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Target Protein-binding Moiety

" in MCE Product Catalog:

674

Inhibitors & Agonists

110

Screening Libraries

15

Dye Reagents

1

Biochemical Assay Reagents

46

Peptides

1

MCE Kits

6

Inhibitory Antibodies

83

Natural
Products

2

Recombinant Proteins

16

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-43723
    PROTAC BET-binding moiety 2

    Ligand for Target Protein for PROTAC Cancer
    PROTAC BET-binding moiety 2 is an inhibitor of BET bromodomain.
  • HY-107442
    PROTAC BRD4-binding moiety 1

    Epigenetic Reader Domain Ligand for Target Protein for PROTAC Cancer
    PROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136).
  • HY-107451
    PROTAC BET-binding moiety 1

    Ligand for Target Protein for PROTAC Cancer
    PROTAC BET-binding moiety 1 is a key intermediate for the synthesis of high-affinity BET inhibitors.
  • HY-107444
    PROTAC Her3-binding moiety 1

    Ligand for Target Protein for PROTAC Cancer
    PROTAC HER3-binding moiety 1 (compound 1b) is a Her3 Ligand for PROTAC.
  • HY-107445
    PROTAC BRD9-binding moiety 1

    Ligand for Target Protein for PROTAC Cancer
    PROTAC BRD9-binding moiety 1 is a compound that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.
  • HY-107445A
    PROTAC BRD9-binding moiety 1 hydrochloride

    Ligand for Target Protein for PROTAC Cancer
    PROTAC BRD9-binding moiety 1 hydrochloride is a compound that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.
  • HY-44103
    Desmethyl-QCA276

    PROTAC BRD4-binding Moiety 4

    Ligand for Target Protein for PROTAC Cancer
    Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM.
  • HY-107452
    SLF-amido-C2-COOH

    PROTAC FKBP12-binding Moiety 1

    Ligand for Target Protein for PROTAC FKBP Cancer
    SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) is a synthetic ligand for FKBP (SLF). SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) can be used in the synthesis of PROTACs.
  • HY-111852
    GNF5-amido-Me

    PROTAC ABL binding Moiety 2

    Ligand for Target Protein for PROTAC Cancer
    GNF5-amido-Me, the GNF5 (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER.
  • HY-111857
    Dasatinib carbaldehyde

    BMS-354825 carbaldehyde; PROTAC ABL binding Moiety 4

    Ligand for Target Protein for PROTAC Cancer
    Dasatinib carbaldehyde (BMS-354825 carbaldehyde), the Dasatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER .
  • HY-111855
    HG-7-85-01-Decyclopropane

    PROTAC ABL binding Moiety 3

    Ligand for Target Protein for PROTAC Cancer
    HG-7-85-01-Decyclopropane, the HG-7-85-01 (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER .
  • HY-P2478
    Human PD-L1 inhibitor V

    PD-1/PD-L1 Inflammation/Immunology
    Human PD-L1 inhibitor V, a human PD-1 protein binding peptide with a Kd value of 3.32 μM. Human PD-L1 inhibitor V inhibit the interaction of hPD-1/hPD-L1.
  • HY-114420
    AP1867-2-(carboxymethoxy)

    PROTAC FKBP12-binding Moiety 2

    FKBP Ligand for Target Protein for PROTAC Cancer
    AP1867-2-(carboxymethoxy), the AP1867 (a synthetic FKBP12 F36V-directed ligand) based moiety, binds to CRBN ligand via a linker to form dTAG molecules.
  • HY-P1348
    GLP-1 moiety from Dulaglutide

    Glucagon Receptor Metabolic Disease
    GLP-1 moiety from Dulaglutide is a 31-amino acid fragment of Dulaglutide which is a glucagon-like peptide 1 receptor (GLP-1) agonist, extracted from patent US 20160369010 A1.
  • HY-111849
    Imatinib carbaldehyde

    CGP-57148B carbaldehyde; STI571 carbaldehyde; PROTAC ABL binding Moiety 1

    Ligand for Target Protein for PROTAC Cancer
    Imatinib carbaldehyde (CGP-57148B carbaldehyde), the Imatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER.
  • HY-P2478A
    Human PD-L1 inhibitor V TFA

    PD-1/PD-L1 Inflammation/Immunology
    Human PD-L1 inhibitor V TFA, a human PD-1 protein binding peptide with a Kd value of 3.32 μM. Human PD-L1 inhibitor V TFA inhibit the interaction of hPD-1/hPD-L1.
  • HY-B1099
    Hycanthone

    DNA/RNA Synthesis Topoisomerase Parasite Infection
    Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.
  • HY-107453
    SirReal1-O-propargyl

    PROTAC Sirt2-binding Moiety 1

    Ligand for Target Protein for PROTAC Cancer
    SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2.
  • HY-12533
    Disopyramide

    Dicorantil; SC-7031

    Sodium Channel Potassium Channel Cardiovascular Disease
    Disopyramide (Dicorantil) is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action.
  • HY-112098
    PROTAC ERα Degrader-1

    PROTACs Estrogen Receptor/ERR Cancer
    PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
  • HY-P1376A
    G-Protein antagonist peptide TFA

    mAChR Adrenergic Receptor Endocrinology
    G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis.
  • HY-100432
    LOC14

    Others Inflammation/Immunology Neurological Disease
    LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding. LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells.
  • HY-12533S
    Disopyramide-d14 tosylate salt

    Sodium Channel Potassium Channel Cardiovascular Disease
    Disopyramide-d14 (Dicorantil-d14) tosylate salt is the deuterium labeled Disopyramide. Disopyramide (Dicorantil) is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action.
  • HY-B0546
    Procaine

    Histone Demethylase DNA/RNA Synthesis Neurological Disease Cancer
    Procaine is a DNA-demethylating agent. Procaine acts through multiple targets and has a slow onset and a short duration of action.
  • HY-B0546A
    Procaine hydrochloride

    Histone Demethylase DNA/RNA Synthesis Neurological Disease Cancer
    Procaine hydrochloride is a DNA-demethylating agent. Procaine hydrochloride acts through multiple targets and has a slow onset and a short duration of action.
  • HY-111606
    DUPA

    Ligand for Target Protein for PROTAC Cancer
    DUPA, belongs to a class of glutamate ureas, is used as the targeting moiety in drug conjugate to selectively deliver cytotoxic drugs to prostate cancer cells.
  • HY-103591
    DUPA(OtBu)-OH

    Others Cancer
    DUPA(OtBu)-OH is a DUPA precursor. DUPA is used as the targeting moiety to actively deliver Docetaxel (DTX) for treatment of Prostate-Specific Membrane Antigen (PSMA) expressing prostate cancer.
  • HY-107443
    I-BET762 carboxylic acid

    Molibresib carboxylic acid; GSK525762A carboxylic acid; PROTAC BRD4-binding Moiety 2

    Ligand for Target Protein for PROTAC Epigenetic Reader Domain Cancer
    I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1.
  • HY-135868
    Mito-apocynin (C2)

    Mitochondrial Metabolism Neurological Disease
    Mito-apocynin (C2), an orally active mitochondria-targeted triphenylphosphonium (TPP)-based compound, is synthesized by conjugating the Apocynin moiety with a TPP + cation. Mito-apocynin (C2) exhibits antineuroinflammatory effect.
  • HY-126664
    Azonafide-PEABA

    ADC Cytotoxin Cancer
    Azonafide-PEABA is a cytotoxic drug moiety.
  • HY-135869
    Mito-apocynin (C11)

    Mitochondrial Metabolism Neurological Disease
    Mito-apocynin (C11), an orally active mitochondria-targeted triphenylphosphonium (TPP)-based compound, is synthesized by conjugating the Apocynin moiety with a TPP + cation. Mito-apocynin (C11) selectively targets mitochondria, and shows neuroprotective effect. Mito-apocynin (C11) prevents hyposmia and corrects deficits in motor function.
  • HY-130802
    5-Aminouridine

    Fungal Influenza Virus Cancer Infection
    5-Aminouridine can modify nucleobases and can be incorporated into the target DNA. 5-Aminouridine exhibits a wide range of biological activity and it inhibits the growth of tumors, fungi and viruses.
  • HY-111850
    Bestatin-amido-Me

    PROTAC IAP binding Moiety 1

    Ligand for E3 Ligase Cancer
    Bestatin-amido-Me, the Bestatin-based IAP ligand, binds to ABL inhibitor via a linker to form SNIPER.
  • HY-130979
    EED226-COOH

    Ligand for Target Protein for PROTAC Cancer
    EED226-COOH is an EED226-derived ligand for target protein EED ligand for PROTAC, binds to a ligand for VHL via linker to form UNC6852 (HY-130708) to degrade PRC2.
  • HY-111853
    MV-1-NH-Me

    PROTAC IAP binding Moiety 2

    Ligand for E3 Ligase Cancer
    MV-1-NH-Me, the MV-1 based IAP ligand, binds to ABL inhibitor via a linker to form SNIPER.
  • HY-125908
    A-1210477-piperazinyl

    PROTAC Mcl1-binding Moiety 1

    Ligand for Target Protein for PROTAC Cancer
    A-1210477-piperazinyl is a compound binds to protein myeloid cell leukemia 1 (MCL1) used for PROTAC technology.
  • HY-134592
    Piperidine-GNE-049-N-Boc

    Ligand for Target Protein for PROTAC Cancer
    Piperidine-GNE-049-N-Boc is a ligand for target protein for PROTAC of dCBP-1 (HY-134582). dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP.
  • HY-106168
    Thymectacin

    NB1011

    Others Cancer
    Thymectacin (NB1011) is an agent selectively targeting tumor cells that have a high expression of thymidylate synthase (TS). Thymectacin is an aryloxy phosphoramidate derivative of BVdU (brivudin).
  • HY-107553
    Chetomin

    HSP Apoptosis Cancer
    Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule.
  • HY-119726
    Fosmanogepix

    APX001; E1211

    Fungal Infection
    Fosmanogepix (APX001) is a first-in-class and orally available broad-spectrum antifungal agent, which targets the highly conserved Gwt1 fungal enzyme. Fosmanogepix (APX001) is an N-phosphonooxymethyl prodrug which is rapidly and completely metabolized by systemic alkaline phosphatases to the active moiety, APX001A. Fosmanogepix (APX001) can be used in development for the treatment of invasive fungal infections.
  • HY-17466
    Sancycline

    Bonomycin; 6-Demethyl-6-deoxytetracycline

    Bacterial Infection
    Sancycline is a rare semi-synthetic tetracycline prepared by hydrogenolysis of the chloro and benzylic hydroxy moieties of Declomycin.
  • HY-135125
    DC4

    ADC Cytotoxin Cancer
    DC4, an ADC cytotoxin, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC4 can be used for the targeted treatment of cancer.
  • HY-N1499
    Nystose

    Others Metabolic Disease
    Nystose is a tetrasaccharide with two fructose molecules linked via beta (1→2) bonds to the fructosyl moiety of sucrose.
  • HY-107824
    D-Melibiose

    Endogenous Metabolite Inflammation/Immunology
    D-Melibiose is a disaccharide which is composed of one galactose and one glucose moiety in an alpha (1-6) glycosidic linkage.
  • HY-135124
    DC44SMe

    ADC Cytotoxin Cancer
    DC44SMe, a phosphate prodrug of cytotoxic DNA alkylator DC44, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC44SMe exhibits IC50s of 2.0 nM, 2.8 nM, and 1.9 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC44SMe can be used for the targeted treatment of cancer.
  • HY-135123
    DC4SMe

    ADC Cytotoxin Cancer
    DC4SMe, a phosphate prodrug of cytotoxic DNA alkylator DC4, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC4SMe exhibits IC50s of 1.9 nM, 2.9 nM, and 1.8 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC4SMe can be used for the targeted treatment of cancer.
  • HY-100217
    DL-3-Indolylglycine

    Others Others
    DL-3-Indolylglycine is an unnatural amino acid that is very similar to Tryptophan, with the indole moiety directly attached to the α-position.
  • HY-130080
    DM3

    Maytansinoid DM3

    ADC Cytotoxin Microtubule/Tubulin Cancer
    DM3 (Maytansinoid DM3) is a maytansine analog bearing disulfide or thiol groups and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs).
  • HY-100503
    Maytansinoid DM4

    ADC Cytotoxin Cancer
    Maytansinoid DM4 is a thiol-containing maytansine derivative with highly potent cytotoxicity. Maytansinoid DM4 can be used as a cytotoxic moiety of ADC.
  • HY-Y0015
    p-Dimethylaminobenzaldehyde

    4-Dimethylaminobenzaldehyde

    Others Others
    p-Dimethylaminobenzaldehyde (4-Dimethylaminobenzaldehyde) is an organic compound containing amine and aldehyde moieties which is used in Ehrlich's reagent and Kovac's reagent to test for indoles.
  • HY-130768
    N-(Azido-PEG3)-N-Fluorescein-PEG3-acid

    PROTAC Linker Cancer
    N-(Azido-PEG3)-N-Fluorescein-PEG3-acid is a PEG-based PROTAC linker which contains azide, fluorescein and carboxylic acid moieties.
  • HY-107447
    N-Deshydroxyethyl Dasatinib

    N-Deshydroxyethyl BMS-354825

    Ligand for Target Protein for PROTAC Cancer
    N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825), the Dasatinib-based moiety, binds to IAP ligand via a linker to form SNIPER to degrade ABL.
  • HY-136594
    BODIPY aminoacetaldehyde

    BAAA

    Aldehyde Dehydrogenase (ALDH) Cancer
    BODIPY aminoacetaldehyde (BAAA) is a fluorescent substrate for both murine and human aldehyde dehydrogenase (ALDH). BODIPY aminoacetaldehyde consists of an aminoacetaldehyde moiety bonded to the BODIPY fluorochrome and can be used to label stem cells.
  • HY-N6681
    15-Acetoxyscirpenol

    Caspase Bacterial Apoptosis Antibiotic Infection
    15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat T cell growth in a dose-dependent manner by activating other caspases independent of caspase-3.
  • HY-130993
    Isatropolone A

    Parasite Infection
    Isatropolone A, a natural product containing a 1,5-diketone moiety, is reisolated from Streptomyces Gö66. Isatropolone A shows potent activity against Leishmania donovani with an IC50 of 0.5 μM.
  • HY-113123
    LysoPC(14:0/0:0)

    Endogenous Metabolite Metabolic Disease Neurological Disease
    LysoPC(14:0/0:0) is a lysophospholipid (LyP). It is a monoglycerophospholipid in which a phosphorylcholine moiety occupies a glycerol substitution site. LysoPC(14:0/0:0) has potent antispasmodic effect.
  • HY-111839
    ATRA-hydroxyimino

    CRABP-II ligand 1

    Ligand for Target Protein for PROTAC Cancer
    ATRA-hydroxyimino (CRABP-II ligand 1), the Retinoic acid (ATRA)-based moiety, binds to cIAP1 ligand (Bestatin) via a linker to form SNIPER to degrade CRABP-II in IMR-32 cells.
  • HY-16138
    Ivaltinostat

    CG-200745

    HDAC Autophagy Apoptosis Cancer
    Ivaltinostat (CG-200745) is a potent HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat inhibits deacetylation of histone H3 and tubulin. Ivaltinostat induces apoptosis.
  • HY-100024
    NTRC 0066-0

    Others Cancer
    NTRC 0066-0 is a selective threonine tyrosine kinase (TTK) inhibitor (IC50=0.9 nM). NTRC 0066-0 can be used for the research of cancer.
  • HY-137820
    Brr2-IN-3

    Others Others
    Brr2-IN-3 is a potent and selective Brr2 helicase allosteric Inhibitor. Brr2-IN-3 inhibits helicase activity in dose-dependent manner with an IC50 value of 1.3 μM.
  • HY-129363
    AP1867-3-(aminoethoxy)

    Ligand for Target Protein for PROTAC FKBP Cancer
    AP1867-3-(aminoethoxy), the AP1867 based moiety, is a synthetic ligand for FKBP. AP1867-3-(aminoethoxy) can be used in the synthesis of PROTAC FKBP12 F36V degrader.
  • HY-B1738A
    Pralidoxime iodide

    AChE Neurological Disease
    Pralidoxime iodide is a reactivator of acetylcholinesterase (AChE). Pralidoxime iodide reactivates nerve agent, which inhibits AChE via direct nucleophilic attack by the oxime moiety on the phosphorus center of the bound nerve agent. Pralidoxime iodide is an antidote for organophosphate poisoning.
  • HY-115545
    DBCO-NHS ester 3

    ADC Linker Cancer
    DBCO-NHS ester 3 (Compound 12) is a cleavable linker that is used for making antibody-drug conjugate (ADC). DBCO-NHS ester 3 is a derivative of Dibenzylcyclooctyne (DBCO) obtained by activation of N-hydroxysuccinimide by the carboxylic acid moiety of both methyl-oxanorbornadiene (MeOND) and dibenzoazacyclooctyne (DIBAC).
  • HY-134640
    AUTAC4

    AUTAC Mitophagy Cancer Neurological Disease
    AUTAC4 is a mitochondria-targeting autophagy-targeting chimera (AUTAC). AUTAC4 downregulates cytosolic proteins and promotes targeted mitochondrial turnover via mitophagy.
  • HY-130994
    Aeruginosin 865

    NF-κB ADC Cytotoxin Cancer Inflammation/Immunology
    Aeruginosin 865, isolated from terrestrial cyanobacterium Nostoc sp. Lukešová 30/93, is the first aeruginosin-type peptide containing both a fatty acid and a carbohydrate moiety. Aeruginosin 865 inhibits translocation of NF-kB to the nucleus. Aeruginosin 865 has anti-inflammatory effect
  • 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-131704
    FGFR4-IN-5

    FGFR Cancer
    FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC50 of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma research.
  • HY-W018772
    D-Ribose(mixture of isomers)

    Endogenous Metabolite Inflammation/Immunology Cancer
    D-Ribose(mixture of isomers) is an energy enhancer, and acts as a sugar moiety of ATP, and widely used as a metabolic therapy supplement for chronic fatigue syndrome or cardiac energy metabolism. D-Ribose(mixture of isomers) is active in protein glycation, induces NF-κB inflammation in a RAGE-dependent manner.
  • HY-112373
    Aurora kinase inhibitor-3

    Aurora Kinase Others
    Aurora kinase inhibitor-3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM. Aurora kinase inhibitor-3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket.
  • HY-B1497
    Silver sulfadiazine

    AgSD

    Bacterial DNA/RNA Synthesis Antibiotic Infection
    Silver sulfadiazine (AgSD), a sulfonamide antibiotic, effects a dual inhibitory action on bacterial growth by its sulfa moiety (SD-SDZ) that prevents bacterial folate absorption and subsequent DNA synthesis. The silver that is released from Silver sulfadiazine binds and disrupts the DNA structure, precluding bacterial DNA replication.
  • HY-100658
    Didesmethyl cariprazine

    5-HT Receptor Dopamine Receptor Neurological Disease
    Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic drug candidate that exhibits high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor.
  • HY-130081
    DM3-SMe

    ADC Cytotoxin Microtubule/Tubulin Cancer
    DM3-SMe is a maytansine derivative and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs), which can be linked to antibody through disulfide bond or stable thioether bond. DM3-SMe shows highly cytotoxic activity in vitro with an IC50 of 0.0011 nM.
  • HY-W010970
    5'-Guanylic acid disodium salt

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

    Endogenous Metabolite Others
    5'-Guanylic acid disodium salt (5'-GMP disodium salt) is composed of guanine, ribose, and phosphate moieties and it is a nucleotide monomer in messenger RNA. Guanosine derivatives are involved in intracellular signal transduction and have been identified in repetitive genomic sequences in telomeres, in ribosomal DNA, immunoglobulin heavy‐chain switch regions, and in the control regions of proto-oncogenes.
  • HY-138064
    4-APC hydrobromide

