1. Search Result
Search Result
Results for "

tumors

" in MCE Product Catalog:

1404

Inhibitors & Agonists

20

Screening Libraries

2

Dye Reagents

2

Biochemical Assay Reagents

68

Peptides

18

Inhibitory Antibodies

259

Natural
Products

1

Recombinant Proteins

45

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • 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-144038
    DNA-PK-IN-5

    DNA-PK Cancer
    DNA-PK-IN-5 is a potent inhibitor of DNA-PK. DNA-PK-IN-5 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-5 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of drug resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021204111A1, compound 2).
  • HY-144039
    DNA-PK-IN-6

    DNA-PK Cancer
    DNA-PK-IN-6 is a potent inhibitor of DNA-PK. DNA-PK-IN-6 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-6 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of drug resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021197159A1, compound 6).
  • HY-13479
    EC144

    HSP Cancer
    EC144 is a potent and selective inhibitor of heat shock protein 90 (Hsp90) with an IC50 of 1.1 nM. EC144 inhibits tumor growth and causes partial tumor regressions. EC144 has the potential for the research of cancer diseases.
  • HY-115514A
    BRK inhibitor P21d hydrochloride

    Others Cancer
    BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models.
  • HY-16110
    Tegafur-Uracil

    UFT; BMS-200604

    Others Cancer
    Tegafur-Uracil is an orally active fluoropyrimidines anticancer agent. Tegafur-Uracil inhibits thymidylate synthase. Tegafur-Uracil can be used for researching anti solid tumors.
  • HY-107665
    Ro 106-9920

    NF-κB Cancer
    Ro 106-9920 is a potent inhibitor of NF-kappaB. Ro 106-9920 has the potential for the research of tumor and cancer diseases.
  • HY-137457A
    Venadaparib hydrochloride

    IDX-1197 hydrochloride

    PARP Cancer
    Venadaparib (IDX-1197) hydrochloride is a potent and selective PARP inhibitor with anticancer activities. Venadaparib hydrochloride can be used for solid tumors research.
  • HY-N7000
    Perillyl alcohol

    Apoptosis Endogenous Metabolite Cancer
    Perillyl alcohol, a monoterpene, is active in inducing apoptosis in tumor cells without affecting normal cells.
  • HY-114377
    p-SCN-Bn-DOTA

    Others Cancer
    p-SCN-Bn-DOTA is a bifunctional chelating agent. p-SCN-Bn-DOTA can simultaneously chelate radionuclides and link monoclonal antibody for radioimmunotherapy of tumor.
  • HY-117737A
    RRD-251

    Raf Apoptosis Cancer
    RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities.
  • HY-P9978
    Toripalimab

    PD-1/PD-L1 Cancer
    Toripalimab is the first domestic anti-tumor PD-1 antibody in China. Toripalimab is a selective, recombinant, humanized monoclonal antibody against PD-1. Toripalimab is able to bind to PD-1 and block the interaction with its ligands. Toripalimab has exhibited primary anti-tumor effects in tumors such as melanoma, lung cancer, digestive tract tumors, hepatobiliary and pancreatic tumors, neuroendocrine neoplasms, nasopharyngeal carcinoma and urothelial carcinoma.
  • HY-105529
    Indicine N-oxide

    (+)-Indicine N-oxide; NSC 132319

    Others Cancer
    Indicine N-oxide (NSC 132319), a pyrrolizidine alkaloid, is an antitumor agent for pediatric cancer and solid tumors research.
  • HY-131991
    Benzyl selenocyanate

    DNA Methyltransferase Cancer
    Benzyl selenocyanate is a chemopreventive agent for various chemically induced tumors in animal models at both the initiation and postinitiation stages. Benzyl selenocyanate is an inhibitor of DNA (cytosine-5)-methyltransferase (Mtase), with an with an IC50 of 8.4 µM.
  • HY-137331
    FAPI-46

    Others Cancer
    FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted radiotracer. FAPI-46 has higher tumor uptake and prolonged tumor accumulation. FAPI-46 can be used for tumor imaging of a multitude of different cancers.
  • HY-40136
    cis-4-Hydroxy-L-proline

    Endogenous Metabolite Cancer Metabolic Disease
    cis-4-Hydroxy-L-proline, a proline analogue, is an inhibitor of collagen production. cis-4-Hydroxy-L-proline could inhibit fibroblast growth by preventing the deposition of triple-helical collagen on the cell layer. cis-4-Hydroxy-L-proline also depresses the growth of primary N-nitrosomethylurea-induced rat mammary tumors.
  • HY-136927
    MSA-2

    STING Cancer Inflammation/Immunology
    MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models.
  • HY-128587
    Mevociclib

    SY-1365

    CDK Cancer
    Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors.
  • HY-133887
    Methotrexate α-tert-butyl ester

    Antifolate DNA/RNA Synthesis Cancer
    Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent.
  • HY-147594
    CD73-IN-13

    CD73 Cancer
    CD73-IN-13 is a potent inhibitor of CD73. CD73 is closely associated with tumor growth, angiogenesis and metastasis. CD73-IN-13 be used for preparing a medicament for tumor-related diseases (extracted from patent CN114437039A, compound 7).
  • HY-147593
    CD73-IN-12

    CD73 Cancer
    CD73-IN-12 is a potent inhibitor of CD73. CD73 is closely associated with tumor growth, angiogenesis and metastasis. CD73-IN-12 be used for preparing a medicament for tumor-related diseases (extracted from patent CN114437038A, compound 9).
  • HY-N3055
    Pinusolide

    Apoptosis Cancer
    Pinusolide is a known platelet-activating factor (PAF) receptor binding antagonist. Pinusolide not only decreases the proliferation activity of tumor cells but specifically induces apoptosis.
  • HY-N0984
    1,3-Diacetylvilasinin

    Diacetylvilasinin

    Others Cancer
    1,3-Diacetylvilasinin (Diacetylvilasinin), a bioactive Triterpenoid from Melia volkensii, shows marginal cytotoxicities against certain human tumor cell lines.
  • HY-N4306
    Sarracenin

    Others Cancer
    Sarracenin is a iridoid isolated from roots and rhizomes of Patrinia heterophylla. Sarracenin shows cytotoxic activities against tumor cells.
  • HY-132292
    ARD-2128

    PROTACs Androgen Receptor Cancer
    ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.
  • HY-147828
    hCAIX-IN-11

    Carbonic Anhydrase Cancer
    hCAIX-IN-11 (Compound 5d) is a selective carbonic anhydrase IX and XII inhibitor with Ki s of 32.7 and 623.5 nM for hCA IX and hCA XII, respectively.  hCA IX and hCA XII are transmembrane isoforms which have been characterized as biomarkers for several types of tumors. The hCA XII assists in maintenance of acid-base homoeostasis in normal as well as tumor cells.
  • HY-134904
    RMC-6272

    RM-006

    mTOR Cancer
    RMC-6272 (RM-006) is a bi-steric mTORC1-selective inhibitor. RMC-6272 exhibits potent and selective (> 10-fold) inhibition of mTORC1 over mTORC2. RMC-6272 shows improved inhibition of mTORC1 in comparison to Rapamycin, and induces more cell death in TSC2 null tumors.
  • HY-147827
    hCAIX-IN-10

    Carbonic Anhydrase Cancer
    hCAIX-IN-10 (Compound 6i) is a selective carbonic anhydrase IX and XII inhibitor with Ki s of 61.5 and 586.8 nM for hCA IX and hCA XII, respectively.  hCA IX and hCA XII are transmembrane isoforms which have been characterized as biomarkers for several types of tumors. The hCA XII assists in maintenance of acid-base homoeostasis in normal as well as tumor cells.
  • HY-P9969
    Matuzumab

    EMD 72000

    EGFR Cancer
    Matuzumab (EMD 72000) is a humanized anti-EGFR monoclonal antibody that blocks EGFR activation and downstream signaling, inhibits tumor growth.
  • HY-13459
    PF-5274857

    Smo Cancer
    PF-5274857 is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.
  • HY-13459A
    PF-5274857 hydrochloride

    Smo Cancer
    PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.
  • HY-124617A
    AMXT-1501 tetrahydrochloride

    Apoptosis Cancer Inflammation/Immunology
    AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells. Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines.
  • HY-137435
    Cirtuvivint

    SM08502

    CDK Cancer
    Cirtuvivint (SM08502) is a potent and orally active CDC-like kinase (CLK) inhibitor. Cirtuvivint can be used for solid tumors research.
  • HY-146780
    TGFβRI-IN-4

    TGF-β Receptor Cancer
    TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model.
  • HY-110201
    Estrogen receptor modulator 1

    Estrogen Receptor/ERR Cancer
    Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.
  • HY-136824
    Napyradiomycin A1

    Bacterial Antibiotic Cancer Infection
    Napyradiomycin A1 is one enantioselective compound of napyradiomycins. napyradiomycins are an intriguing family of halogenated natural products with activity against several tumor cell lines as well as some bacterial strains.
  • HY-136110
    2-Keto-D-galactose

    D-​Galactosone

    DNA/RNA Synthesis Cancer
    2-Keto-D-galactose (D-Galactosone) inhibits DNA synthesis, and inhibits proliferation of in vitro grown Ehrlich ascites tumor cells.
  • HY-139361
    Sulfopin

    PIN1-3

    Others Cancer
    Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors.
  • 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-P3440
    WL12

    PD-1/PD-L1 Cancer
    WL12 is a specifically targeting programmed death ligand 1 (PD-L1) binding peptide. WL12 can be radiolabeled by different radionuclides, generating radiotracers, which can assess the tumor PD-L1 expression.
  • HY-103665A
    STING agonist-3 trihydrochloride

    STING Cancer
    STING agonist-3 trihydrochloride, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pEC50 of 7.5 and 9.5, respectively. STING agonist-3 trihydrochloride has durable anti-tumor effect and tremendous potential to improve treatment of cancer.
  • HY-101931
    hVEGF-IN-1

    VEGFR Cancer
    hVEGF-IN-1, a quinazoline derivative, could specifically bind to the G-rich sequence in the internal ribosome entry site A (IRES-A) and destabilize the G-quadruplex structure. hVEGF-IN-1 binds to the IRES-A (WT) with a Kd of 0.928 μM in SPR experiments. hVEGF-IN-1 could hinder tumor cells migration and repress tumor growth by decreasing VEGF-A protein expression.
  • HY-78884
    Anticancer agent 9

    Others Cancer
    Anticancer agent 9, a glycine derivative, is an anticancer agent. Anticancer agent 9 can inhibit tumor cells viability of myelogenous leukemia and human prostate cancer.
  • 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-N10139
    Myxin

    Others Cancer
    Myxin is a di-N-oxide phenazine produced by Lysobacter antibioticus OH13. Myxin is toxic to many microorganisms and tumor cells.
  • HY-143734
    HER2-IN-6

    Others Cancer
    HER2-IN-6 is a potent inhibitor of HER2. HER2-IN-6 has the potential for the research of wild and/or mutant EGFR and/or HER2 kinase mediated tumor (extracted from patent WO2021164697A1, compound 11).
  • 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-128890
    DOTA-​NHS-​ester

    ADC Linkers Cancer
    DOTA-NHS-ester is a linker for affibody molecules and is applied in small animals PET, SPECT, and CT. DOTA-NHS-ester can be used to label radiotherapeutic agents or imaging probes for the detection of tumors.
  • HY-14934
    Rosabulin

    STA 5312

    Microtubule/Tubulin Cancer
    Rosabulin (STA 5312) is a potent and orally active microtubule inhibitor that inhibits microtubule assembly. Rosabulin has broad-spectrum anti-tumor activity.
  • HY-13917A
    PND-1186 hydrochloride

    VS-4718 hydrochloride; SR-2516 hydrochloride

    FAK Apoptosis Cancer
    PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis.
  • HY-13917
    PND-1186

    VS-4718; SR-2516

    FAK Apoptosis Cancer
    PND-1186 (VS-4718) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis.
  • HY-145734A
    AMXI-5001 hydrochloride

    Microtubule/Tubulin Cancer
    AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors.
  • HY-145734
    AMXI-5001

    Microtubule/Tubulin Cancer
    AMXI-5001 is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 induces complete regression of established tumors, including exceedingly large tumors.
  • HY-145034
    KIF18A-IN-1

    Microtubule/Tubulin Cancer Inflammation/Immunology
    KIF18A-IN-1 is a mitotic kinesin KIF18A inhibitor extracted from patent WO2021026098A1 example 100-13. KIF18A-IN-1 exhibits anti-tumor activity.
  • HY-144720
    BRG1-IN-1

    Others Cancer
    BRG1-IN-1 (Compound 11d) is a potent inhibitor of BRG1. BRG1-IN-1 shows better efficacy than PFI-3 in sensitizing GBM cells to the antiproliferative and cell death inducing effects of Temozolomide in vitro. BRG1-IN-1 enhances the inhibitor effect of Temozolomide on the growth of subcutaneous GBM tumors.
  • HY-136279
    TrxR inhibitor D9

    Apoptosis Cancer
    TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo.
  • HY-N6955
    Eupalinilide B

    Others Cancer
    Eupalinilide B is a guaiane type sesquiterpene lactone that can be found in Eupatorium lindleyanum. Eupalinilide B shows potent cytotoxicity against P-388 and A-549 tumor cell lines.
  • HY-B0109
    Dorzolamide

    L671152; MK507

    Carbonic Anhydrase Cancer
    Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
  • HY-B0109A
    Dorzolamide hydrochloride

    L671152 hydrochloride; MK507 hydrochloride

    Carbonic Anhydrase Others
    Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
  • HY-136201
    Sodium Glucoheptonate

    Others Cancer
    Sodium Glucoheptonate is used as a kit for radio-labeling with Tc-99m. Tc-99m glucoheptonate is kidney- and brain-imaging agent, and can be used in brain-tumor detection.
  • HY-137457
    Venadaparib

    IDX-1197

    PARP Cancer
    Venadaparib (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib does not sensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSB) and can be used for solid tumors research.
  • 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-106218
    Flurocitabine

    5-Fluorocyclocytidine; 5'-Fluorocyclocytidine

    Nucleoside Antimetabolite/Analog Cancer
    Flurocitabine (5-Fluorocyclocytidine) is a fluorinated anlydride analog of cytosine arabinoside, partially hydrolysecl in vivo into two active antitumor substances (arabinosyl-tluorocytosine (ara-FC) and arabinosyl-fluorouracil (ara-FU)). Flurocitabine (5-Fluorocyclocytidine) has antitumor activity during phase I studies in acute leukemia and solid tumors.
  • HY-122590
    Glabrescione B

    Gli Cancer
    Glabrescione B is the first compound that binds the Hedgehog (Hh) modulator Gli1. Glabrescione B impairs its activity by interfering with Gli1-DNA interaction. Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells, the self-renewal ability, and clonogenicity of tumor-derived stem cells.
  • HY-147592
    CD73-IN-11

    CD73 Cancer Inflammation/Immunology
    CD73-IN-11 is a potent inhibitor of CD73. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), and adenosine can induce immunosuppressive effects and promote tumor proliferation and/or metastasis. CD73-IN-11 be used for preparing a medicament for tumor-related diseases (extracted from patent WO2022068929A1, compound 24).
  • HY-147591
    CD73-IN-10

    CD73 Cancer Inflammation/Immunology
    CD73-IN-10 is a potent inhibitor of CD73. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), and adenosine can induce immunosuppressive effects and promote tumor proliferation and/or metastasis. CD73-IN-10 be used for preparing a medicament for tumor-related diseases (extracted from patent WO2022068929A1, compound 4).
  • HY-147589
    CD73-IN-8

    CD73 Cancer
    CD73-IN-8 is a potent inhibitor of CD73. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), and adenosine can induce immunosuppressive effects and promote tumor proliferation and/or metastasis. CD73-IN-8 be used for preparing a medicament for tumor-related diseases (extracted from patent WO2022052886A1, compound 57).
  • HY-147590
    CD73-IN-9

    CD73 Inflammation/Immunology
    CD73-IN-9 is a potent inhibitor of CD73. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), and adenosine can induce immunosuppressive effects and promote tumor proliferation and/or metastasis. CD73-IN-9 be used for preparing a medicament for tumor-related diseases (extracted from patent WO2022068929A1, compound 2).
  • HY-147588
    CD73-IN-7

    CD73 Cancer
    CD73-IN-7 is a potent inhibitor of CD73. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), and adenosine can induce immunosuppressive effects and promote tumor proliferation and/or metastasis. CD73-IN-7 be used for preparing a medicament for tumor-related diseases (extracted from patent WO2022052886A1, compound 13).
  • HY-103711
    Estramustine

    Microtubule/Tubulin Cancer
    Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts.
  • HY-147784
    HZ-A-005

    Btk Cancer
    HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models.
  • HY-10824B
    Talotrexin ammonium

    PT523 ammonium

    Others Cancer
    Talotrexin ammonium is a nonpolyglutamatable antifolate. Talotrexin ammonium improves antitumor activity in a broad spectrum of cancer models by targeting DHFR to inhibit tumor growth.
  • HY-135849
    Catalase

    Reactive Oxygen Species Cancer
    Catalase is a key enzyme in the metabolism of H2O2 and reactive oxygen species (ROS), and its expression and localization is markedly altered in tumors. Free oxygen radical scavenger.
  • HY-N7507
    Sempervirine

    Others Cancer
    Sempervirine is an indole alkaloid isolated from Gelsemium sempervirens with anti-tumor activities. Sempervirine is against sempervirine-sensitive tumor cells with EC50 values of 2.7 μM, 1.77 μM, and 1.96 μM for Raji, MDA-MB-231 and HeLa cells, respectively.
  • HY-137206
    ALV2

    Ligands for E3 Ligase Molecular Glues Cancer
    ALV2 is a potent and selective Helios degrader. ALV2 binds CRBN, with an IC50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable Treg cell phenotype in the inflammatory tumor microenvironment.
  • HY-119529
    Jineol

    3,8-Quinolinediol

    Others Cancer
    Jineol is a cytotoxic alkaloid from the centipede Scolopendra subspinipes. Jineol exhibits modest cytotoxic activity in vitro against the growth of human tumor cell lines.
  • HY-101566A
    Elimusertib hydrochloride

