5 inhibitor with an IC50 of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC50 of 26 nM.
  • HY-128572
    FLT3-IN-6

    FLT3 Cancer
    FLT3-IN-6 is a potent and selective inhibitor of FLT3-ITD (FLT3 mutation) with an IC50 of 1.336 nM.
  • HY-136557
    PAD2-IN-1

    Protein Arginine Deiminase Cancer Inflammation/Immunology
    PAD2-IN-1, a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. PAD2-IN-1 shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold).
  • HY-102048
    STAT5-IN-2

    STAT Cancer
    STAT5-IN-2 is a STAT5 inhibitor with EC50s of 9 μM and 5 μM in K562 and KU812 cells, respectively. Potent antileukemic effect.
  • HY-100891
    CD80-IN-3

    Others Inflammation/Immunology
    CD80-IN-3, a potent CD80 inhibitor, inhibits CD80/CD28 interaction with an EC50 of 630 nM and a Kd of 125 nM.
  • HY-126290
    Tyk2-IN-8

    JAK Inflammation/Immunology
    Tyk2-IN-8 (compound 10) is a selective TYK2 inhibitor, which binds to TYK2 catalytically active JH1 domain with an IC50 of 17 nM, used in the treatment of psoriasis.
  • HY-111745
    Tyk2-IN-5

    JAK Inflammation/Immunology
    Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα. Highly effective in inhibiting IFNγ production in a rat pharmacodynamics model and fully efficacious in a rat adjuvant arthritis model.
  • HY-103620
    ROCK2-IN-2

    ROCK Inflammation/Immunology
    ROCK2-IN-2 is a selective ROCK2 inhibitor extracted from patent US20180093978A1, Compound A-30, has an IC50 of <1 μM.
  • HY-126297
    c-Fms-IN-10

    c-Fms Cancer Inflammation/Immunology
    c-Fms-IN-10 is the derivative of thieno [3,2-d] pyrimidine, an kinase inhibitor of FMS (Colony stimulating factor-1 receptor, CSF-1R) with IC50 of 2 nM. c-Fms-IN-10 has anti-tumor activity.
  • HY-112902
    OGG1-IN-08

    Others Inflammation/Immunology
    OGG1-IN-08 is a potent 8-oxoguanine DNA glycosylase-1 (OGG1) inhibitor with an IC50 value of 0.22 μM. OGG1-IN-08 decreases both the glycosylase and lyase activities of OGG1.
  • HY-112444
    BACE1-IN-2

    Beta-secretase Neurological Disease
    BACE1-IN-2 is a 1,4-Oxazine β-Secretase 1 (BACE1) inhibitor with an IC50 of 22 nM.
  • HY-131132
    SHP2-IN-6

    Phosphatase Cancer
    SHP2-IN-6 is a potent SHP2 inhibitor, extracted from patent WO2017211303A1, compound 7, has an IC50 of 25.8 nM.
  • HY-126242S
    Tyk2-IN-7

    JAK Inflammation/Immunology
    Tyk2-IN-7 (Compound 48) is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 (Compound 48) provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 (Compound 48) provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model.
  • HY-122629
    DRAK2-IN-1

    DAPK Others
    DRAK2-IN-1, compound 16, is a potent, selective and ATP-competitive DRAK2 inhibitor with IC50and Kivalues of 3 nM and 0.26 nM, respectively. DRAK2-IN-1 also has inbitory effect on DRAK1 (IC50=51 nM).
  • HY-112704
    PDE5-IN-2

    Phosphodiesterase (PDE) Cardiovascular Disease
    PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity.
  • HY-18625
    VEGFR-2-IN-5

    VEGFR Cancer
    VEGFR-2-IN-5 is a VEGFR2 inhibitor extracted from patent WO2013055780A1, Page 31.
  • HY-128605
    PD-1-IN-22

    PD-1/PD-L1 Cancer
    PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction inhibitor with an IC50 of 92.3 nM.
  • HY-U00003
    ICAM-1-IN-1

    Integrin Inflammation/Immunology
    ICAM-1-IN-1 is a potent and selective inhibitor of E-selectin and ICAM-1 with IC50 values of 7 and 5 nM, respectively.
  • HY-U00308
    5-Lipoxygenase-In-1

    Lipoxygenase Inflammation/Immunology Cardiovascular Disease
    5-Lipoxygenase-In-1 is a 5-Lipoxygenase inhibitor extracted from patent EP 331232 A2, table 4, compound example 4.10.
  • HY-102049
    IL-15-IN-1

    Interleukin Related Inflammation/Immunology
    IL-15-IN-1 is a potent and selective Interleukin 15 (IL-15) inhibitor, inhibiting the proliferation of IL-15-dependent cells with an IC50 of 0.8 μM.
  • HY-129910
    FABP5-IN-1

    FABP Inflammation/Immunology
    FABP5-IN-1(Compounds 4j) is a selective and high affinity fatty acid binding protein 5 (FABP5) inhibitor with a Ki value of 1.7 μM, and does not bind to both FABP3 and FABP7. FABP5-IN-1 shows potent antinociceptive effects.
  • HY-135858
    SARS-CoV-IN-3

    SARS-CoV Parasite HIV Infection
    SARS-CoV-IN-3 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-3 shows anti-Coronavirus activity with an EC50 of 3.6 μM in Vero cells. SARS-CoV-IN-3 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 11.7 and 20.4 nM; and IC90s of 29.19 and 56 nM; respectively. SARS-CoV-IN-3 reduces HIV-1-induced cytopathic effect with an EC50 of 10 μM in MT-4 cells.
  • HY-124768
    PDE12-IN-3

    Phosphodiesterase (PDE) Infection Inflammation/Immunology
    PDE12-IN-3 is a phosphodiesterase 12 (PDE12) inhibitor with a pXC50 of 7.68. Antiviral activity.
  • HY-13979
    DDR1-IN-1

    Discoidin Domain Receptor Cancer
    DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM).
  • HY-100531
    DprE1-IN-2

    Bacterial Infection
    DprE1-IN-2 (compound 18) is a potent DprE1 inhibitor with an IC50 of 28 nM. DprE1-IN-2 has antituberculosis effect.
  • HY-U00299
    LTB4-IN-1

    Leukotriene Receptor Inflammation/Immunology
    LTB4-IN-1 (Compound 6) is a leukotriene synthesis (LTB4) inhibitor with an IC50 of 70 nM.
  • HY-136362
    c-Fms-IN-12

    c-Fms Cancer Inflammation/Immunology
    c-Fms-IN-12 is a c-Fms inhibitor extracted from patent WO2011079076A1, Compound Example 65, has an IC50 of 93.6-283.7 nM.
  • HY-19544
    JAK3-IN-1

    JAK Cancer
    JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM).
  • HY-103081
    β-Glucuronidase-IN-1

    Bacterial Cancer Infection
    β-Glucuronidase-IN-1 is a potent, selective, uncompetitive, and orally active E. coli bacterial β-glucuronidase inhibitor, exhibiting an IC50 and a Ki of 283 nM and 164 nM, respectively.
  • HY-125841
    EGFR mutant-IN-1

    EGFR Cancer
    EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFR L858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFR WT (IC50 >1.0 μM).
  • HY-100325
    NHE3-IN-1

    Sodium Channel Neurological Disease
    NHE3-IN-1 is a sodium/proton exchanger type 3 (NHE-3) inhibitor extracted from patent WO 2011019784 A1.
  • HY-128766
    CHK1-IN-4

    Checkpoint Kinase (Chk) Cancer
    CHK1-IN-4 (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 has anti-tumor activity.
  • HY-100270
    Rho-Kinase-IN-1

    ROCK Cancer
    Rho-Kinase-IN-1 is a Rho kinase (ROCK) inhibitor (Ki values of 30.5 and 3.9 nM for ROCK1 and ROCK2, respectively) extracted from US20090325960A1, compound 1.008.
  • HY-111471A
    JAK-IN-5 hydrochloride

    JAK Inflammation/Immunology
    JAK-IN-5 hydrochloride is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283.
  • HY-111342
    HDAC8-IN-1

    HDAC Cancer
    HDAC8-IN-1 is a HDAC8 inhibitor with an IC50 of 27.2 nM.
  • HY-128588
    STAT3-IN-3

    STAT Cancer
    STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3).
  • HY-101655
    COX-2-IN-2

    COX Inflammation/Immunology
    COX-2-IN-2 is a selective and inducible COX2 inhibitor with an IC50 of 0.24 μM. COX-2-IN-1 is an anti-inflammatory compound with anti-inflammatory and analgesic activities.
  • HY-136199
    SIRT1-IN-1

    Sirtuin CMV Infection
    SIRT1-IN-1 is a selective SIRT1 inhibitor with an IC50 of 0.205 μM. SIRT1-IN-1 inhibits SIRT2 with an IC50 of 11.5 μM. SIRT1-IN-1, a indole, is a cytomegalovirus (CMV) inhibitors and has antiviral activity.
  • HY-114173
    DDR1-IN-4

    Discoidin Domain Receptor Inflammation/Immunology
    DDR1-IN-4 (Compound 2.45) is a selective and potent Discoidin Domain Receptor 1 (DDR1) autophosphorylation inhibitor, with IC50 values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively.
  • HY-19617A
    EGFR-IN-1 hydrochloride

    EGFR Cancer
    EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-126296
    RIPK1-IN-3

    RIP kinase Inflammation/Immunology
    RIPK1-IN-3 (Example 38), a RIPK1 inhibitor, extracted from patent WO2018148626A1, possesses anti-inflammatory proprieties.
  • HY-109562
    GRK2-IN-1

    Others Cardiovascular Disease
    GRKs-IN-1, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=30 nM) and GRK5 (IC50=7.1 μM). GRKs-IN-1 is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine.
  • HY-112062
    POL1-IN-1

    DNA/RNA Synthesis Cancer
    POL1-IN-1 is a RNA polymerase 1 (POL1, also known as Pol I) inhibitor with an IC50 of less than 0.5 uM. POL1-IN-1 inhibits ribosome biogenesis by inhibiting POL1 transcription.
  • HY-133121
    WDR5-IN-1

    Histone Methyltransferase Apoptosis Cancer
    WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.
  • HY-102039
    CDK9-IN-8

    CDK Cancer
    CDK9-IN-8 is a highly effective and selective CDK9 inhibitor with an IC50 of 12 nM.
  • HY-12425
    DGAT1-IN-1

    Acyltransferase Metabolic Disease
    DGAT1-IN-1 is a potent DGAT1 inhibitor with IC50 of < 10 nM(cell lysate from Hep3B cells overexpressing human DGAT1).
  • HY-128680
    c-Fms-IN-9

    c-Fms Cancer
    c-Fms-IN-9 is a c-FMS inhibitor extracted from patent WO2014145023A1, Compound Example 7. c-Fms-IN-9 inhibits unphosphorylated c-FMS kinase (uFMS) and uKIT with IC50s of <0.01 μM and 0.1-1 μM, respectively.
  • HY-130517
    Cdc7-IN-5

    CDK Cancer
    Cdc7-IN-5 (compound I-B) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
  • HY-130515
    Cdc7-IN-3

    CDK Cancer
    Cdc7-IN-3 (compound I-A) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
  • HY-126256
    PRMT5-IN-1

    Histone Methyltransferase Cancer
    PRMT5 IN-1, a hemiaminal, is a covalent protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.
  • HY-119942
    c-Fms-IN-8

    c-Fms Cancer
    c-Fms-IN-8 (compound 4a) is a colony stimulating factor-1 receptor (CSF-1R, c-FMS) Type II inhibitor, with an IC50 of 9.1 nM.
  • HY-112427
    Sirt2-IN-1