    Others Others
    4-APC hydrobromide is a highly sensitive and selective derivatization agent for aldehydes. 4-APC hydrobromide possesses an aniline moiety for a fast selective reaction with aliphatic aldehydes as well as a quaternary ammonium group for improved MS sensitivity. 4-APC hydrobromide allows highly sensitive and selective MS detection of aldehydes.
  • HY-130809
    DBCO-PEG4-Biotin

    Others Cancer
    DBCO-PEG4-Biotin is an azadibenzocyclooctyne-biotin derivative containing a biotin group and 4 PEGs. DBCO-PEG4-Biotin is a versatile biotinylation reagent used for the introduction of a biotin moiety to azide-labeled biomolecules via copper-free strain-promoted alkyne-azide click chemistry (SPAAC) reaction.
  • HY-138620
    MCU-i4

    Mitochondrial Metabolism Metabolic Disease
    MCU-i4 blocks the IP3-dependent mitochondrial Ca 2+-uptake, maintaining the gatekeeping role of their target.
  • HY-75706
    N-Descyclopropanecarbaldehyde Olaparib

    E3 Ligase Ligand-Linker Conjugate PARP Cancer
    N-Descyclopropanecarbaldehyde Olaparib is an analogue of Olaparib containing DOTA moiety. N-Descyclopropanecarbaldehyde Olaparib is a CRBN-based ligand for synthesizing novel dual EGFR and PARP PROTAC, DP-C-4. N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled F-18 or fluorophore for positron emission tomography (PET) or optical imaging in several types of tumor.
  • HY-130082
    DM4-SMe

    ADC Cytotoxin Microtubule/Tubulin Cancer
    DM4-SMe is a metabolite of antibody-maytansin conjugates (AMCs) and a tubulin inhibitor, and also a cytotoxic moiety of antibody-drug conjugates (ADCs), which can be linked to antibody through disulfide bond or stable thioether bond. DM4-SMe inhibits KB cells with an IC50 of 0.026 nM.
  • HY-133869
    cGMP-HTL

    cGMP-HaloTag-ligand

    Autophagy Cancer
    cGMP-HTL contains a HT-ligand, a linker and the Cys-S-cGMP (autophagy tag). cGMP-HTL increases the K63-linked ubiquitination of mitochondria. AUTAC (autophagy-targeting chimera) is a novel targeted-clearance strategy that contains a degradation tag (guanine derivatives) and a warhead to provide target specificity.
  • HY-P2213
    GPLGIAGQ

    MMP Apoptosis Cancer
    GPLGIAGQ, a MMP2-cleavable polypeptide, is used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers for MMP2-triggered tumor targeting. GPLGIAGQ can be used to synthesis unique MMP2-targeted photosensitizer in photodynamic therapy (PDT).
  • HY-P2213A
    GPLGIAGQ TFA

    MMP Apoptosis Cancer
    GPLGIAGQ TFA, a MMP2-cleavable polypeptide, is used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers for MMP2-triggered tumor targeting. GPLGIAGQ TFA can be used to synthesis unique MMP2-targeted photosensitizer in photodynamic therapy (PDT).
  • HY-13631D
    Dxd

    Exatecan derivative for ADC

    Topoisomerase ADC Cytotoxin Cancer
    Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).
  • HY-17442
    Azathramycin

    Azaerythromycin A; Desmethyl Azithromycin

    Bacterial Antibiotic Infection
    Azathramycin (Azaerythromycin A) is an antibiotic and targets ribosome.
  • HY-U00361
    Itch-Targeting Compound 1

    Others Infection Inflammation/Immunology
    Itch-Targeting Compound 1 is an anti-itching agent.
  • HY-111024
    2,2,5,7,8-Pentamethyl-6-Chromanol

    PMC

    Androgen Receptor Cancer
    2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines.
  • HY-133084
    ERK-IN-2

    ERK Cancer
    ERK-IN-2 is a 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-101949
    LTX-401 dihydrochloride

    Others Inflammation/Immunology
    LTX-401, an oncolytic amino acid derivative, targets the Golgi apparatus.
  • HY-134809
    Cyclotriazadisulfonamide

    CADA

    HIV Infection Inflammation/Immunology
    Cyclotriazadisulfonamide (CADA) is a specific CD4-targeted HIV entry inhibitors. Cyclotriazadisulfonamide (CADA) inhibits the co-translational translocation of human CD4 (huCD4) into the ER lumen in a signal peptide (SP)-dependent way.
  • HY-100875
    Bisantrene

    CL216942

    Topoisomerase Cancer
    Bisantrene is a highly effective antitumor drug, targets eukaryotic type II topoisomerases.
  • HY-130614
    PROTAC EED degrader-1

    PROTACs Histone Methyltransferase Cancer
    PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit.
  • HY-134761
    EN4

    c-Myc Cancer
    EN4 is a covalent ligand that targets cysteine 171 (C171) of MYC. EN4 is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.
  • HY-130615
    PROTAC EED degrader-2

    PROTACs Histone Methyltransferase Cancer
    PROTAC EED degrader-2 is a PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit.
  • HY-18219
    Walrycin B

    Bacterial Antibiotic Infection
    Walrycin B is a novel antibacterial compound specifically targeting the essential WalR response regulator.
  • HY-13901
    GANT 61

    NSC 136476

    Gli Autophagy Cancer
    GANT 61 is an inhibitor of Gli1 and Gli2 targeting the Hedgehog/GLI pathway.
  • HY-14881A
    Bedaquiline fumarate

    R403323; TMC207 fumarate; R207910 fumarate

    Bacterial Antibiotic Infection
    Bedaquiline fumarate, a diarylquinoline antibiotic that targets ATP synthase, is effective for the treatment of Mycobacterium tuberculosis infections.
  • HY-U00393
    Arrhythmic-Targeting Compound 1

    Others Cardiovascular Disease
    Arrhythmic-Targeting Compound 1 is used for the research of arrhythmic disease, with nitrogen-containing spirocycles.
  • HY-U00357
    Urinary Incontinence-Targeting Compound 1

    Others Neurological Disease
    Urinary Incontinence-Targeting Compound 1 is a sulfonanilide derivative, used in the research of urinary incontinence.
  • HY-16366
    Briciclib

    ON 014185

    Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    Briciclib (ON 014185) is a derivative of ON 013100, and has the potential in targeting eIF4E for solid cancers.
  • HY-112879
    Mito-TEMPO

    Mitochondrial Metabolism Inflammation/Immunology
    Mito-TEMPO is a mitochondria-targeted superoxide dismutase mimetic with superoxide and alkyl radical scavenging properties.
  • HY-10990
    Abexinostat

    CRA 024781; PCI-24781

    HDAC Cancer
    Abexinostat (CRA 024781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM.
  • HY-129379
    DC0-NH2

    ADC Cytotoxin Cancer
    DC0-NH2 is an effector moiety for ADC and a simplified analog of DC1 with better stability. DC0-NH2 is about 1000-fold more cytotoxic than commonly used anticancer drugs (ex. Doxorubicin). DC0-NH2 can bind to the minor groove of DNA, followed by alkylation of adenine residues by its propabenzindole (CBI) component.
  • HY-130822
    K-Ras ligand-Linker Conjugate 4

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

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

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

    Target Protein Ligand-Linker Conjugate Cancer
    K-Ras ligand-Linker Conjugate 3 (Compound 001371) incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 3 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
  • HY-119970
    Helenalin

    NF-κB Cancer Inflammation/Immunology
    Helenalin is an anti-inflammatory sesquiterpene lactone. Helenalin selectively inhibits transcription factor NF-κB by directly targeting p65. Helenalin has alkylating activity, targets the cysteine sulfhydryl groups in the p65 subunit of NF-κB, thereby inhibits its DNA binding.
  • HY-13631DS
    Dxd-D5

    Exatecan-D5 derivative for ADC

    Topoisomerase ADC Cytotoxin Cancer
    Dxd-D5 (Exatecan-D5 derivative for ADC) is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) .
  • HY-P9921
    Trastuzumab emtansine

    Ado-Trastuzumab emtansine; PRO132365; T-DM 1

    Antibody-Drug Conjugate (ADC) EGFR Cancer
    Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer.
  • HY-N0352
    Tuberostemonine

    Parasite Infection
    Tuberostemonine, an alkaloid, is an antimalarial agent that targets Plasmodium falciparum ferredoxin-NADP + reductases (pfFNR).
  • HY-N0805A
    Alisol B

    Others Metabolic Disease
    Alisol B is a potentially novel therapeutic compound for bone disorders by targeting the differentiation of osteoclasts as well as their functions.
  • HY-N2146
    Combretastatin A4

    CRC 87-09

    Microtubule/Tubulin Cancer
    Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.
  • HY-P9908
    Adalimumab

    Anti-Human TNF-alpha, Human Antibody

    TNF Receptor Inflammation/Immunology
    Adalimumab is a human monoclonal IgG1 antibody targeting tumour necrosis factor α (TNF-α).
  • HY-100116A
    Mitoquinone mesylate

    MitoQ mesylate; MitoQ10 mesylate

    Reactive Oxygen Species Metabolic Disease Cancer
    Mitoquinone mesylate is a TPP-based, mitochondrially targeted antioxidant in order to protect against oxidative damage.
  • HY-103028
    GSK962

    Others Others
    GSK962 is an inactive enantiomer of GSK963 and can be used to confirm on-target effects.
  • HY-100431
    IMR-1

    Notch Cancer
    IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with an IC50 of 26 μM. IMR-1 prevents the recruitment of Mastermind-like 1 (Maml1) to the Notch Ternary Complex (NTC) on chromatin, inhibits Notch target gene transcription and dramatically inhibits tumor growth.
  • HY-69220
    7-Octynoic acid

    PROTAC Linker Cancer
    7-Octynoic acid (compound 42) is a PROTAC linker and can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-100306
    PNU-176798

    Bacterial Infection
    PNU-176798 is an antimicrobial agent, targeting protein synthesis in a wide spectrum of gram-positive and anaerobic bacteria.
  • HY-W039897
    Methyl α-D-mannopyranoside

    Others Inflammation/Immunology
    Methyl α-D-mannopyranoside could target macrophages in anti-tuberculosis inhalation therapy.
  • HY-101750
    Arrhythmias-Targeting Compound 1

    Others Cardiovascular Disease
    Arrhythmias-Targeting Compound 1 is used in the research of arrhythmias, extracted from patent WO 2001028992 A2.
  • HY-P9968
    Nimotuzumab

    EGFR Cancer
    Nimotuzumab is a humanized IgG1 monoclonal antibody targeting EGFR with a KD of 0.21 nM. Nimotuzumab is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab, a strong antitumor drug, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC).
  • HY-12201
    TAK-901

    Aurora Kinase Cancer
    TAK-901 is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively.
  • HY-U00314
    Anti-neurodegeneration agent 1

    Others Neurological Disease
    Anti-neurodegeneration agent 1 a neurodegeneration-targeting compound extracted from patent WO2008039514A1, Compound I.
  • HY-U00385
    Neuromuscular Disorder-Targeting Compound 1

    Others Neurological Disease
    Neuromuscular Disorder-Targeting Compound 1 is used in the research of neuromuscular disorders such as symptoms of fibromyalgia syndrome and chronic fatigue syndrome.
  • HY-10338
    Foretinib

    XL880; GSK1363089; GSK089; EXEL-2880

    VEGFR c-Met/HGFR Cancer
    Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.
  • HY-122866
    ZT-12-037-01

    Ras Cancer
    ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM.
  • HY-100474
    Visomitin

    SKQ1

    Reactive Oxygen Species Inflammation/Immunology
    Visomitin (SKQ1) is a mitochondrial-targeted antioxidant with the high mitochondrion membrane penetrating ability and potent antioxidant capability.
  • HY-P9911
    Vedolizumab

    Anti-Human lymphocyte α4β7 integrin, Humanized Antibody

    Integrin Inflammation/Immunology
    Vedolizumab is a humanized monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.
  • HY-131139
    Ganglioside GD3 disodium salt

    Others Cancer
    Ganglioside GD3 disodium salt is a melanoma-associated antigen and has been used as a target for the immune therapy of melanomas.
  • HY-13674
    Maytansine

    NSC 153858

    Microtubule/Tubulin Cancer
    Maytansine is a highly potent microtubule-targeted compound that induces mitotic arrest and kills tumor cells at subnanomolar concentrations.
  • HY-139482
    tri-GalNAc-COOH

    LYTAC Cancer
    tri-GalNAc-COOH is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research.
  • HY-17602
    Amcasertib

    BBI503

    Others Cancer
    Amcasertib is an orally administered investigational agent designed to inhibit cancer stem cell pathways, including Nanog, by targeting stemness kinases.
  • HY-W004697
    Boc-GABA-OH

    PROTAC Linker Cancer
    Boc-GABA-OH is a PROTAC linker which can be used to synthesis UNC6852, an EED-targeted PROTAC.
  • HY-P1034
    DAPTA

    D-Ala-peptide T-amide; Adaptavir

    CCR HIV Infection Endocrinology
    DAPTA is a synthetic peptide, functions as a viral entry inhibitor by targeting selectively CCR5, and shows potent anti-HIV activities.
  • HY-N1423
    Glycocholic acid

    Endogenous Metabolite Cancer
    Glycocholic acid is a bile acid with anticancer activity, targeting against pump resistance-related and non-pump resistance-related pathways.
  • HY-13640
    Rabacfosadine

    GS-9219; VDC-1101

    Others Cancer
    Rabacfosadine (GS-9219), a novel prodrug of the nucleotide analogue PMEG, is designed as a cytotoxic agent that preferentially targets lymphoid cells.
  • HY-U00300
    Cancer-Targeting Compound 1

    Others Cancer
    Cancer-Targeting Compound 1 is used in the research of hormone-​related cancer, extracted from patent WO 2008021331 A2.
  • HY-N0239
    Bulleyaconitine A

    Sodium Channel Neurological Disease
    Bulleyaconitine A is an analgesic and antiinflammatory drug isolated from Aconitum plants; has several potential targets, including voltage-gated Na+ channels.
  • HY-U00310
    Neuromuscular-targeting compound 1

    Others Neurological Disease
    Neuromuscular-targeting compound 1, extracted from patent WO2009099594 A1, Paragraph 0100, is useful in treatment of neuromuscular diseases.
  • HY-122909
    GSK2593074A

    GSK'074

    RIP kinase Inflammation/Immunology
    GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3.
  • HY-B2116
    Osalmid

    Oxaphenamide; 4'-Hydroxysalicylanilide

    HBV Infection
    Osalmid is a ribonucleotide reductase small subunit M2 (RRM2) targeting compound; suppresses ribonucleotide reductase activity with an IC50 of 8.23 μM.
  • HY-16596
    CNX-1351

    PI3K Cancer
    CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
  • HY-U00362
    Neurodegenerative Disorder-Targeting Compound 1

    Proteasome Neurological Disease
    Neurodegenerative Disorder-Targeting Compound 1 is a calpain inhibitor extracted from patent WO2010128102A1, compound example 63.
  • HY-102007
    Gamitrinib TPP

    HSP Cancer
    Gamitrinib TPP is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
  • HY-116702
    Flufiprole

    GABA Receptor Others
    Flufiprole is a nonsystemic phenylpyrazole insecticide targeting the GABA receptor used in the rice field. Flufiprole is excellent in controlling a wide range of pests.
  • HY-14796
    Olesoxime

    TRO 19622; NSC 21311

    Mitochondrial Metabolism Neurological Disease
    Olesoxime (TRO 19622) is a mitochondrial-targeted neuroprotective compound with mean EC50 value for increasing cell survival is 3.2±0.2 µM.
  • HY-19341
    Compound 401

    DNA-PK Cancer
    Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM) that also targets mTOR but not PI3K in vitro.
  • HY-N7453
    Fengycin

    Fungal Infection
    Fengycin is a cyclic lipopeptide used as an agricultural fungicide. Fengmycin has an anti-fungal infection effect by damaging the target's cell membrane.
  • HY-W077028
    N-(2-Hydroxypropyl)methacrylamide

    Others Others
    N-(2-Hydroxypropyl)methacrylamide is used to synthesize copolymers for the targeted delivery of antileishmanial agents in Visceral leishmaniasis (VL) .
  • 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-141536
    PSMA-ALB-56

    Drug-Linker Conjugates for ADC Cancer
    PSMA-ALB-56 is a PSMA-targeting radioligand designed by combining the glutamate-urea PSMA-binding entity and an albumin binder.
  • 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-112088
    AZD4573

    CDK Cancer
    AZD4573 is a potent and highly selective CDK9 inhibitor (IC50 of <4 nM) that enables transient target engagement for the treatment of hematologic malignancies.
  • HY-15233
    Letermovir

    AIC246

    CMV Infection
    Letermovir (AIC246) is a potent inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
  • HY-78131
    Ibuprofen

    (±)-Ibuprofen

    COX Inflammation/Immunology Cancer
    Ibuprofen is an anti-inflammatory agent targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-16307
    MB05032

    Phosphatase Metabolic Disease
    MB05032 is a special and efficacious GNG inhibitor targeted the AMP binding site of fructose 1,6-bisphosphatase (FBPase) with an IC50 value of 16 nM.
  • HY-111758
    PROTAC B-Raf degrader 1

    PROTACs Raf Cancer
    PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf. With anti-cancer activity.
  • HY-102075B
    TMP780

    ROR Inflammation/Immunology
    TMP780 is an inverse agonist of RORγt with an IC50 of 13 nM. RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders.
  • HY-10340B
    Tirbanibulin Mesylate

    KX2-391 Mesylate; KX01 Mesylate

    Src Microtubule/Tubulin Cancer
    Tirbanibulin Mesylate (KX2-391 Mesylate) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
  • HY-15359
    Episilvestrol

    Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    Episilvestrol is a derivative of silvestrol, isolated from the fruits and twigs of Aglaia silvestris, and is a specific eIF4A-targeting translation inhibitor, with antitumor activity.
  • HY-10822A
    ONX 0801 trisodium

    BGC 945 trisodium; Idetrexed trisodium; CB 300945 trisodium

    Thymidylate Synthase Cancer
    ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors.
  • HY-12702
    10058-F4

    c-Myc Autophagy Cancer
    10058-F4 is a c-Myc inhibitor that prevents c-Myc-Max dimerization and transactivation of c-Myc target gene expression.
  • HY-N4139
    Protohypericin

    Others Cancer
    Protohypericin is a naturally occurring naphthodianthrone derived from plant Hypericum perforatum. Radioiodinated protohypericin is used in Tumor necrosis targeted radiotherapy.
  • HY-102007A
    Gamitrinib TPP hexafluorophosphate

    HSP Cancer
    Gamitrinib TPP hexafluorophosphate is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP hexafluorophosphate is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
  • HY-136269A
    A 410099.1, amine-Boc

    E3 Ligase Ligand-Linker Conjugate Cancer
    A 410099.1, amine-Bocis a functionalized IAP ligand and can be used for the synthesis of PROTACs, such as PROTACs targeting BTK (PROTACs 4 and 5).
  • HY-136269
    A 410099.1, amine-Boc hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    A 410099.1, amine-Boc hydrochloride is a functionalized IAP ligand and can be used for the synthesis of PROTACs, such as PROTACs targeting BTK (PROTACs 4 and 5).
  • HY-10340
    Tirbanibulin

    KX2-391; KX-01

    Src Microtubule/Tubulin Cancer
    Tirbanibulin (KX2-391) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
  • 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-P2322
    Iturin A

    Fungal
    IturinA exhibits strong antifungal activity against pathogenic yeast and fungi. Iturin A interacts with the cytoplasmic membrane of the target cell forming ion conducting pores.
  • HY-14989
    SQ109

    NSC 722041

    Parasite Bacterial Antibiotic Infection
    SQ109 is a potent inhibitor of the trypomastigote form of the parasite, with IC50 for cell killing of 50±8 nM. SQ109, targets MmpL3, is an antitubercular agent.
  • HY-10340A
    Tirbanibulin dihydrochloride