    BAY 1895344 hydrochloride

    ATM/ATR Cancer
    Elimusertib (BAY 1895344) hydrochloride is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib hydrochloride has anti-tumor activity. Elimusertib hydrochloride can be used for the research of solid tumors and lymphomas.
  • HY-N0797
    (20S)-Protopanaxadiol

    20-Epiprotopanaxadiol; 20(S)-APPD

    P-glycoprotein Reactive Oxygen Species Apoptosis Cancer
    20S-protopanaxadiol (aPPD) is a metabolite of ginseng saponins, inhibits Akt activity and induces apoptosis in various tumor cells.
  • HY-145414
    DYSP-C34

    Others Cancer
    DYSP-C34 is a potent, biocompatible, and ultrasound (US)-triggered multifunctional molecular machine. DYSP-C34 has multiple favorable properties, such as improved lipophilic/hydrophilic balance, intensified US-induced ROS production capacity, and better cellular permeability, resulting in the excellent tumor target efficiency and notable sonodynamic therapy (SDT)-mediated tumor regression. DYSP-C34 exhibits mild immunogenicity by stimulating APCs directly.
  • HY-146185
    CCT373566

    Bcl-2 Family Cancer
    CCT373566 is a potent and orally active degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM. CCT373566 shows strong antiproliferative efficacy in vitro and reduction in tumor growth in vivo.
  • HY-101566
    Elimusertib

    BAY 1895344

    ATM/ATR Cancer
    Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib has anti-tumor activity. Elimusertib can be used for the research of solid tumors and lymphomas.
  • HY-N1381
    Periplocin

    Apoptosis Cancer Inflammation/Immunology
    Periplocin is a cardiotonic steroid isolated from Periploca forrestii. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase.
  • HY-15866
    FR901465

    Others Cancer
    FR901465 is a potent anti-cancer and anti-tumor agent. FR901465 can be used for cancer research.
  • HY-132979
    KRAS G12C inhibitor 18

    Ras Cancer
    KRAS G12C inhibitor 18 is a potent and orally active KRAS G12C inhibitor. Anti-tumor activities.
  • HY-W008449
    1-Methylxanthine

    Endogenous Metabolite Cancer
    1-Methylxanthine, a caffeine derivative, is an essential human urinary metabolite of caffeine and theophylline (1,3-dimethylxanthine, TP). 1-Methylxanthine enhances the radiosensitivity of tumor cells.
  • 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-128075
    Acifluorfen

    Others Cancer
    Acifluorfen, a protoporphyrinogen oxidase (PROTOX) inhibitor herbicide, promotes the accumulation of protoporphyrin IX (PPIX), and induces tumors in the rodent liver. Acifluorfen causes strong photooxidative destruction of pigments and lipids in sensitive plant species.
  • HY-139453
    LP-184

    Others Cancer
    LP-184 (compound 6), an acylfulvene analog, inhibits tumor growth. LP-184 has potent anti-cancer activity in the ovarian, colon, prostate and pancreatic cell lines. (patent WO2007019308A2).
  • HY-125858
    MI-1061

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
  • HY-136174
    RBN-2397

    PARP Cancer
    RBN-2397 is a potent, accross species and orally active NAD + competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors.
  • HY-13062A
    Daunorubicin

    Daunomycin; RP 13057; Rubidomycin

    Topoisomerase DNA/RNA Synthesis ADC Cytotoxin Autophagy Bacterial Antibiotic Apoptosis Cancer Infection Neurological Disease
    Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
  • HY-13062
    Daunorubicin hydrochloride

    Daunomycin hydrochloride; RP 13057 hydrochloride; Rubidomycin hydrochloride

    Topoisomerase DNA/RNA Synthesis ADC Cytotoxin Bacterial Autophagy Apoptosis Antibiotic Cancer Infection Neurological Disease
    Daunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin hydrochloride inhibits DNA and RNA synthesis. Daunorubicin hydrochloride is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin hydrochloride is also an anthracycline antibiotic. Daunorubicin hydrochloride can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
  • HY-135336A
    (S)-Verapamil hydrochloride

    (S)-(-)-Verapamil hydrochloride

    Leukotriene Receptor Calcium Channel Apoptosis Cancer
    (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells.
  • HY-W034551
    DOTA-tri(t-butyl ester)

    Others Others
    DOTA-tri(t-butyl ester) can be used in the synthesis of generations 3 (G3) nanoglobular magnetic resonance imaging (MRI) contrast agents for MR angiography and tumor angiogenesis imaging.
  • HY-115908
    ZDLD13

    CDK Apoptosis Cancer
    ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model.
  • HY-125858A
    MI-1061 TFA

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
  • HY-B0754A
    Hematoporphyrin dihydrochloride

    Hematoporphyrin IX dihydrochloride

    Apoptosis Endogenous Metabolite Cancer
    Hematoporphyrin dihydrochloride (Hematoporphyrin IX dihydrochloride), a photosensitizer, is a substrate for affinity chromatography of heme-binding proteins. Hematoporphyrin dihydrochloride can induce apoptosis in U87 glioma cells and decrease tumor growth in vivo when exposed to red light.
  • HY-B0754
    Hematoporphyrin

    Hematoporphyrin IX

    Apoptosis Endogenous Metabolite Cancer
    Hematoporphyrin (Hematoporphyrin IX), a photosensitizer, is a substrate for affinity chromatography of heme-binding proteins. Hematoporphyrin can induce apoptosis in U87 glioma cells and decrease tumor growth in vivo when exposed to red light.
  • HY-W018723
    4-Aminobenzamidine dihydrochloride

    p-Aminobenzamidine dihydrochloride

    Ser/Thr Protease Cancer
    4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor, also acting as a relatively weak urokinase type plasminogen activator (uPA) inhibitor (Ki=82 μM). 4-Aminobenzamidine can inhibit growth of a human prostate tumor in SCID mice.
  • HY-144443
    PD-1/PD-L1-IN-16

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-16 (Compound M23) is a potent inhibitor of PD-1/PD-L1 with an IC50 value of 53.2 nM. PD-1/PD-L1-IN-16 has the potential for the research of tumor immunotherapy.
  • HY-103665
    STING agonist-3

    STING Cancer
    STING agonist-3, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pIC50 of 7.5 and 9.5, respectively. STING agonist-3 has durable anti-tumor effect and tremendous potential to improve treatment of cancer.
  • HY-144442
    PD-1/PD-L1-IN-15

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-15 (Compound M17) is a potent inhibitor of PD-1/PD-L1 with an IC50 value of 60.1 nM. PD-1/PD-L1-IN-15 has the potential for the research of tumor immunotherapy.
  • HY-144184
    MAT2A-IN-6

    Others Cancer
    MAT2A-IN-6 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally elevated in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-6 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-6 has the potential for the potential for the research of cancer diseases (extracted from patent WO2021254529A1, compound 18).
  • HY-144185
    MAT2A-IN-7

    Others Cancer
    MAT2A-IN-7 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally elevated in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-7 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-7 has the potential for the potential for the research of cancer diseases (extracted from patent WO2021254529A1, compound 24).
  • HY-144181
    MAT2A-IN-5

    Others Cancer
    MAT2A-IN-5 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally elevated in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-5 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-5 has the potential for the potential for the research of cancer diseases (extracted from patent WO2021254529A1, compound 1).
  • HY-19095
    TNP-351

    Antifolate Cancer
    TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.
  • HY-143889
    Senexin C

    CDK Cancer
    Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability.
  • HY-N0247
    Saikosaponin B1

    Smo Cancer
    Saikosaponin B1 is a bioactive constituent of Radix Bupleuri with anticancer activity. Saikosaponin B1 significantly inhibits tumor growth in Medulloblastoma (MB) model by inhibiting the Hedgehog pathway through targeting SMO.
  • HY-129087
    BC-​1258

    Apoptosis Cancer
    BC-1258, an F-box/LRR-repeat protein 2 (FBXL2) activator, can stabilize and upregulate FBXL2 levels. BC-1258 induces apoptosis of tumorigenic cells, and profoundly inhibits tumor formation in mice.
  • HY-P99007
    Aprutumab

    BAY 1179470

    FGFR Cancer
    Aprutumab (BAY 1179470) is a fully human FGFR2 monoclonal antibody, which binds to the FGFR2 isoforms FGFR2-IIIb and FGFR2-IIIc. Aprutumab has the potential for solid tumors research.
  • 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-144029
    RET-IN-13

    RET Cancer
    RET-IN-13 (compound 1), a quinoline compound, is a potent RET inhibitor with IC50s of 0.5 nM, 0.9 nM for RET (WT) and RET (V804M), respectively. RET-IN-13 has the potential for tumors or intestinal diseases related to abnormal activation of RET research.
  • HY-143615
    RET-IN-10

    RET Cancer
    RET-IN-10 is a potent inhibitor of RET. RET loss of function mutations leads to Hirschsprung's disease, while its gain of function mutations is associated with a variety of human tumors. RET-IN-10 has the potential for the research of cancer diseases (extracted from patent WO2021135938A1, compound 18).
  • HY-125102
    AZ12253801

    IGF-1R Cancer
    AZ12253801 is an ATP-competitive IGF-1R tyrosine kinase inhibitor that shows ∼10-fold selectivity over the insulin receptor. AZ12253801 inhibits IGF-1R–driven proliferation in 3T3 mouse fibroblasts (transfected with human IGF-1R) with an IC50 of 17 nmol/L. The IC50 for epidermal growth factor receptor (EGFR)–driven proliferation is 440 nmol/L. Anti-tumor activity.
  • HY-N1493
    14-Deoxycoleon U

    6-Hydroxysalvinolone; 11-Hydroxymontbretol

    Others Cancer
    14-Deoxycoleon U is a natural abietane-type diterpene. 14-Deoxycoleon U exerts an inhibitory effect on tumor cells proliferation. 14-Deoxycoleon U may be a potent anti-cancerous lead compound for lung cancer research.
  • HY-D1464
    CH1055

    Others Cancer
    CH1055 is a NIR-II fluorophore based on a synthetic 970-Da organic molecule. CH1055 is a rapidly excreted dye (∼90% excreted through the kidneys within 24 h). CH1055 also allows targeted molecular imaging of tumors in vivo when conjugated with anti-EGFR Affibody.
  • HY-N10390
    3β-Hydroxylanosta-8,24-dien-21-al

    Others Cancer
    3β-Hydroxylanosta-8,24-dien-21-al is a lanostane-type triterpene. 3β-Hydroxylanosta-8,24-dien-21-al can inhibit the tumor promotion, reducing the percentage of mice bearing papillomas.
  • HY-143869
    HPK1-IN-28

    MAP4K Cancer
    HPK1-IN-28 is a potent inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of the activation response of dendritic cells (DCs), T cells and B cells. HPK1-IN-28 enhances the body's anti-tumor immunity. HPK1-IN-28 has the potential for the research of immune-related diseases, especially tumor (extracted from patent WO2021175270A1, compound 1).
  • HY-143870
    HPK1-IN-29

    MAP4K Cancer
    HPK1-IN-29 is a potent inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of the activation response of dendritic cells (DCs), T cells and B cells. HPK1-IN-29 enhances the body's anti-tumor immunity. HPK1-IN-29 has the potential for the research of immune-related diseases, especially tumor (extracted from patent WO2021175270A1, compound 38).
  • HY-N7623
    Ursonic acid methyl ester

    Others Cancer
    Ursonic acid methyl ester is an esterified derivative of Ursolic acid (HY-N0140). Ursonic acid methyl ester shows growth inhibitory activity against four tumor cell lines, HL-60, BGC, Bel-7402 and Hela with ED50 values of >100 µg/ml.
  • HY-128350A
    FGTI-2734 mesylate

    Farnesyl Transferase Cancer
    FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.
  • HY-109963
    PR5-LL-CM01

    Histone Methyltransferase Cancer
    PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies.
  • HY-115492
    NSC668394

    Others Cancer
    NSC668394 is a potent ezrin (Thr567) phosphorylation inhibitor, with a Kd of 12.59 μM. NSC668394 inhibit ezrin T567 phosphorylation caused by PKCΙ primarily via their binding to ezrin. NSC668394 can be used to prevent tumor metastasis.
  • HY-D0226
    Quinizarin

    1,4-Dihydroxyanthraquinone

    DNA/RNA Synthesis Fungal Cancer Infection
    Quinizarin (1,4-Dihydroxyanthraquinone), a part of the anticancer agents such as Doxorubicin, Daunorubicin, and Adriamycin, interacts with DNA by intercalating mode (Kd=86.1 μM). Quinizarin is used as a fungicide and pesticide chemical and has shown the ability to inhibit tumor cell growth.
  • HY-122856
    AZ12601011

    TGF-β Receptor Cancer
    AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
  • HY-145406
    IHCH-3064

    Adenosine Receptor HDAC Cancer Inflammation/Immunology
    IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.
  • HY-W005288
    4-Vinylphenol

    Apoptosis Endogenous Metabolite Cancer
    4-Vinylphenol is found in the medicinal herb Hedyotis diffusa Willd, wild rice and is also the metabolite of p-coumaric and ferulic acid by lactic acid bacteria in wine. 4-Vinylphenol induces apoptosis and inhibits blood vessels formation and suppresses invasive breast tumor growth in vivo.
  • HY-D0208
    Fluorescein sodium

    Uranine sodium

    Others Cancer
    Fluorescein (Uranine) sodium is widely used as a fluorescent tracer in medicinal and biological applications and tumor infected tissues tracer. Fluorescein (Uranine) sodium is a representative green fluorophore that has been widely used as a scaffold of practically useful green fluorescent probes.
  • HY-100219
    CB1151

    VD/VDR Cancer
    CB1151 is a 20-epi analogue of 1,25 dihydroxyvitamin D3 (VD) with potent anti-tumor effects. CB1151 inhibits MCF-7 cell growth with an IC50 value of 0.82 nM.
  • HY-P3139
    TPP-1

    PD-1/PD-L1 Cancer
    TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function.
  • HY-132173
    GL0388

    Bcl-2 Family Cancer
    GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.
  • HY-P2251
    T-peptide

    HIV Microtubule/Tubulin Cancer Infection Inflammation/Immunology
    T-peptide, a Tuftsin analog, can be used for the research of human immunodeficiency virus (HIV) infection. T-peptide prevents cellular immunosuppression and improves survival rate in septic mice. T-peptide also can inhibit the growth of residual tumor cells after surgical resection.
  • HY-147567
    ATR-IN-15

    ATM/ATR DNA-PK PI3K Cancer
    ATR-IN-15 (compound 1) is an orally active and potent ATR kinase inhibitor, with an IC50 of 8 nM. ATR-IN-15 also inhibits human colon tumor cells LoVo, DNA-PK and PI3K, with IC50 values of 47, 663 and 5131 nM, respectively.
  • HY-128350
    FGTI-2734

    Farnesyl Transferase Cancer
    FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.
  • HY-101266B
    Milademetan tosylate hydrate

    DS-3032b; DS-3032 tosylate hydrate

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis.
  • HY-B0392
    (S)-(+)-Rolipram

    (+)-Rolipram; (S)-Rolipram

    Phosphodiesterase (PDE) Apoptosis Cancer Inflammation/Immunology Neurological Disease
    (S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells.
  • HY-101266
    Milademetan

    DS-3032

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.
  • HY-137473
    Methyl pyropheophorbide-a

    Pyropheophorbide-a methyl ester

    Apoptosis Cancer
    Methyl pyropheophorbide-a (Pyropheophorbide-a methyl ester), a chlorophyll-a derivative, is a potent photosensitizer that can be used in photodynamic therapy (PDT) of cancer. Methyl pyropheophorbide-a has photodynamic activity and can induce apoptosis and inhibit tumor growth.
  • HY-P3139A
    TPP-1 TFA

    PD-1/PD-L1 Cancer
    TPP-1 TFA is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 TFA binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 TFA inhibits human tumor growth in vivo via reactivating T-cell function.
  • HY-75706
    N-Descyclopropanecarbaldehyde Olaparib

    E3 Ligase Ligand-Linker Conjugates 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-N10307
    Anserinone B

    Fungal Bacterial Endogenous Metabolite Cancer Infection
    Anserinone B is an antifungal and antibacterial benzoquinone. Anserinone B causes radial growth reductions of 50% and 37% against S.fimicola and A. furfuraceus, respectively. Anserinones B also displays moderate cytotoxicity in the NCI’s 60 human tumor cell line panel (GI50=4.4 µg/mL).
  • HY-W009245
    Bz-RS-iSer(3-Ph)-OMe

    HIV Infection
    Bz-RS-iSer(3-Ph)-OMe (compound 2), a Taxol derivative, inhibits HSV replication cycle at low cytotoxicity, blocks mitotic divisions of Vero cells, influences M-MSV induced tumor size and affects immune response by inhibiting PHA-induced T lymphocyte proliferation.
  • HY-N1022
    11-Hydroxytephrosin

    NF-κB Cancer Inflammation/Immunology
    11-Hydroxytephrosin is a potent inhibitor of NF-kappaB. NF-kappaB is known to play a crucial role in the regulation of genes controlling the immune system, apoptosis, tumor cell growth, and tissue differentiation.
  • HY-126856
    HC-Toxin

    HDAC Apoptosis Cancer
    HC-Toxin, a cyclic tetrapeptide, is a potent HDAC inhibitor with an IC50 of 30 nM. HC-Toxin induces tumor cell apoptosis and has anticancer effects.
  • HY-124944
    APS6-45

    Ras Cancer
    APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.
  • HY-117563
    CAY10621

    SKI 5C

    SphK Cancer
    CAY10621 (SKI 5C; compound 5c) is a specific sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 3.3 μM. CAY10621 is low toxic toward cells. CAY10621 has the potential for resistant cancer tumors research.
  • HY-N2584A
    Isoxanthohumol