    Sirtuin Cancer Inflammation/Immunology
    Sirt2-IN-1 (Compound 9) is a sirtuin 2 (Sirt2) inhibitor with an IC50 of 163 nM.
  • HY-100631
    FGFR4-IN-1

    FGFR Neurological Disease
    FGFR4-IN-1 is a potent inhibiotr of FGFR4 with IC50 of 0.7 nM.
  • HY-111468
    Mcl1-IN-3

    Bcl-2 Family Cancer
    Mcl1-IN-3 is an inhibitor of Mcl1 extracted from patent WO2015153959A2, compound example 57; has an IC50 and Ki of 0.67 and 0.13 μM, respectively.
  • HY-100762
    Mcl1-IN-11

    Bcl-2 Family Cancer
    Mcl1-IN-11 (Compound G) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.06 and 4.2 μM, respectively.
  • HY-129389
    O-glycosylation-IN-1

    Others Cancer
    O-glycosylation-IN-1 is a potent O-glycosylation inhibitor and is used to reduce mucin on cell surfaces. O-glycosylation-IN-1 inhibits the synthesis of mucin O-glycosylation of cellular models of human pancreatic cancer.
  • HY-111904
    EHMT2-IN-2

    Histone Methyltransferase Cancer
    EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disease or cancer.
  • HY-133145
    hDDAH-1-IN-2

    Others Neurological Disease Inflammation/Immunology
    hDDAH-1-IN-2 is a selective, orally active human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1) inhibitor. hDDAH-1-IN-2 reveals an excellent profile regarding cell toxicity/viability.
  • HY-131247
    Bcl-2-IN-2

    Bcl-2 Family Cancer Inflammation/Immunology
    Bcl-2-IN-2 is a potent and selective Bcl-2 inhibitor with an IC50 of 0.034 nM and also inhibits Bcl-xL with an IC50 of 43 nM, showing >1000-fold selectivity for Bcl-2 over Bcl-xL.
  • HY-128594
    BACE1-IN-4

    Beta-secretase Neurological Disease
    BACE1-IN-4 is a potent and highly selective BACE1 inhibitor, with an IC50 of 3.8 nM and a Ki of 1.9 nM, more selective at BACE1 over BACE2. Anti-Alzheimer’s disease.
  • HY-101295
    Pan-RAS-IN-1

    Ras Cancer
    Pan-RAS-IN-1 is a pan-Ras inhibitor that disrupts the interaction of Ras proteins and their effectors.
  • HY-19771
    amyloid P-IN-1

    Amyloid-β Cancer
    amyloid P-IN-1 is used in the research of diseases or disorders wherein depletion of serum amyloid P component (SAP), including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
  • HY-101796
    SOS1-IN-1

    Others Others
    SOS1-IN-1 is a SOS1 inhibitor.
  • HY-18599A
    Chitinase-IN-2 hydrochloride

    Others Others
    Chitinase-IN-2 hydrochloride is a insect chitinase and N- acetyl hexosaminidase inhibitor and pesticide; 50 uM/20uM compound concentration's inhibitory percentage are 98%/92% for chitinase/N- acetyl-hexosaminidase respectively.
  • HY-112700
    SHIP2-IN-1

    Phosphatase Neurological Disease
    SHIP2-IN-1 is a potent SHIP2 inhibitor, inhibits SHIP2 activity, with an IC50 of 2 µM. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer’s disease.
  • HY-101490
    PDE1-IN-2

    Phosphodiesterase (PDE) Neurological Disease
    PDE1-IN-2 is an inhibitor of PDE1 extracted from patent WO2016/55618 A1, example 31; has IC50 values of 6, 140 and 164 nM for PDE1C, PDE1B and PDE1A, respectvely.
  • HY-12759
    CARM1-IN-1

    Histone Methyltransferase Cancer
    CARM1-IN-1 is a potent and specific CARM1(Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7(IC50 > 600 uM).
  • HY-130241
    Reverse transcriptase-IN-1

    HIV Infection
    Reverse transcriptase-IN-1 (Compound 12z) is a diarylbenzopyrimidine (DABP) analogue and a potent, orally active HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively. Reverse transcriptase-IN-1 also has an IC50 value of 13.7 nM against HIV-1 reverse transcriptase enzyme.
  • HY-111947
    c-Fms-IN-6

    c-Fms Inflammation/Immunology
    c-Fms-IN-6 is a potent inhibitor of c-FMS, with an IC50 of ≤10 nM for unphosphorylated c-FMS, also weakly inhibits unphosphorylated c-KIT and PDGFR (IC50, > 1 μM). Used in the research of autoimmune diseases.
  • HY-126141
    JAK/HDAC-IN-1

    JAK HDAC Cancer
    JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC50s of 4 and 2 nM for JAK2 and HDAC, respectively.
  • HY-101773
    c-Met-IN-2

    c-Met/HGFR Cancer
    c-Met-IN-2 is a potent, selective and orally available c-Met inhibitor, with an IC50 of 0.6 nM, with antitumor activity.
  • HY-130253
    IRAK4-IN-6

    IRAK Cancer
    IRAK4-IN-6 is an orally efficacious and selective IRAK4 inhibitor with an IC50 of 4 nM, and targetes MyD88 L265P mutant diffuse large B cell lymphoma.
  • HY-130609
    Aβ42-IN-1

    γ-secretase Neurological Disease
    Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50 value of 0.091 µM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
  • HY-101762
    TyK2-IN-2

    JAK Phosphodiesterase (PDE) Inflammation/Immunology
    TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively. TyK2-IN-2 also inhibits phosphodiesterase 4 (PDE4) with an IC50 of 62 nM. TyK2-IN-2 can be used for the research of inflammatory and autoimmune diseases.
  • HY-101093
    PD-1-IN-1

    PD-1/PD-L1 Inflammation/Immunology
    PD-1-IN-1 is an inhibitor of programmed cell dealth-1 (PD-1) extracted from patent WO2015033299A1, compound example 4. PD-1-IN-1 can be used as immune modulator.
  • HY-112300
    ERK2 IN-1

    ERK Cancer
    ERK2 IN-1 is a selective ERK2 inhibitor with an IC50 of 7 nM.
  • HY-19773
    beta-lactamase-IN-1

    Bacterial Cancer
    beta-lactamase-IN-1 targets Neisseria gonorrhoeae infection which comprises administering to a subject in need thereof novel Tricyclic nitrogen containing compounds and corresponding pharmaceutical compositions as described herein.
  • HY-10875
    LRRK2-IN-1

    LRRK2 Apoptosis Neurological Disease Cancer
    LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC50 of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.
  • HY-111552
    PIM1-IN-1

    Pim Cancer
    PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity.
  • HY-12401
    Mps1-IN-3

    Mps1 Cancer
    Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC50 of 50 nM.
  • HY-15949
    Kif15-IN-2

    Kinesin Inflammation/Immunology Cardiovascular Disease Cancer
    Kif15-IN-2 is an inhibitor of the mitotic kinesin Kif15, and is used for the research of cellular proliferative diseases.
  • HY-101270
    STK16-IN-1

    Others Cancer
    STK16-IN-1 is a STK16 kinase inhibitor with an IC50 of 295 nM.
  • HY-133670
    DDR1-IN-6

    Discoidin Domain Receptor Cancer
    DDR1-IN-6 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC50 of 9.72 nM. DDR1-IN-6 inhibits auto-phosphorylation DDR1b (Y513) with an IC50 of 9.7 nM. DDR1-IN-6 has anti-cancer activity.
  • HY-128602
    c-Kit-IN-2

    c-Kit Cancer
    c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively.
  • HY-19617B
    EGFR-IN-1 TFA

    EGFR Cancer
    EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-13977A
    PKR-IN-C16

    Others Neurological Disease
    PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. PKR-IN-C16 is able to inhibit the autophosphorylation of PKR and unlock the translation blockade induced by PKR in primary neuronal cultures.
  • HY-112261
    CDK12-IN-3

    CDK Cancer
    CDK12-IN-3 is a potent and selective CDK12 inhibitor with an IC50 of 491 nM in enzymatic assay.
  • HY-111465
    CDK8-IN-4

    CDK Cancer
    CDK8-IN-4 is an inhibitor of CDK8 extracted from patent WO2014090692A1, compound example 16, with an IC50 of 0.2 nM.
  • HY-112128
    USP7-IN-3

    Deubiquitinase Cancer
    USP7-IN-3 (Compound 5) is a potent and selective allosteric ubiquitin-specific protease 7 (USP7) inhibitor.
  • HY-111948
    c-Fms-IN-7

    c-Fms Cancer Inflammation/Immunology
    c-Fms-IN-7 is a cFMS inhibitor extracted from patent WO2011079076A1, example159, has an IC50 of 18.5 nM.
  • HY-18901
    RIPK1-IN-4

    RIP kinase Inflammation/Immunology
    RIPK1-IN-4 (compound 8) is a potent and selective type II kinase inhibitor of receptor interacting protein 1 (RIP1) kinase and binds to a DLG-out inactive form of RIP1 with an IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase.
  • HY-126298
    RAF mutant-IN-1

    Raf Cancer
    RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAF V600E and B-RAF WT, respectively.
  • HY-100763
    Mcl1-IN-12

    Bcl-2 Family Cancer
    Mcl1-IN-12 (Compound F) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively. Anti-tumor activity.
  • HY-18607
    SGK1-IN-1

    SGK Inflammation/Immunology
    SGK1-IN-1 is a highly active and selective inhibitor of SGK-1, with an IC50 of 1 nM.
  • HY-100314
    BCR-ABL-IN-1

    Bcr-Abl Cancer
    BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia.
  • HY-135855
    SARS-CoV-IN-1

    SARS-CoV Parasite Infection
    SARS-CoV-IN-1 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-1 shows anti-Coronavirus activity with an EC50 of 4.9 μM in Vero cells. SARS-CoV-IN-1 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 15.4 and 133.2 nM; and IC90s of 25.7 and 459.1 nM; respectively. Antimalarial and antiviral activities.
  • HY-115470
    CLK-IN-T3

    CDK DYRK Cancer
    CLK-IN-T3 is a high potent, selective, and stable CDC-like kinase (CLK) inhibitor with IC50s of 0.67 nM, 15 nM, and 110 nM for CLK1, CLK2, and CLK3 protein kinases, respectively. CLK-IN-T3 has anti-cancer activity.
  • HY-128571
    FLT3-IN-4

    FLT3 Cancer
    FLT3-IN-4 is a potent and orally effective Fms-like tyrosine receptor kinase 3 (FLT3; IC50=7 nM) inhibitor for treating acute myelogenous leukemia.
  • HY-100863
    BRCA1-IN-1

    PARP Cancer
    BRCA1-IN-1 is a novel small-molecule-like BRCA1 inhibitor with IC50 and Ki of 0.53 μM and 0.71 μM, respecrively.
  • HY-100422
    KDM5-IN-1

    Histone Demethylase Cancer
    KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
  • HY-111369
    CHK1-IN-2

    Checkpoint Kinase (Chk) Cancer
    CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM.
  • HY-111798
    HO-1-IN-1

    Reactive Oxygen Species Cancer
    HO-1-IN-1 (Compound 2) is a heme oxygenase 1 (HO-1) inhibitor with an IC50 of 250 nM.
  • HY-101097
    PD-1-IN-17

    PD-1/PD-L1 Cancer
    PD-1-IN-17 is a programmed cell death-1 (PD-1) inhibitor extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM.
  • HY-101492
    GPR120-IN-1

    GPR120 Metabolic Disease
    GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of −7.62.
  • HY-111530
    GSTO1-IN-1