    KX2-391 dihydrochloride; KX-01 dihydrochloride

    Src Microtubule/Tubulin Cancer
    Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
  • HY-129774
    Phthalimide-PEG4-MPDM-OH

    PROTAC Linker Cancer
    Phthalimide-PEG4-MPDM-OH is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-MPDM-OH can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-130715
    tert-Butyl 11-aminoundecanoate

    PROTAC Linker Cancer
    tert-Butyl 11-aminoundecanoate (compound 6b) is a PROTAC linker, which refers to the PEG composition. tert-Butyl 11-aminoundecanoate can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-129773
    Phthalimide-PEG4-PDM-OTBS

    PROTAC Linker Cancer
    Phthalimide-PEG4-PDM-OTBS is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-PDM-OTBS can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-141594
    Modified MMAF

    Others Cancer
    Modified MMAF, an ADC cytotoxin, can be used in the synthesis of Antibody-drug Conjugate (ADC). Modified MMAF can be used for the targeted treatment of cancer.
  • HY-100419
    BFH772

    VEGFR Cancer
    BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM.
  • HY-G0017A
    N-Desmethyl imatinib mesylate

    Norimatinib mesylate; Imatinib metabolite N-Desmethyl imatinib mesylate

    Drug Metabolite Others
    N-Desmethyl imatinib mesylate (Norimatinib mesylate) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR.
  • HY-111847
    Androstanolone acetate

    Androgen Receptor Ligand for Target Protein for PROTAC Cancer
    Androstanolone acetate is an androgen ligand, which targets androgen receptor (AR). Androstanolone acetate binds to cIAP1 ligand Bestatin via a linker to form PROTACs.
  • HY-15440
    Temsavir

    BMS-626529

    HIV Infection
    Temsavir (BMS-626529) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 + T cells.
  • HY-10331S
    Regorafenib D3

    BAY 73-4506 D3

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib D3 (BAY 73-4506 D3) is a deuterium labeled Regorafenib. Regorafenib is a multi-targeted receptor tyrosine kinase inhibitor.
  • HY-111927
    Pilloin

    Others Cancer Inflammation/Immunology
    Pilloin, a flavonoid isolated from Marrubium cylleneum, exerts a cytotoxic action targeted at the transformed lymphoblasts. Pilloin also possesses anti-inflammatory activity.
  • HY-13442
    Eribulin

    B1939; E7389; ER-086526

    Microtubule/Tubulin Apoptosis Cancer
    Eribulin (E7389) is a microtubule targeting agent that is used for the research of metastatic breast cancer. Eribulin inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules.
  • HY-G0017
    N-Desmethyl imatinib

    Norimatinib; Imatinib metabolite N-Desmethyl imatinib

    Drug Metabolite Others
    N-Desmethyl imatinib (Norimatinib) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR.
  • HY-111651
    Gboxin

    ATP Synthase Mitochondrial Metabolism Cancer
    Gboxin is an oxidative phosphorylation (OXPHOS) inhibitor that targets glioblastoma. Gboxin inhibits the activity of F0F1 ATP synthase. Antitumour activity.
  • HY-10407
    SU 5402

    VEGFR FGFR PDGFR Cancer
    SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
  • HY-P1727
    Super-TDU

    YAP Cancer
    Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model.
  • HY-14456A
    MAC13243

    Bacterial Infection
    MAC13243, an antibacterial agent, is an inhibitor of bacterial lipoprotein targeting chaperone, LolA. MAC13243 is an antibacterial agent with Gram-negative selectivity.
  • HY-12134
    Poloxin

    Polo-like Kinase (PLK) Cancer
    Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC50 of appr 4.8 μM.
  • HY-13442A
    Eribulin mesylate

    B1939 mesylate; E7389 mesylate; ER-086526 mesylate

    Microtubule/Tubulin Apoptosis Cancer
    Eribulin mesylate (E7389 mesylate) is a microtubule targeting agent that is used for the research of metastatic breast cancer. Eribulin mesylate inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules.
  • HY-13650
    Indisulam

    E 7070

    Carbonic Anhydrase Cancer
    Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15.
  • HY-131335
    p38α inhibitor 2

    p38 MAPK Inflammation/Immunology
    p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets.
  • HY-106991A
    Amustaline dihydrochloride

    S-303 dihydrochloride

    HIV Bacterial Infection
    Amustaline (S-303) dihydrochloride, a nucleic acid-targeted alkylator, is an efficient pathogen inactivation agent for blood components containing red blood cells. Amustaline dihydrochloride has three components: an acridine anchor (an intercalator that targets nucleic acids non-covalently), an effector (a bis-alkylator group that reacts with nucleophiles), and a linker (a small flexible carbon chain containing a labile ester bond that hydrolyzes at neutral pH to yield non-reactive breakdown products).
  • HY-101238
    Agmatine sulfate

    Imidazoline Receptor NO Synthase Endogenous Metabolite Neurological Disease Cancer
    Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.
  • HY-119433
    Asoprisnil

    J867

    Progesterone Receptor Endocrinology
    Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.
  • HY-B1408
    Salicylanilide

    2-Hydroxybenzanilide

    HIV Integrase HIV Infection
    Salicylanilide demonstrates a wide range of biological activities including antiviral potency which can inhibit HIV virus by targeting HIV-1 integrase or reverse transcriptase.
  • HY-B1161
    Methoprene

    ZR-515

    Others Others
    Methoprene, an insect juvenile growth hormone mimic, is a growth-regulating insecticide that manifests its toxicity to target organisms by acting as a juvenile hormone agonist.
  • HY-136374
    Haloxyfop-P-methyl

    Others Others
    Haloxyfop-P-methyl is an aryloxyphenoxypropionate herbicide. Haloxyfop-P-methyl can be absorbed by roots or foliage and hampers lipogenesis and increases oxidative stress in target plants.
  • HY-Y1750
    β-Aminopropionitrile

    Monoamine Oxidase Cancer
    β-Aminopropionitrile is a specific and irreversible lysyl oxidase (LOX) inhibitor. β-Aminopropionitrile targets the active site of LOX or LOXL isoenzymes.
  • HY-W010450
    Thymine

    Endogenous Metabolite Cancer Metabolic Disease
    Thymine is one of the four nucleobases in the nucleic acid of DNA and can be a target for actions of 5-fluorouracil (5-FU) in cancer treatment, with a Km of 2.3 μM.
  • HY-14622A
    Necrostatin 2 racemate

    Necrostatin 1S; Nec-1S; 7-Cl-O-Nec1

    RIP kinase Cancer
    Necrostatin 2 racemate (Nec-1S), the Nec-1 stable, is a potent and specific RIPK1 inhibitor lacking the IDO-targeting effect.
  • HY-131341
    Syk-IN-4

    Syk Cancer Inflammation/Immunology
    Syk-IN-4 is a potent, selective and orally bioavailable SYK inhibitor with an IC50 of 0.31 nM. SYK has emerged as a potential target for autoimmunity and hematological cancers.
  • HY-10372
    PP121

    mTOR PDGFR VEGFR Src Apoptosis Cancer
    PP121 is a multi-targeted kinase inhibitor with IC50s of 10, 60, 12, 14, 2 nM for mTOR, DNK-PK, VEGFR2, Src, PDGFR, respectively.
  • HY-108708
    GeA-69

    PARP Cancer
    GeA-69 is a selective, allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2, with a Kd of 2.1 µM.
  • HY-P1727A
    Super-TDU TFA

    YAP Cancer
    Super-TDU TFA is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU TFA suppresses tumor growth in gastric cancer mouse model.
  • HY-130637
    Boc-NH-PEG1-Ph-O-CH2COOH

    PROTAC Linker Cancer
    Boc-NH-PEG1-Ph-O-CH2COOH is a PROTAC Linker which is used for the EED-targeted PROTAC.
  • HY-10501
    SU14813

    PDGFR VEGFR c-Kit Cancer
    SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
  • HY-N6046
    Kamebakaurin

    NF-κB Cancer Inflammation/Immunology
    Kamebakaurin is a natural compound isolated from Isodon japonicus. Kamebakaurin is a potent inhibitor of NF-κB activation by directly targeting DNA-binding activity of p50.
  • HY-N0200
    Albaspidin AP

    Fatty Acid Synthase (FASN) Cancer Metabolic Disease
    Albaspidin AP inhibits fatty acid synthase (FAS) with an IC50 value of 71.7 μM. Fatty acid synthase (FAS) is emerging as a potential therapeutic target for cancer and obesity.
  • HY-B0795
    MHY1485

    mTOR Autophagy Cancer
    MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.
  • HY-10501A
    SU14813 maleate

    PDGFR VEGFR c-Kit Cancer
    SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
  • HY-17369
    Tirofiban hydrochloride monohydrate

    Integrin Cardiovascular Disease
    Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist IC50 value: Target: integrin IIb/IIIa Tirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation.
  • HY-111866
    PROTAC RIPK degrader-2

    PROTACs RIP kinase Inflammation/Immunology
    PROTAC RIPK degrader-2 is a nonpeptidic PROTAC which potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.
  • HY-129939
    PROTAC BRD4 ligand-1

    Epigenetic Reader Domain Ligand for Target Protein for PROTAC Cancer
    PROTAC BRD4 ligand-1 is a potent BET inhibitor and a ligand for target BRD4 protein for PROTACT GNE-987 (HY-129937A).
  • HY-102028
    KY1220

    Wnt β-catenin Cancer
    KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.
  • HY-112901
    DC41

    ADC Cytotoxin Cancer
    DC41 is a DC1 derivative. DC1, a simplified analogue of CC-1065, is an antibody conjugate of cytotoxic DNA alkylators for the targeted treatment of cancer.
  • HY-B0863
    Glyphosate

    Apoptosis Autophagy Cancer
    Glyphosate is an herbicidal derivative of the amino acid glycine. Glyphosate targets and blocks a plant metabolic pathway not found in animals, the shikimate pathway, required for the synthesis of aromatic amino acids in plants.
  • HY-B0323
    Sulfisoxazole

    Sulfafurazole

    Bacterial Endothelin Receptor Antibiotic Cancer Infection Endocrinology
    Sulfisoxazole (Sulfafurazole), an endothelin receptor antagonist, is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A.
  • HY-129772
    Phthalimide-PEG3-C2-OTs

    PROTAC Linker Cancer
    Phthalimide-PEG3-C2-OTs (Compound 5) is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG3-C2-OTs can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-40178
    NH2-C4-NH-Boc

    PROTAC Linker Cancer
    NH2-C4-NH-Boc (compound 15) is a PROTAC linker, which refers to the Alkyl/ether composition. NH2-C4-NH-Boc can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-112611
    H3B-5942

    Estrogen Receptor/ERR Cancer
    H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERα WT or ERα mutations.
  • HY-131014
    FM-479

    JAK Inflammation/Immunology
    FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases. FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
  • HY-15843
    MIR96-IN-1

    MicroRNA Apoptosis Cancer
    MIR96-IN-1 targets the Drosha site in the miR-96 (miRNA-96, microRNA-96) hairpin precursor, inhibiting its biogenesis, derepressing downstream targets, and triggering apoptosis in breast cancer cells. MIR96-IN-1 binds to RNAs with Kds of 1.3, 9.4, 3.4, 1.3 and 7.4 μM for RNA1, RNA2, RNA3, RNA4 and RNA5, respectively.
  • 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-112899
    DC1

    ADC Cytotoxin DNA Alkylator/Crosslinker Cancer
    DC1, an analogue of the minor groove-binding DNA alkylator CC-1065, is a ADC Cytotoxin. DC1 can be used in synthesis of antibody-drug conjugates for the targeted treatment of cancer.
  • HY-109084
    Conteltinib

    CT-707

    FAK Cancer
    Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK, ALK, and Pyk2. Conteltinib exerts significant inhibitory effect on FAK with an IC50 of 1.6 nM.
  • HY-W028047
    JFD01307SC

    Bacterial Infection Inflammation/Immunology
    JFD01307SC is a glutamine synthetase inhibitor and anti-tuberculosis agent. JFD01307SC acts as a mimic of L-Glutamate and thus target enzymes involved in glutamine biosynthesis.
  • HY-N0135
    Tanshinone IIA

    Dan Shen ketone

    VEGFR Cardiovascular Disease Cancer
    Tanshinone IIA (Tan IIA) is one of the main compositions in the root of red-rooted salvia. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2.
  • HY-W004546
    Abametapir

    MMP Parasite Infection
    Abametapir is a metalloproteinase (MMP) inhibitor which is able to target metalloproteinases critical to egg hatching and louse development. Abametapir can inhibit hatching of both head and body louse.
  • HY-13263
    CHIR-124

    Checkpoint Kinase (Chk) FLT3 PDGFR Apoptosis Cancer
    CHIR-124 is a potent and selective Chk1 inhibitor with IC50 of 0.3 nM, and also potently targets PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM.
  • HY-13030A
    (R)-(-)-JQ1 Enantiomer

    Epigenetic Reader Domain Cancer
    (R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (R)-(-)-JQ1 Enantiomer has no effect.
  • HY-136373
    Metazachlor

    Others Others
    Metazachlor is a herbicide of the chloroacetamide class. Metazachlor is an inhibitor of the synthesis of long chain fatty acids and has an effect on cell division or tissue differentiation in the germinating and emerging weed target species.
  • HY-119165
    GSM-1

    γ-secretase Neurological Disease
    GSM-1 is a potent γ-secretase modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1).
  • HY-N1455
    Falcarinol

    Panaxynol; Carotatoxin

    HSP Cancer
    Falcarinol (Panaxynol) is a natural, orally active Hsp90 inhibitor targeting both the N-terminal and C-terminal of Hsp90 with limited toxicities. Falcarinol (Panaxynol) induces apoptosis.
  • HY-15283
    Clopidogrel

    P2Y Receptor Cardiovascular Disease
    Clopidogrel is an orally active platelet inhibitor that targets P2Y12 receptor. Clopidogrel is used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
  • HY-111870
    PROTAC RIPK degrader-6

    PROTACs RIP kinase Cancer
    PROTAC RIPK degrader-6 (example 1) is a PROTAC targeting RIP Kinase degradation wherein the RIP2 kinase inhibitor is linked via a linker to a cereblon binder.
  • HY-114406
    TD-106

    Ligand for E3 Ligase Cancer
    TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation.
  • HY-B1100
    Estradiol (cypionate)

    Estrogen Receptor/ERR Endocrinology Cancer
    Estradiol cypionate is a 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor IC50 value: Target: estrogen receptor Estradiol cypionate is a synthetic ester, is a estrogen.
  • HY-111605
    Macropa-NCS

    Others Cancer
    Macropa-NCS is conjugated to trastuzumab as well as to the prostate-specific membrane antigen-targeting compound RPS-070. A promising therapeutic radionuclide applied in the treatment of soft-tissue metastases.
  • HY-13943
    CNX-774

    Btk Cancer
    CNX-774 is an orally active, irreversible and selective BTK inhibitor, with an IC50 of < 1 nM. CNX-774 specifically targets Cysteine 481 of Btk for covalent modification.
  • HY-N7449
    Neamine

    Bacterial Cancer Infection Neurological Disease Cardiovascular Disease
    Neamine, a degradation product of Neomycin, is a broad-spectrum aminoglycoside antibiotic. Neamine is an anti-angiogenesis agent targeting angiogenin. Neamine has potent antibacterial, antitumor and neuroprotective activities.
  • HY-129937A
    GNE-987

    PROTACs Epigenetic Reader Domain Cancer
    GNE-987 is a highly active chimeric BET degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).
  • HY-129359
    PDP-Pfp

    ADC Linker Cancer
    PDP-Pfp is a reducible ADC linker used for the agents that target for the extracellular loop 1 (ECL1) of TM4SF1 (transmembrane 4 L6 family member 1).
  • HY-B0147A
    Pefloxacin mesylate

    Pefloxacinium mesylate

    Bacterial Antibiotic Infection
    Pefloxacin mesylate is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse) Target: DNA gyrase Pefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections.
  • HY-111876
    SNIPER(TACC3)-1

    SNIPER Cancer
    SNIPER(TACC3)-1 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway. SNIPER(TACC3)-1 induces cancer cell death.
  • HY-B0147
    Pefloxacin

    Pefloxacinium

    Bacterial Antibiotic Infection
    Pefloxacin is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse) Target: DNA gyrase Pefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections.
  • HY-P1674A
    Murepavadin TFA

    POL7080 TFA

    Bacterial Antibiotic Infection
    Murepavadin (TFA), a 14-amino-acid cyclic peptide, is a highly potent, specific antibiotic for the treatment of bacterial infections caused by Pseudomonas aeruginosa. Murepavadin (TFA) targets the lipopolysaccharide transport portin D .
  • HY-B1418
    Tazobactam

    CL-298741; YTR-830H

    Bacterial Antibiotic Infection
    Tazobactam is a beta Lactamase Inhibitor with antibacterial activity Target: Antibacterial Tazobactam is a pharmaceutical drug that inhibits the action of bacterial β-lactamases, especially those belonging to the SHV-1 and TEM groups.
  • HY-78695
    JQ-1 (carboxylic acid)

    Epigenetic Reader Domain Cancer
    JQ-1 carboxylic acid is a (+)-JQ1 derivative (a BET bromodomain inhibitor). JQ-1 carboxylic acid can be used as a precursor to synthesize PROTACs, which targets BET bromodomains.
  • 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-111877
    SNIPER(TACC3)-2

    SNIPER Cancer
    SNIPER(TACC3)-2 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway. SNIPER(TACC3)-2 induces cancer cell death.
  • HY-N2065
    Withaferin A

    NF-κB Ferroptosis Cancer Inflammation/Immunology
    Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
  • HY-12423A
    Pamufetinib mesylate

    TAS-115 mesylate

    VEGFR c-Met/HGFR Cancer
    Pamufetinib (TAS-115) mesylate is a potent VEGFRand hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
  • HY-10339
    KW-2449

    FLT3 FGFR Bcr-Abl Aurora Kinase Apoptosis Cancer
    KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABL T315I and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, respectively.
  • HY-122816
    HLY78

    Wnt Cancer Neurological Disease
    HLY78 is an activator of the Wnt/β-catenin signaling pathway, which targets the DIX domain of Axin and potentiates the Axin-LRP6 association to promote Wnt signaling transduction.
  • HY-126121
    2-Hydroxy Ibuprofen

    (±)-2-Hydroxy Ibuprofen

    COX Cancer Inflammation/Immunology
    2-Hydroxy Ibuprofen is a metabolite of Ibuprofen. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-12423
    Pamufetinib

    TAS-115

    VEGFR c-Met/HGFR Cancer
    Pamufetinib (TAS-115) is a potent VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
  • HY-131633A
    (+)-JQ-1-aldehyde

    Epigenetic Reader Domain Cancer
    (+)-JQ-1-aldehyde is the aldehyde form of (+)-JQ1. (+)-JQ-1-aldehyde can be uesd as a precursor to synthesize PROTACs, which targets BET bromodomains.
  • 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-107615
    TC LPA5 4

    LPL Receptor Cancer
    TC LPA5 4 is a LPA5 (GPR92)-specific non-lipid antagonist. TC LPA5 4 inhibits LPA-induced aggregation of isolated human platelet (LPA5-RH7777 cell line) with an IC50 of 800 nM. TC LPA5 4 displays selectivity for LPA5 over 80 other screened drug targets. TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells.
  • HY-N6257
    Cafestol

    ERK PGE synthase COX NF-κB Cancer Inflammation/Immunology
    Cafestol, one of the major components of coffee, is a coffee-specific diterpene from. Cafestol is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway. Cafestol contributes to its beneficial effects through various biological activities such as chemopreventive, antitumorigenic, hepatoprotective, antioxidative and antiinflammatory effects.
  • HY-131259
    Ibuprofen Impurity F

    COX Inflammation/Immunology
    Ibuprofen Impurity F is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-13615A
    EC-17 disodium salt