    HSV Cancer Infection
    Isoxanthohumol is a prenylflavonoid from hops and beer. Isoxanthohumol exhibits an antiproliferative activity against several human cancer cell lines. Isoxanthohumol inhibits the development of lung metastatic foci in tumor-challenged animals. Isoxanthohumol shows an antiviral activity towards herpes viruses (HSV1 and HSV2) and bovine viral diarrhea virus (BVDV).
  • HY-144669
    ALDH1A3-IN-2

    Aldehyde Dehydrogenase (ALDH) Cancer
    ALDH1A3-IN-2 (Compound 15) is a potent inhibitor of ALDH1A3 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH1A3-IN-2 has the potential for the research of cancer diseases.
  • HY-144671
    ALDH3A1-IN-2

    Aldehyde Dehydrogenase (ALDH) Cancer
    ALDH3A1-IN-2 (Compound 19) is a potent inhibitor of ALDH3A1 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH3A1-IN-2 has the potential for the research of cancer diseases.
  • HY-146323
    Antitumor agent-58

    Apoptosis Cancer
    Antitumor agent-58 (Compound C18) is an anti-tumor agent. Antitumor agent-58 effectively inhibits colony formation and cell migration of MGC-803 cells. Antitumor agent-58 induces apoptosis of MGC-803 cells through activation of the p38 and JNK signaling pathways. Antitumor agent-58 induces mitochondrial dysfunction of MGC-803 cells. Antitumor agent-58 effectively inhibits tumor growth of xenograft model bearing MGC-803 cells.
  • HY-50895B
    Gefitinib dihydrochloride

    ZD 1839 dihydrochloride

    EGFR Autophagy Apoptosis Cancer
    Gefitinib (ZD 1839) dihydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib dihydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib dihydrochloride also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
  • HY-50895
    Gefitinib

    ZD1839

    EGFR Autophagy Apoptosis Cancer
    Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
  • HY-142533
    HL-PEG2k

    Others Cancer
    HL-PEG2k is a second near-infrared Ru(II) polypyridyl complex. HL-PEG2k exhibits a wavelength bathochromic shift, enhanced photothermal conversion efficiency (41.77%), and an antineoplastic effect against glioma. HL-PEG2k displays a superior biocompatibility and thus can be a potential theranostic platform to combat the growth and recurrence of tumors.
  • HY-16726
    Polmacoxib

    CG100649

    COX Carbonic Anhydrase Cancer
    Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory drug (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase. Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models.
  • 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-116217
    5-Fluoro-2'-deoxycytidine

    DNA Methyltransferase Cancer
    5-Fluoro-2'-deoxycytidine, a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective prodrug of the potent thymidylate synthase inhibitor 5-fluoro-2′-dUMP.
  • 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-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-132192
    PD-1/PD-L1-IN-9

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model.
  • HY-108417
    Debio 0617B

    STAT JAK Bcr-Abl Cancer
    Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34 + stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors.
  • HY-144070A
    (Rac)-ErSO-DFP

    Estrogen Receptor/ERR Cancer
    (Rac)-ErSO-DFP is a derivative of ErSO-DFP and a selective small molecule Erα biomodulator. (Rac)-ErSO-DFP againsts ERα+ breast cancer (including resistant tumors) by hyperactiving the Erα-dependent a-UPR (extracted from patent WO2022087234A1).
  • HY-133590
    Heliotrine N-oxide

    Others Cancer
    Heliotrine N-oxide is the corresponding PA (pyrrolizidine alkaloid) N-oxide of Heliotrine (HY-126128). Heliotrine N-oxide leads to the formation of pyrrolic DNA adducts and potential initiation of PA-induced liver tumors in vivo.
  • HY-108647
    EO 1428

    p38 MAPK Inflammation/Immunology
    EO 1428 is a highly specific inhibitor of p38 of the aminobenzophenone class. EO 1428 (1 μM ) markedly attenuates LPS-induced tumor necrosis factor α-converting enzyme (TACE) activity up-regulation.
  • HY-146540
    GEM-5

    HIF/HIF Prolyl-Hydroxylase Apoptosis MDM-2/p53 Cancer
    GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth.
  • HY-135899
    SIRT7 inhibitor 97491

    Sirtuin Apoptosis Cancer
    SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..
  • 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. MYLS22 can inhibit mitochondrial fusion and exacerbate the mitochondrial damage.
  • HY-N2420
    Flavokawain A

    Apoptosis Cancer
    Flavokawain A, a proming anticarcinogenic agent, is a chalcone from kava extract with anti-tumor activity. Flavokawain A induces cell apoptosis by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway. Flavokawain A has the potential for the study of bladder cancer.
  • HY-16405
    PR-104

    DNA Alkylator/Crosslinker Cancer
    PR-104 is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104, as a nitrogen mustard pre-prodrug, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A.
  • HY-16406
    PR-104 sodium

    DNA Alkylator/Crosslinker Cancer
    PR-104 (sodium) is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104 (sodium), as a nitrogen mustard pre-prodrug, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A.
  • HY-147696
    SMTIN-T140

    HSP AMPK Reactive Oxygen Species Cancer
    SMTIN-T140 (compound 6a) is a potent TRAP1 (tumor-necrosis-factor-receptor associated protein 1) inhibitor, with an IC50 of 1.646 μM. SMTIN-T140 shows anticancer activity. SMTIN-T140 leads to mitochondrial dysfunction, increases mitochondrial ROS production and activates AMPK. SMTIN-T140 potently suppressed tumor growth without any noticeable in vivo toxicity in a mouse model xenografted with PC3 prostate cancer cells.
  • HY-145441
    GEM–IB

    Others Cancer
    GEM–IB is the conjugate of gemcitabine (GEM)-5'-phosphate with ibandronate (IB). GEM–IB as a single agent or in combination with Docetaxel (DTX) demonstrates reduced tumor burden, preservation of the bone architecture, and improved the survival in a murine model of osteosarcoma (OS).
  • HY-119339
    SX-682

    CXCR Cancer Inflammation/Immunology Endocrinology
    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.
  • HY-115537
    NAE-IN-M22

    Apoptosis Cancer
    NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.
  • HY-P99115
    Envafolimab

    ASC 22; KN 035

    PD-1/PD-L1 Cancer
    Envafolimab (ASC 22; KN 035) is a recombinant protein of a humanized single-domain anti- PD-L1 antibody. Envafolimab is created by a fusion of the of anti-PD-L1 domain with Fc fragment of human IgG1 antibody. Envafolimab blocks interaction between PD-L1 and PD-1 with an IC50 value of 5.25 nm. Envafolimab shows antitumor activity. Envafolimab has the potential for the research of solid tumors.
  • HY-147413
    Unecritinib

    TQ-B3101

    EGFR Cancer
    Unecritinib (TQ-B3101) is a potent EGFR tyrosine kinase inhibitor. Unecritinib shows anticancer activity. Unecritinib inhibits ALK, ROS1, and MET. Unecritinib has the potential for the research of solid tumor and relapsed or refractory ALK-positive anaplastic large cell lymphoma.
  • HY-136220A
    AHR antagonist 5 hemimaleate

    Aryl Hydrocarbon Receptor Cancer
    AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC50 of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39).
  • HY-139180
    PRGL493

    Others Cancer
    PRGL493 is a potent and selective long-chain acyl-CoA synthetase 4 (ACSL4) inhibitor. PRGL493 blocks cell proliferation and tumor growth in both breast and prostate cellular and animal models. PRGL493 is used for cancer research.
  • HY-50896
    Erlotinib

    CP-358774; NSC 718781; OSI-774

    EGFR Autophagy Cancer
    Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer.
  • HY-142452
    Pan-RAF kinase inhibitor 1

    Others Cancer
    Pan-RAF kinase inhibitor 1 is a potent inhibitor of Pan-RAF kinase. Pan-RAF kinase inhibitor 1 regulates MAPK signaling by inhibiting RAF kinase, thereby exerting an effect on the proliferation of RAS-mutant tumor cells. Pan-RAF kinase inhibitor 1 has the potential for the research of cancer diseases (extracted from patent WO2021110141A1, compound 16B).
  • HY-136220
    AHR antagonist 5

    Aryl Hydrocarbon Receptor Cancer
    AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 µΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.
  • HY-101021
    Ascochlorin

    Ilicicolin D

    STAT Apoptosis Cancer Inflammation/Immunology
    Ascochlorin (Ilicicolin D), an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. Ascochlorin induces apoptosis. Anti-inflammatory activity.
  • HY-144670
    ALDH3A1-IN-1

    Aldehyde Dehydrogenase (ALDH) Cancer
    ALDH3A1-IN-1 (Compound 18) is a potent inhibitor of ALDH3A1 with an IC50 of 1.61 μM. ALDH3A1-IN-1 is more potent than DEAB against patient-derived primary prostate tumor epithelial cells, as single agents or in combination treatment with docetaxel.
  • HY-141464
    Fmoc-L-Asn(beta-D-GlcNAc(Ac)3)-OH

    Fmoc-Asn(Ac3AcNH-beta-Glc)-OH

    Others Cancer
    Fmoc-L-Asn(beta-D-GlcNAc(Ac)3)-OH (Fmoc-Asn(Ac3AcNH-beta-Glc)-OH) can be used in the synthesis of silicon-fluoride acceptor (SiFA) derivatized octreotate derivatives. SiFA-octreotate analogues, as tumor imaging agents, are useful tool for the research of positron emission tomography (PET).
  • HY-N3737
    Derrone

    Aurora Kinase ROS Kinase PERK Cancer
    Derrone, a prenylated isoflavones, is an Aurora kinase inhibitor, with IC50 values of 6 and 22.3 μM against Aurora B and Aurora A, respectively. Derrone shows anti-tumor activity.
  • HY-116804
    ZLD1039

    Histone Methyltransferase Cancer
    ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis.
  • HY-144256
    CHD1Li 6.11

    Others Cancer
    CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties.
  • HY-139662
    HB007

    E1/E2/E3 Enzyme Cancer
    HB007 is a small ubiquitin-related modifier 1 (SUMO1) degrader. HB007 induces ubiquitination and degradation of SUMO1, resulting in reduced tumor growth in vivo. HB007 can be used for the research of brain, breast, colon, and lung cancers.
  • HY-115581
    Thymidine 3',5'-disphosphate

    Deoxythymidine 3′,5′-diphosphate; pdTp

    Others Cancer
    Thymidine 3',5'-disphosphate (Deoxythymidine 3′,5′-diphosphate; pdTp) is a selective small molecule inhibitor of SND1 (the miRNA regulatory complex RISC subunit) and inhibits SND1 activity. Thymidine 3',5'-disphosphate is an anti-HCC agent and exhibits anti-tumor efficacy in vivo.
  • HY-18981
    Decursin

    (+)-Decursin

    PKC Apoptosis CXCR Cancer Inflammation/Immunology
    Decursin ((+)-Decursin) is a cytotoxic agent and a potent protein kinase C activator from the Root of Angelica gigas. Decursin inhibits tumor growth, migration, and invasion in gastric cancer by down-regulating CXCR7 expression. Decursin inhibits the growth of HepG2 cells via Hippo/YAP signaling pathway.
  • HY-135199
    Ubiquitination-IN-1

    E1/E2/E3 Enzyme Cancer
    Ubiquitination-IN-1 (compound 24) is a ubiquitination and Cksl-Skp2 protein-protein interaction (IC50=0.17 μM) inhibitor. Ubiquitination-IN-1 increases levels of p27. Ubiquitination-IN-1 has the potential for treatment disease by blocking the degradation of tumor suppressors.
  • HY-134471
    TNF-α-IN-2

    TNF Receptor Inflammation/Immunology
    TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis.
  • HY-100128
    DM1-SMe

    Microtubule/Tubulin ADC Cytotoxin Cancer
    DM1-SMe is an unconjugated form of the Maytansinoid in IMGN901. DM1-SMe is about 3-10-fold more potent than the parent drug Maytansine, with IC50s ranging from 0.003 to 0.01 nM for DM1-SMe in a panel of human tumor cell lines.
  • HY-P1022
    Kisspeptin-54(human)

    Metastin(human)

    GnRH Receptor Cancer Endocrinology
    Kisspeptin-54(human) (Metastin(human)) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) hinders tumor metastasis and stimulates gonadotropin secretion.
  • HY-143439
    LX-039

    Estrogen Receptor/ERR Cancer
    LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity.
  • HY-119696
    MTIC

    Drug Metabolite Cancer Neurological Disease
    MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the drug’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane.
  • HY-144746
    PD-1/PD-L1-IN-26

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-26 (Compound II-14) is a potent inhibitor of PD-1/PD-L1 with an IC50 of 0.0380 μM. PD-1/PD-L1-IN-26 activates the immune microenvironment by promoting the infiltration of CD4+ T cells into tumor tissues. PD-1/PD-L1-IN-26 has the potential for the research of cancer diseases.
  • HY-144749
    AKR1C3-IN-5

    Others Cancer
    AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells.
  • HY-139104
    Thailanstatin D

    DNA/RNA Synthesis Apoptosis Cancer
    Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3' splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis.
  • HY-145687
    HDAC-IN-32

    HDAC Cancer
    HDAC-IN-32 is a potent HDAC inhibitor with IC50s of 5.2, 11, and 28 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-32 possesses potent antiproliferation activities against tumor cells. HDAC-IN-32 shows potent antitumor efficacy in vivo That trigger antitumor immunity.
  • HY-145110
    IGF-1R inhibitor-2

    IGF-1R Cancer
    IGF-1R inhibitor-2 (example 121) is an insulin-like growth factor-1 receptor (IGF-1R) inhibitor. Downregulation of IGF-1R can reverse the transformed phenotype of tumor cells and potentially render them susceptible to apoptosis.
  • HY-145688
    HDAC-IN-33

    HDAC Cancer
    HDAC-IN-33 is a potent HDAC inhibitor with IC50s of 24, 46, and 47 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-33 possesses potent antiproliferation activities against tumor cells. HDAC-IN-33 shows potent antitumor efficacy in vivo That trigger antitumor immunity.
  • HY-131347
    PD-1/PD-L1-IN-NP19

    PD-1/PD-L1 Cancer Inflammation/Immunology
    PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects.
  • HY-13580
    Budesonide

    Glucocorticoid Receptor Cancer Inflammation/Immunology
    Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
  • HY-P1022A
    Kisspeptin-54(human) TFA

    Metastin(human) TFA

    GnRH Receptor Cancer Endocrinology
    Kisspeptin-54(human) TFA (Metastin(human) TFA) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) TFA binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) TFA hinders tumor metastasis and stimulates gonadotropin secretion.
  • HY-19827
    Aeroplysinin 1

    (+)-Aeroplysinin-1

    Bacterial HIV Apoptosis Cancer Infection
    Aeroplysinin 1 ((+)-Aeroplysinin-1), a secondary metabolite isolated from marine sponges, shows potent antibiotic effects on Gram-positive bacteria and exerts antiviral activity against HIV-1 (IC50=14.6 μM). Aeroplysinin 1 has anti-inflammatory, anti-angiogenic and anti-tumor activities. Aeroplysinin 1 induces apoptosis in endothelial cells.
  • HY-144424
    Trk-IN-11

    Trk Receptor Cancer
    Trk-IN-11 (Compound 14h) is a potent inhibitor of TRK (IC50 = 1.4, 1.8 nM, against TrkA, TrkA G595R, respectively). As a receptor tyrosine kinase (RTK), tropomyosin receptor kinase (Trk) is a key drug target in solid tumors. Trk-IN-11 has the potential for the research of cancer disease.
  • HY-144657
    PROTAC SOS1 degrader-2

    PROTACs Ras Cancer
    PROTAC SOS1 degrader-2 is a potent PROTAC SOS1 degrader. PROTAC SOS1 degrader-2 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. PROTAC SOS1 degrader-2 significantly inhibits the tumor growth in vivo.
  • HY-119711
    NNGH

    MMP Cancer
    NNGH is a stromelysin-1 (MMP-3) inhibitor. MMP-3 is both a direct transcriptional target and a necessary contributor of the Wnt/β-catenin signaling pathway. Matrix metalloproteinases (MMPs) play a well-defined role in later stages of tumor progression.
  • HY-108640
    HLI373

    MDM-2/p53 Parasite Apoptosis Cancer Infection
    HLI373 is an efficacious Hdm2 inhibitor. HLI373 inhibits the ubiquitin ligase activity of Hdm2. HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.
  • HY-108640A
    HLI373 dihydrochloride

    MDM-2/p53 Parasite Apoptosis Cancer Infection
    HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.
  • HY-15888
    PTC-209

    Autophagy Cancer
    PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment.
  • HY-144169
    DHODH-IN-19

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Cancer Inflammation/Immunology
    DHODH-IN-19 is a potent inhibitor of DHODH. DHODH is present in the inner membrane of human mitochondria and is an iron-containing flavin-dependent enzyme. DHODH-IN-19 inhibits tumor growth. DHODH-IN-19 has the potential for the research of cancer and inflammation disease (extracted from patent WO2021238881A1, compound 1).
  • HY-W039442
    2′-Deoxy-2′-fluoroadenosine

    Nucleoside Antimetabolite/Analog Cancer
    2′-Deoxy-2′-fluoroadenosine can be used for the synthesis of 2′-Deoxy-2′-fluoro-modified oligonucleotides hybridized with RNA. 2′-Deoxy-2′-fluoroadenosine can be cleaved efficiently by E. coli purine nucleoside phosphorylase (PNP) to the toxic agent 2-fluoroadenine (FAde). 2′-Deoxy-2′-fluoroadenosine shows excellent in vivo activity against tumors expressing E. coli PNP.
  • HY-138742
    HPK1-IN-7

    MAP4K Cancer
    HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1.
  • HY-144371
    DHODH-IN-20

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Cancer Inflammation/Immunology
    DHODH-IN-20 (Compound 133) is a potent inhibitor of DHODH. DHODH is present in the inner membrane of human mitochondria and is an iron-containing flavin-dependent enzyme. DHODH-IN-20 inhibits tumor growth. DHODH-IN-20 has the potential for the research of acute myelogenous leukemia.
  • HY-132229
    LPM4870108

    Trk Receptor Cancer
    LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC50s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkA G595R and TrkA G667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC50=182 nM). LPM4870108 exhibits anti-tumor activity.
  • HY-144638
    JMX0293