    Gutathione S-transferase Cancer
    GSTO1-IN-1 is a potent glutathione S-transferase omega 1 (GSTO1) inhibitor with an IC50 of 31 nM.
  • HY-124700
    LYPLAL1-IN-1

    Others Metabolic Disease
    LYPLAL1-IN-1 (Compound 11) is an selective covalent small-molecule inhibitor of Lysophospholipase-like 1 (LYPLAL1) with an IC50 of 0.006 μM. LYPLAL1-IN-1 increases glucose production.
  • HY-130519
    Cdc7-IN-7

    CDK Cancer
    Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
  • HY-130850
    CDK9-IN-10

    CDK Ligand for Target Protein for PROTAC Cancer
    CDK9-IN-10 is a potent CDK9 inhibitor. CDK9-IN-10 is the ligand for the PROTAC CDK9 degrader-2 (HY-112811).
  • HY-15843
    MIR96-IN-1

    MicroRNA Apoptosis Cancer
    MIR96-IN-1 selectively inhibits biogenesis of microRNA-96, upregulating a protein target (FOXO1) and inducing apoptosis in cancer cells.
  • HY-135670A
    β-glycosidase-IN-1

    Others Metabolic Disease
    β-glycosidase-IN-1 (Compound 33) is a piperidine derivative and a β-glycosidase inhibitor. β-glycosidase-IN-1 has hypoglycemic activity.
  • HY-101093B
    PD-1-IN-20

    PD-1/PD-L1 Cancer
    PD-1-IN-20 is the less active enantiomer of PD-1-IN-1. PD-1-IN-1 is an inhibitor of programmed cell dealth-1 (PD-1) extracted from patent WO 2015033299 A1, compound example 4.
  • HY-13231
    CDK9-IN-1

    CDK HIV Infection
    CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection, with an IC50 of 39 nM for CDK9/CycT1, extracted from reference, compound 87.
  • HY-101022
    CXCR2-IN-1

    CXCR Inflammation/Immunology Endocrinology
    CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3.
  • HY-129181
    FGFR4-IN-4

    FGFR Cancer
    FGFR4-IN-4 (compound 693) is a FGFR4 inhibitor with anti-tumor activity, extracted from patent WO2018113584A1.
  • HY-130607
    IDO1-IN-2

    Indoleamine 2,3-Dioxygenase (IDO) Cancer Inflammation/Immunology
    IDO1-IN-2 (compound 16) is a potent and selective IDO1 inhibitor with IC50s of 81 nM, 59 nM (mouse) and 28 nM (rat), respectively. IDO1-IN-2 has anti-cancer activity.
  • HY-18850
    MAPK13-IN-1

    p38 MAPK Autophagy Others
    MPAK13-IN-1 is a MAPK13 (p38δ) inhibitor, with an IC50 of 620 nM.
  • HY-130262
    PDE1-IN-3

    Phosphodiesterase (PDE) Inflammation/Immunology
    PDE1-IN-3, compound 4 (WO2019156861), is a selective human phosphodiesterase 1 (PDE1) inhibitor. PDE1-IN-3 inhibits PDE4D and PDE6AB with IC50 values of 23.99 μM and 10 μM, respectively.
  • HY-12813
    PDE10-IN-1

    Phosphodiesterase (PDE) Neurological Disease
    PDE10-IN-1 is a potent PDE10-IN-1 inhibitor extracted from Patent WO 2013192273 A1, for treating CNS and metabolic disorders.
  • HY-103617
    PKM2-IN-1

    Pyruvate Kinase Cancer
    PKM2-IN-1 is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM.
  • HY-136300
    PHD-1-IN-1

    HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology Cardiovascular Disease
    PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM. PHD-1-IN-1 has a unique monodentate binding interaction with the active site Fe 2+ ion and induces the formation of an “Arg367-out” pocket.
  • HY-111790
    LMP7-IN-1

    Proteasome Cancer
    LMP7-IN-1 is an inhibitor of immunoproteasome (LMP7), may used in the research of inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and cancer.
  • HY-129490
    Enpp-1-IN-1

    Others Cancer
    Enpp-1-IN-1 is a Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) inhibitor extracted from patent WO2019046778, Example 55.
  • HY-112713
    SMS2-IN-2

    Others Inflammation/Immunology
    SMS2-IN-2 is a potent, highly selective and orally active sphingomyelin synthase 2 (SMS2) inhibitor, with IC50s of 100 nM and 56 μM for SMS2 and SMS1, respectively. Anti-chronic inflammatory activity.
  • HY-135856
    SARS-CoV-IN-2

    SARS-CoV Parasite HIV Infection
    SARS-CoV-IN-2 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-2 shows anti-Coronavirus activity with an EC50 of 1.9 μM in Vero cells. SARS-CoV-IN-2 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 21.5 and 30 nM; and IC90s of 51.0 and 99.9 nM; respectively. SARS-CoV-IN-2 reduces HIV-1-induced cytopathic effect with an EC50 of 2.9 μM in MT-4 cells. Antimalarial and Antiviral Activities.
  • HY-136658
    STAT3-IN-7

    STAT Apoptosis Cancer
    STAT3-IN-7 is a Sorafenib analogue and potently inhibits the phosphorylation of STAT3. STAT3-IN-7 induces cell apoptosis through SHP-1 dependent STAT3 inactivation. STAT3-IN-7 does not inhibit kinase activity and has anticancer effects.
  • HY-13298
    Mps1-IN-1

    Mps1 Cancer
    Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM.
  • HY-136561
    GRK5-IN-2

    Others Metabolic Disease
    GRK5-IN-2 (compound 707), a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. GRK5-IN-2 regulates the expression and/or release of insulin and is useful for the metabolic disease research.
  • HY-135954
    PDK4-IN-1

    PDHK Apoptosis Cancer Metabolic Disease Inflammation/Immunology
    PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity.
  • HY-13979A
    DDR1-IN-1 dihydrochloride

    Discoidin Domain Receptor Cancer
    DDR1-IN-1 dihydrochloride is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM).
  • HY-112145
    FLT3-IN-3

    FLT3 Cancer
    FLT3-IN-3 is a potent FLT3 inhibitor with IC50s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively.
  • HY-100315
    Tyrosine kinase-IN-1

    VEGFR PDGFR FGFR Cardiovascular Disease
    Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.
  • HY-100758
    FUBP1–IN-1

    Others Cancer
    FUBP1–IN-1 is a potent FUSE binding protein 1 (FUBP1) inhibitor which interferes with the binding of FUBP1 to its single stranded target DNA FUSE sequence , with an IC50 value of 11.0 μM.
  • HY-U00343
    MAO-B-IN-1

    Monoamine Oxidase Neurological Disease
    MAO-B-IN-1 is an inhibitor of monoamine oxidase B, used for the research of neurological diseases.
  • HY-111540
    IDO1-IN-5

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
  • HY-111810
    SMYD2-IN-1

    Histone Methyltransferase Cancer
    SMYD2-IN-1 is a SMYD2 inhibitor extracted from patent WO2016166186A1, compound example 1.1, has an IC50 of 4.45 nM.
  • HY-15948
    Kif15-IN-1

    Kinesin Cancer Inflammation/Immunology Cardiovascular Disease
    Kif15-IN-1 is an inhibitor of the mitotic Kinesin family member 15 (Kif15), and is used for the research of cellular proliferative diseases.
  • HY-101857
    MGAT2-IN-1

    Acyltransferase Metabolic Disease
    MGAT2-IN-1 is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.
  • HY-128704
    c-Kit-IN-3

    c-Kit Cancer
    c-Kit-IN-3 (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC50s of 4 nM, 8 nM for c-KIT wt and c-KIT T670I, respectively. c-Kit-IN-3 displays great potencies against most of the gain-offunction mutations in the juxtamembrane domain, drugresistant mutations in the ATP binding pocket, and activation loops.
  • HY-18674
    K-Ras-IN-1

    Ras Cancer
    K-Ras-IN-1 is a K-Ras inhibitor, by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.(the detailed information refer to the reference)
  • HY-128601
    CHK1-IN-3

    Checkpoint Kinase (Chk) Cancer
    CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM.
  • HY-128681
    PGAM1-IN-1

    Phosphatase Cancer
    PGAM1-IN-1 is a phosphoglycerate mutase 1 (PGAM1) inhibitor with an IC50 of 6.4 μM.
  • HY-129531
    MuRF1-IN-1

    Others Neurological Disease
    MuRF1-IN-1 is a muscle ring finger 1 (MuRF1) inhibitor that attenuates skeletal muscle atrophy and dysfunction in cardiac cachexia.
  • HY-133125
    ERAP1-IN-1

    Others Inflammation/Immunology
    ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor. ERAP1-IN-1 competitively inhibits ERAP1 activity towards a nonamer peptide representative of physiological substrates.
  • HY-115688A
    (S)-TXNIP-IN-1

    Others Others
    (S)-TXNIP-IN-1 is the S-enantiomer of TXNIP-IN-1 (HY-115688). TXNIP-IN-1 is a TXNIP-TRX complex inhibitor which can be used in the research of TXNIP-TRX complex associated metabolic disorder (diabetes), cardiovascular disease, or inflammatory disease
  • HY-12841A
    KHK-IN-1 hydrochloride

    Others Others
    KHK-IN-1 hydrochloride is a potent ketohexokinase (KHK) inhibitor with IC50 of 12 nM, interacts with Asp-27B in the ATP-binding region of KHK.
  • HY-136485
    FEN1-IN-4

    Others Cancer
    FEN1-IN-4 (Compound 2) is a human flap endonuclease-1 (hFEN1) inhibitor.
  • HY-100753
    STAT3-IN-1

    STAT Apoptosis Cancer
    STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis.
  • HY-111463
    CDK8-IN-3

    CDK Cancer Metabolic Disease Inflammation/Immunology
    CDK8-IN-3 is an inhibitor of CDK8 extracted from patent WO2016041618A1, compound example 1.7.
  • HY-101976
    JAK3-IN-6

    JAK Inflammation/Immunology
    JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.
  • HY-131065
    MET kinase-IN-2

    c-Met/HGFR Cancer
    MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity.
  • HY-P2244
    YAP-TEAD-IN-1

    YAP Cancer
    YAP-TEAD-IN-1 is a potent and competitive inhibitor of YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM).
  • HY-A0298
    EZH2-​IN-​2

    Histone Methyltransferase Cancer
    EZH2-IN-2 is a EZH2 inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC50 of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity.
  • HY-16709
    USP7-IN-1

    Deubiquitinase Cancer
    USP7-IN-1 is a selective and reversible inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 77 μM, and can be used for the research of cancer.
  • HY-115579
    MALAT1-IN-1

    Others Cancer
    MALAT1-IN-1 (compounds 5) is a potent and specific Malat1 (Metastasis-associated lung adenocarcinoma transcript 1) inhibitor. MALAT1-IN-1 modulated Malat1 downstream genes in a dose-dependent manner without affecting expression of nuclear enriched abundant transcript 1 (Neat1) .
  • HY-129035
    Vanin-1-IN-1

    Others Metabolic Disease Inflammation/Immunology
    Vanin-1-IN-1 is an inhibitor of vanin-1 enzyme which is a cell surface associated, giycosyiphosphatidyS inositol (GPi) anchored protein and plays an important role in metabolism and inflammation.
  • HY-U00279
    Nitracrine

    DNA/RNA Synthesis Cancer
    Nitracrine inhibits RNA synthesis and covalently, reversibly binds to DNA but also forms covalent adducts with DNA in vivo. Nitracrine, a 1-nitroacridine derivative, is a potent hypoxia-selective agent in vitro and antitumor drug. Nitracrine has cytotoxicity towards most cells.
  • HY-B0840
    Chlorfenapyr