    Others Cancer
    EC-17 (disodium salt) is a folate receptor alpha (FRα) targeting contrast agent with fluorescent properties in the visible light spectrum. The peak excitation and emission wavelengths of EC-17 are 470/520 nm.
  • HY-D1267
    PAO-Nap

    Apoptosis Cancer
    PAO-Nap is the modified PAO attached a naphthalimide fluorophore using aminocaproic acid as a linker. PAO induces oxidative stress-mediated apoptosis in HL-60 cells by selectively targeting thioredoxin reductase.
  • HY-141549
    BPK-21

    Others Inflammation/Immunology
    BPK-21, an active acrylamide, suppresses T cell activation through blockade of ERCC3 function. BPK-21 specifically targets C342 in the helicase ERCC3.
  • HY-12703
    KSI-3716

    c-Myc Autophagy Cancer
    KSI-3716 is a potent c-Myc inhibitor that blocks c-MYC/MAX binding to target gene promoters. KSI-3716 is an effective intravesical chemotherapy agent for bladder cancer.
  • HY-B0147B
    Pefloxacin mesylate dihydrate

    Pefloxacinium mesylate dihydrate

    Bacterial Antibiotic Infection
    Pefloxacin mesylate dehydrate is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse) Target: DNA gyrase Pefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections.
  • HY-108547
    Alexidine dihydrochloride

    Fungal Apoptosis Infection
    Alexidine dihydrochloride is an anticancer agent that targets a mitochondrial tyrosine phosphatase, PTPMT1, in mammalian cells and causes mitochondrial apoptosis. Alexidine dihydrochloride has antifungal and antibiofilm activity against a diverse range of fungal pathogens.
  • HY-P2203A
    SAHM1 TFA

    Notch
    SAHM1 TFA is a Notch pathway inhibitor. SAHM1 TFA stabilizes hydrocarbon-stapled alpha helical peptide. SAHM1 TFA targets the protein-protein interface and prevents Notch complex assembly.
  • HY-100806
    Kynurenic acid

    Quinurenic acid

    iGluR Endogenous Metabolite Apoptosis Inflammation/Immunology Neurological Disease Endocrinology
    Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
  • HY-131258
    Ibuprofen impurity 1

    COX Inflammation/Immunology
    Ibuprofen impurity 1 is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-131260
    Ibuprofen Impurity K

    COX Inflammation/Immunology
    Ibuprofen Impurity K is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-N4053
    Heraclenin

    Others Inflammation/Immunology
    Heraclenin, a natural furanocoumarin, significantly inhibits T cell receptor-mediated proliferation in human primary T cells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT).
  • HY-13613
    Dutasteride

    GG 745; GI 198745

    5 alpha Reductase Apoptosis Cancer
    Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT.
  • HY-107512
    Kynurenic acid sodium

    iGluR Apoptosis Inflammation/Immunology Neurological Disease Endocrinology
    Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
  • HY-13217
    Vanoxerine dihydrochloride

    GBR-12909 dihydrochloride; I893 dihydrochloride

    Dopamine Transporter Neurological Disease
    Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT).
  • HY-13217A
    Vanoxerine

    GBR 12909; I893

    Dopamine Transporter Neurological Disease
    Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine (GBR-12909) binds to the target site on the dopamine transporter (DAT).
  • HY-18179
    AZD2932

    PDGFR VEGFR FLT3 c-Kit Cancer
    AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC50s of 8, 4, 7 and 9 nM in cell assay, respectively.
  • HY-P3108
    Alamandine

    Angiotensin Receptor Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Alamandine, a member of the renin-angiotensin system (RAS), a vasoactive peptide, is an endogenous ligand of the G protein-coupled receptor MrgD. Alamandine targets to protect the kidney and heart through anti-hypertensive actions.
  • HY-N6062
    Perivine

    Perivin

    Others Neurological Disease
    Perivine (Perivin) targets protein retinoblastoma-associated proteins (RbAp48) and resolves the instability of the RbAp48-FOG-1 complex. Perivine can be used for the study of Alzheimer's disease.
  • HY-101354
    R-IMPP

    PF-00932239

    Ser/Thr Protease Cancer Cardiovascular Disease
    R-IMPP (PF-00932239) is an anti-secretagogue of PCSK9 (IC50=4.8 μM), which targets the 80S ribosome to inhibit PCSK9 protein translation.
  • HY-115349
    Neamine tetrahydrochloride

    Bacterial Cancer Infection Neurological Disease
    Neamine tetrahydrochloride, a degradation product of Neomycin, is a broad-spectrum aminoglycoside antibiotic. Neamine tetrahydrochloride is an anti-angiogenesis agent targeting angiogenin. Neamine tetrahydrochloride has potent antibacterial, antitumor and neuroprotective activities.
  • 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-17369B
    Tirofiban

    L700462; MK383

    Integrin Cardiovascular Disease
    Tirofiban(L700462;MK383) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist Target: integrin IIb/IIIa Tirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation.
  • HY-141729
    Biotin-NH-PSMA-617

    Others Cancer
    Biotin-NH-PSMA-617 is a biotin-tagged PSMA-617. PSMA-617 is a small molecule targeting the prostate-specific membrane antigen (PSMA), which is directly expressed by the tumor cells .
  • HY-N6850
    Calenduloside E

    HSP Endogenous Metabolite
    Calenduloside E (CE) is a natural pentacyclic triterpenoid saponin extracted from Aralia elata. Calenduloside E (CE) has anti-apoptotic potent by targeting heat shock protein 90 (Hsp90).
  • 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-119989
    Cyclopyrimorate

    Others Infection
    Cyclopyrimorate, a highly effective bleaching herbicide for weed control in rice fields, targets homogentisate solanesyltransferase (HST). HST is a downstream enzyme of 4-hydroxyphenylpyruvate dioxygenase in the plastoquinone (PQ) biosynthesis pathway.
  • HY-18312
    PF-4618433

    Pyk2 Metabolic Disease
    PF-4618433 is a potent and selective PYK2 inhibitor, with an IC50 of 637 nM. PF-4618433 may be suitable for the research of osteoporosis, craniofacial and appendicular skeletal defects and for targeted bone regeneration.
  • HY-112306
    Ripretinib

    DCC-2618

    c-Kit PDGFR FLT3 VEGFR Apoptosis Cancer
    Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2). DCC-2618 exerts antineoplastic effect and induces apoptosis.
  • HY-P2657
    Verucopeptin

    HIF/HIF Prolyl-Hydroxylase Proton Pump Endogenous Metabolite Cancer
    Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
  • HY-130618
    Boc-C1-PEG3-C4-OH

    PROTAC Linker Cancer
    Boc-C1-PEG3-C4-OH is a PROTAC linker, which refers to the Alkyl/ether composition. Boc-C1-PEG3-C4-OH can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-10981A
    Lenvatinib mesylate

    E7080 mesylate

    VEGFR FGFR PDGFR RET c-Kit Cancer
    Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-109000
    Afabicin

    Debio 1450; AFN-1720

    Bacterial Infection
    Afabicin (Debio 1450) is the prodrug of Debio1452, specifically targeting staphylococci without significant activity against other Gram-positive or Gram-negative species. Debio1452 is an inhibitor FabI, an enzyme critical to fatty acid biosynthesis in staphylococci.
  • HY-13017
    Ivacaftor

    VX-770

    CFTR Autophagy Endocrinology
    Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
  • HY-10517
    Orantinib

    SU6668; TSU-68

    PDGFR FGFR VEGFR Apoptosis Cancer
    Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.
  • HY-128938
    EC1167

    Others Cancer
    EC1167 is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC).
  • HY-10065
    Axitinib

    AG-013736

    VEGFR PDGFR Cancer
    Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.
  • 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-10981
    Lenvatinib

    E7080

    VEGFR FGFR PDGFR c-Kit RET Cancer
    Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-19567
    PK 11195

    RP 52028

    Parasite Infection
    PK 11195 (RP 52028) is a ligand of translocator protein (TSPO), which targets Leishmania chemotherapy, with IC50s of 14.2 μM, 8.2 μM, 3.5 μM for L. amazonensis, L. major and L. braziliensis, respectively.
  • HY-107093
    MBC-11

    Others Cancer
    MBC-11 is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). MBC-11 has the potential for tumor-induced bone disease (TIBD) research.
  • HY-131388
    ABM-14

    Ligand for Target Protein for PROTAC Cancer
    ABM-14 is a ligand for targeting androgen receptor (AR) for PROTAC. ABM-14 binds to a ligand for VHL via linker to form ARCC-4 (HY-130492) to degrade AR.
  • HY-13077
    MK-8245 Trifluoroacetate

    Stearoyl-CoA Desaturase (SCD) Metabolic Disease
    MK-8245 trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.
  • HY-117985B
    Evogliptin tartrate

    DA-1229 tartrate

    Dipeptidyl Peptidase Metabolic Disease Inflammation/Immunology
    Evogliptin tartrate is a potent, orally bioavailable and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, with antidiabetic activity. Evogliptin tartrate has potential for anti-atherosclerosis therapy that targets arterial inflammation.
  • HY-112197
    PKG drug G1

    Others Cardiovascular Disease
    PKG drug G1 targets C42 of PKG Iα. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.
  • HY-N7142
    DL-Norepinephrine hydrochloride

    Adrenergic Receptor Neurological Disease Endocrinology
    DL-Norepinephrine hydrochloride is a synthetic phenylethylamine that mimics the sympathomimetic actions of the endogenous norepinephrine.DL-Norepinephrine hydrochloride is a neurotransmitter targets α1 and β1 adrenoceptors, has an increasing effect on subendocardial oxygen tension.
  • HY-133735A
    GRP-60367 hydrochloride

    Others Infection
    GRP-60367 hydrochloride is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains. GRP-60367 hydrochloride specifically targets the RABV G protein.
  • HY-132828
    Odatroltide

    DHDMIQK(KAP)

    Others Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    Odatroltide, as a nanoscale P-selectin inhibitor, is a nano-delivery system of 6,7-dihydroxyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid and KPAK to target the thrombus.
  • HY-100341
    M2I-1

    Others Others
    M2I-1 is a Mad2 inhibitor targeting the binding of Mad2 to Cdc20, an essential protein-protein interaction (PPI) within the spindle assembly checkpoint (SAC).
  • HY-131187
    BMS-1166-N-piperidine-COOH

    Ligand for Target Protein for PROTAC Cancer
    BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
  • HY-133781
    cis-Clopidogrel-MP Derivative

    Clopidogrel-MP-AM

    Others Others
    cis-Clopidogrel-MP Derivative (Clopidogrel-MP-AM) is a 3’-methoxyacetophenone derivative of Clopidogrel active metabolite. Clopidogrel is an orally active platelet inhibitor that targets P2Y12 receptor.
  • HY-N1374
    Magnolin

    ERK Inflammation/Immunology
    Magnolin, a major component of Magnolia flos (Shin-Yi), inhibits the Ras/ERKs/RSK2 signaling axis by targeting the active pocket of ERK1 and ERK2 with IC50s of 87 nM and 16.5 nM, respectively.
  • HY-19794
    MP-A08

    SphK Cancer
    MP-A08 is a highly selective ATP competitive sphingosine kinase (SPHK1) inhibitor that targets both SphK1 and SphK2 with Ki values of 6.9 ± 0.8 μM and 27 ± 3 μM, respectively.
  • HY-12754
    ML228

    CID-46742353

    HIF/HIF Prolyl-Hydroxylase Cancer
    ML228 (CID-46742353) is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM. ML228 potently activates HIF in vitro as well as its downstream target VEGF.
  • HY-15749
    XL228

    Aurora Kinase Bcr-Abl IGF-1R Src Cancer Endocrinology
    XL228 is a multi-targeted tyrosine kinase inhibitor with IC50s of 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src and Lyn, respectively.
  • HY-124040
    BI-1950

    Integrin Inflammation/Immunology
    BI-1950 is a highly potent lymphocyte function associated antigen-1 (LFA-1) inhibitor. LFA-1 is an essential component in normal immune system function and a target for drug discovery.
  • HY-15440A
    Fostemsavir

    BMS-663068

    HIV Infection
    Fostemsavir (BMS-663068) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir (BMS-663068) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 + T cells.
  • HY-N1404
    Sodium aescinate

    Others Cancer Inflammation/Immunology
    Sodium aescinate is a triterpene saponin derived from Aesculus hippocastanum seeds, with anti-inflammatory and antioxidant activities. Sodium aescinate inhibits hepatocellular carcinoma growth by targeting CARMA3/NF-κB pathway.
  • HY-15662
    Tulathromycin A

    Tulathromycin; CP 472295

    Antibiotic Bacterial Infection
    Tulathromycin A (Tulathromycin), a macrolide antibiotic, inhibits protein synthesis (IC50=0.26 µM) by targeting bacterial ribosome. Tulathromycin A is used for the research of respiratory disease in cattle and swine. Immunomodulatory effects.
  • HY-101653
    MHP 133

    AChE mAChR 5-HT Receptor Neurological Disease
    MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
  • HY-B1057S2
    Nefopam D3

    Fenazoxine D3

    β-catenin Neurological Disease
    Nefopam D3 (Fenazoxine D3) is a deuterium labeled Nefopam (Fenazoxine). Nefopam is a centrally-acting but non-opioid analgesic drug, and Nefopam targets β-catenin protein level in mesenchymal cells.
  • HY-12201S
    TAK-901-d3

    Aurora Kinase Cancer
    TAK-901-d3 is the deuterium labeled TAK-901. TAK-901 is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively.
  • HY-12009
    Pazopanib Hydrochloride

    GW786034 (Hydrochloride)

    PDGFR VEGFR FGFR c-Kit c-Fms Autophagy Cancer
    Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
  • HY-B1953
    Thiacloprid

    Parasite Infection
    Thiacloprid, a chloronicotinyl insecticide, is targeted chiefly to control aphid pest species in orchards and vegetables. Thiacloprid destabilizes DNA. Thiacloprid changes the structure and stability of DNA through binding into the minor groove by hydrophobic or hydrogen interactions.
  • HY-139245
    MC-Ala-Ala-Asn-PAB

    Others Cancer
    MC-Ala-Ala-Asn-PAB is a linker extracted from patent CN104147612A, page 14. MC-Ala-Ala-Asn-PAB can be used to synthesis the tumor microenvironment specific activated micromolecular targeted conjugate.
  • HY-111950
    (-)-Ibuprofenamide

    (R)-Ibuprofenamide

    Others Inflammation/Immunology
    (-)-Ibuprofenamide is an amide prodrug of Ibuprofen with anti-inflammatory activity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-100538
    DTP3

    DNA/RNA Synthesis JAK Cancer
    DTP3 TFA is a potent and selective GADD45β/MKK7 inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.
  • HY-138539
    CBP/p300 ligand 2

    Ligand for Target Protein for PROTAC Cancer
    CBP/p300 ligand 2 is a ligand for target protein for PROTAC of dCBP-1. dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP.
  • HY-107093B
    MBC-11 triethylamine

    Others Cancer
    MBC-11 triethylamine is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). MBC-11 triethylamine has the potential for tumor-induced bone disease (TIBD) research.
  • HY-129372
    PDdB-Pfp

    ADC Linker Cancer
    PDdB-Pfp is a cleavable ADC linker used for the agents that target for the extracellular loop 1 (ECL1) of TM4SF1 (transmembrane 4 L6 family member 1).
  • HY-79369
    Succinic anhydride

    ADC Linker Cancer
    Succinic anhydride is a cyclic anhydride and a nonclaevable ADC linker extracted from patent WO2009064913A1. Succinic anhydride can react with compound 4 of the patent to link the prodrug to an amine or hydroxy 1 group of a targeting polypeptide.
  • HY-107093A
    MBC-11 trisodium

    Others Cancer
    MBC-11 trisodium is a first-in-class conjugate of the bone-targeting bisphosphonate HEDP covalently linked to the antimetabolite Ara-C. MBC-11 trisodium has the potential for tumor-induced bone disease (TIBD) research.
  • HY-130296
    Palbociclib-propargyl

    PROTAC CDK6 ligand 1

    Ligand for Target Protein for PROTAC Cancer
    Palbociclib-propargyl is a ligand for target protein CDK6 for PROTAC, and binds to CRBN ligand via a PEG linker to make a PROTAC CP-10. CP-10 shows a DC50 of 2.1 nM for CDK6.
  • HY-134832
    Mito-LND

    Mito-Lonidamine

    Mitochondrial Metabolism Reactive Oxygen Species Autophagy Cancer
    Mito-LND (Mito-Lonidamine) is an orally active and mitochondria-targeted inhibitor of oxidative phosphorylation (OXPHOS). Mito-LND inhibits mitochondrial bioenergetics, stimulates the formation of reactive oxygen species, and induces autophagic cell death in lung cancer cells.
  • HY-112721
    FDI-6

    Others Cancer
    FDI-6 is an inhibitor of FOXM1. FDI-6 binds directly to FOXM1 protein, to displace FOXM1 from genomic targets in MCF-7 breast cancer cells, and induce concomitant transcriptional down-regulation.
  • HY-117602
    TLR7 agonist 3

    Toll-like Receptor (TLR) Inflammation/Immunology
    TLR7 agonist 3 (Compound 2) is a potent agonist of toll-like receptor 7 (TLR7). TLR7 has an important role in immune activation processes and represents an emerging drug discovery target for the development of immunomodulators.
  • HY-P0122
    iRGD peptide

    c(CRGDKGPDC)

    Integrin Cancer
    iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of drugs by first binding to av integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
  • HY-106409
    Tefinostat

    CHR-2845

    HDAC Cancer
    Tefinostat (CHR-2845) is a monocyte/macrophage-targeted pan HDAC inhibitor, cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Anti-monocytoid lineage leukaemias activity.
  • HY-139305
    CL4H6

    Others Cancer
    CL4H6 is a pH-sensitive cationic lipid. CL4H6 is the main component of lipid nanoparticles (LNPs), which can be used to target and deliver siRNA, and induces a potent gene-silencing response.
  • HY-13070
    MK-8245

    Stearoyl-CoA Desaturase (SCD) Metabolic Disease
    MK-8245 is a potent, liver-targeted stearoyl-CoA desaturase (SCD) inhibitor, with IC50s of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with antidiabetic and antidyslipidemic efficacy.
  • HY-B1227
    Carprofen

    COX FAAH Autophagy Inflammation/Immunology
    Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively.
  • HY-136446
    MYLS22

    Others Cancer Cardiovascular Disease
    MYLS22 is a first-in-class and selective optic atrophy 1 (OPA1) inhibitor. MYLS22 can target endothelial OPA1 to curtail tumor growth and inhibits angiogenesis by impinging on NFkB activity and on angiogenic gene expression.
  • HY-N0003
    Honokiol

    NSC 293100

    Akt Autophagy HCV ERK Cancer
    Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt. Honokiol can readily cross the blood brain barrier.
  • HY-130619
    Boc-C1-PEG3-C4-OBn

    PROTAC Linker Cancer
    Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PROTAC linker, which refers to the PEG composition. Boc-C1-PEG3-C4-OBn can be used in the synthesis of a series of PROTACs, such as PROTAC SGK3 degrader-1 (HY-125878). PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-124726
    Aumitin

    Autophagy Cancer Neurological Disease
    Aumitin is a diaminopyrimidine-based autophagy inhibitor which inhibits mitochondrial respiration by targeting complex I. Aumitin inhibits starvation- and rapamycin induced autophagy dose dependently with IC50s of 0.12 μM and 0.24 μM, respectively.
  • HY-N6744
    Chaetoglobosin A

    Apoptosis Cancer Infection
    Chaetoglobosin A, the active principle within the extract of Penicillium aquamarinium, is a member of the cytochalasan family. Chaetoglobosin A preferentially induces apoptosis. Chaetoglobosin A targets filamentous actin in CLL cells and thereby induces cell-cycle arrest and inhibits membrane ruffling and cell migration.
  • HY-N7674A
    Angoline hydrochloride