    Apoptosis Cancer
    JMX0293 is an O-alkylamino-tethered salicylamide derivative compound. JMX0293 maintains good potency against MDA-MB-231 cell line (IC50 = 3.38 μM) while exhibiting very low toxicity against human non-tumorigenic breast epithelial cell line MCF-10A (IC50> 60 μM). JMX0293 inhibits STAT3 phosphorylation and contribute to apoptosis in TNBC MDA-MB-231 cells. JMX0293 significantly suppresses MDA-MB-231 xenograft tumor growth in vivo without significant toxicity.
  • HY-144273
    IDO1-IN-13

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO1-IN-13 (compound 27a) is a potent IDO1 inhibitor with an IC50 of 61.6 nM. IDO1-IN-13 has cellular IDO1 inhibition (HeLa EC50= 30 nM). IDO1-IN-13 decreases 51% of the kyn/trp ratio in SK-OV-3 xenograft tumor tissues.
  • HY-146497
    Topoisomerase I inhibitor 7

    Topoisomerase Cancer
    Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants. Topoisomerase I inhibitor 7 indicates prospects for further search of new antitumor drug candidates among the heteroarene-fused anthraquinones.
  • HY-134595
    SENP1-IN-2

    E1/E2/E3 Enzyme Cancer
    SENP1-IN-2 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 30. SENP1-IN-2 is developed for tumor radiosensitivity enhancement.
  • HY-134594
    SENP1-IN-1

    E1/E2/E3 Enzyme Cancer
    SENP1-IN-1 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 29. SENP1-IN-1 is developed for tumor radiosensitivity enhancement.
  • HY-134597
    SENP1-IN-4

    E1/E2/E3 Enzyme Cancer
    SENP1-IN-4 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 21. SENP1-IN-4 is developed for tumor radiosensitivity enhancement.
  • HY-134596
    SENP1-IN-3

    E1/E2/E3 Enzyme Cancer
    SENP1-IN-3 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 17. SENP1-IN-3 is developed for tumor radiosensitivity enhancement.
  • HY-147783
    Anticancer agent 68

    MDM-2/p53 Cancer
    Anticancer agent 68 is (Compound 12) is an anti-cancer agent. Anticancer agent 68 arrests the cells at the G2/M phase and induces programmed cell death. Anticancer agent 68 induces upregulation of tumor suppression via activation of p53 & PTEN.
  • HY-B0091A
    Adapalene sodium salt

    CD 271 sodium salt

    RAR/RXR Autophagy Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity.
  • HY-B0091
    Adapalene

    CD271

    RAR/RXR Autophagy Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity.
  • HY-124813
    PDZ1i

    113B7

    FAK EGFR MMP Cancer
    PDZ1i is a potent, BBB-penetrated and specific MDA-9/Syntenin inhibitor. PDZ1i inhibits crucial GBM (glioblastoma multiforme) signaling involving FAK and EGFRvIII. PDZ1i reduces MMP secretion. PDZ1i can improve survival of brain tumor-bearing mice and reduce tumor invasion.
  • HY-115400
    1V209

    TLR7 agonist T7

    Toll-like Receptor (TLR) Cancer
    1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity.
  • HY-103397
    Nanaomycin A

    DNA Methyltransferase Parasite Cancer Infection
    Nanaomycin A is the first selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells. Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM.
  • HY-147753S
    CXCR4 probe 1

    CXCR Cancer Inflammation/Immunology
    CXCR4 probe 1 (compound 5) is a potent and specific CXCR4-targeted PET tracer with an IC50 value of 6.9 nM against CXCR4-specific antagonist peptide, TN14003. CXCR4 probe 1 has potential to be used as CXCR4-specific imaging probe to diagnose and monitor the prognosis of inflammatory diseases, CXCR4-positive tumors, and metastatic cancers.
  • HY-15888A
    PTC-209 hydrobromide

    Autophagy Cancer
    PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment.
  • HY-146384
    CRM1 degrader 1

    CRM1 Cancer
    CRM1 degrader 1 (1l) is a low toxic chromosome region maintenance 1 (CRM1) degrader. CRM1 is the sole nuclear exporter of several tumor suppressor, a growth regulatory protein as an attractive cancer drug target. CRM1 degrader 1 induces the apoptosis in gastric carcinoma and selectively inhibits proliferation of gastric cancer.
  • HY-114357A
    DS-1205b free base

    TAM Receptor c-Met/HGFR Trk Receptor Cancer
    DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo.
  • HY-116683
    116-9e

    MAL2-11B

    HSP DNA/RNA Synthesis Cancer Infection
    116-9e (MAL2-11B) is a Hsp70 co-chaperone DNAJA1 inhibitor. 116-9e inhibits Simian Virus 40 (SV40) replication and DNA synthesis. 116-9e inhibits tumor antigen (TAg)’s endogenous ATPase activity and the TAg-mediated activation of Hsp70.
  • HY-101870B
    Uzansertib phosphate

    INCB053914 phosphate

    Pim Cancer
    Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.
  • HY-101870
    Uzansertib

    INCB053914

    Pim Cancer
    Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines.
  • HY-101597
    NVX-207

    Apoptosis Cancer
    NVX-207, a Betulinic acid-derived anti-cancer compound, shows anti-tumor activity (mean IC50=3.5 μM) against various human and canine cell lines. NVX-207-induced apoptosis is associated with activation of the intrinsic apoptotic pathway via cleavage of caspases -9, -3, -7 and of PARP.
  • HY-144036
    DNA-PK-IN-3

    DNA-PK Cancer
    DNA-PK-IN-3 is a potent inhibitor of DNA-PK. DNA-PK-IN-3 synergistically enhances the effect of radiotherapy and chemotherapy and effectively inhibits tumor growth. DNA-PK-IN-3 also effectively reduces the damage to normal cells and reducing side effects. DNA-PK-IN-3 has the potential for the research of cancer disease (extracted from patent WO2021213460A1, compound 4).
  • HY-142683
    SCP1-IN-2

    Others Cancer Neurological Disease
    SCP1-IN-2 (Compound SH T-65) is a potent and selective covalent inhibitor against SCP1. SCP1-IN-2 promotes REST degradation and reduces transcriptional activity. A high level of REST protein drives the tumor growth in some glioblastoma cells. SCP1-IN-2 has the potential for the research of glioblastoma whose growth is driven by REST transcription activity.
  • HY-142682
    SCP1-IN-1

    Others Cancer Neurological Disease
    SCP1-IN-1 (compound SH T-62) is a potent and selective covalent inhibitor against SCP1. SCP1-IN-1 promotes REST degradation and reduces transcriptional activity. A high level of REST protein drives the tumor growth in some glioblastoma cells. SCP1-IN-1 has the potential for the research of glioblastoma whose growth is driven by REST transcription activity.
  • HY-12168
    Tanomastat

    BAY 12-9566

    MMP Cancer
    Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models.
  • HY-122181A
    OTS186935 trihydrochloride

    Histone Methyltransferase Cancer
    OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells.
  • HY-14389
    LP-261

    Microtubule/Tubulin Cancer
    LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM. LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research.
  • HY-139874
    CXCR2 antagonist 3

    CXCR Cancer Inflammation/Immunology
    CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3 + T lymphocytes into the Pan02 tumor tissues.
  • HY-12624
    ON123300

    CDK AMPK Cancer
    ON123300, a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent ON123300 causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors. ON123300 inhibits CDK6 with an IC50 of 9.82 nM.
  • HY-133016
    M8891

    Others Cancer Cardiovascular Disease
    M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM). M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity.
  • HY-144423
    Trk-IN-10

    Trk Receptor Cancer
    Trk-IN-10 (Compound 14j) is a potent inhibitor of TRK (IC50 = 0.86, 6.92 nM, against TrkA, TrkA G595R, respectively). As a receptor tyrosine kinase (RTK), tropomyosin receptor kinase (Trk) is a key drug target in solid tumors. Trk-IN-10 (IC50 = 350 nM against ALK) has a higher selectivity of Trk inhibition, which may be of great significance for reducing toxicity.
  • HY-134813
    MRTX1133

    Ras Cancer
    MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations.
  • HY-12168B
    (Rac)-Tanomastat

    (Rac)-BAY 12-9566

    MMP Cancer
    (Rac)-Tanomastat ((Rac)-BAY 12-9566) is the racemate of Tanomastat. Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models.
  • HY-147915
    Benz-AP

    ROS Kinase Cancer
    Benz-AP is a potent photosensitizer. Benz-AP produces singlet oxygen, with a negative correlation with hCES2 (Human carboxylesterase 2) activity. Benz-AP displays a higher photocytotoxicity potency in cancer cells under low hCES2 environments. Upon TPE (Two-photon excitation), Benz-AP produces ROS and kills cancer cells and tumor spheroids.
  • HY-143321
    STING agonist-13

    STING Cancer
    STING agonist-13 is a stimulator of interferon genes (STING) agonist, for cancer immunity via STING-mediated immune activation. STING agonist-13 can stimulate STING downstream signaling and promoting type I interferon immune responses. STING agonist-13 significantly decreases tumor volume and shows immunological memory-derived cancer inhibition.
  • HY-121524
    DJ101

    Microtubule/Tubulin Cancer
    DJ101 is a potent and metabolically stable tubulin inhibitor. DJ101 targets the colchicine binding site and overcomes taxane resistance. DJ101 also inhibits melanoma tumor growth and lung metastasis. DJ101 can be used for prostate cancer research.
  • HY-P3448
    Certepetide

    CEND-1; iRGD

    Integrin Complement System Cancer
    Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary drug conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors.
  • HY-144707
    AK-778-XXMU

    Apoptosis Cancer
    AK-778-XXMU is a potent inhibitor of DNA Binding 2 (ID2) antagonist with a KD of 129 nM. AK-778-XXMU can inhibit cell migration and invasion of glioma cell lines, induce apoptosis, and more importantly, slow down the tumor growth.
  • HY-136244
    PF-06952229

    TGF-β Receptor Cancer
    PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction. PF-06952229 is a promising antineoplastic agent for the study solid tumors, especifically metastatic breast cancer.
  • HY-10252
    NVP-ADW742

    ADW742; GSK 552602A; ADW

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.
  • HY-103190
    MRS1220

    Adenosine Receptor Cancer Neurological Disease
    MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo.
  • HY-110243
    CAIX Inhibitor S4

    Carbonic Anhydrase Cancer
    CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth.
  • HY-105129
    Pimonidazole hydrochloride

    Others Cancer
    Pimonidazole is a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in tumor. Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group, it can be used for qualitative and quantitative assessment of tumor hypoxia .
  • HY-105129A
    Pimonidazole

    Others Cancer
    Pimonidazole is a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in tumor. Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group, it can be used for qualitative and quantitative assessment of tumor hypoxia .
  • HY-145428
    BT-GSI

    Notch γ-secretase Cancer
    BT-GSI is a γ-secretase inhibitor (GSI) and a bone-targeted Notch inhibitor. BT-GSI has dual anti-myeloma and anti-resorptive properties, which can be used for the research of multiple myeloma and associated bone disease. BT-GSI inhibits tumor growth and osteolytic disease progression.
  • HY-124179
    IT-901

    NF-κB Cancer
    IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 µM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD).
  • HY-124675
    MYCMI-6

    NSC354961

    c-Myc Apoptosis Cancer
    MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis.
  • HY-143881
    FGFR4-IN-6

    FGFR Cancer
    FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity.
  • HY-146215
    IDO1-IN-20

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    Hy-146215 is an enzyme that catalyzes the oxidative metabolism of tryptophan. It can immunosuppress tumors in the tumor microenvironment.
  • HY-120793
    CMC2.24

    TRB-N0224

    Ras Apoptosis MMP Cancer Inflammation/Immunology
    CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis.
  • HY-101849
    Fasentin

    GLUT Cancer Cardiovascular Disease
    Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity.
  • HY-145769
    N2S2-CBMBC

    PD-1/PD-L1 Cancer
    N2S2-CBMBC, an N2S2 bromo-benzyl ether derivative, acts as a ligand and use 99mTc-labelled complexes 99mTc-N2S2-CBMBC can be used as an imaging agent to be applied to the aspect of detecting PD-L1 expression, realize the real-time, comprehensive and convenient detection of the PD-L1 level of tumors, and overcome the defects of an immunohistochemical method.
  • HY-111786
    LHC-165

    Toll-like Receptor (TLR) Cancer
    LHC-165 is a TLR7 agonist. Has potential to treat solid tumors.
  • HY-A0096
    Iloprost

    Ciloprost; ZK 36374

    Prostaglandin Receptor Endogenous Metabolite Endocrinology Cancer
    Iloprost (ZK 36374; Ciloprost) is a prostacyclin (PGI2) analogue, involves in embryo development and inflammation improvement, and inhibits tumor metastasis. Iloprost can be used for peripheral vascular research.
  • HY-124711
    TBOPP

    Others Cancer
    TBOPP is a selective inhibitor of DOCK1 with an IC50 of 8.4 μM. TBOPP binds to the DOCK1 DHR-2 domain with high affinity (Kd of 7.1 μM), has anti-tumor activity for broader types of tumors.
  • 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-142949
    ALK5-IN-7

    ALK Cancer Inflammation/Immunology
    ALK5-IN-7 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-7 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 4).
  • HY-142950
    ALK5-IN-6

    ALK Cancer Inflammation/Immunology
    ALK5-IN-6 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-6 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 1).
  • HY-135748
    Polyinosinic-polycytidylic acid sodium

    Poly(I:C) sodium

    Toll-like Receptor (TLR) Apoptosis Cancer Inflammation/Immunology
    Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis.
  • HY-N0438
    Pimpinellin

    Apoptosis Cancer
    Pimpinellin is a constituent of Cyrtomium fortumei (J.). Pimpinellin inhibits the growth of tumor cells via the induction of tumor cell apoptosis.
  • HY-N0211
    Cyasterone

    EGFR Apoptosis Cancer
    Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors.
  • HY-11080A
    PKI-179 hydrochloride

    PI3K mTOR Cancer
    PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo.
  • HY-11080
    PKI-179

    PI3K mTOR Cancer
    PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo.
  • 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-17419S1
    Ifosfamide-d4

    DNA Alkylator/Crosslinker Cancer
    Ifosfamide-d4 is the deuterium labeled Ifosfamide. Ifosfamide is an alkylating chemotherapeutic agent with activity against a wide range of tumors.
  • HY-143407
    FAK-IN-3

    FAK Cancer
    FAK-IN-3 (Compound 36) is a potent inhibitor of focal adhesion kinase (FAK). FAK-IN-3 not only decreases migration and invasion of PA-1 cells, but also reduces expression of MMP-2 and MMP-9. FAK-IN-3 inhibits tumor growth and metastasis, and no obvious adverse effects. FAK-IN-3 has the potential for the research of ovarian cancer.
  • HY-145102
    NCT-58

    HSP Apoptosis Cancer
    NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells.
  • HY-116624
    MAZ51

    VEGFR Apoptosis Cancer
    MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity.
  • HY-12564
    Phthalazinone pyrazole

    Aurora Kinase Cancer
    Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells.
  • HY-U00337A
    Datelliptium chloride hydrochloride

    DNA/RNA Synthesis Cancer
    Datelliptium chloride hydrochloride is a DNA-intercalating agent derived from Ellipticine (HY-15753). Datelliptium chloride hydrochloride is effective in vivo against a variety of murine solid tumors.
  • HY-137573
    Trotabresib

    CC-90010

    Epigenetic Reader Domain Cancer
    CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors.
  • HY-17419S
    2’-Oxo Ifosfamide-d4

    DNA Alkylator/Crosslinker Cancer
    2’-Oxo Ifosfamide-d4 is the deuterium labeled Ifosfamide. Ifosfamide is an alkylating chemotherapeutic agent with activity against a wide range of tumors.
  • HY-13582
    Carbendazim

    Fungal Infection Cancer
    Carbendazim is a potent and orally active broad-spectrum benzimidazole fungicide and can be acts as a pesticide for fungal diseases research, such as SeproriaFusarium and Sclerotina. Carbendazim is a benzimidazole (HY-Y1825) derivative with antitumor activity and used for cancer research, especially advanced solid tumors and lymphoma.
  • HY-143402
    Topoisomerase I/II inhibitor 2

    Topoisomerase Cancer
    Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in treating liver cancer.
  • HY-126730
    Rubratoxin A

    Phosphatase Cancer
    Rubratoxin A is a natural mycotoxin and competitive inhibitor of protein phosphatase 2A (PP2A) with an IC50 of 170 nM. Rubratoxin A causes suppression of tumor metastasis and reduction of primary tumor volume in mouse xenografts.
  • HY-114306
    EC0489

    Antifolate Cancer
    EC0489, a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (FR). Refractory or metastatic Tumor. Small molecule-drug conjugate (SMDC).
  • HY-Y0520
    Itaconic acid

    Endogenous Metabolite Inflammation/Immunology
    Itaconic acid, a precursor of polymers, chemicals, and fuels, can be synthesized by many fungi. Itaconic acid also is a macrophage-specific metabolite. Itaconic acid mediates crosstalk between macrophage metabolism and peritoneal tumors.
  • HY-115760
    Okadaic acid ammonium salt

    Phosphatase Cancer Neurological Disease
    Okadaic acid ammonium salt, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid ammonium salt has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid ammonium salt increases of phosphorylation of a number of proteins by inhibiting PP, and acts as a tumor promoter. Okadaic acid ammonium salt induces tau phosphorylation.
  • HY-123673
    MCP110

    Ras Raf Cancer
    MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 blocks the interaction of Ras with Raf. MCP110 disrupts this interaction might can be used for the research of human tumors.
  • HY-121087
    BCI-215

    Phosphatase Cancer
    BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells.
  • HY-146307
    TrxR-IN-3

    Others Cancer
    TrxR-IN-3 (Compound 2c) is a potent inhibitor of TrxR. TrxR-IN-3 exhibits potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. TrxR-IN-3 increases ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. TrxR-IN-3 also triggers the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins.
  • HY-130612
    PROTAC BRD2/BRD4 degrader-1