    Others Others
    Chlorfenapyr is a pyrrole pro-insecticide that is metabolized in vivo into CL 303268 by mixed function oxidases. Chlorfenapyr is active against a variety of insects including those susceptible and resistant to pyrethroid and organophosphate insecticides. Formulations containing Chlorfenapyr have been used to control termites and in agriculture to control various insects.
  • HY-126324
    IV-23

    Apoptosis Cancer
    IV-23 (Compound 20) is a potent Noxa mediated apoptosis inducer, and it is a promising anticancer agent with potential. IV-23 inhibits cell growths in vitro and in vivo, reduces colony formation, arrests cell cycle at M phase, and induces esophageal squamous cell carcinoma (ESCC).
  • HY-109587A
    BM635 hydrochloride

    Bacterial Infection
    BM635 hydrochloride is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 hydrochloride has an MIC50 of 0.08 μM against M.tuberculosis H37Rv. BM635 hydrochloride doubles the in vivo exposure with respect to the free base BM635.
  • HY-128775
    JHU395

    Others Cancer
    JHU395 is an orally-bioavailable and a plasma stable lipophilic glutamine antagonists (GA) prodrug. JHU395 delivers 6-diazo-5-oxo-L-norleucine (DON) to malignant peripheral nerve sheath tumor (MPNST) in vitro and in vivo, and has antitumor activity in MPNST.
  • HY-15178
    Oglemilast

    GRC 3886

    Phosphodiesterase (PDE) Inflammation/Immunology
    Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases.
  • HY-119322
    Tifenazoxide

    NN414

    Potassium Channel Metabolic Disease
    Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective K ATP channels opener. Tifenazoxide has antidiabetic effect, can inhibit glucose stimulated insulin release in vitro and in vivo, and has a beneficial effect on glucose homeostasis.
  • HY-100435
    Oxaquin

    MCB-3837; DNV3837

    Bacterial Infection
    Oxaquin (MCB-3837) is a water-soluble, injectable prodrug that is rapidly converted to the active sub-stance MCB3681 in vivo following intravenous (i.v.) administration, active against Gram-positive bacterial species. Oxaquin (MCB-3837) itself has no antimicrobial effects.
  • HY-100431A
    IMR-1A

    Notch Drug Metabolite Cancer
    IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitors with an IC50 of 0.5 μM. IMR-1A has a 50-fold increase in potency with respect to IMR-1. IMR-1 can metabolize in vivo to IMR-1A.
  • 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-100726
    GNE-272

    Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300.
  • HY-N5020
    Carabrone

    Bacterial Infection
    Carabrone is isolated from the fruits of Carpesium abrotanoides , is a well-known sesquiterpene and exhibits significant anti-bacterial and anti-tumor activities. Carabrone exhibits antifungal activities in vitro and in vivo against Botrytis cinerea, Colletotrichum lagenarium(EC50=7.10 μg/mL) and Erysiphe graminis.
  • HY-103265
    ARL67156 trisodium salt

    Phosphatase Cardiovascular Disease
    ARL67156 trisodium salt is an inhibitor of ecto-ATPase. ARL 67156 trisodium salt is a weak competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12 μM, respectively. ARL67156 trisodium salt prevents in vivo the development of calcific aortic valve disease.
  • HY-P1110
    AF12198

    Interleukin Related Inflammation/Immunology
    AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo.
  • HY-109112
    Brilaroxazine

    RP5063

    Dopamine Receptor 5-HT Receptor Inflammation/Immunology Neurological Disease
    Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.
  • HY-B2099
    Buformin

    1-Butylbiguanide

    AMPK Cancer Metabolic Disease
    Buformin (1-Butylbiguanide) is a potent and orally active biguanide antidiabetic agent, an AMPK activator. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).
  • HY-115514A
    BRK inhibitor P21d hydrochloride

    Others Cancer
    BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models.
  • HY-101058
    PD1-PDL1-IN 1

    PD-1/PD-L1 Inflammation/Immunology
    PD1-PDL1-IN 1 is a potent programmed cell death 1 (PD-1) inhibitor. PD1-PDL1-IN 1 is useful as immune modulator.
  • HY-112081
    BAY-707

    DNA/RNA Synthesis Cancer
    BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy.
  • HY-N6950
    Hederacolchiside A1

    PI3K Akt mTOR Parasite Apoptosis Cancer Infection
    Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro.
  • HY-18767
    Ivosidenib

    AG-120

    Isocitrate Dehydrogenase (IDH) Cancer Metabolic Disease
    Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity.
  • HY-N3446
    IVHD-valtrate

    Apoptosis Cancer
    IVHD-valtrate, an active Valeriana jatamansi derivative, is against human ovarian cancer cells in vitro and in vivo. IVHD-valtrate induces cancer cells apoptosis and arrests the ovarian cancer cells in the G2/M phase. IVHD-valtrate has the potential to be a novel chemotherapeutic agent for the human ovarian cancer research.
  • HY-133015
    Mcl-1 inhibitor 3

    Bcl-2 Family Cancer
    Mcl-1 inhibitor 3 (compound 1) is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay). Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.
    .
  • HY-120395
    UC-514321

    STAT Apoptosis Cancer Inflammation/Immunology
    UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.
  • HY-N4298
    Epitheaflagallin 3-O-gallate

    Others Metabolic Disease Inflammation/Immunology
    Epitheaflagallin 3-O-gallate is a minor polyphenol in black tea. Epitheaflagallin 3-O-gallate exhibits versatile physiological functions in vivo and in vitro, including antioxidative activity, pancreatic lipase inhibition, Streptococcus sorbinusglycosyltransferase inhibition, and an inhibiting effect on the activity of matrix metalloprotease-1 and -3 and their synthesis by human gingival fibroblasts.
  • HY-133149
    Lp-PLA2-IN-3

    Phospholipase Cardiovascular Disease
    Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2).
  • HY-114645
    PDK1-IN-RS2

    PDK-1 Cancer
    PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1.
  • HY-135128
    Dot1L-IN-5

    Histone Methyltransferase Cancer
    Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.17 nM.
  • HY-U00324
    p38 MAPK-IN-2

    p38 MAPK Autophagy Cancer
    p38 MAPK-IN-2 is an inhibitor of p38 kinase.
  • HY-111787
    CSF1R-IN-2

    Src c-Met/HGFR c-Fms Cancer
    CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.
  • HY-114459
    Mutant IDH1-IN-4

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells.
  • HY-102998
    Nav1.7-IN-6

    Sodium Channel Neurological Disease
    Nav1.7-IN-6 (example 346) is a Nav1.7 selective inhibitor, which is extracted from patent WO2015078374A1.
  • HY-19949
    HIF-2α-IN-1

    HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    HIF-2α-IN-1 is a HIF-2α inhibitor has an IC50 of less than 500 nM in HIF-2α scintillation proximity assay.
  • HY-124652
    TBK1/IKKε-IN-4

    IKK Cancer
    TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR.
  • HY-19798
    PI4KIIIbeta-IN-9

    PI4K PI3K Cancer
    PI4KIIIbeta-IN-9 is a potent PI4KIIIβ inhibitor with an IC50 of 7 nM. PI4KIIIbeta-IN-9 also inhibits PI3Kδ and PI3Kγ with IC50s of 152 nM and 1046 nM, respectively.
  • HY-112044
    β-catenin/CBP-IN-1

    Wnt β-catenin Epigenetic Reader Domain Cancer Inflammation/Immunology
    β-catenin/CBP-IN-1 is a potent and selective CBP/β-catenin antagonist, extracted from the patent WO2014092154A1. β-catenin/CBP-IN-1 has the potential for the study of liver fibrosis induced by hepatitis virus.
  • HY-135127
    Dot1L-IN-4

    Histone Methyltransferase Cancer
    Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM.
  • HY-126244
    CDK4/6-IN-3

    CDK Cancer
    CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor with Kis of <0.3 nM and 2.2 nM, respectively. CDK4/6-IN-3 inhibits CDK1 with a Ki of 110 nM. CDK4/6-IN-3 can be used for the treatment of glioblastoma.
  • HY-12836
    IFN alpha-IFNAR-IN-1

    IFNAR Inflammation/Immunology
    IFN alpha-IFNAR-IN-1 is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR; inhibit MVA-induced IFN-α responses by BM-pDCs (IC50=2-8 uM).
  • HY-109562A
    GRK2-IN-1 hydrochloride

    Others Cardiovascular Disease
    GRKs-IN-1 hydrochloride, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=130 nM) and GRK5 (IC50=7.1 μM). GRKs-IN-1 hydrochloride is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine.
  • HY-19757
    Lp-PLA2 -IN-1

    Phospholipase Cancer
    Lp-PLA2 -IN-1 inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
  • HY-128704A7
    c-Kit-IN-3 tartrate

    c-Kit Cancer
    c-Kit-IN-3 tartrate (Compound 18) is a potent c-KIT kinase inhibitor, which is potent and selective against BaF3-tel-c-KIT (IC50 of 4 nM) and a broad spectrum of drug-resistant mutants (IC50 of 8 nM for BaF3-tel-c-KIT-T670I) with improved bioavailability.
  • HY-12039
    Lyn-IN-1

    Bafetinib analog

    Bcr-Abl Cancer
    Lyn-IN-1 (Bafetinib analog) is a potent and selective dual Bcr-Abl/Lyn inhibitor, extracted from patent WO2014169128A1.
  • HY-111540B
    (S)-IDO1-IN-5

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    (S)-IDO1-IN-5 (Example 1B) is an active S-isomer of IDO1-IN-5. (S)-IDO1-IN-5 binds to IDOL with an IC50 value less than 1.5 µΜ. IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
  • HY-18770A
    IDO-IN-6

    NLG-1486

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO-IN-6 (NLG-1486) is an indoleamine 2,3-dioxygenase (IDO) inhibitor extracted from patent WO WO2012142237A1, Compound 1486, has an IC50 of <1 μM.
  • HY-111427
    CDK8/19-IN-1

    CDK Cancer
    CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.
  • HY-108540
    LAT1-IN-1

    BCH

    Apoptosis Cancer
    LAT1-IN-1 (BCH) is a selective and competitive inhibitor of large neutral amino acid transporter 1 (LAT1) significantly inhibit cellular uptake of amino acids and mTOR phosphorylation, which induces the suppression of cancer growth and apoptosis.
  • HY-128761
    CBP/EP300-IN-2

    Epigenetic Reader Domain Cancer
    CBP/EP300-IN-2 is an inhibitor of CBP/EP300 with IC50 values of 1.07 nM and 5.96 nM for CBP/HTRF and Myc, respectively. CBP/EP300-IN-2, example 25, is extracted from patent WO2017205538A1.
  • HY-130794
    ALK/ROS1-IN-1

    ALK ROS Cancer
    ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
  • HY-100328
    CB2R-IN-1

    Cannabinoid Receptor Neurological Disease
    CB2R-IN-1 is a potent cannabinoid CB2 receptor inverse agonist with a Ki of 0.9 nM.
  • HY-U00457
    TBK1/IKKε-IN-1

    IKK Cancer
    TBK1/IKKε-IN-1 is a dual TBK1 and IKKε inhibitor extracted from patent US20160376283 A1, Compound 274 in Example 60, has IC50s of <100 nM.
  • HY-15133
    PTP1B-IN-3

    Phosphatase Metabolic Disease
    PTP1B-IN-3 is a potent and selective PTP1B inhibitor with IC50s of 120 nM (PTP1B) and 120 nM (TCPTP), respectively.
  • HY-100132
    P300/CBP-IN-5