    STAT Cancer
    Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
  • HY-B0030
    D-Cycloserine

    iGluR Bacterial Antibiotic Infection Neurological Disease
    D-Cycloserine is an antibiotic which targets sequential bacterial cell wall peptidoglycan biosynthesis enzymes. D-Cycloserine is a partial NMDA agonist that can improve cognitive functions. D-Cycloserine can be used for multidrug-resistant tuberculosis research.
  • HY-111895B
    Macropa-NH2 TFA

    Others Others
    Macropa-NH2 TFA is the precursor of Macropa-NCS. Macropa-NCS is conjugated to trastuzumab as well as to the prostate-specific membrane antigen-targeting compound RPS-070 and is a promising therapeutic radionuclide applied in the treatment of soft-tissue metastases.
  • HY-10208
    Pazopanib

    GW786034

    VEGFR c-Kit PDGFR Autophagy FGFR Cancer
    Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
  • HY-B1881
    Pirimiphos-methyl

    Parasite AChE Infection
    Pirimiphos-methyl is a rapid-acting organophosphorus insecticide and acaricide, causing inhibition of AChE in target organisms. Pirimiphos-methyl is often used for prevention and control of beetles, snout beetles, moths and Ephestia cautella during storage of agricultural grains.
  • HY-138683
    STING-IN-3

    STING Inflammation/Immunology
    STING-IN-3 is an inhibitor of stimulator of interferon genes (STING). STING-IN-3 efficiently inhibits both hsSTING and mmSTING through covalently target the predicted transmembrane cysteine residue 91 and thereby block the activation-induced palmitoylation of STING.
  • HY-N7674
    Angoline

    STAT Cancer
    Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
  • HY-N8471
    Niazinin

    Parasite SARS-CoV Infection Inflammation/Immunology
    Niazinin is a thiocarbamate glycoside with antileishmanial activities, with an IC50 value of 5.25 μM. Niazinin also shows a binding affinity with the target protein 3CL protease. Niazinin has promising leishmanicidal, anti-inflammatory and anti-pyretic activity.
  • HY-100550
    MSDC 0160

    Mitoglitazone; CAY10415

    Insulin Receptor Mitochondrial Metabolism Neurological Disease Endocrinology
    MSDC 0160 (Mitoglitazone) is a mitochondrial target of thiazolidinediones (mTOT)-modulating insulin sensitizer and a modulator of mitochondrial pyruvate carrier (MPC). MSDC 0160 is a thiazolidinedione (TZD) with antidiabetic and neuroprotective activities. MSDC 0160 has the potential for Alzheimer′s disease.
  • 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-133870
    Itaconate-alkyne

    ITalk

    Others Inflammation/Immunology
    Itaconate-alkyne (ITalk) is a specific bioorthogonal probe for quantitative and site-specific chemoproteomic profiling of Itaconation in living cells. Itaconate-alkyne, a functional analogue of Itaconate, exhibits comparable antiinflammatory effect with Itaconate and enables the labeling of bona fide targets of Itaconate.
  • HY-16984
    GNE-4997

    Itk Inflammation/Immunology
    GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity.
  • HY-138936
    SSK1

    Apoptosis Inflammation/Immunology
    SSK1, a senescence-specific killing compound, is a β-galactosidase-targeted prodrug attenuates inflammation. SSK1 is activated by lysosomal β-galactosidase and selectively killed senescent cells through the activation of p38 MAPK and induction of apoptosis.
  • HY-136538
    LQZ-7I

    Survivin Cancer
    LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors.
  • HY-114176B
    (S,R,S)-AHPC-C4-NH2 dihydrochloride

    VH032-C4-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C4-NH2 dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC.
  • HY-12047
    Ponatinib

    AP24534

    Bcr-Abl PDGFR VEGFR FGFR Src Autophagy Cancer
    Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
  • HY-P1268
    α-Conotoxin PIA

    nAChR Neurological Disease
    α-Conotoxin PIA is a nicotinic acetylcholine receptor (nAChR) antagonist that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
  • HY-138684
    MRTX9768

    Histone Methyltransferase Cancer
    MRTX9768 is a potent, orally active PRMT5 inhibitor. MRTX9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors.
  • HY-114489B
    Haemanthamine hydrochloride

    Apoptosis Influenza Virus Parasite Cancer Infection Neurological Disease
    Haemanthamine hydrochloride is a crinine-type alkaloid isolated from the Amaryllidaceae plants with potent anticancer activity. Haemanthamine hydrochloride targets ribosomal that inhibits protein biosynthesis during the elongation stage of translation. Haemanthamine hydrochloride has pro-apoptotic, antioxidant, antiviral, antimalarial and anticonvulsant activities.
  • HY-114176
    (S,R,S)-AHPC-C4-NH2 hydrochloride

    VH032-C4-NH2 hydrochloride; VHL Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 28

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC.
  • HY-15440B
    Fostemsavir Tris

    BMS-663068 Tris

    HIV Infection
    Fostemsavir Tris (BMS-663068 (Tris)) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir Tris (BMS-663068 (Tris)) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 + T cells.
  • HY-114489A
    Haemanthamine

    Apoptosis Influenza Virus Parasite Cancer Infection Neurological Disease
    Haemanthamine is a crinine-type alkaloid isolated from the Amaryllidaceae plants with potent anticancer activity. Haemanthamine targets ribosomal that inhibits protein biosynthesis during the elongation stage of translation. Haemanthamine has pro-apoptotic, antioxidant, antiviral, antimalarial and anticonvulsant activities.
  • HY-16399
    Pladienolide B

    Apoptosis Cancer
    Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B induces apoptosis.
  • HY-114176A
    (S,R,S)-AHPC-C4-NH2

    VH032-C4-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC.
  • HY-P1268A
    α-Conotoxin PIA TFA

    nAChR Neurological Disease
    α-Conotoxin PIA TFA is a nicotinic acetylcholine receptor (nAChR) antagonist that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
  • HY-15729
    Rociletinib

    CO-1686; AVL-301; CNX-419

    EGFR Cancer
    Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
  • HY-B1057S
    Nefopam D3 hydrochloride

    β-catenin Neurological Disease
    Nefopam D3 hydrochloride is the deuterium labeled Nefopam hydrochloride. 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-P9927
    Secukinumab

    AIN457

    Interleukin Related Inflammation/Immunology
    Secukinumab (AIN457) is a high affinity, human monoclonal antibody targeted against interleukin (IL)-17A. Secukinumab is the first-in-class anti-IL-17 agent used for the research of plaque psoriasis, ankylosing spondylitis and psoriatic arthritis.
  • HY-108638
    NSC 146109 hydrochloride

    MDM-2/p53 Apoptosis Cancer
    NSC 146109 hydrochloride is a small-molecule p53 activator that target MDMX and can be used for breast cancer research. NSC 146109 hydrochloride is a pseudourea derivative, promotes breast cancer cells to undergo apoptosis through activating p53 and inducing expression of proapoptotic genes.
  • 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-B0497C
    Niclosamide olamine

    BAY2353 olamine

    STAT Parasite Antibiotic Autophagy Cancer Infection
    Niclosamide olamine (BAY2353 olamine) is an anthelmintic that disrupts mitochondrial metabolism in parasitic worms and animal models. Niclosamide olamine inhibits STAT3 (IC50 = 0.25 μM) and stimulates autophagy by reversibly inhibiting mammalian target of Rapamycin complex 1 (mTORC1) signaling.
  • HY-126316
    Zapalog

    FKBP Others
    Zapalog is a photocleavable small-molecule heterodimerizer that can be used to repeatedly initiate, and instantaneously terminate, a physical interaction between two target proteins. Zapalog dimerizes any two proteins tagged with the FKBP and DHFR domains until exposure to light causes its photolysis.
  • HY-17449
    Fosbretabulin disodium

    CA 4DP; CA 4P; Combretastatin A4 disodium phosphate

    Microtubule/Tubulin Apoptosis Cancer
    Fosbretabulin disodium (CA 4DP) is a tubulin destabilizing agent. Fosbretabulin disodium is the Combretastatin A4 prodrug that selectively targets endothelial cells, induces regression of nascent tumour neovessels, reduces tumour blood flow and causes central tumour necrosis.
  • HY-130988A
    Ipatasertib-NH2 dihydrochloride

    GDC-0068-NH2 dihydrochloride; RG7440-NH2 dihydrochloride

    Ligand for Target Protein for PROTAC Cancer
    Ipatasertib-NH2 dihydrochloride is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase.
  • HY-19726
    NSC59984

    MDM-2/p53 Cancer
    NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway. NSC59984 acts by targeting GOF-mutant p53 and stimulates p73 to restore the p53 pathway signaling.
  • HY-137331
    FAPI-46

    Others Cancer
    FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted radiotracer. FAPI-46 has higher tumor uptake and prolonged tumor accumulation. FAPI-46 can be used for tumor imaging of a multitude of different cancers.
  • HY-130800
    Eragidomide

    CC-90009

    Ligand for E3 Ligase Molecular Glue Apoptosis Cancer Inflammation/Immunology
    Eragidomide (CC-90009) is a first-in-class GSPT1-selective cereblon (CRBN) E3 ligase modulator, acts as a molecular glue. Eragidomide coopts the CRL4 CRBN to selectively target GSPT1 for ubiquitination and proteasomal degradation.
  • HY-13418
    Dorsomorphin dihydrochloride

    Compound C dihydrochloride; BML-275 dihydrochloride

    AMPK TGF-β Receptor Autophagy Cancer
    Dorsomorphin dihydrochloride (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride induces autophagy.
  • HY-138687
    PF-07321332

    SARS-CoV Infection Inflammation/Immunology
    PF-07321332 is a potent and orally active SARS-CoV 3C-like protease (3CL PRO) inhibitor . PF-07321332 targets to the SARS-CoV-2 virus and can be used for COVID-19 reseacrch.
  • HY-141644
    PY-60

    YAP Inflammation/Immunology
    PY-60 is a robust and specific activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a Kd of 1.4 µM. PY-60 directly binds to ANXA2 and antagonizes its normal cellular function of repressing YAP activity.
  • HY-B0341
    Nicorandil

    SG-75

    Potassium Channel Cardiovascular Disease
    Nicorandil (SG-75) is a potent potassium channel activator and targets vascular nucleoside diphosphate-dependent K + channels and cardiac ATP-sensitive K + channels (KATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases.
  • HY-10423
    OSI-027

    ASP7486

    mTOR Autophagy Cancer
    OSI-027 (ASP7486) is a potent, selective, orally active and ATP-competitive mTOR kinase activity inhibitor with an IC50 of 4 nM. OSI-027 targets both mTORC1 and mTORC2 with IC50s of 22 nM and 65 nM, respectively.
  • HY-13308
    Regorafenib Hydrochloride

    BAY 73-4506 hydrochloride

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-124629
    DB2313

    Apoptosis Cancer
    DB2313 is a potent transcription factor PU.1 inhibitor with an apoptosis of 14 nM. DB2313 disrupts the interaction of PU.1 with target gene promoters. DB2313 induces apoptosis of acute myeloid leukemia (AML) cells, and has anticancer effects.
  • HY-10331A
    Regorafenib monohydrate

    BAY 73-4506 monohydrate

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib monohydrate (BAY 73-4506 monohydrate) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-136592
    1-Hydroxy-ibuprofen

    COX Cancer Inflammation/Immunology
    1-Hydroxy Ibuprofen is a metabolite of Ibuprofen in P. australis. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-128776
    Antitumor agent-19

    Others Cancer
    Antitumor agent-19 is an antitomor agent targeting tumor-associated macrophages (TAMs) to serve as an effective TAMs modulator. The EC50 values of Antitumor agent-19 in the RAW 264.7 cells and the BMDM cells are 17.18 μM and 18.87 μM, respectively.
  • HY-121899
    1-Oxo Ibuprofen

    Ibuprofen EP impurity J

    Others Others
    1-Oxo Ibuprofen (Ibuprofen EP impurity J) is a degradation product and a potential impurity in preparations of Ibuprofen. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  • HY-102046
    FM-381

    JAK Inflammation/Immunology
    FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
  • HY-15729A
    Rociletinib hydrobromide

    CO-1686 hydrobromide; AVL-301 hydrobromide; CNX-419 hydrobromide

    EGFR Cancer
    Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
  • HY-120697
    MSAB

    Wnt β-catenin Cancer
    MSAB is a potent and selective inhibitor of Wnt/β-catenin signaling. MSAB binds to β-catenin promoting its degradation, and specifically downregulates Wnt/β-catenin target genes. MSAB exhibits potent anti-tumor effects selectively on Wnt-dependent cancer cells.
  • HY-10331
    Regorafenib

    BAY 73-4506

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
  • HY-N2472
    Medicagenic acid

    Castanogenin

    Bacterial Infection
    Medicagenic acid (Castanogenin) is isolated from the roots of Herniaria glabra L, exhibits potent fungistatic effects against several plant pathogens and human dermatophytes. Medicagenic acid (Castanogenin) has low enzyme inhibitory activities, the target enzymes are xanthine oxidase, collagenase, elastase, tyrosinase, ChE.
  • HY-130297
    PROTAC BCR-ABL1 ligand 1

    Bcr-Abl Cancer
    PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1.
  • HY-N0592
    Demethyleneberberine

    NF-κB AMPK Metabolic Disease Inflammation/Immunology
    Demethyleneberberine is a natural mitochondria-targeted antioxidant. Demethyleneberberine alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine could serve as a AMPK activator for treating non-alcoholic fatty liver disease (NAFLD).
  • HY-129040A
    Iobenguane sulfate

    MIBG sulfate

    Others Cancer
    Iobenguane sulfate (MIBG sulfate) is an analogue of the neurotransmitter norepinephrine with antitumor activity. Radioiodinated Iobenguane sulfate is clinically used as a tumor-targeted radiopharmaceutical in the diagnosis and treatment of adrenergic tumors. Iobenguane sulfate is a high-affinity substrate for cholera toxin that interferes with cellular mono(ADP-ribosylation).
  • HY-128671
    6-​Thioinosine

    6TI; 6-Mercaptopurine riboside

    Nucleoside Antimetabolite/Analog Metabolic Disease
    6-​Thioinosine (6TI) is a purine antimetabolite, acts as an anti-adipogenesis agent, downregulates mRNA levels of PPAR γ and C/EBPα, as well as PPAR γ target protein such as LPL, CD36, aP2, and LXRα.
  • HY-14776
    Quarfloxin

    CX-3543

    DNA/RNA Synthesis Cancer
    Quarfloxin (CX-3543), a fluoroquinolone derivative with antineoplastic activity, targets and inhibits RNA pol I activity, with IC50 values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template.
  • HY-136272
    A 410099.1 amide-PEG3-amine-Boc

    E3 Ligase Ligand-Linker Conjugate Cancer
    A 410099.1 amide-PEG3-amine-Boc is a functionalized IAP ligand for PROTACs that incorporates an IAP ligand and an amide-PEG3 linker with terminal amine. A 410099.1 amide-PEG3-amine-Boc can conjugates with target protein ligands.
  • HY-128384
    Benzyldodecyldimethylammonium chloride dihydrate

    Bacterial Infection
    Benzyldodecyldimethylammonium chloride dihydrate is a quaternary ammonium compound (QAC) and can be used as a biocide to target antibiotic-resistant bacteria, such as methicillin-resistant Staphylococcus aureus (MRSA), multidrug-resistant (MDR) P. aeruginosa et. al. Benzyldodecyldimethylammonium chloride dihydrate, an antimicrobial agent, bacteriostatic or bactericidal properties depending on the concentration.
  • HY-B0436
    Salbutamol hemisulfate

    Albuterol hemisulfate; AH-3365 hemisulfate

    Adrenergic Receptor Autophagy Inflammation/Immunology Endocrinology Cancer
    Salbutamol Hemisulfate (Albuterol hemisulfate) is a short-acting β2 adrenergic receptor agonist Target: β2 Adrenergic Receptor Salbutamol Hemisulfate (Albuterol hemisulfate) is a short-acting, selective beta2-adrenergic receptor agonist used in the treatment of asthma and COPD.
  • HY-14881
    Bedaquiline

    TMC207; R207910

    Bacterial Antibiotic Infection
    Bedaquiline (TMC207) is a diarylquinoline drug and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit. Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-drug resistant tuberculosis.
  • HY-N6025
    Clemastanin B

    Influenza Virus Infection Inflammation/Immunology
    Clemastanin B, a lignin, has potent anti-influenza activities by inhibiting the virus multiplication, prophylaxsis and blocking the virus attachment. Clemastanin B targets viral endocytosis, uncoating or ribonucleoprotein (RNP) export from the nucleus. Clemastanin B has antioxidant and anti-inflammatory activities.
  • HY-136273
    A 410099.1 amide-PEG2-amine-Boc

    E3 Ligase Ligand-Linker Conjugate Cancer
    A 410099.1 amide-PEG2-amine-Boc is a functionalized IAP ligand for PROTACs that incorporates an IAP ligand and an amide-PEG3 linker with terminal amine. A 410099.1 amide-PEG2-amine-Boc can conjugates with target protein ligands.
  • HY-P0023
    Cyclo(-RGDfK)

    Integrin Cancer
    Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
  • HY-D0835
    Hydroxylapatite

    Hydroxyapatite

    Others Others
    Hydroxylapatite (Hydroxyapatite) is a naturally occurring calcium phosphate which is a major mineral component of bone and teeth bones. Nano-scale Hydroxylapatite particles are increasingly being used as carriers for controlled and targeted delivery of bioactive agents like drugs, proteins, and nucleic acids due to their high porosity, negative charge, and biodegradability .
  • HY-136274
    Boc-A 410099.1 amide-alkylC4-amine

    E3 Ligase Ligand-Linker Conjugate Cancer
    Boc-A 410099.1 amide-alkylC4-amine is a functionalized IAP ligand for PROTACs that incorporates an IAP ligand and an amide-alkylC4 linker with terminal amine. Boc-A 410099.1 amide-alkylC4-amine can conjugates with target protein ligands.
  • HY-111558A
    Bobcat339 hydrochloride

    DNA Methyltransferase Cancer
    Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
  • HY-111895A
    Macropa-NH2 hydrochloride

    Others Cancer
    Macropa-NH2 hydrochloride is the precursor of Macropa-NCS. Macropa-NCS is conjugated to Anti-Human HER2 (HY-P9907) as well as to the prostate-specific membrane antigen-targeting compound RPS-070 and is a promising therapeutic radionuclide applied in the treatment of soft-tissue metastases.
  • HY-120075
    TJ191

    Apoptosis Cancer
    TJ191 is a potent and specific anti-cancer agent that targets low TβRIII-expressing malignant T-cell leukemia/lymphoma cells. TJ191 has no affects on the proliferation of other cancer cells or normal fibroblasts or immune cells. TJ191 can be used for cancer research.
  • HY-134333
    ICCB280

    Apoptosis Cancer
    ICCB280 is a potent inducer of C/EBPα. ICCB280 exhibits anti-leukemic properties including terminal differentiation, proliferation arrest, and apoptosis through activation of C/EBPα and affecting its downstream targets (such as C/EBPε, G-CSFR and c-Myc).
  • HY-B0791
    Altiratinib

    DCC-2701

    VEGFR c-Met/HGFR FLT3 Trk Receptor Cancer
    Altiratinib (DCC-2701) is a multi-targeted kinase inhibitor with IC50s of 2.7, 8, 9.2, 9.3, 0.85, 4.6, 0.83 nM for MET, TIE2, VEGFR2, FLT3, Trk1, Trk2, and Trk3 respectively.
  • HY-12745A
    Nalfurafine hydrochloride

    TRK-820 hydrochloride

    Opioid Receptor Neurological Disease
    Nalfurafine hydrochloride (TRK-820 hydrochloride) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential. Nalfurafine hydrochloride (TRK-820 hydrochloride) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment.
  • HY-141622
    SDZ 224-015