    Epigenetic Reader Domain PROTACs Cancer
    PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A.
  • HY-107271
    Imperialine 3-β-D-glucoside

    Others Cancer
    Imperialine 3-β-D-glucoside is the glycoside of Imperialine. Imperialine 3-β-D-glucoside may exhibit anti-tumor properties against multi-drug resistant tumor cells.
  • HY-116399
    MMP-2/MMP-9-IN-1

    MMP Cancer
    MMP-2/MMP-9-IN-1 is a highly selective, orally active and potent type IV collagenase (MMP-9 and MMP-2) inhibitor with IC50s of 0.24 and 0.31 μM for MMP-9 and MMP-2, respectively. MMP-2/MMP-9-IN-1 is orally active in animal models of tumor growth and metastasis. MMP-2/MMP-9-IN-1 can be used for the research of cancer.
  • HY-144099
    Keap1-Nrf2-IN-4

    E1/E2/E3 Enzyme Apoptosis Cancer
    Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC50=2.55 µM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity.
  • 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-12628
    GNE-618

    NAMPT Cancer
    GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity.
  • HY-144188
    PRMT5-IN-17

    Histone Methyltransferase Cancer
    PRMT5-IN-17 (Compound 6) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification.
  • HY-144187
    PRMT5-IN-16

    Histone Methyltransferase Cancer
    PRMT5-IN-16 (Compound 20) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification.
  • HY-141687
    NSC 107512

    CDK Cancer
    NSC 107512 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9). NSC 107512 is a class of sangivamycin-like molecules (SLM). NSC 107512 inhibits growth and induces apoptosis of multiple myeloma tumors.
  • HY-134463
    NHWD-870

    Epigenetic Reader Domain Apoptosis Cancer
    NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation.
  • HY-13598
    Valecobulin

    CKD-516

    Microtubule/Tubulin Cancer
    Valecobulin (CKD516) is a valine prodrug of (S516) and a vascular disrupting agent (VDA). Valecobulin is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
  • HY-N8430
    Poricoic acid AM

    Others Cancer
    Poricoic acid AM is a triterpenoid with ant-tumor activities.
  • HY-12797
    GF 15

    Others Cancer
    GF 15 is a potent inhibitor of centrosomal clustering in tumor cells.
  • HY-124284
    Hexamethylene bisacetamide

    HMBA

    Others Cancer
    Hexamethylene bisacetamide is a tumor cell-differentiating agent.
  • HY-145729
    Danvatirsen

    AZD 9150

    STAT Cancer
    Danvatirsen is an antisense oligonucleotide targeting STAT3 with potential antitumor activity. Danvatirsen binds to STAT3 mRNA, thereby inhibiting translation of the transcript. Suppression of STAT3 expression induces tumor cell apoptosis and decreases tumor cell growth.
  • HY-145925B
    CFT8634

    Epigenetic Reader Domain Cancer
    CFT8634 is a degrader targeting BRD9 extracted from patent WO2021178920A1 compound 173. CFT8634 can be used for the research of synovial sarcoma and SMARCB1-deleted solid tumors.
  • HY-19319
    MI-136

    Epigenetic Reader Domain Androgen Receptor Apoptosis Cancer
    MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors.
  • HY-147682
    NF-κB-IN-5

    NF-κB Apoptosis Cancer
    NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase.
  • HY-16938
    5'-Methylthioadenosine

    5'-(Methylthio)-5'-deoxyadenosine; 5'-Deoxy-5'-(methylthio)adenosine; 5'-S-Methyl-5'-thioadenosine

    Endogenous Metabolite Apoptosis Cancer Metabolic Disease
    5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis.
  • HY-119823
    PGP-4008

    P-glycoprotein Cancer
    PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple drug resistance (MDR) solid tumor model when given in combination with Doxorubicin.
  • HY-N0156
    Oleanolic Acid

    Oleanic acid; Caryophyllin

    Autophagy Endogenous Metabolite HIV Cancer
    Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities.
  • HY-17419
    Ifosfamide

    DNA Alkylator/Crosslinker Cancer
    Ifosfamide is an alkylating chemotherapeutic agent with activity against a wide range of tumors.
  • HY-136173
    TNO155

    Phosphatase Cancer
    TNO155 is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). TNO155 has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors.
  • HY-D0067
    7ACC1

    DEAC; Coumarin D 1421; D 1421

    Monocarboxylate Transporter Cancer
    7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
  • HY-16475
    TAK-441

    Hedgehog Cancer
    TAK-441 (compound 11d) is a highly potent and oral hedgehog (Hh) signaling inhibitor with an IC50value of 4.4 nM. TAK-441 (compound 11d) has strong antitumor activity in solid tumors.
  • HY-128766
    CHK1-IN-4

    Checkpoint Kinase (Chk) Cancer
    CHK1-IN-4 (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 has anti-tumor activity.
  • HY-146358
    Anticancer agent 49

    Microtubule/Tubulin Cancer
    Anticancer agent 49 (compound 69) is a broad spectrum anticancer agent. Anticancer agent 49 inhibits tubulin polymerization. Anticancer agent 49 shows antiproliferative activity. Anticancer agent 49 has the potential for the research of solid and hematological tumors.
  • HY-13598A
    Valecobulin hydrochloride

    CKD-516 hydrochloride

    Microtubule/Tubulin Cancer
    Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine prodrug of S516 (HY-130233) and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
  • HY-106381
    Aurothiomalate sodium

    PKC Cancer Inflammation/Immunology
    Aurothiomalate sodium is a potent and selective oncogenic PKCι signaling inhibitor. Aurothiomalate sodium inhibits tumor cell proliferation and not cell apoptosis. Aurothiomalate sodium is a potent thioredoxin reductase (TrxR) inhibitor. Aurothiomalate sodium, an anti-rheumatoid agent, exhibits potent anti-tumor activity.
  • HY-P1860
    TNF-α (31-45), human

    Others Inflammation/Immunology
    TNF-α (31-45), human is a peptide of tumor necrosis factor-α.
  • HY-15721
    FH535

    PPAR Wnt β-catenin Cancer
    FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities.
  • HY-16509
    UNBS5162

    CXCR Autophagy Cancer Endocrinology
    UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.
  • HY-128973
    Pyropheophorbide-a

    Others Cancer
    Pyropheophorbide-a (Ppa) is a promising photosensitizer for tumor photodynamic therapy (PDT).
  • HY-U00337
    Datelliptium chloride

    DNA/RNA Synthesis Cancer
    Datelliptium chloride is a DNA-intercalating agent derived from ellipticine, with anti-tumor activities.
  • HY-147991
    PDE5/HDAC-IN-1

    Phosphodiesterase (PDE) HDAC Apoptosis Cancer
    PDE5/HDAC-IN-1 (Compound 26) is a potent phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC50 values of 46.3 nM and 14.5 nM, respectively. PDE5/HDAC-IN-1 induces cell apoptosis and shows anticancer activities.
  • HY-130625
    PD-1/PD-L1-IN 6

    PD-1/PD-L1 Cancer Inflammation/Immunology
    PD-1/PD-L1-IN 6 (compound A13) is a potent PD-1/PD-L1 interaction inhibitor, with an IC50 of 132.8 nM. PD-1/PD-L1-IN 6 exhibits outstanding immunoregulatory activity. PD-1/PD-L1-IN 6 significantly elevates interferon-γ secretion in a Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model, without significant toxic effect. PD-1/PD-L1-IN 6 restores the immune response in a T cell-tumor co-culture model.
  • HY-131246
    DM-01

    Histone Methyltransferase Cancer
    DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors.
  • HY-144125
    Antitumor agent-41

    Apoptosis Cancer
    Antitumor agent-41 (compound N-12), a potent antitumor agent, enhibits excellent antimigration and anti-invasion activity. Antitumor agent-41 (compound N-12) induces tumor inhibition via tumor necrosis and inflammatory response.
  • HY-112802A
    AZD3229 Tosylate

    c-Kit Cancer
    AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
  • HY-10249A
    AKT Kinase Inhibitor

    Akt Cancer
    AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity.
  • HY-N0235
    Bakuchiol

    (S)-(+)-Bakuchiol

    p38 MAPK Autophagy Cancer
    Bakuchiol is a phytoestrogen isolated from the seeds of Psoralea corylifolia L; has anti-tumor effects.
  • HY-N1977
    Podophyllotoxin glucoside

    Others Cancer
    Podophyllotoxin glucoside is a podophyllotoxin derivative, has anti-tumor effects.
  • HY-112802
    AZD3229

    c-Kit Cancer
    AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
  • HY-B0172
    Lithocholic acid

    3α-Hydroxy-5β-cholanic acid

    Autophagy Endogenous Metabolite Apoptosis Metabolic Disease
    Lithocholic acid is a toxic secondary bile acid, causes intrahepatic cholestasis, has tumor-promoting activity.
  • HY-16114
    BNC105

    Microtubule/Tubulin Cancer
    BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
  • HY-113450
    10Z-Nonadecenoic acid

    Endogenous Metabolite Metabolic Disease Cancer
    10Z-Nonadecenoic acid is a kind of long-chain fatty acid with anti-tumor activity.
  • HY-15701B
    ADH-503

    (Z)-Leukadherin-1 choline

    Complement System Cancer
    ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allosteric CD11b agonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
  • HY-120046
    YF479

    HDAC Cancer
    YF479 is a potent inhibitor of histone deacetylase. YF479 abates cell viability, suppresses colony formation and tumor cell motility. YF479 significantly inhibits breast tumor growth and metastasis. YF479 has the potential for the research of clinical trials for breast cancer.
  • HY-118672
    HNHA

    HDAC MMP HIF/HIF Prolyl-Hydroxylase Cancer
    HNHA is a potent histone deacetylase (HDAC) inhibitor. HNHA arrests the cell cycle at the G1/S phase via p21 induction. HNHA inhibits tumor growth and tumor neovascularization. HNHA may be a potent anti-cancer agent against breast cancer.
  • HY-Y0520S
    Itaconic acid-13C5

    Endogenous Metabolite Inflammation/Immunology
    Itaconic acid-13C5 is the 13C labeled Itaconic acid. Itaconic acid, a precursor of polymers, chemicals, and fuels, can be synthesized by many fungi. Itaconic acid also is a macrophage-specific metabolite. Itaconic acid mediates crosstalk between macrophage metabolism and peritoneal tumors.
  • HY-147204
    Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE

    Others Cancer
    Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE (compound S6) is a potent anticancer agent, which can be specific activated by tumor microenvironment. Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE can suppress tumor growth in mice (extracted from patent CN104147612A).
  • HY-14947
    Balamapimod

    MKI 833

    MEK Cancer
    Balamapimod (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity.
  • HY-16496
    Thiarabine

    OSI-7836

    DNA/RNA Synthesis Cancer Inflammation/Immunology
    Thiarabine (OSI-7836) shows potent anti-tumor activity and inhibition of DNA synthesis.
  • HY-147081
    AS 1411

    AGRO-100

    Others Cancer
    AS1411 is a quadruplex-forming oligonucleotide aptamer that targets nucleolin. It has anti-tumor activity.
  • HY-139858
    TGFβR-IN-1

    TGF-β Receptor Cancer
    TGFβR-IN-1 is a long-acting tumor-activated prodrug of a TGFβR inhibitor.
  • HY-N10353
    4-Methyl withaferin A

    Others Cancer Inflammation/Immunology
    4-Methyl withaferin A is a withaferin A-analogue with anti-tumor activity.
  • HY-N8197
    Epigambogic acid

    Others Cancer
    Epigambogic acid is a natural anti-tumor, antitussive, expectorant and anti-inflammatory compound.
  • HY-U00379
    LM985

    Others Cancer
    LM985 is one of a series of compounds based on the flavone ring structure, with anti-tumor activities.
  • HY-16271
    Kevetrin hydrochloride

    4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride

    MDM-2/p53 Cancer
    Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
  • HY-13727A
    Pixantrone

    BBR 2778

    Topoisomerase Cancer
    Pixantrone (BBR 2778) dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
  • HY-N4124
    Poricoic acid B

    Others Cancer
    Poricoic acid B, isolated from Poria cocos, possesses anti-tumor activity.
  • HY-N9400
    Lucidenic acid F

    Others Cancer Inflammation/Immunology
    Lucidenic acid F, a natural triterpenoid, possesses anti-Inflammatory and anti-tumor activity.
  • HY-N0837
    Veratramine

    NSC17821; NSC23880

    Others Cancer
    Veratramine(NSC17821; NSC23880) is useful as a signal transduction inhibitor for treating tumors.
  • HY-N0517
    Erianin

    Bacterial Cancer Neurological Disease
    Erianin, often used as an antipyretic and analgesic agent, could inhibit IDO-induced tumor angiogenesis.
  • HY-108986
    JFD00244

    Sirtuin Cancer
    JFD00244 is a sirtuin 2 (SIRT2) inhibitor. Anti-tumor effect.
  • HY-N6988
    Cimigenol

    Others Cancer
    Cimigenol is an active compound isolated from Cimicifuga, with potent anti-tumor activity.
  • HY-N10447
    Kurzipene D

    Apoptosis Cancer
    Kurzipene D (compound 4) is a potent anticancer agent. Kurzipene D induces the apoptosis and arrested the HepG2 cell cycle at S stage. Kurzipene D shows anti-tumor effects using in vivo zebrafish model. Kurzipene D has the property of inhibiting tumor proliferation and migration.
  • HY-N10355
    27-TBDMS-4-Dehydrowithaferin A

    Apoptosis Cancer
    27-TBDMS-4-Dehydrowithaferin A, a withaferin A derivative, exhibits potent antiproliferative effects on the tumor cells.27-TBDMS-4-Dehydrowithaferin A induces tumor cells apoptosis. 27-TBDMS-4-Dehydrowithaferin A is a anticancer agent.
  • HY-15701A
    (Z)-Leukadherin-1

    ADH-503 free base

    Complement System Cancer
    (Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
  • HY-N0462
    Corilagin

    Reverse Transcriptase Bacterial Cancer Infection Inflammation/Immunology
    Corilagin, a gallotannin, inhibits activity of reverse transcriptase of RNA tumor viruses. Corilagin inhibits the growth of Staphylococcus aureus with a MIC of 25 μg/mL. Corilagin shows good anti-tumor activity on hepatocellular carcinoma and ovarian cancer. Corilagin shows a low level of toxicity toward normal cells and tissues.
  • HY-11005
    BX-912

    PDK-1 Apoptosis Cancer
    BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis.
  • HY-146357
    Anticancer agent 48

    Microtubule/Tubulin Cancer
    Anticancer agent 48 (compound 48) is a broad spectrum anticancer agent. Anticancer agent 48 inhibits tubulin polymerization. Anticancer agent 48 shows antiproliferative activity. Anticancer agent 48 shows antitumor activity in vivo. Anticancer agent 48 has the potential for the research of solid and hematological tumors.
  • HY-100693
    SYP-5

    HIF/HIF Prolyl-Hydroxylase Cancer
    SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.
  • HY-16503
    Treosulfan

    NSC 39069; Treosulphan

    DNA Alkylator/Crosslinker Cancer
    Treosulfan (NSC 39069) is a bifunctional alkylating agent with activity in ovarian cancer and other solid tumor types.
  • HY-N0184
    Glycyrrhizic acid

    Glycyrrhizin

    Virus Protease Cancer Metabolic Disease
    Glycyrrhizic acid is a triterpenoid saponinl, acting as a direct HMGB1 antagonist, with anti-tumor, anti-diabetic activities.
  • HY-N2596
    Isoscabertopin

    Others Cancer Inflammation/Immunology
    Isoscabertopin is a sesquiterpene lactone isolated from Elephantopus scaber L and shows anti-tumor activities.
  • HY-128937
    EC1454

    Others Cancer
    EC1454 is an anti-tumor compound, extracted from US20170348376A1.
  • HY-B1436
    Nifuroxazide

    STAT Bacterial Cancer Infection
    Nifuroxazide is an effective inhibitor of STAT3, also exerts potent anti-tumor and anti-metastasis activity.
  • HY-13742
    Ropidoxuridine

    IPdR

    Others Cancer
    Ropidoxuridine (IPdR) is a novel orally available, halogenated thymidine analog and is a potential radiosensitizer for use in human tumors.
  • HY-N9390
    Wilforlide B

    Others Cancer
    Wilforlide B, a natural norditerpenoid, possesses anti-tumor activity in human cancer cells.
  • HY-16212
    FR901464

    Others Cancer
    FR901464 is a potent spliceosome inhibitor with prominent anti-tumor and anti-cancer effects.
  • HY-142965
    HDAC-IN-28

    HDAC Cancer
    HDAC-IN-28, a novel HDAC inhibitor, shows potent activities against tumor growth and metastasis
  • HY-104044
    Pamiparib

    BGB-290

    PARP Cancer
    Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor.
  • HY-N2306A
    Aclacinomycin A hydrochloride

    Aclarubicin hydrochloride

    Proteasome Topoisomerase Cancer
    Aclacinomycin A hydrochloride (Aclarubicin hydrochloride), a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II. An effective anthracycline chemotherapeutic agent for hematologic cancers and solid tumors.
  • HY-136979
    RBN012759

    PARP Cancer Inflammation/Immunology
    RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants.
  • HY-50895A
    Gefitinib hydrochloride

    ZD-1839 hydrochloride

    EGFR Cancer
    Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity.
  • HY-143510
    RMC-4627

    mTOR Cancer
    RMC-4627 is a selective mTORC1 inhibitor that activates 4EBP1 and inhibits tumor growth.
  • HY-145938
    OncoFAP

    Others Cancer
    OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential.
  • HY-N0370
    Bergapten

    5-Methoxypsoralen

    Cytochrome P450 Autophagy Cancer
    Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
  • HY-10964
    Vadimezan

    DMXAA; ASA-404

    STING IFNAR Influenza Virus Cancer Infection
    Vadimezan (DMXAA; ASA-404), the tumor vascular disrupting agent (tumor-VDA), is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines. Vadimezan has anti-influenza virus H1N1-PR8 activities.
  • HY-10330
    Toceranib