    Histone Acetyltransferase Cancer
    P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor extracted from patent WO2016044770A1, Example 715, has an IC50 of 18.8 nM.
  • HY-18717
    Mutant IDH1-IN-2

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.6 nM in Fluorescence biochemical assay.
  • HY-135129
    Dot1L-IN-6

    Histone Methyltransferase Cancer
    Dot1L-IN-6 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.19 nM.
  • HY-117427
    D5D-IN-326

    Others Metabolic Disease
    D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice.
  • HY-128876
    P300/CBP-IN-3

    Histone Acetyltransferase Cancer
    P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1.
  • HY-103046
    UbcH5c-IN-1

    E1/E2/E3 Enzyme Inflammation/Immunology
    UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent.
  • HY-135954A
    PDK4-IN-1 hydrochloride

    PDHK Apoptosis Cancer Metabolic Disease Inflammation/Immunology
    PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity.
  • HY-111753A
    WDR5-IN-4 TFA

    Histone Methyltransferase Cancer
    WDR5-IN-4 TFA is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity.
  • HY-101115
    PI3K-IN-6

    PI3K Cancer
    PI3K-IN-6 (compound 20a) is an oral active and highly selective phosphoinositide 3-kinase (PI3K) β/δ inhibitor, with IC50 values of 7.8 nM/5.3 nM for PI3K β/δ, respectively. PI3K-IN-6 (compound 20a) has potential top treat phosphatase and tensin homolog (PTEN) feficient tumors.
  • HY-12453
    TBK1/IKKε-IN-2

    IKK Inflammation/Immunology
    TBK1/IKKε-IN-2 is a dual TBK1 and IKKε inhibitor.
  • HY-129388B
    LSD1-IN-7 benzenesulfonate

    Histone Demethylase Cancer
    LSD1-IN-7 benzenesulfonate is a potent and orally active inhibitor of lysine specific demethylase-1 (LSD1) with anticancer activity extracted from patent WO2017079670A1, compound 4-[2-(4-amino-piperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydro-pyrimidin-4-yl]-2-fluorobenzonitrile.
  • HY-101520
    Dot1L-IN-1

    Histone Methyltransferase Cancer
    Dot1L-IN-1 is a highly potent, selective and structurally novel Dot1L inhibitor with a Ki of 2 pM.
  • HY-P2244A
    YAP-TEAD-IN-1 TFA

    YAP Cancer
    YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM).
  • HY-101928
    KDM4D-IN-1

    Histone Demethylase Cancer
    KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM.
  • HY-128679
    TBK1/IKKε-IN-5

    IKK Cancer
    TBK1/IKKε-IN-5 (compound 1) is a dual TBK1 and IKKε inhibitor, with IC50 values of 1 nM and 5.6 nM for TBK1 and IKKε, respectively.
  • HY-111420
    CBP/EP300-IN-1

    Epigenetic Reader Domain Cancer
    CBP/EP300-IN-1 is a CBP/EP300 bromodomain inhibitor.
  • HY-131062
    yGsy2p-IN-1

    Others Metabolic Disease
    yGsy2p-IN-1 is a potent inhibitor for yeast glycogen synthase 2 (yGsy2p). yGsy2p-IN-1 is a competitive human glycogen synthase 1 (hGYS1) inhibitor with an IC50 of 2.75 µM and a Ki of 1.31 µM for wild-type hGYS1. yGsy2p-IN-H23 a pyrazole inhibitor, is used for glycogen storage diseases (GSDs).
  • HY-136285
    P300/CBP-IN-6

    Histone Acetyltransferase Cancer
    P300/CBP-IN-6 is a p300/CBP histone acetyltransferase (HAT) inhibitor extracted from patent WO2019161162A1, compound 33, has an IC50 of 330 nM for p300 HAT.
  • HY-129388
    LSD1-IN-7 Methylbenzenesulfonate

    Histone Demethylase Cancer
    LSD1-IN-7 Methylbenzenesulfonate is a potent and orally active inhibitor of lysine specific demethylase-1 (LSD1) with anticancer activity extracted from patent WO2017079670A1, compound 4-[2-(4-amino-piperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydro-pyrimidin-4-yl]-2-fluorobenzonitrile.
  • HY-12839
    p38 MAPK-IN-1

    p38 MAPK Autophagy Inflammation/Immunology
    p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC50 of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.
  • HY-101097A
    PD-1-IN-17 (TFA)

    PD-1/PD-L1 Cancer
    PD-1-IN-17 TFA is a programmed cell death-1 (PD-1) inhibitor extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM.
  • HY-12971
    Nampt-IN-1

    LSN3154567

    Nampt Cancer
    Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.
  • HY-102034
    Complement factor D-IN-1

    Others Inflammation/Immunology
    Complement factor D-IN-1 is a potent and selective small-molecule reversible factor d inhibitor, with IC50s of 0.006 and 0.05 μM in FD Thioesterolytic Fluorescent Assay and a MAC Deposition Assay, respectively.
  • HY-133145A
    hDDAH-1-IN-2 sulfate

    Others Cancer Inflammation/Immunology
    hDDAH-1-IN-2 is a selective, orally active human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1) inhibitor. hDDAH-1-IN-2 reveals an excellent profile regarding cell toxicity/viability.
  • HY-101648
    ACAT-IN-1 cis isomer

    Acyltransferase Metabolic Disease
    ACAT-IN-1 cis isomer is a potent ACAT inhibitor with an IC50 of 100 nM.
  • HY-128704A1
    c-Kit-IN-3 hydrochloride

    c-Kit Cancer
    c-Kit-IN-3 hydrochloride (Compound 18) is a potent c-KIT kinase inhibitor, which is potent and selective against BaF3-tel-c-KIT (IC50 of 4 nM) and a broad spectrum of drug-resistant mutants (IC50 of 8 nM for BaF3-tel-c-KIT-T670I) with improved bioavailability.
  • HY-13592
    HDAC-IN-7

    Chidamide impurity

    HDAC Cancer
    HDAC-IN-7 (Chidamide impurity) is an impurity of Chidamide. Chidamide is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor.
  • HY-111540A
    (Rac)-IDO1-IN-5

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    (Rac)-IDO1-IN-5 (Example 1) is a racemate of IDO1-IN-5. IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
  • HY-131312
    Mutant IDH1-IN-6

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes.
  • HY-100198
    PI4KIIIbeta-IN-10

    PI4K Infection
    PI4KIIIbeta-IN-10 is a potent PI4KIIIβ inhibitor with an IC50 of 3.6 nM.
  • HY-128978
    PTP1B-IN-8

    Phosphatase Metabolic Disease
    PTP1B-IN-8 is a potent and selective potent protein tyrosine phosphatase-1B (PTP1B) inhibitor extracted from patent CN103626692A, example 1.
  • HY-119402
    BCL6-IN-8c

    Bcl-2 Family Cancer
    BCL6-IN-8c is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 µM in cell-free enzyme-linked immunosorbent assay.
  • HY-135860
    SARS-CoV-2-IN-1

    Virus Protease SARS-CoV Infection
    SARS-CoV-2-IN-1 is a potent Mpro inhibitor. SARS-CoV-2-IN-1 inhibits the purified recombinant SARS-CoV-2 Mpro, SARS-CoV Mpro and MERS-CoV Mpro with IC50s of 0.67, 0.90 and 0.58 μM, respectively.
  • HY-108939
    Aminoacyl tRNA synthetase-IN-1

    Bacterial Aminoacyl-tRNA Synthetase Infection
    Aminoacyl tRNA synthetase-IN-1 is a bacterial aminoacyl tRNA synthetase (aaRS) inhibitor.
  • HY-W054146
    PTP1B-IN-9

    Proteasome Cancer
    PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor. PTP1B-IN-9 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. PTP1B-IN-9 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity.
  • HY-U00413
    5-HT3-In-1

    5-HT Receptor Neurological Disease Cardiovascular Disease
    5-HT3-In-1 is extracted from patent EP0748807A1, compound example 8. It shows 5-HT3 inhibition activity.
  • HY-133029
    PI3K-IN-9

    PI3K Cancer
    PI3K-IN-9 (compound 1-14) is a potent and selective PI3Kδ inhibitor with an IC50 of 8.9 nM.
  • HY-128342
    Complement C5-IN-1

    Complement System Inflammation/Immunology
    Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). Complement C5-IN-1 interacts with C5 to prevent its cleavage by the C5 convertase and blocks zymosan-induced the membrane-attack complex (MAC) deposition in 50% human whole blood with an IC50 of 0.77 µM.
  • HY-129336
    CDK4/6-IN-4

    CDK Cancer
    CDK4/6-IN-4, the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor for the treatment of cancer.
  • HY-128704A4
    c-Kit-IN-3 maleate

    c-Kit Cancer
    c-Kit-IN-3 maleate (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC50 of 4 nM. c-Kit-IN-3 maleate displays great potencies against c-KIT kinase and a broad spectrum of drug-resistant mutants in the biochemical assay. c-Kit-IN-3 maleate has improved bioavailability.
  • HY-15617
    JNK-IN-7

    JNK inhibitor

    JNK Cancer
    JNK-IN-7 is a potent JNK inhibitor with IC50 of 1.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3, respectively.
  • HY-U00376
    5α-reductase-IN-1

    Others Metabolic Disease
    5α-reductase-IN-1 is an inhibitor of 5α-reductase, used for the research of patterned alopecia in combination with minoxidil.
  • HY-115555
    K-Ras-PDEδ-IN-1

    Phosphodiesterase (PDE) Cancer
    K-Ras-PDEδ-IN-1 is a novel and potent competitive K-Ras-PDEδ inhibitor. K-Ras-PDEδ-IN-1 binds to the farnesyl binding pocket of PDEδ with a low nanomolar Kd of 8 nM.
  • HY-101789
    Nav1.7-IN-3

    Sodium Channel Neurological Disease
    Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration.
  • HY-107575
    TLR4-IN-C34

    Toll-like Receptor (TLR) Inflammation/Immunology
    TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.
  • HY-133126A
    hDDAH-1-IN-1 TFA

    Others Cancer Inflammation/Immunology
    hDDAH-1-IN-1 TFA (compound 8a) is a potent and selective non-amino acid catalytic site inhibitor of human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1), with a Ki of 18 µM.
  • HY-18770
    IDO-IN-5

    NLG-1489

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO-IN-5 (NLG-1489) is an indoleamine 2,3-dioxygenase (IDO) inhibitor extracted from patent WO WO2012142237A1, compound 1489, has an IC50 of 1-10 μM.
  • HY-130264
    HIF-2α-IN-2

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-2 is a hypoxia-inducible factors (HIF-2α) inhibitor extracted from patent WO2015035223A1, Compound 232, has an IC50 of 16 nM in scintillation proximity assay (SPA).
  • HY-111798A
    HO-1-IN-1 hydrochloride

    Reactive Oxygen Species Cancer
    HO-1-IN-1 hydrochloride (Compound 2) is a heme oxygenase 1 (HO-1) inhibitor with an IC50 of 250 nM.
  • HY-126246
    CDC25B-IN-1

    Phosphatase Cancer
    CDC25B-IN-1 (compound 4a) is a potent inhibitor of cell division cycle 25B (CDC25B) phosphatase, with a Ki of 8.5 μM. CDC25B-IN-1 potently inhibits cell proliferation and colony formation, causes an increase of the G2/M phase.
  • HY-13464
    ALK-IN-1

    Brigatinib analog

    ALK Cancer
    ALK-IN-1 (Brigatinib analog) is a potent and selective active inhibitor of anaplastic lymphoma kinase(ALK), Patent US20140066406 A1.
  • HY-12475
    Mutant IDH1-IN-1