    Interleukin Related Caspase SARS-CoV Infection Inflammation/Immunology
    SDZ 224-015 is an orally active inhibitor of the interleukin-1 beta (IL-1β) converting enzyme and caspase-1. SDZ 224-015 possesses anti-COVID-19 activity, targeting M pro (IC50 of 30 nM).
  • HY-I0678
    Regorafénib N-oxyde (M2)

    Drug Metabolite Cancer
    Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-17600
    Acalabrutinib

    ACP-196

    Btk Cancer
    Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
  • HY-10255A
    Sunitinib

    SU 11248

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-130638
    (S,R,S)-AHPC-O-Ph-PEG1-NH-Boc

    VH032-O-Ph-PEG1-NH-Boc

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-O-Ph-PEG1-NH-Boc (VH032-O-Ph-PEG1-NH-Boc) is a synthesized E3 ligase ligand-linker conjugate which is used for the EED-targeted PROTAC.
  • HY-111558
    Bobcat339

    DNA Methyltransferase Cancer
    Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
  • HY-P0023A
    Cyclo(-RGDfK) TFA

    Integrin Cancer
    Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
  • HY-15003
    ATH686

    FLT3 Apoptosis Cancer
    ATH686 is a potent, selective and ATP-competitive FLT3 inhibitor. ATH686 target mutant FLT3 protein kinase activity and inhibit the proliferation of cells harboring FLT3 mutants via induction of apoptosis and cell cycle inhibition. ATH686 has antileukemic effects.
  • HY-12745
    Nalfurafine

    TRK-820

    Opioid Receptor Neurological Disease
    Nalfurafine (TRK-820) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential. Nalfurafine (TRK-820) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment.
  • HY-13314
    Tesevatinib

    XL-647; EXEL-7647; KD-019

    EGFR VEGFR Ephrin Receptor Cancer
    Tesevatinib (XL-647; EXEL-7647; KD-019) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, KDR, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.
  • HY-139149
    NiCur

    Histone Acetyltransferase Cancer
    NiCur is a potent and selective CBP histone acetyltransferase (HAT) inhibitor with an IC50 value of 0.35 μΜ. NiCur, which blocks CBP HAT activity and downregulates p53 activation upon genotoxic stress. NiCur can be used for performing mechanistic studies without affecting the expression of target proteins.
  • HY-101920
    Autophinib

    Autophagy PI3K Cancer Neurological Disease
    Autophinib is a potent, selective autophagy inhibitor with IC50s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC50 of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34.
  • HY-N6769
    Radicicol

    Monorden

    HSP Bacterial Antibiotic Infection
    Radicicol is an inhibitor of Hsp90 with an IC50 value of 1 μM. Radicicol binds to the ATPase domain of Hsp90 and prevents maturation of Hsp90 clients, leading to proteasomal degradation. Radicicol is an antifungal antibiotic with antimalarial activity, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB.
  • HY-123561
    MMV008138

    Parasite Infection
    MMV008138 is a species-selective IspD (enzyme 2-C-methyl-d-erythritol 4-phosphate cytidylyltransferase)-targeting antimalarial agent, with an IC50 of 44 nM for PfIspD (P. falciparum IspD). MMV008138 inhibits the growth of P. falciparum Dd2 strain with an IC50 of 250 nM.
  • HY-N1127
    Tricin

    CMV Cancer Infection
    Tricin is a natural flavonoid present in large amounts in rice bran. Tricin can inhibit human cytomegalovirus (HCMV) replication by inhibiting CDK9. Tricin inhibits the proliferation and invasion of C6 glioma cells via the upregulation of focal-adhesion-finase (FAK)-targeting microRNA-7.
  • HY-15827
    NSC 405020

    MMP Cancer
    NSC 405020 is a novel small molecule inhibitor of MT1-MMP that specifically targets PEX domain rather than the catalytic domain of MT1-MMP with IC50 >100 μM and does not inhibit the catalytic activity of MT1-MMP or MMP-2.
  • HY-126810
    NP213

    Fungal Infection
    NP213 is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 is effective and well-tolerated in resolving nail fungal infections.
  • HY-128976
    10β,17β-dihydroxyestra-1,4-dien-3-one

    DHED

    Estrogen Receptor/ERR Metabolic Disease
    10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-targeting bioprecursor prodrug of the main human estrogen, 17β-estradiol, alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain.
  • HY-133512
    NCGC00249987

    Phosphatase Cancer
    NCGC00249987 is a highly selective and allosteric Tyr phosphatase activity of Eya2 inhibitor with IC50s of 3 μM and 6.9 μM for Eya2 ED and MBP-Eya2 FL. NCGC00249987 specifically targets migration, invadopodia formation, and invasion of lung cancer cells.
  • HY-P1328
    TAT-14

    Keap1-Nrf2 Others
    TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
  • HY-B1881S
    Pirimiphos-methyl-d6

    Parasite AChE Infection
    Pirimiphos-methyl-d6 is the deuterium labeled Pirimiphos-methyl. Pirimiphos-methyl is a rapid-acting organophosphorus insecticide and acaricide, causing inhibition of AChE in target organisms. Pirimiphos-methyl is often used for prevention and control of beetles, snout beetles, moths and Ephestia cautella during storage of agricultural grains.
  • HY-N2098
    Obtusifolin

    NF-κB Cancer
    Obtusifolin, isolated from the seeds of Cassia obtusifolia, regulates the gene expression and production of MUC5AC mucin in airway epithelial cells via inhibiting NF-kB pathway. Obtusifolin suppresses phthalate esters-induced breast cancer bone metastasis by targeting parathyroid hormone-related protein.
  • HY-B0836
    λ-Cyhalothrin

    Parasite Sodium Channel Infection Endocrinology Neurological Disease
    λ-Cyhalothrin is a high efficiency, broad-spectrum type II synthetic pyrethroid insecticide containing α-cyano group. λ-Cyhalothrin is used to control a wide range of pests in a variety of applications. λ-Cyhalothrin is a neurotoxin that targets sodium channels in the membranes of neurons in the central nervous system.
  • HY-124729
    BL-918

    ULK Autophagy Neurological Disease
    BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment.
  • HY-N7043
    Isosilybin A

    Apoptosis Cancer
    Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis.
  • HY-P1380A
    Difopein TFA

    Apoptosis Cancer
    Difopein (TFA), a specific and competitive inhibitor of 14-3-3 protein (a highly conserved eukaryotic regulatory molecule), blocking the ability of 14-3-3 to bind to target proteins and inhibits 14-3-3/Ligand interactions. Difopein (TFA) leads to induction of apoptosis and enhances the ability of cisplatin to kill cells.
  • HY-126323
    TCMDC-135051

    Parasite Infection
    TCMDC-135051 is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 has antiparasiticidal activity (EC50=320 nM).
  • HY-100433
    PACMA 31

    Others Cancer
    PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC50 of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues.
  • 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-13332
    Calcifediol-D6

    VD/VDR Metabolic Disease
    Calcifediol-D6 is the deuterated form of Calcifediol(25-hydroxy Vitamin D3), which is a prehormone that is produced in the liver by hydroxylation of vitamin D3 (cholecalciferol) by the enzyme cholecalciferol 25-hydroxylase IC50 value: Target: This metabolite is being measured by physicians worldwide to determine a patient's vitamin d status.
  • HY-120129
    Ancremonam

    BOS-228; LYS-228

    Bacterial Infection
    Ancremonam (LYS-228) is a low toxicity, potent and single-agent monobactam antibiotic targeting penicillin binding protein 3 with potent activity against Enterobacteriaceae. Ancremonam kills bacteria by inhibiting cell wall synthesis through covalent modification of the active-site serine of penicillin binding protein 3.
  • HY-100573
    Necrosulfonamide

    Mixed Lineage Kinase Cancer
    Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis.
  • HY-134813
    MRTX1133

    Ras Cancer
    MRTX1133 is a highly selective, first-in-class inhibitor of KRAS G12D. MRTX1133 targets the KRAS G12D protein in both active and inactive states. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells.
  • HY-16100
    BI 99179

    Fatty Acid Synthase (FASN) Cancer Metabolic Disease
    BI 99179 is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC50 of 79 nM. BI 99179 is a tool compound suitable for the in vivo validation of FAS as a target for lipid metabolism related diseases. BI 99179 exhibits significant exposure (both peripheral and central) upon oral administration in rats.
  • HY-10227
    Bortezomib

    PS-341; LDP-341; NSC 681239

    Proteasome NF-κB Apoptosis Autophagy Cancer
    Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.
  • HY-10255
    Sunitinib Malate

    SU 11248 Malate

    PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-N4113
    Glycycoumarin

    Autophagy Cancer
    Glycycoumarin is a major bioactive coumarin of licorice. Glycycoumarin inhibits hepatocyte lipoapoptosis through activation of autophagy and inhibition of ER stress-mediated JNK and GSK-3-mediated mitochondrial pathway. Glycycoumarin exerts anti-liver cancer activity by directly targeting T-LAK cell-originated protein kinase .
  • HY-126323B
    TCMDC-135051 hydrochloride

    Parasite Infection
    TCMDC-135051 hydrochloride is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 hydrochloride prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 hydrochloride has antiparasiticidal activity (EC50=320 nM).
  • 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-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-136477
    Pentagamavunon-1

    PGV-1

    Apoptosis COX VEGFR NF-κB Cancer
    Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation.
  • HY-18666
    D77

    HIV Infection
    D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).
  • HY-12047S
    Ponatinib D8

    AP24534 D8

    Bcr-Abl PDGFR VEGFR FGFR Src Autophagy Cancer
    Ponatinib D8 (AP24534 D8) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
  • HY-N0249
    Saikosaponin C

    Amyloid-β Neurological Disease
    Saikosaponin C is a bioactive component found in radix bupleuri, targets amyloid beta and tau in Alzheimer's disease. Saikosaponin C inhibits the secretion of both Aβ1-40 and Aβ1-42, and suppresses abnormal tau phosphorylation, but shows no effect on BACE1 activity and expression.
  • HY-18522
    AA26-9

    Phospholipase Metabolic Disease
    AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. AA26-9 targets included serine peptidases, lipases, amidases, esterases, and thioesterases. AA26-9 shows inhibitory activity against approximately 1/3 of the 40+ serine hydrolases detected in immortalized T cell lines .
  • HY-122051
    AC1903

    TRP Channel Metabolic Disease
    AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model.
  • HY-141521
    NX-13

    NOD-like Receptor (NLR) Inflammation/Immunology
    NX-13 is a first-in-class, orally active and gut-restricted agent that selectively targets and activates the NLRX1 pathway to induce immunometabolic changes. NX-13 results in lower inflammation and responses in inflammatory bowel disease. NX-13 can be used for the research of crohn's disease and ulcerative colitis.
  • HY-112900
    DC41SMe

    ADC Cytotoxin Cancer
    DC41SMe, a DC1 derivative, shows cytotoxicity in Ramos, Namalwa, and HL60/s cells with IC50s ranging from 18-25 pM. DC1, a simplified analogue of CC-1065, is an antibody conjugate of cytotoxic DNA alkylators for the targeted treatment of cancer.
  • HY-122534
    Mensacarcin

    Mitochondrial Metabolism ADC Cytotoxin Apoptosis Cancer
    Mensacarcin, a highly complex polyketide, strongly inhibits cell growth universally in cancer cell lines and potently induces apoptosis in melanoma cells. Mensacarcin targets to mitochondria, affects energy metabolism in mitochondria, and activates caspase-dependent apoptotic pathways. Mensacarcin, an antibiotic, can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
  • HY-10545
    Taribavirin

    HBV HCV Infection
    Taribavirin is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin, is a ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia.
  • HY-126810A
    NP213 TFA

    Fungal Infection
    NP213 TFA is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 TFA targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 TFA is effective and well-tolerated in resolving nail fungal infections.
  • HY-16706A
    Remodelin hydrobromide

    Histone Acetyltransferase Cancer
    Remodelin, a specific inhibitor of N-acetyltransferase NAT10, can ameliorate Hutchinson-Gilford Progeria Syndrom (HGPS) cellular phenotypes. Remodelin acts in a progerin- and FTI-independent pathway, by targeting and inhibiting NAT10. NAT10 is a protein with histone acetylation activity and primarily identified to be involved in regulation of telomerase activity.
  • HY-B0062
    Dovitinib lactate hydrate

    TKI258 lactate hydrate; CHIR-258 lactate hydrate

    FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib lactate hydrate (TKI258 lactate hydrate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
  • HY-100538A
    DTP3 TFA

    DNA/RNA Synthesis JNK Cancer
    DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.
  • HY-141662
    2',3'-cGAMP-C2-PPA

    STING Drug-Linker Conjugates for ADC Cancer
    2',3'-cGAMP-C2-PPA (45), A cyclic di-nucleotide, is a STING agonist (US20210015941A1). 2',3'-cGAMP-C2-PPA is a drug-linker conjugate for ADC that can be used in synthesis of antibody-drug conjugates for the targeted treatment of cancer.
  • HY-D0162
    Malachite green oxalate

    IKK NF-κB Apoptosis Cancer
    Malachite green oxalate is a triphenylmethane dye which can be used to detect the release of phosphate in enzymatic reactions. Malachite green oxalate is also a potent and selective inhibitor of IKBKE, and inhibits its downstream targets such as IκBα, p65 and IRF3. Malachite green oxalate exhibits antitumor activity in vitro and in vivo.
  • HY-19980
    Eprenetapopt

    APR-246; PRIMA-1Met

    MDM-2/p53 Autophagy Apoptosis Ferroptosis Cancer
    Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.
  • HY-10207
    Dovitinib lactate

    CHIR-258 lactate; TKI-258 lactate

    FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
  • HY-B1369
    Imipenem monohydrate

    N-Formimidoyl thienamycin monohydrate

    Bacterial Antibiotic Infection
    Imipenem monohydrate, a member of the carbapenem class of antibiotics isolated from the soil organism Streptomyces cattleya, is an intravenous β-lactam antibiotic effective against a wide range of Gram-positive and Gram-negative bacteria, including several multi-drug resistant bacterial species. Imipenem acts as cell wall-targeting antibiotic.
  • HY-N8441
    Neriifolin

    17β-Neriifolin

    Na+/K+ ATPase Apoptosis Cancer Inflammation/Immunology
    Neriifolin, a CNS-penetrating cardiac glycoside, is an inhibitor of the Na +, K +-ATPase. Neriifolin can target beclin 1, inhibits the formation of LC3-associated phagosomes and ameliorates experimental autoimmune encephalomyelitis (EAE) development. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells[2.
  • HY-10293
    Aderbasib

    INCB007839; INCB7839

    MMP Cancer
    Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 + breast cancer, gliomas, et al.
  • HY-141429
    AS-99

    Histone Methyltransferase Apoptosis Cancer
    AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.
  • HY-10545A
    Taribavirin hydrochloride

    HBV HCV Infection
    Taribavirin hydrochloride is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin hydrochloride is a Ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia.
  • HY-P1328A
    TAT-14 TFA

    Keap1-Nrf2 Others
    TAT-14 TFA is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 TFA has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
  • HY-10065S1
    Axitinib-d3

    AG-013736-d3

    VEGFR Cancer
    Axitinib-d3 (AG-013736-d3) is deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.
  • HY-130641
    Br-C10-methyl ester

    PROTAC Linker Cancer
    Br-C10-methyl ester is a PROTAC linker, which refers to the alkyl/ether composition. Br-C10-methyl ester is used in the synthesis of a series of PROTACs (MS432).  PROTACs contain two different ligands connected by a linker; one is the VHL ligand portion and the other is for the target protein.
  • HY-124801
    ABMA

    Bacterial Influenza Virus Parasite Infection
    ABMA is a broad-spectrum inhibitor of intracellular toxins and pathogens. ABMA efficiently protects cells against various toxins and pathogens including viruses, intracellular bacteria and parasite. ABMA selectively acts at host cell late endosomes rather than targeting toxin or pathogen itself. ABMA has broad-spectrum anti-infection activity.
  • 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-P2264
    KYL peptide

    Ephrin Receptor Inflammation/Immunology
    KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor. KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses.
  • HY-117383
    NGI-1

    ML414

    Virus Protease Cancer
    NGI-1 (ML414) is a potent oligosaccharyltransferase (OST) inhibitor, directly targeting and blocking the function of the OST catalytic subunits STT3A and STT3B. NGI-1 is a cell permeable inhibitor and can effectively reduce virus infectivity without affecting cell viability.
  • HY-N7030
    5,7,3',4'-Tetramethoxyflavone

    Fungal Parasite Infection
    5,7,3',4'-Tetramethoxyflavone, one of the major polymethoxyflavones (PMFs) isolated from M. exotica, possesses various bioactivities, including anti-fungal, anti-malarial, anti-mycobacterial, and anti-inflammatory activities. 5,7,3',4'-Tetramethoxyflavone exhibits chondroprotective activity by targeting β-catenin signaling.
  • HY-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-129941
    (S,R,S)-AHPC-C10-NH2

    VH032-C10-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for BET-Targeted PROTAC.
  • HY-10971A
    Alisertib sodium

    MLN 8237 sodium

    Aurora Kinase Autophagy Apoptosis Cancer
    Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
  • HY-129941A
    (S,R,S)-AHPC-C10-NH2 dihydrochloride

    VH032-C10-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C10-NH2 dihydrochloride (VH032-C10-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for BET-Targeted PROTAC.
  • HY-100765
    BI-0252

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis.
  • HY-10969
    Obatoclax Mesylate

    GX15-070 Mesylate

    Bcl-2 Family Autophagy Parasite Cancer Infection
    Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity.
  • HY-114237
    GDC-0276

    Sodium Channel Neurological Disease
    GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects.
  • HY-N8188
    Dehydrojuncusol

    HCV HCV Protease Infection
    Dehydrojuncusol, a potent HCV inhibitor, targets HCV NS5A and is able to inhibit RNA replication of replicons harboring resistance mutations to anti-NS5A direct-acting antivirals. Dehydrojuncusol significantly inhibits HCV infection when added after virus inoculation of HCV genotype 2a (EC50=1.35 µM).
  • HY-15176
    Pyridostatin

    RR82

    G-quadruplex Cancer
    Pyridostatin (RR82) is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets the proto-oncogene Src. Pyridostatin reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells.
  • HY-14422
    SR1078

    ROR Cancer
    SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription.
  • HY-N0242
    Fraxinellone

    PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT Cancer Inflammation/Immunology
    Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1.
  • HY-10987A
    ENMD-2076

    Aurora Kinase FLT3 VEGFR FGFR PDGFR Src Apoptosis Cancer
    ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
  • HY-117684A
    DDD107498 succinate

    DDD-498 succinate

    Parasite CaMK Autophagy Infection
    DDD107498 succinate (DDD-498 succinate) is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7. DDD107498 succinate inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2.
  • HY-128588
    STAT3-IN-3

    STAT Apoptosis Cancer
    STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research.
  • HY-101254
    Luzindole

    N-0774

    Melatonin Receptor Neurological Disease
    Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity.
  • HY-15176A
    Pyridostatin hydrochloride

    RR82 hydrochloride

    G-quadruplex Cancer
    Pyridostatin (RR82) hydrochloride is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin hydrochloride promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin hydrochloride targets the proto-oncogene Src. Pyridostatin hydrochloride reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells.
  • HY-127105
    Iptacopan

    LNP023

    Complement System Metabolic Disease Inflammation/Immunology
    Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G).
  • HY-12993
    RSV604

    A-60444

    RSV Infection
    RSV604 (A-60444) is an inhibitor of respiratory syncytial virus (RSV) replication. RSV604 targets the nucleocapsid protein, with a Kd of 1.6 μM. RSV604 displays submicromolar activity against numerous clinical isolates of both the A and B subtypes of RSV (average EC50s=0.8 μM).
  • HY-108361
    CCG-203971