    SU11654; PHA 291639E

    PDGFR VEGFR c-Kit Cancer
    Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.
  • HY-145835
    PERK-IN-5

    PERK Cancer
    PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model.
  • HY-128910
    MC-VC(S)-PABQ-Tubulysin M

    Drug-Linker Conjugates for ADC Cancer
    MC-VC(S)-PABQ-Tubulysin M is a drug-linker conjugate for ADC with potent antitumor activity by using Tubulysin M (a tubulin inhibitor), linked via the ADC linker MC-VC(S)-PABQ. MC-VC(S)-PABQ-Tubulysin M is effective against multidrug-resistant lymphoma cell lines and tumors.
  • 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-10330A
    Toceranib phosphate

    SU11654 phosphate; PHA 291639E phosphate

    PDGFR VEGFR c-Kit Cancer
    Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .
  • HY-13725
    Pirarubicin

    THP

    Topoisomerase Autophagy Bacterial Antibiotic Cancer Infection
    Pirarubicin is an anthracycline antibiotics, acts as a topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors.
  • HY-103471
    Y11

    Others Cancer
    Y11 inhibits FAK1 autophosphorylation by blocking phosphorylation of Y397 and decreases tumor growth.
  • HY-N6722
    Swainsonine

    Tridolgosir

    Bacterial Antibiotic Cancer Infection
    Swainsonine is an alkaloid isolated from Astragalus, acts as an inhibitor of α-mannosidase, with anti-tumor activity.
  • HY-13727
    Pixantrone free base

    BBR 2778 free base

    Topoisomerase Cancer
    Pixantrone (BBR 2778 (free base)), a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
  • HY-100138
    2-Aminoethyl-mono-amide-DOTA-tris(tBu ester)

    ADC Linkers Cancer
    2-Aminoethyl-mono-amide-DOTA-tris(tBu ester) is a macrocycle DOTA derivative for tumor pretargeting.
  • HY-128939
    EC0488

    Antifolate Cancer
    EC0488 is used to synthesize EC0531 with folate receptor (FR)-specific and anti-tumor activities.
  • HY-N0428
    Obacunone

    Apoptosis Cancer
    Obacunone, isolated from seeds of Marsh White grapefruit, exhibits anti-tumor activity by the induction of apoptosis.
  • HY-N4255
    Resibufagin

    Others Cancer
    Resibufagin is a kind of bufadienolide isolated from the venom of Bufo bufo gargarizans, has anti-tumor activities.
  • HY-N0140
    Ursolic acid

    Prunol; Urson; Malol

    Autophagy Endogenous Metabolite Cancer
    Ursolic acid (Prunol) is a natural pentacyclic triterpenoid carboxylic acid, exerts anti-tumor effects and is an effective compound for cancer prevention and therapy.
  • HY-13725A
    Pirarubicin Hydrochloride

    THP Hydrochloride

    Topoisomerase Autophagy Bacterial Antibiotic Cancer Infection
    Pirarubicin Hydrochloride is an anthracycline antibiotics, acts as a topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors.
  • HY-N1128
    Trichorabdal A

    (-)-Trichorabdal A

    Others Cancer
    Trichorabdal A is a diterpenoid compound isolated from Rabdosia trichocarpa. Trichorabdal A has potent anti-tumor activity.
  • HY-U00155
    NCI172112

    NSC172112; NSC268497

    Others Cancer
    NCI172112 is a classical bifunctional alkylating agent synthesized in an effort to develop antitumor agents effective against CNS tumors.
  • 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-147834
    STING agonist-9

    STING Cancer
    STING agonist-9 (Compound 45) is a potent STING agonist with an EC50 of 1.2 nM and 32.82 μM against h-STING and m-STING, respectively. STING agonist-9 shows antitumor activity.
  • HY-N8204
    Siaresinolic acid 28-O-β-D-glucopyranosyl ester

    Others Cancer Metabolic Disease
    Siaresinolic acid 28-O-β-D-glucopyranosyl ester possesses anti-tumor and antidiabetic effect activity.
  • HY-18985
    Phorbol 12,13-dibutyrate

    Phorbol dibutyrate; PDBu

    PKC Cancer
    Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator and a potent skin tumor promoter.
  • HY-N0743
    Senkyunolide A

    Others Cancer
    Senkyunolide A, isolated from Ligusticum chuanxiong Hort, has cytoprotective and antiproliferative activities. Anti-tumor activity.
  • HY-N8091
    Lehmannine

    Bacterial Cancer Infection
    Lehmannine is a quinolizidine bioalkaloid isolated from S. alopecuroides L, has antibacterial, anti-inflammatory and anti-tumor activities.
  • HY-16674
    10-Oxo Docetaxel

    Docetaxel Impurity 1

    Microtubule/Tubulin Cancer
    10-Oxo Docetaxel (Docetaxel Impurity 1) is a novel taxoid having remarkable anti-tumor properties and a Docetaxel intermediate.
  • HY-122760
    Bax activator-1

    Bcl-2 Family Apoptosis Cancer
    Bax activator-1 (compound 106) is a Bax activator that induces Bax-dependent tumor cell apoptosis.
  • HY-N8131
    Pangelin

    Bacterial Cancer Infection
    Pangelin is a coumarin that can be found in Ducrosia anethifolia. Pangelin exhibits anti-mycobacterial and anti-tumor activities.
  • HY-N2242
    Hosenkoside G

    Others Cancer
    Hosenkoside G, a baccharane glycoside isolated from the seeds of Impatiens Balsamina L., possesses anti-tumor activity.
  • HY-10517A
    (Z)-Orantinib

    (Z)-SU6668; (Z)-TSU-68

    VEGFR PDGFR FGFR Cancer
    (Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors.
  • HY-133779
    Gefitinib impurity 5

    Others Others
    Gefitinib impurity 5 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-16231
    GGTI-2418

    ROS Kinase Apoptosis Cancer
    GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors.
  • HY-131257
    Gefitinib impurity 1

    Others Others
    Gefitinib impurity 1 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-114277
    Sotorasib

    AMG-510

    Ras Cancer
    Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors.
  • HY-136093
    HL271

    IM156 hydrochloride; HL156A hydrochloride

    AMPK Cancer Neurological Disease
    HL271 (IM156 hydrochloride; HL156A hydrochloride), a chemical derivative of Metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. HL271 attenuates aging-associated cognitive impairment in animal model. HL271 is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors.
  • HY-128758
    DYRKs-IN-1

    DYRK Cancer
    DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 has antitumor activity.
  • HY-P1344A
    DAPK Substrate Peptide TFA

    DAPK Cancer
    DAPK Substrate Peptide TFA is a synthetic peptide substrate for death associated protein kinase (DAPK), with a Km of 9 μM.
  • HY-130797
    TLR7/8 agonist 3

    Toll-like Receptor (TLR) Cancer
    TLR7/8 agonist 3 is a potent TLR7 and TLR8 agonist, extracted from patent WO2016057618 (compound of formula (II)).
  • HY-128758A
    DYRKs-IN-1 hydrochloride

    DYRK Cancer
    DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity.
  • HY-N2322
    Khasianine

    Others Cancer
    Khasianine is a steroidal glycoalkaloid which is obtained from black nightshade (Solanum Nigrum L.), which displays antitumor activity.
  • HY-129602
    SD-36

    PROTACs STAT Apoptosis Cancer
    SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase.
  • HY-14941
    Elacytarabine

    CP 4055

    Others Cancer
    Elacytarabine (CP 4055) is a lipid-conjugated derivative of the nucleoside analog cytarabine. Elacytarabine (CP 4055) is an antineoplastic drug with cytotoxicity in solid tumors.
  • HY-112181
    KO-947

    ERK Cancer
    KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential utility in MAPK pathway dysregulated tumors.
  • HY-13551
    Amsacrine

    m-AMSA; acridinyl anisidide

    Topoisomerase Autophagy Cancer
    Amsacrine (m-AMSA; acridinyl anisidide) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
  • HY-P0073
    Tyr-Gly-Gly-Phe-Met-OH

    Met-Enkephalin; Methionine enkephalin

    Opioid Receptor Neurological Disease Cancer
    Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor.
  • HY-121649
    AQ4

    Topoisomerase Cancer
    AQ4 is a topoisomerase II inhibitor and DNA intercalator as a chemically stable cytotoxic agent in many human tumor lines.
  • HY-135317
    CA-4948

    IRAK FLT3 Cancer Inflammation/Immunology
    CA-4948 is a potent IRAK4/FLT3 inhibtor with anti-tumor activity.
  • HY-N0183
    Formononetin

    Biochanin B; Flavosil; Formononetol

    FGFR Apoptosis Cancer Cardiovascular Disease
    Formononetin is a potent FGFR2 inhibitor with an IC50 of ~4.31 μM. Formononetin potently inhibits angiogenesis and tumor growth.
  • HY-N2542
    Tubeimoside III

    Others Cancer Inflammation/Immunology
    Tubeimoside III, a triterpenoid saponin, shows anti-inflammatory, anti-tumor, anti-tumorigenic activities, and acute toxicity in vivo.
  • HY-13551A
    Amsacrine hydrochloride

    m-AMSA hydrochloride; acridinyl anisidide hydrochloride

    Topoisomerase Autophagy Cancer
    Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
  • HY-N2604
    Loureirin C

    Others Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease
    Loureirin C has anti-bacterial, anti-spasmodic, anti-inflammatory, analgesic, anti-diabetic, and anti-tumor activities.
  • HY-N6075
    Specneuzhenide

    Nuezhenide

    Others Cancer
    Specneuzhenide (Nuezhenide) is a phenol glycoside isolated from Ligustrum sinense. Specneuzhenide (Nuezhenide) possesses anti-tumor activity.
  • HY-N0400
    Wogonin

    CDK Wnt Autophagy Apoptosis Cancer Inflammation/Immunology
    Wogonin is a naturally occurring mono-flavonoid, can inhibit the activity of CDK8 and Wnt, and exhibits anti-inflammatory and anti-tumor effects.
  • HY-W008253
    5-Hydroxyindole-3-acetic acid

    Endogenous Metabolite Cancer Neurological Disease
    5-Hydroxyindole-3-acetic acid is the main metabolite of serotonin or metanephrines, which can be used as a biomarker of neuroendocrine tumors.
  • HY-N0271
    Echinocystic acid

    Reactive Oxygen Species Apoptosis Inflammation/Immunology Cancer
    Echinocystic acid a pentacyclic triterpene isolated from the fruits of Gleditsia sinensis Lam, has potent antioxidant, anti-inflammatory and anti-tumor properties.
  • HY-100663
    Gefitinib impurity 2

    Others Others
    Gefitinib impurity 2 is the impurity of Gefitinib. Gefitinib (ZD1839; HY-50895) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-143432A
    (S)-Cdc7-IN-18

    CDK Cancer
    (S)-Cdc7-IN-18 is a potent inhibitor of CDC7. Overexpression of huCdc7 promotes overactivation of MCM2, an important marker of tumor cells, and thus promotes aberrant proliferation of tumor cells. (S)-Cdc7-IN-18 has the potential for the research of cancer diseases (extracted from patent WO2020239107A1, compound 1-1).
  • HY-136093A
    IM156

    HL156A; HL271 acetate

    AMPK Cancer Neurological Disease
    IM156 (HL156A; HL271 acetate), a chemical derivative of Metformin (HY-B0627), is a potent and orally active AMPK activator that increases AMPK phosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model. IM156 is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors.
  • HY-W011845
    DMBA

    Others Cancer
    DMBA has carcinogenic activity as a polycyclic aromatic hydrocarbon (PAH). DMBA is used to induce tumor formation in various rodent models.
  • HY-P1728
    Super-TDU (1-31)

    YAP Cancer
    Super-TDU (1-31) is a peptide of Super-TDU, which is an inhibitor of YAP-TEADs, shows potent anti-tumor activity.
  • HY-130995
    Agrochelin

    Antibiotic ADC Cytotoxin Infection
    Agrochelin, an alkaloid cytotoxic antibiotic, is produced by the fermentation of a marine Agrobacterium sp. Agrochelin has cytotoxic activity in tumor cell lines.
  • HY-132234
    M-1211

    Epigenetic Reader Domain Cancer
    M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.
  • HY-13727B
    Pixantrone hydrochloride

    BBR 2778 hydrochloride

    Topoisomerase Cancer
    Pixantrone (BBR 2778 (free base)) hydrochloride, a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
  • HY-P99041
    Panitumumab

    ABX-EGF

    EGFR Cancer
    Panitumumab (ABX-EGF) is a fully human IgG2 anti-EGFR monoclonal antibody. Panitumumab has an anti-tumor activity.
  • HY-132922
    EEDi-5273

    Histone Methyltransferase Cancer
    EEDi-5273 is an exceptionally potent and orally efficacious EED inhibitor (IC50 = 0.2 nM) capable of achieving complete and persistent tumor regression.
  • HY-P1728A
    Super-TDU (1-31) (TFA)

    YAP Cancer
    Super-TDU (1-31) is a peptide of Super-TDU, which is an inhibitor of YAP-TEADs, shows potent anti-tumor activity.
  • HY-14153
    Tegaserod

    5-HT Receptor Cancer Metabolic Disease
    Tegaserod is a serotonin receptor 4 agonist (HTR4) used in the treatment of irritable bowel syndrome (IBS). Anti-tumor activity.
  • HY-110203
    R-7050

    TNF-α Antagonist III

    TNF Receptor Cancer
    R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.
  • HY-14808
    Adarotene

    ST1926

    Apoptosis Cancer
    Adarotene is an effective apoptosis inducer, which surprisingly produces DNA damage and exhibites a potent antiproliferative activity on a large panel of human tumor cells.
  • HY-102001
    Tomaymycin DM

    ADC Cytotoxin Cancer
    Tomaymycin DM, a DNA alkylator, is a derivative of Tomaymycin, it is a PBD dimer, which is attached to tumor targeting antibodies to create antibody-drug conjugates (ADCs).
  • HY-124584
    Minnelide

    Apoptosis Cancer
    Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide promotes apoptosis.
  • HY-N0714
    Berbamine

    NF-κB Autophagy Cancer
    Berbamine is a natural compound extracted from traditional Chinese medicine Barberry with anti-tumor, immunomodulatory and cardiovascular effects. Berbamine is a calcium channel blocker.
  • HY-146743
    Antitumor agent-53

    Apoptosis Cancer
    Antitumor agent-53 is a potent antitumor agent. Antitumor agent-53 induces cell cycle arrest at the G2/M phase. Antitumor agent-53 inhibits the PI3K/AKT pathway to induce the apoptosis of HGC-27 cells. Antitumor agent-53 has the potential for the research of gastrointestinal tumors.
  • HY-119367
    ODM-203

    FGFR VEGFR Cancer
    ODM-203 is a potent FGFR and VEGFR families inhibitor with IC50s of 11, 16, 6, 35 nM towards recombinant FGFR1, FGFR2, FGFR3 and FGFR4 as well as 26, 9, 5 nM towards VEGFR1, VEGFR2 and VEGFR3, respectively. ODM-203 exhibits strong anti-tumor activity and induces anti-tumor immunity.
  • HY-139719
    IMD-biphenylC

    NF-κB Inflammation/Immunology
    IMD-biphenylC is a novel imidazoquinolinone-NF-κB immunomodulator dimer that inhibits tumor proliferation while induces low systemic inflammation and reduces adjuvant toxicity.
  • HY-50909
    Perifosine

    KRX-0401; NSC 639966; D21266

    Akt Autophagy Apoptosis Cancer
    Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
  • HY-13468
    KW-2478

    HSP Cancer
    KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.
  • HY-111634
    Epsilon-momfluorothrin

    Others Cancer
    Epsilon-momfluorothrin is a type I synthetic pyrethroid insecticide, activates constitutive androstane receptor (CAR), and induces hepatocellular tumors in rats.
  • HY-N0834
    Pulsatilla saponin D

    SB365; Hederacolchiside A

    Apoptosis Cancer
    Pulsatilla saponin D (SB365), isolated from the root of Pulsatilla koreana Nakai, is an anti-tumor agent.
  • HY-N4189
    Isocucurbitacin B

    Others Cancer
    Isocucurbitacin B is a potent cytotoxic compound isolated from Helicteres rswa L. (Sterculiaceae). Isocucurbitacin B possesses anti-tumor acticity.
  • HY-U00095
    Hepsulfam

    NCI 329680; ZINC01574758

    Others Cancer
    Hepsulfam (NCI 329680; ZINC01574758) is a anticancer agent that shows excellent antileukemic activity with an median IC50 of 0.91 μg/mL in a panel of different tumors.
  • HY-126330
    SS-208

    HDAC Cancer
    SS-208 is a selective HDAC6 inhibitor, with an IC50 of 12 nM. SS-208 possesses anti-tumor activity in melanoma.
  • HY-12885
    ADU-S100

    MIW815; ML RR-S2 CDA

    STING Inflammation/Immunology
    ADU-S100 (MIW815), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity.
  • HY-P1009
    Z-YVAD-FMK

    Caspase Cancer
    Z-YVAD-FMK is a cell-permeable caspase-1 and -4 inhibitor with anti-inflammatory and anti-tumor activities.
  • HY-114535
    Jaceidin

    EGFR Cancer
    Jaceidin is a promising lead molecule for potent VEGFR inhibitor with excellent membrane permeability and oral bioavailability. Jaceidin exhibits anti-tumor activities.
  • HY-108491
    N,N-Dimethylsphingosine

    SphK Cancer
    N,N-Dimethylsphingosine is a potent inhbitor of SphK (sphingosine kinase) as an endogenous metabolite of sphingosine produced in various tissues and tumor cell lines.
  • 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-139718
    IMD-biphenylB

    NF-κB Inflammation/Immunology
    IMD-biphenylB is a potent imidazoquinolinone-NF-κB immunomodulator dimer that inhibits tumor proliferation while induces low systemic inflammation and reduces adjuvant toxicity.
  • HY-18310
    NIBR-17

    PI3K Cancer
    NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth.
  • HY-145668
    Cyclopentenyl uracil

    Others Cancer
    Cyclopentenyl uracil, a non-cytotoxic inhibitor of uridine kinase, effectively blocks the salvage of circulating uridine by host and tumor tissues in the intact mouse.
  • HY-N8207
    Gypenoside LI