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.
  • HY-102031
    PI3Kδ-IN-2

    PI3K Cancer Inflammation/Immunology
    PI3Kδ-IN-2 is a potent and selective inhibitor of PI3Kδ extracted from patent WO 2015055071 A1, compound 10; has an IC50 of 6.4 nM.
  • HY-12759A
    CARM1-IN-1 hydrochloride

    Histone Methyltransferase Cancer
    CARM1-IN-1 hydrochloride is a potent and specific CARM1(Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7(IC50 > 600 uM).
  • HY-100014
    KDM5A-IN-1

    Histone Demethylase Cancer
    KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
  • HY-133148
    Lp-PLA2-IN-2

    Phospholipase Inflammation/Immunology
    Lp-PLA2-IN-2 is a potent and selective lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 0f 120 nM for recombinant human Lp-PLA2.
  • HY-131179
    Influenza A virus-IN-1

    Influenza Virus Infection
    Influenza A virus-IN-1 is a dihydropyrrolidones derivative and is a potent inhibitor against wide subtypes of influenza A virus (IAV) with IC50 values from 3.11 μM to 7.13 μM. Influenza A virus-IN-1 efficiently inhibits replication of IAV, up-regulates the expression of key antiviral cytokines IFN-β and antiviral protein MxA.
  • HY-18370
    HIF-2α-IN-3

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-3, an allosteric inhibitor of hypoxia inducible factor-2α (HIF-2α), exhibits an IC50 of 0.4 µM and a KD of 1.1 µM. Anticancer agent.
  • HY-136606
    SARS-CoV MPro-IN-1

    SARS-CoV Infection
    SARS-CoV MPro-IN-1 is a SARS-CoV-2 3CLpro covalent inhibitor, with an IC50 of 40 nM. SARS-CoV MPro-IN-1 shows good anti-SARS-CoV-2-infection activity in cell culture with an EC50 of 0.33 μM. SARS-CoV MPro-IN-1 has the potential for COVID-19 research.
  • HY-131063
    CDK6/9-IN-1

    CDK Cancer
    CDK6/9-IN-1 (compound 66) is an oral available and dual CDK 6 and CDK 9 inhibitor, with IC50 values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively.
  • HY-18770C
    IDO-IN-8

    NLG-1487

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO-IN-8 (NLG-1487) is an indoleamine 2,3-dioxygenase (IDO) inhibitor extracted from patent WO WO2012142237A1, compound 1487, has an IC50 of 1-10 μM.
  • HY-100445
    αvβ1 integrin-IN-1

    Integrin Cancer Cardiovascular Disease
    αvβ1 integrin-IN-1 (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC50 of 0.63 nM. Antifibrotic effects.
  • HY-12834A
    MK2-IN-1 hydrochloride

    MAPKAPK2 (MK2) Inflammation/Immunology
    MK2-IN-1 hydrochloride is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.
  • HY-114428
    P110δ-IN-1

    PI3K Cancer
    P110δ-IN-1 is a potent and selective inhibitor of P110δ extracted from patent WO 2014055647 A1, with an IC50 of 8.4 nM.
  • HY-19366
    Nav1.7-IN-2

    Sodium Channel Neurological Disease
    Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels (Nav), in particular Nav 1.7, with IC50 of 80 nM.
  • HY-117203A
    CDK12-IN-E9

    CDK Cancer
    CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM.
  • HY-12022
    3-Aminobenzamide

    PARP-in-1

    PARP Cancer
    3-Aminobenzamide (PARP-IN-1) is a potent inhibitor of PARP with IC50 of appr 50 nM in CHO cells, and acts as a mediator of oxidant-induced myocyte dysfunction during reperfusion.
  • HY-101517
    PI3K-IN-2

    PI3K Cancer
    PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC50=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC50=13/190 nM, respectively).
  • HY-100462
    PTP1B-IN-2

    Phosphatase Metabolic Disease
    PTP1B-IN-2 is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 50 nM.
  • HY-15756
    PTP1B-IN-4

    Phosphatase Metabolic Disease
    PTP1B-IN-4 is a non-competitive allosteric inhibitor of the protein tyrosine phosphatase PTP1B, with an IC50 of 8 μM. PTP1B-IN-4 is potentail for the research of obesity and diabetes.
  • HY-101587
    PGS-IN-1

    KME-4

    PGE synthase Lipoxygenase Inflammation/Immunology
    PGS-IN-1 is a potent inhibitor of prostaglandin synthetase (PGS) with an IC50 of 0.28 μM; also inhibits 5-lipoxygenase with an IC50 of 1.05 μM.
  • HY-130676
    CLK-IN-T3N

    CDK Cancer
    CLK-IN-T3N, the negative control of CLK-IN-T3 (HY-115470), is a chemical probe for CDC-like kinase (CLK).
  • HY-111390
    Dot1L-IN-2

    Histone Methyltransferase Cancer
    Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively.
  • HY-101774
    CSF1R-IN-1

    c-Fms Cancer
    CSF1R-IN-1 is a CSF1R inhibitor with an with an IC50 of 0.5 nM.
  • HY-114339
    CDK4/6-IN-2

    CDK Cancer
    CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor extracted from patent US20180000819A1, Compound 1, has IC50s of 2.7 and 16 nM for CDK4 and CDK6, respectively.
  • HY-112191
    PI3K-IN-10

    PI3K Cancer
    PI3K-IN-10 is a potent pan-PI3K inhibitor as a benzimidazole derivative, compound 332, extracted from patent WO2018057808A1.
  • HY-101921
    PI3Kδ-IN-1

    PI3K Inflammation/Immunology
    PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM.
  • HY-W016420
    Fosfomycin sodium

    MK-0955 sodium

    Bacterial Antibiotic Infection
    Fosfomycin sodium (MK-0955 sodium) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin sodium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
  • HY-136234
    9-cis-β-Carotene

    Others Others
    9-cis-β-Carotene, a precursor of retinal, is cleaved by beta-carotene oxygenase 1 (BCMO1) to produce 9-cis-retinal. 9-cis-β-Carotene inhibits photoreceptor degeneration and restores retinal function in vivo. 9-cis-β-Carotene has the potential for the study of congenital stationary night blindness and fundus albipunctatus.
  • HY-P2336
    CCZ01048

    Melanocortin Receptor Cancer
    CCZ01048, a α-melanocyte-stimulating hormone (α-MSH) analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma.
  • HY-P2336A
    CCZ01048 TFA

    Melanocortin Receptor Cancer
    CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma.
  • HY-P1390
    d[Cha4]-AVP

    Vasopressin Receptor
    d[Cha4]-AVP is a potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). d[Cha4]-AVP stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo.
  • HY-136404
    Melanin probe-1

    Others Cancer
    Melanin probe-1 is an 18F-picolinamides based PET probe. Melanin probe-1 can be used for PET imaging of malignant melanoma. Melanin probe-1 exhibits high tumor targeting efficiency, excellent tumor imaging contrasts, desirable biodistribution patterns, and good in vivo stability.
  • HY-N6263
    EGCG Octaacetate

    Bacterial Infection Cardiovascular Disease
    EGCG Octaacetate is a prodrug of Green tea epigallocatechin-3-gallate (EGCG), utilized to enhance the stability and bioavailability of EGCG in vivo. EGCG Octaacetate has high efficacy, bioavailability, anti-oxidation and anti-angiogenesis capacities. EGCG octaacetate is the potential antibacterial compound for gram-positive bacteria (GPB) and gram-negative bacteria (GNB) .
  • HY-N3387
    Licoricidin

    Apoptosis NF-κB Akt MMP Cancer Inflammation/Immunology
    Licoricidin (LCD) is isolated from Glycyrrhiza uralensis Fisch, possesses anti-cancer activities. Licoricidin (LCD) inhibit SW480 cells (IC50=7.2 μM) by inducing cycle arrest, apoptosis and autophagy, and is a potential chemopreventive or chemotherapeutic agent against colorectal cancer. Licoricidin (LCD) inhibits Lung Metastasis by inhibition of tumor angiogenesis and lymphangiogenesis as well as changes in the local microenvironment of tumor tissues the anticarcinogenic effect. Licoricidin enhanced gemcitabine-induced cytotoxicity in Osteosarcoma (OS) cells by inactivation of the Akt and NF-κB pathways in vitro and in vivo. Licoricidin blocks UVA-induced photoaging via ROS scavenging, limits the activity of MMP-1, it can be considered as an active ingredient in new topically applied anti-ageing formulations.
  • HY-101364A
    CHPG sodium salt

    mGluR NF-κB ERK Akt Inflammation/Immunology Neurological Disease
    CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways..
  • HY-107563A
    ROS 234 dioxalate

    Histamine Receptor Inflammation/Immunology
    ROS 234 dioxalate is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 dioxalate diaplays poor central access.
  • HY-P1390A
    d[Cha4]-AVP TFA

    Vasopressin Receptor
    d[Cha4]-AVP TFA is a potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). d[Cha4]-AVP TFA stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo.
  • HY-15491
    AG-024322

    COX Cancer
    AG-024322 is a potent ATP-competitive pan-CDK inhibitor against cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range. AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis.
  • HY-B0609
    Fosfomycin tromethamine

    MK-0955 tromethamine

    Bacterial Antibiotic Infection
    Fosfomycin tromethamine (MK-0955 tromethamine) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin tromethamine shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
  • HY-101364
    CHPG

    mGluR NF-κB ERK Akt Inflammation/Immunology Cardiovascular Disease
    CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways.
  • HY-128357
    ACX-362E

    Bacterial DNA/RNA Synthesis Infection
    ACX-362E is an orally available DNA polymerase IIIC (pol IIIC) inhibitor, acts as an antimicrobial agent to treat Gram-positive infections, with a MIC50 of 2 μg/mL for C. difficile. ACX-362E displays very potent in vitro and in vivo activities against broad spectrum of C. difficile pathogens.
  • HY-P1439
    RS 09

    Toll-like Receptor (TLR) Inflammation/Immunology
    RS 09 is a TLR4 agonist. RS 09 promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 acts as an adjuvant in vivo; RS 09 enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.
  • HY-13995B
    Sevelamer carbonate

    Others Metabolic Disease
    Sevelamer carbonate is an orally active and non-calcium-based phosphate binding agent and used for the hyperphosphatemia of chronic kidney disease (CKD)research. Sevelamer carbonate effectively lowers serum phosphorus levels hile having minimal effect on serum calcium or serum chloride levels in vivo. Sevelamer carbonate is considered as an improved, buffered form of sevelamer (HY-13995).
  • HY-129172A
    PD-1/PD-L1-IN 5

    PD-1/PD-L1 Cancer Infection Inflammation/Immunology
    PD-1/PD-L1-IN 5 is a PD-1/PD-L1 protein/protein interaction inhibitor extracted from patent WO2017222976A1, compound Example 1, has an IC50 of ≤100 nM.
  • HY-12836A
    IFN alpha-IFNAR-IN-1 hydrochloride

    IFNAR Inflammation/Immunology
    IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR; inhibit MVA-induced IFN-α responses by BM-pDCs (IC50=2-8 uM).
  • HY-114009
    AKR1C1-IN-1

    Others Neurological Disease
    AKR1C1-IN-1 is a potent and selective inhibitor of human 20α-hydroxysteroid dehydrogenase (AKR1C1), with a Ki value of 4 nM for AKR1C1.
  • HY-130247
    JAK2/FLT3-IN-1

    JAK FLT3 Cancer
    JAK2/FLT3-IN-1 is a potent and orally effective dual JAK2/FLT3 (Janus kinase 2/ FMS-like tyrosine kinase 3) inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity.
  • HY-107379
    AKR1C3-IN-1