    Ras Inflammation/Immunology Cancer
    CCG-203971 is a second-generation Rho/MRTF/SRF pathway inhibitor. CCG-203971 potently targets RhoA/C-activated SRE-luciferase (IC50 =6.4 μM). CCG-203971 inhibits PC-3 cell migration with an IC50 of 4.2 μM. Potential anti-metastasis Agent.
  • HY-13898
    Taselisib

    GDC-0032; RG-7604

    PI3K Cancer
    Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
  • HY-15257
    Mavoglurant

    AFQ056

    mGluR Neurological Disease
    Mavoglurant (AFQ056) is a potent, selective, non-competitive and orally active mGluR5 antagonist, with an IC50 of 30 nM. Mavoglurant shows a >300 fold selectivity for the mGluR5 over all targets (238) tested. Mavoglurant can be used for the research of Fragile X syndrome (FXS), and L-dopa induced dyskinesias in Parkinson's disease.
  • HY-N4100
    Trilobatin

    HIV SGLT Infection
    Trilobatin, a natural sweetener derived from Lithocarpus polystachyus Rehd, Trilobatin is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope. Neuroprotective effects. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells.
  • HY-15507
    VGX-1027

    GIT 27

    Interleukin Related TNF Receptor Metabolic Disease Inflammation/Immunology
    VGX-1027 is an orally active isoxazole compound that exhibits various immunomodulatory properties. VGX-1027 targets macrophages, reducing the production of the proinflammatory mediators TNF-α, IL-1β, IL-10. VGX-1027 has antidiabetogenic effects by limiting cytokine-mediated immunoinflammatory events.
  • HY-N0104
    Curcumol

    (-)-Curcumol

    Apoptosis Cancer
    Curcumol ((-)-Curcumol), a bioactive sesquiterpenoid, possesses numerous pharmacological activities like anticancer, antimicrobial, antifungal, antiviral, and antiinflammatory. Curcumol is a potent inducer of apoptosis in numerous cancer cells via targeting key signaling pathways as MAPK/ERK, PI3K/Akt and NF-κB which are generally deregulated in several cancers.
  • HY-126323A
    TCMDC-135051 TFA

    Parasite Infection
    TCMDC-135051 TFA is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 TFA prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 TFA has antiparasiticidal activity (EC50=320 nM).
  • HY-10969A
    Obatoclax

    GX15-070

    Bcl-2 Family Autophagy Parasite Cancer Infection
    Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity.
  • HY-126327
    UNC4976

    Histone Methyltransferase Cancer
    UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
  • HY-138281
    Complement factor D-IN-2

    Complement System Inflammation/Immunology
    Complement factor D-IN-2 is an inhibitor of complement factor D extracted from patent WO2015130838A1, compound 190. Complement factor D-IN-2 targets factor D and inhibits the complement cascade at an early and essential point in the alternative complement pathway. Complement factor D-IN-2 can be used for the research of autoimmune diseases.
  • HY-15491
    AG-024322

    COX Apoptosis 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-15142
    Doxorubicin hydrochloride

    Hydroxydaunorubicin hydrochloride

    Topoisomerase ADC Cytotoxin AMPK Autophagy Apoptosis HIV HBV Mitophagy Antibiotic Bacterial Cancer Infection
    Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy.
  • HY-125834
    GMB-475

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

    PROTACs Epigenetic Reader Domain Cancer
    β-NF-JQ1 is a PROTAC that recruits AhR E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity.
  • HY-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-109172
    Ezeprogind

    AZP-2006

    Amyloid-β Neurological Disease
    Ezeprogind (AZP-2006) is an orally active neurotrophic inducer. Ezeprogind targets all causes of neurodegeneration and is not only aiming at markers such as Abeta protein or tau protein. Ezeprogind is a potent neuroprotectant and can be used for the research of neurological disorders, including progressive supranuclear palsy (PSP), tauopathies, alzheimer’s and parkinson’s diseases, et al.
  • HY-112683
    V-9302

    Others Cancer
    V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
  • 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-16658
    Z-VAD(OMe)-FMK

    Z-Val-Ala-Asp(OMe)-FMK

    Caspase Cancer
    Z-VAD(OMe)-FMK (Z-Val-Ala-Asp(OMe)-FMK) is a cell-permeable and irreversible pan-caspase inhibitor. Z-VAD(OMe)-FMK is an ubiquitin carboxy-terminal hydrolase L1 (UCHL1) inhibitor. Z-VAD(OMe)-FMK irreversibly modifies UCHL1 by targeting the active site of UCHL1.
  • HY-N7434
    N-Nitrosodiethylamine

    DNA/RNA Synthesis Cancer
    N-Nitrosodiethylamine is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
  • HY-126147
    J22352

    HDAC Cancer
    J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1.
  • HY-118341
    Clitocine

    Apoptosis Bcl-2 Family Cancer
    Clitocine, an adenosine nucleoside analog isolated from mushroom, is a potent and efficacious readthrough agent. Clitocine acts as a suppressor of nonsense mutations and can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer activity.
  • HY-111845
    Estrone-N-O-C1-amido

    ERα ligand 1

    Estrogen Receptor/ERR Ligand for Target Protein for PROTAC Cancer
    Estrone-N-O-C1-amido (ERα ligand 1) is an Estrone-based estrogen ligand, which targets estrogen receptor α (ERα). Estrone-N-O-C1-amido (ERα ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER.
  • HY-131961
    Triciferol

    VD/VDR HDAC Cancer
    Triciferol functions as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR (IC50=87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Antiproliferative and cytotoxic activities.
  • HY-112683A
    V-9302 hydrochloride

    Others Cancer
    V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
  • HY-10971
    Alisertib

    MLN 8237

    Aurora Kinase Autophagy Apoptosis Cancer
    Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
  • HY-16050
    Aplidine

    Plitidepsin

    DNA/RNA Synthesis SARS-CoV Cancer Infection
    Aplidine (Plitidepsin) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM). Aplidine possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Aplidine is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research.
  • HY-132174
    CHIKV-IN-2

    Dihydroorotate Dehydrogenase Infection
    CHIKV-IN-2 is a potent inhibitor against Chikungunya virus (CHIKV), with excellent cellular antiviral activity (EC90=270 nM) and improved liver microsomal stability. CHIKV-IN-2 shows inhibitory activity against a cellular target Dihydroorotate Dehydrogenase (DHODH), which interacts with various viruses and regulate their replication via depleting intracellular pyrimidine pools.
  • HY-109008
    Nacubactam

    OP0595 free acid

    Bacterial Infection
    Nacubactam (OP0595 free acid) is a potent non-β-lactam-β-lactamase inhibitor with activity against class A and class C β-lactamases. Nacubactam (OP0595 free acid) acts as a penicillin binding protein (PBP) 2-active antibacterial, and gives β-lactamase-independent potentiation of β-lactams targeting other PBPs.
  • HY-10987
    ENMD-2076 Tartrate

    Aurora Kinase FLT3 VEGFR FGFR Src PDGFR Apoptosis Cancer
    ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
  • HY-124593
    PTC299

    VEGFR Dihydroorotate Dehydrogenase DNA/RNA Synthesis Cancer
    PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies.
  • HY-121212
    Icosabutate

    Others Metabolic Disease Inflammation/Immunology
    Icosabutate, an orally active ω-3 polyunsaturated fatty acid, is an aeicosapentaenoic acid (EPA) derivative. Icosabutate overcomes the drawbacks of unmodified EPA for liver targeting and improves insulin sensitivity, hepatic inflammation and fibrosis. Icosabutate is well tolerated, and efficacious in lowering non-high-density lipoprotein cholesterol (non-HDL-C) levels in persistent hypertriglyceridemia .
  • HY-10255AS
    Sunitinib D10

    SU 11248 D10

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib D10 (SU 11248 D10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-10230
    Midostaurin

    PKC412; CGP 41251

    PKC Cancer
    Midostaurin (PKC412; CGP 41251) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
  • HY-B0341S
    Nicorandil-d4

    Potassium Channel Cardiovascular Disease
    Nicorandil-d4 (SG-75-d4) is the deuterium labeled Nicorandil. Nicorandil (SG-75) is a potent potassium channel activator and targets vascular nucleoside diphosphate-dependent K + channels and cardiac ATP-sensitive K + channels (KATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases.
  • HY-110078
    Eeyarestatin I

    p97 Apoptosis Cancer
    Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects.
  • HY-114169
    WRG-28

    Discoidin Domain Receptor Cancer
    WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor with an IC50 of 230 nM. WRG-28 uniquely inhibits receptor-ligand interactions via allosteric modulation of the receptor. WRG-28 inhibits tumor invasion and migration, as well as tumor-supporting roles of the stroma, and inhibits metastatic breast tumor cell colonization in the lungs by targeting DDR2.
  • HY-114419
    Zetomipzomib

    KZR-616

    Proteasome Inflammation/Immunology
    Zetomipzomib (KZR-616), a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib has the potential for the research of multiple autoimmune diseases.
  • HY-130988
    Ipatasertib-NH2

    GDC-0068-NH2; RG7440-NH2

    Ligand for Target Protein for PROTAC Cancer
    Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase.
  • 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-130854
    Thalidomide-NH-C6-NH-Boc

    E3 Ligase Ligand-Linker Conjugate Cancer
    Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A).
  • HY-124631
    NLX-204

    5-HT Receptor Neurological Disease
    NLX-204 is an orally active, potent, highly affinity and selective 5-HT1A receptor-biased agonist (pKi=10.19). NLX-204 shows relatively higher affinity for α1 and D2 receptors than for other off-targets. NLX-204 can be used for the research of antidepressant.
  • HY-114236
    Ezeprogind disulfate

    AZP-2006 disulfate

    Amyloid-β Neurological Disease
    Ezeprogind (AZP-2006) disulfate is an orally active neurotrophic inducer. Ezeprogind disulfate targets all causes of neurodegeneration and is not only aiming at markers such as Abeta protein or tau protein. Ezeprogind disulfate is a potent neuroprotectant and can be used for the research of neurological disorders, including progressive supranuclear palsy (PSP), tauopathies, alzheimer’s and parkinson’s diseases, et al.
  • HY-75800
    Lomibuvir

    VX-222

    DNA/RNA Synthesis HCV Infection
    Lomibuvir (VX-222), a selective, non-nucleoside polymerase inhibitor, targets thumb pocket 2 of the HCV NS5B polymerase (RdRp) with a Kd of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC50 of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo-initiated RNA synthesis.
  • HY-100421
    CPI-455

    Histone Demethylase Cancer
    CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
  • HY-114419A
    Zetomipzomib maleate

    KZR-616 maleate

    Proteasome Inflammation/Immunology
    Zetomipzomib (KZR-616) maleate, a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib maleate has the potential for the research of multiple autoimmune diseases.
  • 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-111843
    Ch55-O-C3-NH2

    RAR ligand 1

    RAR/RXR Ligand for Target Protein for PROTAC Autophagy Cancer
    Ch55-O-C3-NH2 (RAR ligand 1) is a Ch 55-based ligand, which targets RAR. Ch55-O-C3-NH2 (RAR ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER.
  • HY-124631A
    NLX-204 hydrochloride

    5-HT Receptor Neurological Disease
    NLX-204 (hydrochloride) is an orally active, potent, highly affinity and selective 5-HT1A receptor-biased agonist (pKi=10.19). NLX-204 (hydrochloride) shows relatively higher affinity for α1 and D2 receptors than for other off-targets. NLX-204 (hydrochloride) can be used for the research of antidepressant.
  • HY-21997
    Dmt-2'fluoro-da(bz) amidite

    DNA/RNA Synthesis Others
    Dmt-2'fluoro-da(bz) amidite, an uniformly modified 2'-deoxy-2'-fluoro phosphorothioate oligonucleotide, is a nuclease-resistant antisense compound with high affinity and specificity for RNA targets. Dmt-2'fluoro-da(bz) amidite is also an intermediate for 5’-DMT-3’-phosphoramidite synthesis.
  • HY-135396
    (1S,2S)-Bortezomib

    Proteasome Apoptosis Cancer
    (1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.
  • HY-114209
    MRK-740

    Histone Methyltransferase Cancer
    MRK-740 is a potent, selective and substrate-competitive PRDM9 histone methyltransferase inhibitor with an IC50 of 80 nM. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 reduces PRDM9-dependent trimethylation of H3K4 (IC50 = 0.8 µM).
  • HY-34758
    N-Nitroso-N-methylurea

    NMU; MNU; NMH

    DNA Alkylator/Crosslinker Cancer
    N-Nitroso-N-methylurea (NMU;MNU;NMH) is a potent carcinogen, mutagen and teratogenand. N-Nitroso-N-methylurea is a direct-acting alkylating agent that interacts with DNA. N-Nitroso-N-methylurea targets multiple animal organs to cause various cancer and/or degenerative disease. N-Nitroso-N-methylurea is also a precursor in the synthesis of diazomethane.
  • HY-W014622
    CRT0044876

    DNA/RNA Synthesis Cancer
    CRT0044876 is a potent and selective apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor (IC50=~3 μM). CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1, and is a specific inhibitor of the exonuclease III family of enzymes to which APE1 belongs. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds.
  • HY-137262
    Protein deglycase DJ-1 against-1

    Others Neurological Disease
    Protein deglycase DJ-1 against-1, a DJ-1-binding compound, dependently targets DJ1. Protein deglycase DJ-1 against-1 penetrates through the blood brain barrier (BBB). Protein deglycase DJ-1 against-1 is used as a neuroprotective agent and has the potential for Parkinson's disease research.
  • HY-135902
    Synucleozid

    NSC 377363

    DNA/RNA Synthesis Neurological Disease
    Synucleozid (NSC 377363) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein (IC50=1.5 μM). Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
  • HY-50905
    Dovitinib

    CHIR-258; TKI258

    FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively.
  • HY-15147
    XAV-939

    β-catenin PARP Cancer
    XAV-939 is a potent tankyrase inhibitor that targets Wnt/β-catenin signaling. XAV-939 stabilizes axin by inhibiting tankyrase 1 and tankyrase 2 (IC50s of 5 and 2 nM, respectively), thereby stimulating β-catenin degradation. XAV939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 (Kds of 99 and 93 nM, respectively).
  • HY-135902A
    Synucleozid hydrochloride

    NSC 377363 hydrochloride

    DNA/RNA Synthesis Neurological Disease
    Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein (IC50=1.5 μM). Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
  • HY-128171
    Diflapolin

    FLAP Epoxide Hydrolase Inflammation/Immunology
    Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP)/soluble epoxide hydrolase (sEH) inhibitor with marked anti-inflammatory efficacy and high target selectivity. Diflapolin inhibits 5-LOX product formation in intact human monocytes and neutrophils with IC50s of  30 and 170 nM, respectively, and suppressed the activity of isolated sEH (IC50=20 nM).
  • HY-13295
    Vinpocetine

    Ethyl apovincaminate

    Sodium Channel IKK Phosphodiesterase (PDE) Inflammation/Immunology Neurological Disease Cardiovascular Disease Cancer
    Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na + channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.
  • HY-15176B
    Pyridostatin TFA

    RR82 TFA

    G-quadruplex Cancer
    Pyridostatin (RR82) TFA is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin TFA promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin TFA targets the proto-oncogene Src. Pyridostatin TFA reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells.
  • HY-110261
    GS143

    IKK E1/E2/E3 Enzyme NF-κB Inflammation/Immunology
    GS143 is a selec­tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCF βTrCP1-mediated IκBα ubiquitylation. GS143 sup­presses NF-κB acti­va­tion and tran­scrip­tion of tar­get genes and does not inhibit proteasome activity. GS143 has anti-asthma effect.
  • HY-13912
    IWP-2

    Wnt Porcupine Casein Kinase Cancer
    IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ.
  • HY-10185
    TG 100572 Hydrochloride

    Src VEGFR FGFR PDGFR Inflammation/Immunology
    TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-10255AS1
    Sunitinib-d4

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib-d4 (SU 11248-d4) is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-10206
    Amuvatinib

    MP470; HPK 56

    c-Kit PDGFR RAD51 FLT3 c-Met/HGFR RET Apoptosis Cancer
    Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
  • HY-13856
    (R)-PS210

    PDK-1 Cancer
    (R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment.
  • HY-19985A
    (3S,4S)-PF-06459988

    Others Cancer
    (3S, 4S)-PF-06459988 is the S enantiomer of PF-06459988 with less active. PF-06459988 is a potent irreversible inhibitor of T790M mutant epidermal growth factor receptor (EGFR). PF-06459988 has excellent selectivity against EGFR wild-type while possessing a minimally reactive electrophile that reduces the propensity of off-target labeling.
  • HY-10206A
    Amuvatinib hydrochloride

    MP470 hydrochloride; HPK 56 hydrochloride

    c-Kit PDGFR RAD51 FLT3 c-Met/HGFR RET Cancer
    Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
  • HY-N1500
    Pulegone

    TRP Channel Endogenous Metabolite Inflammation/Immunology
    Pulegone, the major chemical constituent of Calamintha nepeta (L.) Savi essential oil which is an aromatic herb with a mint-oregano flavor, is one of avian repellents. The molecular target for the repellent action of Pulegone in avian species is nociceptive TRP ankyrin 1 (TRPA1). Pulegone stimulates both TRPM8 and TRPA1 channel in chicken sensory neurons and suppresses the former but not the latter at high concentrations.
  • HY-P1399
    Pep2m, myristoylated

    Myr-Pep2m

    PKC Neurological Disease
    Pep2m, myristoylated (Myr-Pep2m) is a cell-permeable peptide. Pep2m, myristoylated can disrupt the protein kinase ζ (PKMζ) downstream targets, N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2) interactions. PKMζ is an autonomously active isozyme of protein kinase C (PKC).
  • HY-10184
    TG 100572

    Src VEGFR PDGFR FGFR Cancer
    TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-N2500
    Deoxypodophyllotoxin

    Microtubule/Tubulin Apoptosis Autophagy Infection Cardiovascular Disease
    Deoxypodophyllotoxin (DPT), a derivative of podophyllotoxin, is a lignan with potent antimitotic, anti-inflammatory and antiviral properties isolated from rhizomes of Sinopodophullumhexandrum (Berberidaceae). Deoxypodophyllotoxin, targets the microtubule, has a major impact in oncology not only as anti-mitotics but also as potent inhibitors of angiogenesis. Deoxypodophyllotoxin induces cell autophagy and apoptosis. Deoxypodophyllotoxin evokes increase of intracellular Ca 2+ concentrations in DRG neurons.
  • HY-136431
    BC-DXI-843

    Others Cancer
    BC-DXI-843 is a potent and specific AIMP2-DX2 inhibitor with an IC50 of 0.92 μM, more than 100-fold selectivity over AIMP2 (IC50 >100 μM) in a luciferase assay. BC-DXI-843 acts as a promising lead targeting AIMP2-DX2 in lung cancer.
  • HY-117800
    BJE6-106

    B106

    PKC Apoptosis Cancer Inflammation/Immunology
    BJE6-106 (B106) is a potent, selective 3 rd generation PKCδ inhibitor with an IC50 of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC50=50 μM). BJE6-106 (B106) induces caspase-dependent apoptosis. BJE6-106 (B106) possesses tumor-specific effect.
  • HY-100348
    EPI-001

    Androgen Receptor PPAR Apoptosis Cancer
    EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer.
  • HY-B0965
    Thioridazine hydrochloride

    Dopamine Receptor Apoptosis 5-HT Receptor Autophagy Bacterial Cancer Infection Neurological Disease
    Thioridazine hydrochloride, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
  • HY-109118A
    Masupirdine mesylate

    SUVN-502 mesylate

    5-HT Receptor Neurological Disease
    Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate (SUVN-502 mesylate) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease.
  • HY-P3101
    GLP-1(28-36)amide