    Apoptosis MicroRNA Cancer
    Gypenoside LI, a gypenoside monomer, possesses anti-tumor activity. Gypenoside LI induces cell apoptosis, cell cycle and migration.
  • HY-147317
    Epothilone E

    Microtubule/Tubulin Cancer
    Epothilone E is a related compound of epothilone, which inhibits microtubule protein function and blocks cell division, and has anti-tumor activity.
  • HY-105061
    Misonidazole

    Ro 7-0582; SR 1354

    Bacterial Cancer Infection
    Misonidazole (Ro 7-0582; SR 1354) is a hypoxic tumor cell radiosensitizer. Misonidazole also has antimicrobial effects.
  • HY-N4109
    Decursinol

    Others Cancer Inflammation/Immunology
    Decursinol, isolated from the roots of Angelica gigas, possesses antinociceptive effect with orally bioavailability. Decursinol possesses anti-tumor and anti-metastasis activity.
  • HY-101120
    666-15

    Epigenetic Reader Domain Cancer
    666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model.
  • HY-N2997
    Ganoderic acid LM2

    Others Cancer
    Ganoderic acid LM2 is a natural terpenoid isolated from the Fungus Ganoderma lucidum. Ganoderic acid LM2 possesses potential anti-tumor activity.
  • HY-137442
    Inupadenant

    EOS-850

    Adenosine Receptor Cancer
    Inupadenant is an orally active, highly selective A2A receptor antagonist. Inupadenant is not brain-penetrant. Inupadenant has potent anti-tumor activity.
  • HY-17592A
    Bithionol sulfoxide

    Parasite Cancer
    Bithionol sulfoxide(Bitin-S) is a clinically approved anti-parasitic drug; has been shown to inhibit solid tumor growth in several preclinical cancer models.
  • HY-143655
    QW24

    Autophagy Cancer
    QW24 exerts potent anti-tumor activity by down-regulating BMI-1 and is used as an effective therapeutic agent for clinical colorectal cancer treatment.
  • HY-147894
    PCAF-IN-1

    Others Cancer
    PCAF-IN-1 is a highly selective PCAF inhibitor. PCAF-IN-1 is a antitumor agents, which can be used in tumor treatment research.
  • HY-B1436S
    Nifuroxazide-d4

    STAT Bacterial Antibiotic Cancer Infection
    Nifuroxazide-d4 is the deuterium labeled Nifuroxazide. Nifuroxazide is an effective inhibitor of STAT3, also exerts potent anti-tumor and anti-metastasis activity.
  • HY-115453
    UBCS039

    Sirtuin Autophagy Cancer
    UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC50 of 38 μM.
  • HY-N6004
    (Rac)-Shikonin

    Shikalkin

    Others Cancer
    (Rac)-Shikonin (Shikonin) possesses anti-tumor activity. (Rac)-Shikonin (Shikonin) circumvents cancer drug resistance by induction of a necroptotic death.
  • HY-12444
    Y15

    FAK Inhibitor 14

    FAK Cancer
    Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
  • HY-141896
    RET-IN-7

    RET Cancer
    RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.
  • HY-16516
    Vitamin CK3

    Others Cancer
    Vitamin CK3 is the combination of Vitamin C and vitamin K3 (100:1 ratio) and has been shown to inhibit tumor growth and lung metastasis.
  • 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-N2632
    Uvarigrin

    Apoptosis Cancer
    Uvarigrin, isolated from the roots of Uvaria calamistrata, induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation.
  • HY-13701
    Nelarabine

    506U78; GW 506U78; Nelzarabine

    Nucleoside Antimetabolite/Analog Apoptosis Cancer
    Nelarabine (Arranon, 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.
  • HY-N0429
    Diosbulbin B

    Others Cancer
    Diosbulbin B is a diterpene lactone isolated from D. bulbifera L., with anti-tumor activity. Diosbulbin B can induce liver injury.
  • HY-136718
    CLEFMA

    Apoptosis Cancer
    CLEFMA is a curcuminoid with antitumor activity. CLEFMA inhibits tumor growth is associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects.
  • HY-146819
    CAIX/CAXII-IN-1

    Carbonic Anhydrase Cancer
    Compound 9 is the most effective against tumor specific Ca ix/ca XII (ki=29.1 and 8.8 nm), so it is possible to evaluate its cytotoxicity and selectivity to HepG-2, HCT-116 and MCF-7 cancer cell lines in vitro, and its IC50 values to tumor cells are 1.78, 1.94 and 3.07, respectively μ M. It showed that it had obvious cytotoxicity.
  • HY-50895S2
    Gefitinib-d3

    EGFR Autophagy Cancer
    Gefitinib-d3 (ZD1839-d3) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-50895S1
    Gefitinib-d6

    ZD1839-d6

    EGFR Autophagy Cancer
    Gefitinib-d6 (ZD1839-d6) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • 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-13016A
    Cabozantinib hydrochloride

    XL184 hydrochloride; BMS-907351 hydrochloride

    VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis Cancer
    Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.
  • HY-13016
    Cabozantinib

    XL184; BMS-907351

    VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis Cancer
    Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.
  • HY-130996
    Diacetyl Agrochelin

    ADC Cytotoxin Cancer
    Diacetyl Agrochelin is an acetyl derivative of Agrochelin, which is produced by the fermentation of a marine Agrobacterium sp. Diacetyl Agrochelin has cytotoxic activity in tumor cell lines.
  • HY-14754
    Salirasib

    S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS

    Ras Autophagy Cancer
    Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
  • HY-N9350
    Ganoderic acid ε

    Others Cancer
    Ganoderic acid ε is a natural terpenoid isolated from the Fungus Ganoderma lucidum. Ganoderic acid ε exhibits an ED50 of 12.2 μg/mL in Meth-A tumor cells
  • HY-121410
    Narasin

    Bacterial Parasite NF-κB Antibiotic Cancer Infection
    Narasin is a cationic ionophore and coccidiostat agent. Narasin inhibits NF-κB signaling and induces tumor cells apoptosis. Narasin has antimicrobial and anticancer activity.
  • HY-N4116
    Xanthyletin

    Fungal Cancer Infection
    Xanthyletin is a coumarin isolated from Citrus, with anti-tumor and anti-bacterial activities. Xanthyletin also inhibits symbiotic fungus cultivated by leaf-cutting ants.
  • HY-145726
    ISIS 104838

    TNF Receptor Inflammation/Immunology
    ISIS 104838 is an antisense oligonucleotide drug that reduces the production of tumor necrosis factor (TNF-alpha), a substance that contributes to joint pain and swelling in rheumatoid arthritis.
  • HY-N3442
    Juglanin

    JNK Apoptosis Autophagy Cancer Inflammation/Immunology
    Juglanin, a natural occurring flavonoid, is a JNK acticator, with inflammation and anti-tumor activities. Juglanin can induce apoptosis and autophagy on human breast cancer cells.
  • HY-112129
    AGI-25696

    Others Cancer
    AGI-25696 is a methionine adenosyltransferase 2A (MATA2 ) inhibitors useful for treatment of cancer. AGI-25696 blocks growth of MTAP-deleted tumors in vivo.
  • HY-117260
    Coformycin

    Adenosine Deaminase Bacterial Cancer Infection
    Coformycin, a nucleoside antibiotic, is a potent inhibitor of adenosine deaminase (ADA) from Streptomyces species. Coformycin possesses anti-tumor and anti-bacterial activity.
  • HY-N0370S
    Bergapten-d3

    5-Methoxypsoralen-d3

    Cytochrome P450 Autophagy Cancer
    Bergapten-d3 is deuterium labeled Bergapten. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
  • HY-N2104
    Daurinoline

    Others Cancer
    Daurinoline is an alkaloid that can be isolated from the roots of Menispermum dauricum. Daurinoline may be a potential anti-tumor agent or chemosensitizer for chemo-resistant NSCLC research.
  • HY-N7225
    Yuanhuacine

    Gnidilatidin

    Others Cancer
    Yuanhuacine (Gnidilatidin), a daphnane diterpenoid from the flowers of Daphne genkwa with extensive anti-tumor activity. Yuanhuacine is a DNA-damaging agent with orally active.
  • HY-12885B
    ADU-S100 ammonium salt

    MIW815 ammonium salt; ML RR-S2 CDA ammonium salt

    STING Inflammation/Immunology
    ADU-S100 ammonium salt (MIW815 ammonium salt), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity.
  • HY-14807
    Tosedostat

    CHR-2797

    Aminopeptidase Cancer
    Tosedostat (CHR-2797) is an orally active aminopeptidase inhibitor. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines.
  • HY-10251
    BMS-599626

    AC480

    EGFR Cancer
    BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
  • HY-139643A
    CXCR7 antagonist-1 hydrochloride

    CXCR Cancer Inflammation/Immunology
    CXCR7 antagonist-1 hydrochloride is a CXCR7 antagonist that inhibits the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR7. CXCR7 antagonist-1 hydrochloride is useful in preventing tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases (extracted from patent WO2014085490A1, compound 1.128).
  • HY-139643
    CXCR7 antagonist-1

    CXCR Cancer Inflammation/Immunology
    CXCR7 antagonist-1 is a CXCR7 antagonist that inhibits the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR7. CXCR7 antagonist-1 is useful in preventing tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases (extracted from patent WO2014085490A1, compound 1.128).
  • HY-10330S
    Toceranib-d8

    PDGFR VEGFR c-Kit Cancer
    Toceranib-d8 (SU11654-d8) is the deuterium labeled Toceranib. Toceranib (SU11654) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib (SU11654) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.
  • HY-12010
    BMS-599626 Hydrochloride

    AC480 Hydrochloride

    EGFR Cancer
    BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 Hydrochloride inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
  • HY-N7611
    7-Prenyloxyaromadendrin

    Others Cancer
    7-Prenyloxyaromadendrin is a flavonoid from Pterocaulon alopecuroides with antitumor activity. 7-Prenyloxyaromadendrin shows good antiproliferative activity in tumor cell lines.
  • HY-N4322
    Decursinol angelate

    PKC Cancer Inflammation/Immunology
    Decursinol angelate, a cytotoxic and protein kinase C (PKC) activating agent from the root of Angelica gigas, possesses anti-tumor and anti-inflammatory activities.
  • HY-103088
    E7046

    Prostaglandin Receptor Cancer Endocrinology
    E7046 is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM. E7046 exhibits anti-tumor activities.
  • HY-139716
    IMD-catechol

    NF-κB Inflammation/Immunology
    IMD-catechol is a novel imidazoquinolinone-NF-κB immunomodulator dimer that improves efficacy in a CT26 mouse colon carcinoma tumor model while eliciting minimal adjuvant toxicity.
  • 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-P1043A
    NGR peptide Trifluoroacetate

    Aminopeptidase Cancer
    NGR peptide Trifluoroacetate containing the asparagine-glycine-arginine (NGR) motif is recognized by CD13/aminopeptidase N (APN) receptor isoforms that are selectively overexpressed in tumor neovasculature.
  • HY-144434
    RSK-IN-1

    Ribosomal S6 Kinase (RSK) Cancer
    RSK-IN-1 (compound 7d) is a RSK inhibitor that inhibits the YB-1 phosphorylation. RSK-IN-1 has anti-tumor effects.
  • HY-13648
    Incyclinide

    CMT-3; COL-3

    MMP Cancer
    Incyclinide (CMT-3, COL-3) is a matrix metalloproteinase (MMP) inhibitor, thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis.
  • HY-128599
    NMS-P515

    PARP Cancer
    NMS-P515 is a potent, orally active and stereospecific PARP-1 inhibitor, with a Kd of 16 nM and an IC50 of 27 nM (in Hela cells). Anti-tumor activity.
  • HY-N0124
    Dioscin

    Collettiside III; CCRIS 4123

    Autophagy Apoptosis Cancer
    Dioscin(CCRIS 4123; Collettiside III) is a natural steroid saponin derived from several plants, showing potent anti-cancer effect against a variety of tumor cell lines.
  • HY-N0011
    Baohuoside I

    Icariin-II; Icariside-II

    CXCR Apoptosis Cancer Inflammation/Immunology Endocrinology
    Baohuoside I, a flavonoid isolated from Epimedium koreanum Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 expression, induces apoptosis and shows anti-tumor activity.
  • HY-129181
    FGFR4-IN-4

    FGFR Cancer
    FGFR4-IN-4 (compound 693) is a FGFR4 inhibitor with anti-tumor activity, extracted from patent WO2018113584A1.
  • HY-P99057
    Varlilumab

    CDX-1127

    TNF Receptor Cancer
    Varlilumab (CDX-1127) is a first-in-class human IgG1 anti-CD27 monoclonal antibody. Varlilumab has an anti-tumor activity.
  • HY-N0344
    Farrerol

    Others Cancer Inflammation/Immunology Neurological Disease
    Farrerol is a bioactive constituent of Rhododendron, with broad activities such as anti-oxidative, anti-inflammatory, anti-tumor, neuroprotective and hepatoprotective effects.
  • HY-12449
    Crenigacestat

    LY3039478

    Notch γ-secretase Cancer
    Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC50 of 1 nM in most of the tumor cell lines tested.
  • HY-150577
    HDAC-IN-45

    HDAC Cancer
    HDAC-IN-45 (Compound 14) is a small molecule HDAC inhibitor and has anticancer activity, also can forms a hydrogen bond with residue Y303. HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively.
  • HY-129168
    USP7-IN-5

    Deubiquitinase Cancer
    USP7-IN-5 is a potent ubiquitin specific protease 7 (USP7) inhibitor extracted from patent WO2017212012A1, example 40, has an IC50 of 49.9 nM.
  • HY-129169
    USP7-IN-6

    Deubiquitinase Cancer
    USP7-IN-6 is a potent ubiquitin specific protease 7 (USP7) inhibitor, extracted from patent WO2017212010A1, example 25, has an IC50 of 6.8 nM.
  • HY-118916
    FTI-2148

    Farnesyl Transferase Cancer
    FTI-2148 is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.
  • HY-115769
    1,2-Didecanoylglycerol

    PKC Endocrinology
    1,2-Didecanoylglycerol, a synthetic diacylglycerol, is metabolized by platelets to 1,2-didecanoylphosphatidic acid (PA10) and activates protein kinase C (PKC).
  • HY-136563
    RA375

    Proteasome Apoptosis Reactive Oxygen Species Cancer
    RA375 is a RPN13 (26S proteasome regulatory subunit) inhibitor. RA375 activates UPR signaling, ROS production and apoptosis. RA375 exhibits ten-fold greater activity against cancer lines than RA190, reflecting its nitro ring substituents and the addition of a chloroacetamide warhead.
  • HY-147665
    hCAIX-IN-7

    Carbonic Anhydrase Cancer
    hCAIX-IN-7 (compound 6c) is a potent and selective hCAIX inhibitor with KIs of >10000, >10000, 43.0, 410.6 nM for hCAI, hCAII, hCAIV, hCAIX, respectively.
  • HY-147662
    hCAIX-IN-5

    Carbonic Anhydrase Cancer
    hCAIX-IN-5 (compound 6b) is a potent and selective hCAIX inhibitor with KIs of >10000, >10000, 130.7, 829.1 nM for hCAI, hCAII, hCAIV, hCAIX, respectively.
  • HY-15865
    FR901463

    Others Cancer
    FR901463 is a potent anti-cancer agent and can be used for cancer research. FR901463 enhances the transcriptional activity of the promoter of SV40 DNA virus.
  • HY-137246
    CD73-IN-3

    CD73 Cancer
    CD73-IN-3 is a potent CD73 inhibitor (IC50=7.3 nM in Calu6 human cell assay). CD73-IN-3, example 2 extracted from patent WO2019168744 A1, has the potential for cancer research.
  • HY-122577
    EN40

    Aldehyde Dehydrogenase (ALDH) Cancer
    EN40 is a potent, selective aldehyde dehydrogenase 3A1 (ALDH3A1) inhibitor as a covalent ligand, exhibits an IC50 value of 2 uM
  • HY-N0102
    Isoliquiritigenin

    GU17; ISL; Isoliquiritigen; SJ000286237

    Aldose Reductase Influenza Virus Autophagy Apoptosis Cancer Infection Inflammation/Immunology
    Isoliquiritigenin is an anti-tumor flavonoid from the root of Glycyrrhiza glabra, which inhibits aldose reductase with an IC50 of 320 nM. Isoliquiritigenin is a potent inhibitor of influenza virus replication with an EC50 of 24.7 μM.
  • HY-147664
    hCAXII-IN-1

    Carbonic Anhydrase Cancer
    These compounds show selective inhibition on tumor related subtypes HCA IX and XII, and are also considered as the leading molecules for the development of future cancer therapeutic drugs based on new mechanisms of action.
  • HY-133558
    VII-31

    E1/E2/E3 Enzyme Apoptosis Cancer
    VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways.
  • HY-12460
    SPDB-DM4

    Drug-Linker Conjugates for ADC Cancer
    SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4, a tubulin inhibitor) via a SPDB linker, exhibiting potent anti-tumor activity.
  • HY-N4000
    Digitonin

    Others Cancer
    Digitonin, a glycoside obtained from Digitalis purpurea, could increase cell permeability by binding to cholesterol molecules and reduce tumor growth. Digitonin is an natural detergent.
  • HY-W005629
    Leelamine

    Cannabinoid Receptor PDHK Cancer
    Leelamine is a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine also inhibits pyruvate dehydrogenase kinases (PDKs). Leelamine exhibits anti-tumor activity.
  • HY-N2432
    Paederoside

    HBV Cancer Infection
    Paederoside is a monoterpene S-methyl thiocarbonate isolated from Paederia pertomentosa. Paederoside shows a high anti-tumor promoting activity against the Epstein-Barr virus activation.
  • HY-128589
    CHMFL-KIT-033

    c-Kit Cancer
    CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC50 of 0.045 μM.
  • HY-147316
    TP-5801

    Others Cancer
    TP-5801 is an orally active TNK1 (non-receptor tyrosine kinase) inhibitor (IC50=1.40 nM), and shows anti-tumor activity.
  • HY-N0205
    Pulchinenoside C