    Others Others
    AKR1C3-IN-1 is a potent, highly selective inhibitor of AKR1C3, with an IC50 of 13 nM.
  • HY-129702
    MCL-1/BCL-2-IN-4

    Bcl-2 Family Cancer
    MCL-1/BCL-2-IN-4 (Compound 7) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor.
  • HY-111102
    FL-411

    BRD4-in-1

    Epigenetic Reader Domain Cancer
    FL-411 is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4(1).
  • HY-111414
    Hsp90-Cdc37-IN-1

    HSP Cancer
    Hsp90-Cdc37-IN-1 is an Hsp90-Cdc37 interaction disruptor that inhibit cell migration and reverse drug resistance, with an IC50 of 140 nM.
  • HY-129681
    MCL-1/BCL-2-IN-1

    Bcl-2 Family Cancer
    MCL-1/BCL-2-IN-2 (Compound Nap-1) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 4.45 and 3.18 μM, respectively.
  • HY-U00427
    PDE2/PDE10-IN-1

    Phosphodiesterase (PDE) Neurological Disease
    PDE2/PDE10-IN-1 is a phosphodiesterase 2 (PDE2) and PDE10 inhibitor with IC50s of 29 and 480 nM, respectively.
  • HY-101941
    BTK IN-1

    SNS062 analog

    Btk Cancer Inflammation/Immunology
    BTK IN-1 (SNS062 analog) is a potent BTK inhibitor, with an IC50 of <100 nM.
  • HY-136534
    RET V804M-IN-1

    RET Cancer
    RET V804M-IN-1 (compound 5) is a wt-RET -selective inhibitors of RETV804M kinase, with an IC50 of 20 nM.
  • HY-12790
    CB1-IN-1

    BPRCB1184

    Cannabinoid Receptor Neurological Disease
    CB1-IN-1 (BPRCB1184) is a peripherally restricted CB1R antagonist, with Ki of 0.3 nM and 21 nM for CB1R (EC50 = 3 nM) and CB2R, respectively.
  • HY-136310
    PIP4K-IN-a131

    Others Cancer
    PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9 µM and 0.6 µM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways.
  • HY-114320
    BuChE-IN-TM-10

    TM-10

    AChE Neurological Disease
    BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC50 of 8.9 nM. BuChE inhibitor 1 inhibits and disaggregates self-induced Aβ aggregation, exhibiting potent antioxidant activity and good blood-brain barrier (BBB) penetration. Has potential to treat Alzheimer’s disease.
  • HY-101785
    eIF4A3-IN-2

    Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 (eIF4A3) inhibitor with an IC50 of 110 nM.
  • HY-16905
    T338C Src-IN-1

    Src Cancer
    T338C Src-IN-1 is a potent mutant-Src T338C inhibitor; exhibited the most potent inhibition of T338C(IC50=111 nM) relative to WT c-Src (10-fold increase).
  • HY-112219A
    H3R-IN-1 Hydrochloride

    Histamine Receptor Inflammation/Immunology Endocrinology
    H3R-IN-1 Hydrochloride is a histamine receptor 3 (H3R) inverse agonist extracted from patent WO2013107336A1, compound example 2.
  • HY-18874
    p38-α MAPK-IN-1

    p38 MAPK Autophagy Others
    p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
  • 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-12960
    SKLB4771

    FLT3-​in-​1

    FLT3 Cancer
    SKLB4771 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.
  • HY-135816
    CK2/PIM1-IN-1

    Casein Kinase Pim Cancer Inflammation/Immunology
    CK2/PIM1-IN-1 is an inhibitor of CK2 and PIM1, with IC50s of 3.787 μM and 4.327 μM for CK2 and PIM1, respectively. CK2/PIM1-IN-1 is developed for the research of proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders.
  • HY-111905A
    BRD7-IN-1 free base

    Epigenetic Reader Domain Cancer
    BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively).
  • HY-133124
    PARP/PI3K-IN-1

    PARP PI3K Apoptosis Cancer
    PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases.
  • HY-13033
    CDK-IN-2

    CDK inhibitor II

    CDK Cancer
    CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM, extracted from reference 1, example 4.
  • HY-125012
    MAP4K4-IN-3

    MAP4K Metabolic Disease
    MAP4K4-IN-3 (Compound 17) is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, an IC50 of 470 nM in cell assay. Antidiabetic agent.
  • HY-16906
    T338C Src-IN-2

    Src Cancer
    T338C Src-IN-2 is a potent mutant c-Src T338C kinase inhibitor with IC50 of 317 nM; also inhibits T338C/V323A and T338C/V323S with IC50 of 57 nM/19 nM.
  • HY-100445A
    αvβ1 integrin-IN-1 TFA

    Integrin Cancer Cardiovascular Disease
    αvβ1 integrin-IN-1 TFA (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC50 of 0.63 nM. Antifibrotic effects.
  • HY-128704A6
    c-Kit-IN-3 L-tartrate

    c-Kit Cancer
    c-Kit-IN-3 L-tartrate (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC50s of 4 nM, 8 nM for c-KIT wt and c-KIT T670I, respectively. c-Kit-IN-3 L-tartrate displays great potencies against most of the gain-offunction mutations in the juxtamembrane domain, drugresistant mutations in the ATP binding pocket, and activation loops.
  • HY-135906
    CK2/ERK8-IN-1

    Casein Kinase ERK Pim DYRK Apoptosis Cancer
    CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy.
  • HY-136379
    CID44216842

    Cdc42-in-1

    Ras Cancer
    CID44216842 (Cdc42-IN-1) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 1.0 and 1.2 μM in GTP binding assay, respectively. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 0.3 and 0.5 μM in GDP binding assay, respectively. Use as a molecular probe.
  • HY-112436
    Trk-IN-4

    PF-6683324 isomer

    Trk Receptor Neurological Disease
    Trk-IN-4 (PF-6683324 isomer) is a potent pan-Trk inhibitor in cell-based assays with IC50s of 1.9 nM, 2.6 nM and 1.1 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.
  • HY-128582
    PI3K/HDAC-IN-1

    PI3K HDAC Cancer
    PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K/HDAC, potently inhibits PI3Kδ and HDAC1 with IC50s of 8.1 nM and 1.4 nM, respectively.
  • HY-128598
    MD2-TLR4-IN-1

    Toll-like Receptor (TLR) Cancer Inflammation/Immunology
    MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.
  • HY-129701
    MCL-1/BCL-2-IN-3

    Bcl-2 Family Cancer
    MCL-1/BCL-2-IN-3 (Compound 2) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 5.95 and 4.78 μM, respectively.
  • HY-U00423
    CRTH2-IN-1

    Ramatroban analog

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    CRTH2-IN-1 (Ramatroban analog) is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist with an IC50 of 6 nM in a human DP2 binding assay.
  • HY-114334
    Glutaminase-IN-1

    CB839 derivative

    Glutaminase Cancer
    Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.
  • HY-79511
    FAAH-IN-2

    O-Desmorpholinopropyl Gefitinib

    FAAH Autophagy Others
    FAAH-IN-2 (O-Desmorpholinopropyl Gefitinib) is a potent FAAH(fatty acid amide hydrolase) inhibitor extracted from Patent WO/2008/100977A2.
  • HY-130259
    LC3-mHTT-IN-AN2

    Autophagy Neurological Disease
    LC3-mHTT-IN-AN2 (Compound AN2) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN2 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.
  • HY-135281
    CYP11B2-IN-1

    Cytochrome P450 Cardiovascular Disease
    CYP11B2-IN-1 is a CYP11B2 inhibitor with an IC50 of 2.3 nM. CYP11B2-IN-1 inhibits CYP11B1 with an IC50 of 142 nM.
  • HY-44688
    S.pombe lumazine synthase-IN-1

    Bacterial Fungal Infection
    S.pombe lumazine synthase-IN-1 is an inhibitor of lumazine synthases with Ki values of 243 μM and 9.6 μM for Schizosaccharomyces pombe and Mycobacterium tuberculosis lumazine synthases, respectively.
  • HY-101513
    eIF4A3-IN-1

    Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM), which binds to a non-ATP binding site of eIF4A3 and shows significant cellular nonsense-mediated RNA decay (NMD) inhibition at 10 and 3 μM and can be as a probe for further study of eIF4A3, the exon junction complex (EJC), and NMD.
  • HY-100877
    GCN2-IN-1

    A-92

    Eukaryotic Initiation Factor (eIF) Cancer
    GCN2-IN-1 (A-92) is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with an IC50 of <0.3 μM in the enzyme assay and an IC50 of 0.3-3 μM in the cell assay.
  • HY-128704A5
    c-Kit-IN-3 D-tartrate

    c-Kit Cancer
    c-Kit-IN-3 (D-tartrate) (Compound 18) is a potent c-KIT kinase inhibitor, which is potent and selective against BaF3-tel-c-KIT (IC50 of 4 nM) and a broad spectrum of drug-resistant mutants (IC50 of 8 nM for BaF3-tel-c-KIT-T670I) with improved bioavailability.
  • HY-U00325
    11β-HSD1-IN-1

    Others Neurological Disease
    11β-HSD1-IN-1 is an inhibitor of 11β-hydroxydehydrogenase 1 (11β-HSD1), with an IC50 of 52 nM, and used for the treatment of pain.
  • HY-16694
    BAMB-4

    ITPKA-in-C14

    Others Cancer
    BAMB-4(ITPKA-IN-C14) is a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A((ITPKA) with IC50 of 37 μM in ADP-Glo Assay.
  • HY-78869
    Mutated EGFR-IN-1

    Osimertinib analog

    EGFR Cancer
    Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
  • HY-U00326
    PI3Kα/mTOR-IN-1

    PI3K mTOR Cancer
    PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.
  • HY-101286
    Rpn11-IN-1

    Capzimin intermediate

    Proteasome Cancer
    Rpn11-IN-1 (Capzimin intermediate) is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM.
  • HY-129700
    MCL-1/BCL-2-IN-2

    Bcl-2 Family Cancer
    MCL-1/BCL-2-IN-2 (Compound 6) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor.
  • HY-80002
    BMX-IN-1

    BMX kinase inhibitor

    Btk BMX Kinase Cancer
    BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys 496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.
  • HY-100005A
    Fumarate hydratase-IN-2 sodium salt

    Mitochondrial Metabolism Cancer
    Fumarate hydratase-IN-2 sodium salt (compound 3) is a cell-permeable and competitive fumarate hydratase inhibitor (Ki=4.5 μM) with nutrient-dependent cytotoxicity .
  • HY-130258
    LC3-mHTT-IN-AN1

    Autophagy Neurological Disease
    LC3-mHTT-IN-AN1 (Compound AN1) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN1 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.
  • HY-130609A
    Aβ42-IN-1 free base

    γ-secretase Neurological Disease
    Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
  • HY-12098
    Verubulin hydrochloride

    MPC-6827 hydrochloride

    Microtubule/Tubulin Cancer
    Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types.
  • HY-128204
    AN3661

    Parasite Infection
    AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains (mean IC50=32 nM), Ugandan field isolates (mean ex vivo IC50=64 nM), and murine P. berghei and P. falciparum infections.
  • HY-122607
    DPA-714

    Others Cancer Inflammation/Immunology
    DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. [18F]DPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model.
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-103048A
    PD-1/PD-L1-IN 3 TFA

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN 3 TFA is a PD-1/PD-L1 interaction inhibitor extracted from patent WO2014151634A1, compound 1. PD-1/PD-L1-IN 3 TFA inhibits the binding of human PD-1 to PD-Ll with an IC50 of 9 nM.
  • HY-129172
    PD-1/PD-L1-IN 5 TFA