    Glucagon Receptor Metabolic Disease Cardiovascular Disease
    GLP-1(28-36)amide, a C-terminal nonapeptide of GLP-1, is a major product derived from the cleavage of GLP-1 by the neutral endopeptidase (NEP). GLP-1(28-36)amide is an antioxidant and targets to mitochondrion, inhibits mitochondrial permeability transition (MPT). GLP-1(28-36)amide has anti-diabetic and cardioprotection effects.
  • HY-19625
    MCB-613

    Others Cancer
    MCB-613 is a potent Steroid receptor coactivator SRC small molecule ‘stimulator’ (SMS), super-stimulates SRCs’ transcriptional activity. MCB-613 increases SRCs’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). MCB-613 is a SMS that target oncogenes can be exploited as anti-cancer agents by over-stimulating the SRC oncogenic program.
  • HY-111360
    SPL-707

    γ-secretase Inflammation/Immunology
    SPL-707 is an orally active, selective signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 77 nM for hSPPL2a. SPL-707 inhibits γ-secretase (IC50=6.1 μM) and SPP (IC50=3.7 μM). SPL-707 has the potential for autoimmune diseases research by targeting B cells and dendritic cells.
  • HY-N4215
    11(α)-Methoxysaikosaponin F

    Others Inflammation/Immunology
    11(α)-Methoxysaikosaponin F is a triterpenoid saponin isolated from Bupleurum marginatum Wall.ex DC(ZYCH) which is a promising therapeutic for liver fibrosis. 11(α)-Methoxysaikosaponin F has an IC50 of 387.7 nM with viability of hepatic stellate cells-T6 (HSCs-T6). Triterpenoid saponins have numerous targets, important network positions, and strong inhibitory activity.
  • HY-112898
    DC1SMe

    ADC Cytotoxin Cancer
    DC1Sme, a DC1 derivative, exhibits IC50 values of 22 pM, 10 pM, 32 pM and 250 pM for Ramos, Namalwa, HL60/s and COLO 205 cancer cells, respectively. DC1, an analogue of the minor groove-binding DNA alkylator CC-1065, is a ADC Cytotoxin. DC1 can be used in synthesis of antibody-drug conjugates for the targeted treatment of cancer.
  • HY-P1428
    RFRP-1(human)

    Neuropeptide Y Receptor Endocrinology
    RFRP-1(human) is a gonadotropin-inhibitory hormone (GnIH) homolog. RFRP-1(human) targets human gonadotropin-releasing hormone (GnRH) neurons and gonadotropes and potently inhibits gonadotropin. RFRP-1(human) is a potent Neuropeptide FF (NPFF) receptor agonist with EC50s of 0.0011 nM and 29 nM for NPFF2 and NPFF1, 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-108442
    JW67

    Wnt Cancer
    JW67 inhibits the canonical Wnt signaling with an IC50 of 1.17μM. JW67 affects the multiprotein complex consisting of β-catenin/GSK-3β/AXIN/APC/CK1 that rapidly reduces active β-catenin with a subsequent downregulation of Wnt target genes. JW67 also inhibits colorectal cancer cell growth.
  • HY-126124
    AP39

    Others Neurological Disease Cardiovascular Disease
    AP39 is a triphenylphosphonium derivatised anethole dithiolethione and mitochondria-targeting hydrogen sulfide (H2S) donor. AP39 increases intracellular H2S levels. AP39 exerts cytoprotective effects and maintains mitochondrial DNA integrity under oxidative stress conditions. AP39 protects against myocardial reperfusion injury in mice model and has the potential for Alzheimer's disease research.
  • HY-111817
    ACT-451840

    Parasite Infection
    ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial.
  • HY-P1399A
    Pep2m, myristoylated TFA

    Myr-Pep2m TFA

    PKC Neurological Disease
    Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable peptide. Pep2m, myristoylated TFA can disrupt the protein kinase ζ (PKMζ) downstream targets, N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2) interactions. PKMζ is an autonomously active isozyme of protein kinase C (PKC).
  • HY-104036
    IDH-305

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1 R132H), 28 nM (IDH1 R132C), 6.14 µM (IDH1 WT)).
  • HY-128656
    LML134

    Histamine Receptor Neurological Disease Endocrinology
    LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders.
  • HY-117025A
    Manzamine A hydrochloride

    GSK-3 CDK Parasite HIV Proton Pump Autophagy Cancer Infection Neurological Disease
    Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 and 1.5μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1.
  • HY-N6022
    Byakangelicin

    Others Metabolic Disease
    Byakangelicin, one of the active compounds found in the roots of Angelica gigas, can serve as a modulator to improve brain accumulation of diverse active compounds (Umb, Cur, and Dox) and enhance therapeutic effects. Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of drug-drug interactions. Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones.
  • HY-124697
    BMP signaling agonist sb4

    TGF-β Receptor Cancer
    BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC50 value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. BMP signaling agonist sb4 activates BMP4 target genes (inhibitors of DNA binding, Id1 and Id3) canonical BMP signaling.
  • HY-13072
    Cenisertib

    AS-703569; R-763

    Aurora Kinase Bcr-Abl Akt STAT FLT3 Cancer
    Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.
  • HY-137464A
    OATD-01

    Others Inflammation/Immunology
    OATD-01 is a highly potent, first-in-class, orally active and selective chitinase inhibitor with low nanomolar activity toward CHIT1 (hCHIT1,IC50=23 nM). OATD-01 shows excellect PK profile in multiple species and is selectivity against a panel of other off-targets. OATD-01 exhibits significant antifibrotic efficacy in vivo and can be used for pulmonary fibrosis (IPF) research.
  • HY-131328
    Pirtobrutinib

    LOXO-305

    Btk Cancer
    Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM.
  • HY-124526
    Chiauranib

    CS2164

    VEGFR PDGFR c-Kit Aurora Kinase c-Fms Cancer
    Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects.
  • HY-138078
    Lufotrelvir

    PF-07304814

    SARS-CoV Infection
    Lufotrelvir (PF-07304814), a phosphate prodrug of PF-00835231, acts as a potent 3CL pro protease (M pro) inhibitor with SARS-CoV-2 antiviral activity. Lufotrelvir binds and inhibits SARS-CoV-2 3CL pro activity with a Ki of 174nM. Lufotrelvir is promising single antiviral agent and also can be used for the research of combination with other antivirals that target other critical stages of the coronavirus life cycle.
  • HY-128718
    Carbodine

    Influenza Virus Infection
    Carbodine (Carbocyclic cytidine) is a broad-spectrum antiviral agent active against DNA viruses, (+)RNA viruses, (-)RNA viruses, paramyxo, rhabdo and (+/-)RNA viruses, targets CTP synthetase that converts UTP to CTP. Carbodine (Carbocyclic cytidine) possesses significant antiviral activity against influenza virus types A0/PR-8/34 and A2/Aichi/2/68 in vitro.
  • HY-127146
    Platensimycin

    Antibiotic Bacterial
    Platensimycin is an antibiotic produced by S. platensis that inhibits gram-positive bacteria by selectively inhibiting cellular lipid biosynthesis (IC50=0.1 μM). Platensimycin targets the β-ketoacyl-acyl-carrier-protein synthase I/II, FabF/B, an enzyme that participates in the biosynthesis of fatty acids (IC50s=48 nM and 160 nM for S.aureus and E.coli enzymes, respectively). Platensimycin is a promising agent for overcoming antibiotic resistance.
  • HY-N6796
    Manumycin A

    Farnesyl Transferase Ras Apoptosis Phospholipase Cancer Infection
    Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (Ki =1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity . Manumycin A suppresses exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling. Manumycin A is a nSMase inhibitor (EC50=0.25 μM).
  • HY-126396
    Sordarin sodium

    Fungal Antibiotic Infection Inflammation/Immunology
    Sordarin is a potent diphthamide-dependent eEF2 inhibitor with antifungal properties. Sordarin targets eEF2 so as to inhibit protein translation by blocking eEF2-mediated translocation of tRNAs. Sordarin inhibits translation specifically in certain fungi (e.g. C. albicansC. glabrata, and C. neoformans) while unable to do so in some other fungal species (e.g. Candida parapsilosis and Candida lusitaniae).
  • HY-125877
    PROTAC Mcl1 degrader-1

    PROTACs Bcl-2 Family Cancer
    PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity.
  • HY-126249
    AAPK-25

    Aurora Kinase Polo-like Kinase (PLK) Apoptosis Cancer
    AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3 Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM.
  • HY-107390A
    AX-024 hydrochloride

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-19824
    3PO

    Autophagy Cancer
    3PO is a novel small-molecule inhibitor of the PFKFB3 isozyme, 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μM) IC50 value Target: PFKFB3 isozyme in vitro: 3PO inhibits recombinant PFKFB3 activity, suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.
  • HY-112671
    CDDO-dhTFEA

    RTA dh404

    Keap1-Nrf2 NF-κB Inflammation/Immunology
    CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB. CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats.
  • HY-12276
    MALT1 inhibitor MI-2

    MALT1 Cancer
    MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to animals.
  • HY-15614A
    SC144 hydrochloride

    Interleukin Related Apoptosis Cancer
    SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells.
  • HY-121629
    PS210

    PDK-1 Cancer
    PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K.
  • HY-124858
    SC99

    STAT JAK Apoptosis Cancer Cardiovascular Disease
    SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities.
  • HY-108831
    Natalizumab

    Integrin Inflammation/Immunology
    Natalizumab is a recombinant, humanized monoclonal antibody, binds to α4β1-integrin and blocks its interaction with vascular cell adhesion molecule-1 (VCAM-1). Natalizumab can be used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease. Natalizumab is also the first targeted therapy which blocks an essential mechanism for lymphocyte entry to the CNS and thus prevents acute demyelinating relapses.
  • HY-120599
    Sabizabulin

    VERU-111; ABI-231

    Microtubule/Tubulin Apoptosis Cancer
    VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer.
  • HY-15614
    SC144

    Interleukin Related Apoptosis Cancer
    SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells.
  • HY-12076
    BMS 777607

    BMS 817378

    c-Met/HGFR TAM Receptor Cancer
    BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases.
  • HY-122630
    TH-257

    LIM Kinase (LIMK) Cancer
    TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM.
  • HY-124828
    CMLD-2

    Apoptosis Cancer
    CMLD-2, an inhibitor of HuR-ARE interaction, competitively binds HuR protein disrupting its interaction with adenine-uridine rich elements (ARE)-containing mRNAs (Ki=350 nM). CMLD-2 induces apoptosis exhibits antitumor activity in different cancer cells as colon, pancreatic, thyroid and lung cancer cell lines. Hu antigen R (HuR) is an RNA binding protein, can regulate target mRNAs stability and translation.
  • HY-126214
    JH-RE-06

    DNA/RNA Synthesis Cancer
    JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Kd=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 improves chemotherapy.
  • HY-124745
    KY-05009

    MAP4K Wnt Apoptosis Cancer
    KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.
  • HY-16558
    Butein

    2’,3,4,4’-tetrahydroxy Chalcone

    EGFR Autophagy Apoptosis Phosphodiesterase (PDE) Cancer
    Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
  • HY-P3101A
    GLP-1(28-36)amide TFA

    Glucagon Receptor Metabolic Disease Cardiovascular Disease
    GLP-1(28-36)amide TFA, a C-terminal nonapeptide of GLP-1, is a major product derived from the cleavage of GLP-1 by the neutral endopeptidase (NEP). GLP-1(28-36)amide TFA is an antioxidant and targets to mitochondrion, inhibits mitochondrial permeability transition (MPT). GLP-1(28-36)amide TFA has anti-diabetic and cardioprotection effects.
  • HY-18371
    TC-S 7009

    HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM. TC-S 7009 is more selective for HIF-2α than HIF-1α (Kd ≫ 5 μM). TC-S 7009 disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression.
  • HY-107390
    AX-024

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-101544
    ARQ 069

    FGFR Cancer
    ARQ 069, an analog of ARQ 523, inhibits FGFR in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC50s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC50s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner.
  • HY-N1372A
    Fangchinoline

    HIV FAK Apoptosis Autophagy Cancer Infection
    Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK. Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer.
  • HY-N2278
    Kushenol A

    Leachianone E

    Tyrosinase Glucosidase Cancer
    Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC50 and Kivalues of 1.1 μM and 0.4 μM, respectively. Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase. Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging.
  • HY-116749
    Ethaselen

    BBSKE

    Others Cancer
    Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC50s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR.
  • HY-13488
    HG-10-102-01

    LRRK2 Neurological Disease
    HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2(IC50=23.3 nM) and the G2019S mutant(IC50=3.2 nM) IC50 Value: 23.3 nM (WT LRRK2); 3.2 nM (LRRK2 G2019S) [1] Target: LRRK2 HG-10-102-01 maintains the ability to potently inhibit the biochemical activity of wild-type and G2019S mutant LRRK2.
  • HY-107146
    PZ-128

    P1pal-7

    Protease-Activated Receptor (PAR) Cancer Cardiovascular Disease
    PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects.
  • HY-124295
    MPT0E028

    HDAC Akt Apoptosis Cancer
    MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. MPT0E028 reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. MPT0E028 has good anticancer activity.
  • HY-128206
    I3MT-3

    HMPSNE

    Hippo (MST) Metabolic Disease
    I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM). I3MT-3 is inactive for other H2S/sulfane sulfur-producing enzymes. I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST.
  • HY-15477A
    YS-49 monohydrate

    Akt PI3K Angiotensin Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology
    YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
  • HY-122653
    CCT367766

    PROTACs Cancer
    CCT367766 is a potent and the third generation heterobifunctional and PROTAC-based pirin targeting protein degradation probe (PDP), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein.
  • 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-16591
    Birinapant

    TL32711

    IAP Apoptosis HIV Cancer
    Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.
  • HY-P9976
    Isatuximab

    Apoptosis Cancer
    Isatuximab is a monoclonal antibody targeting the transmembrane receptor and ectoenzyme CD38, a protein highly expressed on hematological malignant cells, including those in multiple myeloma (MM). Isatuximab has antitumor activity via multiple biological mechanisms, including antibody-dependent cellular-mediated cytotoxicity, complement-dependent cytotoxicity, antibody-dependent cellular phagocytosis, and direct induction of apoptosis without crosslinking. Isatuximab also directly inhibits CD38 ectoenzyme activity, which is implicated in many cellular functions.
  • HY-123986
    CTPI-2

    Mitochondrial Metabolism Cancer Inflammation/Immunology
    CTPI-2 is a third-generation mitochondrial citrate carrier SLC25A1 inhibitor with a KD of 3.5 μM. CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. CTPI-2 halts salient alterations of NASH reverting steatosis, preventing the evolution to steatohepatitis, reducing inflammatory macrophage infiltration in the liver and adipose tissue, and starkly mitigating obesity induced by a high-fat diet. Antitumor activity.
  • HY-15477
    YS-49

    Akt PI3K Angiotensin Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology
    YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
  • HY-16350
    NKP-1339

    IT-139; KP-1339

    DNA/RNA Synthesis Apoptosis Cancer
    NKP-1339 (IT-139; KP-1339) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. NKP-1339 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. NKP-1339 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu.
  • HY-109118
    Masupirdine free base

    SUVN-502 free base

    5-HT Receptor Neurological Disease
    Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base (SUVN-502 free base) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease.
  • HY-10187
    TG 100801 Hydrochloride

    VEGFR FGFR PDGFR Src Cancer
    TG 100801 Hydrochloride is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-50905S
    Dovitinib-D8

    FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib-D8 (CHIR-258-D8) is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively.
  • HY-132301
    MCT4-IN-1

    Monocarboxylate Transporter Cancer
    MCT4-IN-1 is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MCT4-IN-1 targets to the cytosolic domain of MCT4. MCT4-IN-1 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MCT4-IN-1 has the potential for MCT4 transporter inhibition research.
  • HY-110208
    BRD9876

    Kinesin Microtubule/Tubulin Cancer
    BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research.
  • HY-N2187
    Deoxyshikonin

    Bacterial HIF/HIF Prolyl-Hydroxylase Cancer Infection Cardiovascular Disease
    Deoxyshikonin is isolated from Lithospermum erythrorhizon Sieb with antitumor activity. Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF, indicates a prolymphangiogenesis as well as a proangiogenesis effect in vitro. Deoxyshikonin shows significant synergic antimicrobial activity against S. pneumonia (MIC=17 μg/mL), also shows significantly inhibitory activities against MRSA.
  • HY-50751
    Linifanib

    ABT-869; AL-39324

    PDGFR VEGFR FLT3 c-Fms c-Kit Autophagy Apoptosis Cancer
    Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.
  • HY-10186
    TG 100801

    VEGFR FGFR PDGFR Src Cancer
    TG 100801 is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-P9949
    Reslizumab

    Sch 55700

    Interleukin Related Inflammation/Immunology
    Reslizumab (Sch 55700) is humanized monoclonal antibodies that target interleukin-5 (IL-5) for the treatment of eosinophilic asthma. Reslizumab is effective in neutralizing the function of IL-5. Reslizumab inhibits IL-5-dependent cell proliferation, with an IC50 value of approximately 91.1pM. Reslizumab has high binding affinity for human IL-5, with KD values of 109 pM and 4.3 pM in the the Biacore surface plasmon resonance and Kinetic Exclusion Assay, respectively.
  • HY-110374
    NVS-CECR2-1

    Epigenetic Reader Domain Apoptosis Cancer
    NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC50=47 nM; KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism.
  • HY-15244
    Alpelisib

    BYL-719

    PI3K Cancer
    Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity.
  • HY-N4226
    1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid

    Others Inflammation/Immunology Cancer
    1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid is from Cordyceps bassiana, which is one of Cordyceps species with anti-oxidative, anti-cancer, anti-inflammatory, anti-diabetic, anti-obesity, anti-angiogenic, and anti-nociceptive activities. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid targets to block AP-1-mediated luciferase activity, implying it has an anti-inflammatory function.
  • HY-130711A
    (S,R,S)-AHPC-C3-NH2 TFA

    VH032-C3-NH2 TFA

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C3-NH2 TFA (VH032-C3-NH2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader.
  • HY-119293
    K777

    Cathepsin CCR Cytochrome P450 Cancer Infection
    K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively.
  • HY-130711
    (S,R,S)-AHPC-C3-NH2

    VH032-C3-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader.
  • HY-18980
    Rottlerin

    Mallotoxin; NSC 56346; NSC 94525

    PKC Autophagy Apoptosis HIV Infection Cancer
    Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection.
  • HY-136351
    THZ-P1-2

    Autophagy Cancer
    THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.
  • HY-100008
    Peretinoin

    NIK333

    RAR/RXR SphK Autophagy HCV Cancer Infection
    Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM.
  • HY-130816
    (S,R,S)-AHPC-O-Ph-PEG1-NH2

    VH032-O-Ph-PEG1-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) is E3 ligase ligand-linker conjugate and incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-O-Ph-PEG1-NH2 is used in PROTAC EED degrader-1 (HY-130614). PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02.
  • HY-121638A
    (5Z,2E)-CU-3

    Apoptosis Cancer
    (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
  • HY-18676
    OSU-T315

    Integrin Autophagy Apoptosis Cancer
    OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.
  • HY-16561
    Resveratrol

    trans-Resveratrol; SRT501

    IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Keap1-Nrf2 Cancer Infection Inflammation/Immunology
    Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
  • HY-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-111373
    RapaLink-1

    mTOR Autophagy Cancer
    RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity.
  • HY-121638
    CU-3

    Apoptosis Cancer Inflammation/Immunology
    CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
  • HY-122578
    P53R3

    MDM-2/p53 Cancer
    P53R3 is a potent p53 reactivator and restores sequence-specific DNA binding of p53 hot spot mutants, including p53 R175H, p53 R248W and p53 R273H. P53R3 induces p53-dependent antiproliferative effects with much higher specificity than PRIMA-1. P53R3 enhances the recruitment of wild-type p53 and p53 M237I to several target gene promoters. P53R3 strongly enhances the mRNA, total protein and cell surface expression of the death receptor death receptor 5 (DR5). P53R3 is used for cancer research.