    PD-1/PD-L1 Cancer Infection Inflammation/Immunology
    PD-1/PD-L1-IN 5 TFA is a PD-1/PD-L1 protein/protein interaction inhibitor extracted from patent WO2017222976A1, compound Example 1, has an IC50 of ≤100 nM.
  • HY-B1075
    Fosfomycin calcium

    MK-​0955 calcium

    Bacterial Antibiotic Infection
    Fosfomycin calcium (MK-​0955 calcium) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin calcium (MK-​0955 calcium) shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
  • HY-10581A
    Gatifloxacin hydrochloride

    AM-1155 hydrochloride; BMS-206584 hydrochloride; PD135432 hydrochloride

    Bacterial Topoisomerase Antibiotic Infection
    Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
  • HY-10581B
    Gatifloxacin mesylate

    AM-1155 mesylate; BMS-206584 mesylate; PD135432 mesylate

    Bacterial Topoisomerase Antibiotic Infection
    Gatifloxacin mesylate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin mesylate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin mesylate can be used to treat bacterial conjunctivitis in vivo.
  • HY-P1439A
    RS 09 TFA

    Toll-like Receptor (TLR) Inflammation/Immunology
    RS 09 TFA is a TLR4 agonist. RS 09 TFA promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 TFA acts as an adjuvant in vivo; RS 09 TFA enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.
  • HY-125039
    N-Acetyl lysyltyrosylcysteine amide

    Glutathione Peroxidase Neurological Disease Cardiovascular Disease
    N-Acetyl lysyltyrosylcysteine amide is a potent, reversible, specific, and non-toxic tripeptide inhibitor of myeloperoxidase (MPO). N-Acetyl lysyltyrosylcysteine amide effectively inhibits MPO generation of toxic oxidants in vivo. N-Acetyl lysyltyrosylcysteine amide reduces neuronal damage and preserves brain tissue and neurological function in the stroked brain. N-Acetyl lysyltyrosylcysteine amide inhibits MPO-dependent hypochlorous acid (HOCl) generation, protein nitration, and LDL oxidation.
  • HY-N0631
    Cornuside

    p38 MAPK NF-κB Inflammation/Immunology
    Cornuside is a secoiridoid glucoside isolated from the fruit of Cornus officinalis Sieb. et Zucc., which is a traditional oriental medicine for treating inflammatory diseases and invigorating blood circulation. Cornuside inhibits mast cell-mediated allergic response by down-regulating MAPK and NF-κB signaling pathways. Cornuside has anti-allergic effects in vivo and in vitro which suggests a therapeutic application of this agent in inflammatory allergic diseases.
  • HY-105064D
    Zoniporide hydrochloride hydrate

    CP-597396 hydrochloride hydrate

    Sodium Channel Cardiovascular Disease
    Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM).
  • HY-10581
    Gatifloxacin

    AM-1155; BMS-206584; PD135432

    Bacterial Topoisomerase Antibiotic Infection
    Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50=0.109 μg/ml). Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.
  • HY-10581C
    Gatifloxacin sesquihydrate

    AM-1155 sesquihydrate; BMS-206584 sesquihydrate; PD135432 sesquihydrate

    Bacterial Topoisomerase Antibiotic Infection Inflammation/Immunology
    Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin sesquihydrate can be used to treat bacterial conjunctivitis in vivo.
  • HY-U00347
    COX/5-LO-IN-1

    Atreleuton analog

    COX Lipoxygenase Inflammation/Immunology
    COX/5-LO-IN-1 (Atreleuton analog) is an inhibitor of cylooxygenase and 5-lipoxygenase (5-LO), used for the research of inflammatory and allergic disease states.
  • HY-100468
    REV7/REV3L-IN-1

    Others Cancer
    REV7/REV3L-IN-1 is a REV7/REV3L interaction inhibitor with an IC50 of 78 μM, which directly binds to REV7 in nuclear magnetic resonance analyses, and inhibits the reactivation of a reporter plasmid containing an interstrand crosslink (ICL) in between the promoter and reporter regions.
  • HY-50862
    Akt1 and Akt2-IN-1

    Akt Cancer
    Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity.
  • HY-18676B
    ILK-IN-2

    OSU-T315 analog

    Integrin Cancer
    ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor.
  • HY-108706
    KDM2A/7A-IN-1

    Histone Demethylase Cancer
    KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases.
  • HY-110195
    Smurf1-IN-A01

    A01

    Others Others
    Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation.
  • HY-18605
    K-Ras G12C-IN-2

    Ras Cancer
    K-Ras G12C-IN-2 is an irreversible covalent K-Ras G12C inhibitor.
  • HY-12682
    Glutaminase C-IN-1

    Compound 968

    Glutaminase Cancer
    Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
  • HY-18604
    K-Ras G12C-IN-1

    Ras Cancer
    K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C extracted from patent WO 2014152588 A1.
  • HY-128771
    K-Ras G12C-IN-4

    Ras Cancer
    K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRAS G12C.
  • HY-112294
    TIE-2/VEGFR-2 kinase-IN-1

    VEGFR Cancer Inflammation/Immunology Cardiovascular Disease
    TIE-2/VEGFR-2 kinase-IN-1 is used for the synthesis of TIE-2 and/or VEGFR-2 inhibitors, extracted from patent WO2003022852, example 14. TIE-2/VEGFR-2 kinase-IN-1 is used for the study of diseases associated with inappropriate angiogenesis.
  • HY-18606
    K-Ras G12C-IN-3

    Ras Cancer
    K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.
  • HY-103484
    GATA4-NKX2-5-IN-1

    Others Cardiovascular Disease
    GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC50 of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.
  • HY-P1723
    Spexin

    Neuropeptide Q

    Neuropeptide Y Receptor
    Spexin is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Spexin exhibits no significant activity at galanin receptor 1. Spexin is an endogenous satiety-inducing peptide; Spexin inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Spexin attenuates LH secretion in goldfish. Spexin exhibits anxiolytic effects in vivo.
  • HY-124754
    BTRX-335140

    CYM-53093

    Opioid Receptor Metabolic Disease
    BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. BTRX-335140 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) .
  • HY-18346
    Mozavaptan

    OPC-31260

    Vasopressin Receptor Cancer Endocrinology Metabolic Disease
    Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment.
  • HY-123593
    Mozavaptan hydrochloride

    OPC-31260 hydrochloride

    Vasopressin Receptor Cancer Endocrinology Metabolic Disease
    Mozavaptan hydrochloride (OPC-31260 hydrochloride) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan hydrochloride shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan hydrochloride has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment.
  • HY-136383
    AZA1

    Rac1/Cdc42-in-1

    Ras Apoptosis Cancer
    AZA1 is a potent dual inhibitor of Rac1 and Cdc42. AZA1 induces prostate cancer cells apoptosis and inhibits prostate cancer cells proliferation, migration and invasion.
  • HY-P1723A
    Spexin TFA

    Neuropeptide Q TFA

    Neuropeptide Y Receptor
    Spexin TFA is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Spexin TFA exhibits no significant activity at galanin receptor 1. Spexin TFA is an endogenous satiety-inducing peptide; Spexin TFA inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Spexin TFA attenuates LH secretion in goldfish. Spexin TFA exhibits anxiolytic effects in vivo.
  • HY-128892
    EN6

    Autophagy Proton Pump Neurological Disease
    EN6 is a small-molecule in vivo activator of autophagy that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal the vacuolar H + ATPase (v-ATPase). EN6-mediated ATP6V1A modification decouples the v-ATPase from the Rags, leading to inhibition of mTORC1 signaling, increased lysosomal acidification and activation of autophagy. EN6 clears TDP-43 aggregates, a causative agent in frontotemporal dementia, in a lysosome-dependent manner.
  • HY-106019C
    Liarozole dihydrochloride

    R75251 dihydrochloride

    Cytochrome P450 Cancer Inflammation/Immunology
    Liarozole dihydrochloride (R75251; R85246) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase). Liarozole dihydrochloride prevents the catabolism of retinoic acid via inhibition of 4-hydroxylase and exhibits retinoid sparing and retinoid-mimetic effects in vivo. Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.
  • HY-13983
    IDO-IN-7

    NLG-919 analogue; GDC-0919 analogue

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO-IN-7 (NLG-919 analogue) is a a potent IDO1 inhibitor with an IC50 of 38 nM.
  • HY-10704
    PTP1B-IN-1

    PTP1B inhibitor

    Phosphatase Metabolic Disease
    PTP1B-IN-1 is a potent protein tyrosine phosphatase-1B (PTP1B) inhibitor with IC50 of 1.6 mM; 1,2,5-thiadiazolidin-3-one-1,1-dioxide scaffold for derivatives synthesis.
  • HY-P2161
    TAK-683

    Others Cancer
    TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
  • HY-112535
    α-2,3-sialyltransferase-IN-1

    Lith-O-Asp analog

    Others Cancer Inflammation/Immunology
    α-2,3-sialyltransferase-IN-1 (Lith-O-Asp analog) is a noncompetitive α-2,3-sialyltransferase inhibitor with an IC50 of 6 μM.
  • HY-12068
    PI3K-IN-1

    XL-147 derivative 1

    PI3K Cancer
    PI3K-IN-1 (XL-147 derivative 1) is a potent inhibitor of PI3K. PI3K-IN-1 (25 μM) blocks PI3K/Akt signaling pathways.
  • HY-116716
    PIN1 inhibitor API-1

    MicroRNA Cancer
    PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development.
  • HY-W018035
    DL-Glyceric Acid

    Glyceric Acid (20% in Water,ca.2 mol/L)

    Endogenous Metabolite Metabolic Disease
    DL-Glyceric Acid is a compound that is secreted excessively in the urine by patients suffering from D-glyceric aciduria.
  • HY-P1459
    Sphistin Synthetic Peptide(12-38,Fitc in N-Terminal-Fluorescently Labeled Peptide)

    Bacterial Infection
    Sphistin Synthetic Peptide (12-38, Fitc in N-Terminal-Fluorescently Labeled Peptide) is a truncated fragments of Sphistin Synthetic Peptide that shows potent antimicrobial activity.
  • HY-10371
    Pim1/AKK1-IN-1

    LKB1/AAK1 dual inhibitor

    Pim Cancer
    Pim1/AKK1-IN-1 is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.
  • HY-108556
    RWJ-56110

    Protease-Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis.
  • HY-N5072
    Desmethylglycitein

    4',6,7-Trihydroxyisoflavone

    CDK PI3K PKC Cancer
    Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.
  • HY-10319
    ROCK-IN-2

    Azaindole 1; TC-S 7001

    ROCK Cardiovascular Disease
    ROCK-IN-2 (Azaindole 1; TC-S 7001) is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively.
  • HY-P1404
    R8-T198wt

    Pim
    R8-T198wt is a cell-permeable peptide inhibitor of Pim-1 kinase, derived from p27Kip1. R8-T198wt inhibits Pim-1 phosphorylation of p27Kip1 and Bad; induces cell cycle arrest (at G1) and apoptosis in DU145 prostate cancer cells. R8-T198wt also inhibits Pim-1-dependent growth of DU145 cells in vitro and in vivo. R8-T198wt displays no effect on the growth of normal prostate epithelial RPWE-1 cells at concentrations of 10 and 20 μM.
  • HY-U00288
    Xanthine oxidase-IN-1

    4-(3-Cyano-5,6-difluoroindol-1-yl)-2-hydroxybenzoic acid

    Xanthine Oxidase Metabolic Disease
    Xanthine oxidase-IN-1 is a xanthine oxidase inhibitor extracted from patent WO2008126898A1, page 68, compound example 3, with an IC50 of 6.5 nM.
  • HY-120944
    BAY-7598

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