    Anemoside B4

    Others Cancer
    Pulchinenoside C (Anemoside B4) is Pulsatilla koreana Nakai that have many numerous biological effects in vitro, including enhancing hypoglycemic, anti-tumor, neuroprotective and anti-angiogenic activity.
  • HY-129467
    (Rac)-Idroxioleic acid

    2-Hydroxyoleic acid; 2-OHOA

    Apoptosis Cancer
    (Rac)-Idroxioleic acid (2-Hydroxyoleic acid) is a synthetic oleic acid (OA) derivative that binds to the plasma membrane and alters lipid organization. (Rac)-Idroxioleic acid has anti-tumor effect.
  • HY-W011522
    Taurolidine

    Bacterial Apoptosis Antibiotic Cancer Infection
    Taurolidine is a broad-spectrum antimicrobial for the prevention of central venous catheter-related infections. Taurolidine has a direct and selective antineoplastic effect on brain tumor cells by the induction of apoptosis.
  • HY-N6985
    Baccatin III

    Others Cancer
    Baccatin III is a natural product isolated from Pacific yew tree and related species. Baccatin III reduces tumor progression by inhibiting the accumulation and suppressive function of MDSCs.
  • HY-135898
    DGK-IN-1

    Others Cancer Inflammation/Immunology
    DGK-IN-1 is a T cell activator extracted from patent WO2020006018A1, example 25. DGK-IN-1 can be used for tumor immunity.
  • HY-101450
    PF-6274484

    EGFR Cancer
    PF-6274484 is a potent EGFR inhibitor with Kis of 0.14 nM and 0.18 nM for EGFR-L858R/T790M and WT EGFR, respectively. PF-6274484 inhibits EGFR-L858R/T790M autophosphorylation in H1975 tumor cells and EGFR WT in A549 tumor cells with IC50s of 6.6 and 5.8 nM, respectively.
  • HY-U00179
    CDC801

    Phosphodiesterase (PDE) TNF Receptor Cancer
    CDC801 is a potent and orally active phosphodiesterase 4 (PDE4) and tumor necrosis factor-α (TNF-α) inhibitor with IC50 of 1.1 μM and 2.5 μM, respectively.
  • HY-131493
    PF-06939999

    PRMT5-IN-3

    Histone Methyltransferase Cancer
    PF-06939999 (PRMT5-IN-3) is a PRMT5 inhibitor that exhibits synthetic lethality to tumor cells but produce few side effects combined with DNA damaging agents.
  • HY-N6049
    Lup-20(29)-en-28-oic acid

    Others Cancer Inflammation/Immunology
    Lup-20(29)-en-28-oic acid, a triterpenoid saponins of Pulsatilla koreana Root, possesses anti-inflammatory and anti-tumor effect.
  • HY-146863
    Tubulin polymerization-IN-10

    Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-10 is a potent tubulin polymerization inhibitor with an IC50 of 4.25±0.75 μM. Tubulin polymerization-IN-10 has anti-tumor effects.
  • HY-120149
    Inotodiol

    Others Cancer
    Inotodiol (compound 3) is a lanostane-type triterpenoid compound isolated from the sclerotia of Inonotus obliquus. Inotodiol exhibits the potent anti-tumor promoting activity in the in vivo carcinogenesis test.
  • HY-P99039
    Oleclumab

    MEDI9447

    CD73 Cancer
    Oleclumab (MEDI9447) is a human IgG1λ anti-CD73 monoclonal antibody that inhibits CD73 function. Oleclumab has an anti-tumor activity.
  • HY-145306
    DX3-234

    Mitochondrial Metabolism Cancer
    DX3-234 is an oxidative phosphorylation (OXPHOS) inhibitor. DX3-234 shows significant tumor suppression in the Pan02 syngeneic model of pancreatic cancer.
  • HY-N2198
    Podocarpusflavone A

    Topoisomerase Apoptosis Cancer
    Podocarpusflavone A is a DNA topoisomerase I inhibitor. Podocarpusflavone A has moderated anti-proliferative activity and induces cell apoptosis in MCF-7. Podocarpusflavone A is developing anti-tumor drugs.
  • HY-N0114A
    (±)-Evodiamine

    Topoisomerase Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    (±)-Evodiamine, a quinazolinocarboline alkaloid, is a Top1 inhibitor. Evodiamine exhibits anti-inflammatory, antiobesity, and antitumor effects. (±)-Evodiamine inhibits the proliferation of a wide variety of tumor cells by inducing their apoptosis.
  • HY-131096
    L-Proline 4-methoxy-β-naphthylamide hydrochloride

    H-Pro-4MβNA hydrochloride

    Others Cancer
    L-Proline 4-methoxy-β-naphthylamide hydrochloride (H-Pro-4MβNA hydrochloride) can be used for Fap-activated anti-tumor compounds preparaction.
  • HY-14617
    Paradol

    [6]-Gingerone; [6]-Paradol

    COX Cancer
    Paradol is a pungent phenolic substance found in ginger and other Zingiberaceae plants. Paradol is an effective inhibitor of tumor promotion in mouse skin carcinogenesis, binds to cyclooxygenase (COX)-2 active site.
  • HY-111838A
    ZZW-115 hydrochloride

    Apoptosis Cancer
    ZZW-115 hydrochloride is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 hydrochloride induces tumor cell death by necroptosis and apoptosis. Anticancer activity.
  • HY-111838
    ZZW-115

    Apoptosis Cancer
    ZZW-115 is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 induces tumor cell death by necroptosis and apoptosis. Anticancer activity.
  • HY-145443
    Fludarabine-Cl

    Others Cancer
    Fludarabine-Cl has inhibition effect on RNA adenosine deaminase 1(ADAR1), and can be used for preventing and/or treating cancer or tumor-related diseases.
  • HY-W024604
    4,4-Dimethyl-2-cyclopenten-1-one

    4,4-Dimethylcyclopent-2-enone

    Others Cancer
    4,4-Dimethyl-2-cyclopenten-1-one, a natural compound from Apocyniveneti Folium, displays higher tumor-specific cytotoxicity.
  • HY-132995
    DP-1

    Drug Metabolite Others
    DP-1, a degradation product of SDC-TRAP-0063, is a fragment of Ganetespib. Ganetespib is a heat shock protein 90 (HSP90) inhibitor with anti-tumor activity.
  • HY-14429
    (-)-Irofulven

    MGI 114; 6-Hydroxymethylacylfulvene; NSC 683863

    DNA Alkylator/Crosslinker Apoptosis Cancer
    (-)-Irofulven (MGI 114), an Illudin S analog, is a DNA alkylating agent. (-)-Irofulven inhibits the replication of DNA, induces tumor cells apoptosis, and has potent antitumor activity.
  • HY-N10408
    Tripchlorolide

    Apoptosis Autophagy Cancer Neurological Disease
    Tripchlorolide is a neuroprotective agent that can be found in Tripterygium wilfordii. Tripchlorolide prevents tumor growth by inducing apoptosis and autophagy. Tripchlorolide improves cognitive deficits in Alzheimer's disease.
  • HY-W008469
    2-Fluoroadenine

    DNA/RNA Synthesis Cancer
    2-Fluoroadenine is a toxic purine bases. 2-Fluoroadenine has toxicity in nonproliferating and proliferating tumor cells. 2-Fluoroadenine can be used for researching anticancer.
  • HY-100395
    F16

    Apoptosis Cancer
    F16 is a potent growth inhibitor of the neu-overexpressing cells and also selectively inhibits proliferation of mammary epithelial as well as a variety of mouse mammary tumor and human breast cancer cell lines.
  • HY-18295
    Erteberel

    LY500307

    Estrogen Receptor/ERR Neurological Disease
    Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. Anti-tumor activities.
  • HY-114277A
    Sotorasib racemate

    AMG-510 racemate

    Ras Cancer
    Sotorasib (AMG-510) racemate is the racemate of Sotorasib (AMG-510). AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity.
  • HY-N6892
    3'-​O-​Acetylhamaudol

    Others Cancer
    3'-O-Acetylhamaudol, isolated from Angelica japonica roots, exhibits anti-tumor activity through dual actions, anti-angiogenesis and intestinal intraepithelial lymphocyte activation.
  • HY-135152
    CYPMPO

    Others Cancer
    CYPMPO is a spin-trapping reagent. CYPMPO, a cyclic DEPMPO-type nitrone, is evaluated for spin-trapping capabilities toward hydroxyl and superoxide radicals. anti-oxidant and anti-tumor activity.
  • HY-117253
    PHA-782584

    Drug Metabolite Cancer
    PHA-782584 is a metabolite of sunitinib. Sunitinib is an oral multitargeted tyrosine kinase inhibitor with antitumor activities.
  • HY-132832
    Sirpiglenastat

    DRP-104

    Others Cancer
    Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.
  • HY-13538
    Gemcitabine elaidate

    CP-4126; CO-101; Gemcitabine 5'-elaidate

    Nucleoside Antimetabolite/Analog Autophagy Apoptosis Cancer
    Gemcitabine elaidate (CP-4126) is lipophilic pro-drug of Gemcitabine. Gemcitabine elaidate is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate exhibits anti-tumor activity.
  • HY-145598
    Sovleplenib

    HMPL-523

    Syk Cancer
    Sovleplenib (HMPL-523) is a highly potent, orally available and selective SYK inhibitor with an IC50 of 25 nM. Anti-tumor activity. Sovleplenib can be used for the research of immune thrombocytopenia (ITP).
  • HY-136447
    ASP4132

    AMPK Cancer
    ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.
  • HY-129180
    XY028-133

    PROTACs CDK Cancer
    XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for von Hippel-Lindau and CDK.
  • HY-124584S
    Minnelide-d3

    Apoptosis Cancer
    Minnelide-d3 is the deuterium labeled Minnelide. Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide promotes apoptosis.
  • HY-N4127
    3'-Demethylnobiletin

    Others Cancer
    3'-Demethylnobiletin, a derivative of Nobiletin, is a polymethoxyflavonoid in citrus fruits. Nobiletin exhibits anticancer activity and inhibits tumor angiogenesis by regulating Src, FAK, and STAT3 signaling.
  • HY-N6958
    2-O-β-D-Glucopyranosyl-L-ascorbic acid

    AA-2βG

    Others Cancer Metabolic Disease
    2-O-β-D-Glucopyranosyl-L-ascorbic acid (AA-2βG), isolated from Lycium Fruit, is a stable vitamin C analog with anti-tumor activity.
  • HY-143320
    STING agonist-17

    STING Cancer
    STING agonist-17 (compound 4a) is a potent STING agonist with an IC50 value of 0.062 nM. STING agonist-17 has anti-cancer activity for tumor immunization.
  • HY-13538A
    Gemcitabine elaidate hydrochloride

    CP-4126 hydrochloride; CO-101 hydrochloride; Gemcitabine 5'-elaidate hydrochloride

    Nucleoside Antimetabolite/Analog Autophagy Apoptosis Cancer
    Gemcitabine elaidate (CP-4126) hydrochloride is lipophilic pro-drug of Gemcitabine. Gemcitabine elaidate hydrochloride is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate hydrochloride exhibits anti-tumor activity.
  • HY-110244
    Tilfrinib

    Others Cancer
    Tilfrinib (compound 4f) is a potent and selective inhibitor of breast tumor kinase (Brk) with an IC50 of 3.15 nM, which displays anti-proliferative activity and acts as a promising antitumor agent.
  • HY-B1436S1
    Nifuroxazide-13C6

    STAT Bacterial Antibiotic Cancer Infection
    Nifuroxazide-13C6 is the 13C6 labeled Nifuroxazide. Nifuroxazide is an effective inhibitor of STAT3, also exerts potent anti-tumor and anti-metastasis activity.
  • HY-40136S
    cis-4-Hydroxy-L-proline-d3

    Endogenous Metabolite
    cis-4-Hydroxy-L-proline-d3 is the deuterium labeled cis-4-Hydroxy-L-proline. cis-4-Hydroxy-L-proline, a proline analogue, is an inhibitor of collagen production. cis-4-Hydroxy-L-proline could inhibit fibroblast growth by preventing the deposition of triple-helical collagen on the cell layer. cis-4-Hydroxy-L-proline also depresses the growth of primary N-nitrosomethylurea-induced rat mammary tumors.
  • HY-146366
    Tubulin inhibitor 26

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight.
  • HY-W009732
    Sinapinic acid

    Sinapic acid

    HDAC Angiotensin-converting Enzyme (ACE) Reactive Oxygen Species Apoptosis Cancer Metabolic Disease
    Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM, and also inhibits ACE-I activity. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells. Sinapinic acid shows antioxidant and antidiabetic activities. Sinapinic acid reduces total cholesterol, triglyceride, and HOMA-IR index, and also normalizes some serum parameters of antioxidative abilities and oxidative damage in ovariectomized rats.
  • HY-101115
    PI3K-IN-6

    PI3K Cancer
    PI3K-IN-6 (compound 20a) is an oral active and highly selective phosphoinositide 3-kinase (PI3K) β/δ inhibitor, with IC50 values of 7.8 nM/5.3 nM for PI3K β/δ, respectively. PI3K-IN-6 (compound 20a) has potential top treat phosphatase and tensin homolog (PTEN) feficient tumors.
  • HY-13208
    Xevinapant hydrochloride

    AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride

    IAP Cancer
    Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors.
  • HY-101150
    DGN462

    DNA Alkylator/Crosslinker Cancer
    DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML). DGN462 can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
  • HY-13547
    ADPM06

    Apoptosis Cancer
    ADPM06, a lead candidate azadipyrromethene, is a novel nonporphyrin photodynamic therapeutic (PDT) agent. ADPM06 exhibits IC50 values in the micro-molar range in human tumor cells and induces apoptosis.
  • HY-101150A
    sulfo-DGN462 sodium

    DNA Alkylator/Crosslinker ADC Cytotoxin Cancer
    sulfo-DGN462 sodium is degraded to DGN462 in culture medium and plasma. DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML).
  • HY-10822
    Idetrexed

    BGC 945; ONX-0801

    Thymidylate Synthase Others
    Idetrexed is a thymidylate synthase inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylate synthase with a Ki of 1.2 nmol/L.
  • HY-136640
    BCL6-IN-4

    Bcl-2 Family Cancer
    BCL6-IN-4 is a potent B-cell lymphoma 6 (BCL6) inhibitor with an IC50 of 97 nM. BCL6-IN-4 has anti-tumor activities.
  • HY-16126
    Carboxyamidotriazole

    L-651582; CAI

    Calcium Channel Cancer Inflammation/Immunology
    Carboxyamidotriazole (L-651582) is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole shows anti-tumor, anti-inflammatory and antiangiogenic effects.
  • HY-N1451
    Betulonic acid

    Betunolic acid; Liquidambaric acid; (+)-Betulonic acid

    Parasite HSV Cancer Infection Inflammation/Immunology
    Betulonic acid (Betunolic acid), a naturally occurring triterpene, is found in many plants. Betulonic acid has anti-tumor, anti-inflammatory, antiparasitic and anti-viral (HSV-1) activities.
  • HY-N6644
    Crocin III

    Others Cancer Inflammation/Immunology
    Crocin III is a crocetin from saffron (Crocus sutivus L.). Crocetins inhibit cell growth of tumor cells and has anti-inflammatory activity. Crocins serve as spices and coloring agents.
  • HY-14949
    Cevipabulin

    TTI-237

    Microtubule/Tubulin Cancer
    Cevipabulin (TTI-237) is an oral, microtubule-active antitumor compound and inhibits the binding of [ 3H] vinblastine to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line.
  • HY-114228
    PROTAC BET degrader-2

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
  • HY-129188
    CCT369260

    Bcl-2 Family Cancer
    CCT369260 (compound 1) is an orally avtive B-cell lymphoma 6 (BCL6) inhibitor with anti-tumor activity. CCT369260 (compound 1) exhibits an IC50 of 520 nM.
  • HY-15649
    UNC1215

    Histone Methyltransferase Apoptosis Cancer
    UNC1215 is a potent and selective inhibitor for the methyllysine (Kme) reading domain function of L3MBTL3 with a Kd value of 120 nM and an IC50 of 40 nM. UNC1215 has the potential to treat malignant brain tumor.
  • HY-139399
    JNJ-67856633

    MALT1 Cancer
    JNJ-67856633 is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. JNJ-67856633 in some cases lead to tumor stasis.
  • HY-P99040
    Onvatilimab

    JNJ-61610588

    PD-1/PD-L1 Cancer
    Onvatilimab (JNJ-61610588) is a human IgG1κ anti-VISTA (V-domain Ig Suppressor of T-cell Activation) monoclonal antibody. Onvatilimab has an anti-tumor activity.
  • HY-P1599
    Valorphin

    Opioid Receptor Cancer Neurological Disease
    Valorphin is an endogenous hemoglobin β-chain (33-39) fragment with opioid analgesic activity, binds to rat mu-opioid receptor, with an IC50 of 14 nM; Valorphin also shows anti-tumor activity.
  • HY-113303
    FAPy-adenine

    Endogenous Metabolite Cancer Neurological Disease
    FAPy-adenine is an oxidized DNA base. Fapy-adenine shows an increased trend levels in the Alzheimer's disease brain. Oxidized nucleosides are biochemical markers for tumors, aging, and neurodegenerative diseases.
  • HY-147902
    VEGFR-2-IN-24

    VEGFR Cancer
    VEGFR-2-IN-24 is a potent VEGFR-2 inhibitor with IC50 value of 0.22 µM. VEGFR-2-IN-24 can be used for tumor research.
  • 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-N10332
    Leptosphaerodione

    Proteasome Cancer
    Leptosphaerodione, isolated from Remotididymella sp. Fungus, is a potent ubiquitin-proteasome system (UPS) inhibitor. Leptosphaerodione exhibits cytotoxicity in HeLa cells with IC50 value of 3.2 μM. Anti-tumor agent.
  • HY-N6932
    Voacamine

    Cannabinoid Receptor P-glycoprotein Cancer Metabolic Disease
    Voacamine, an indole alkaloid, exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.
  • HY-108623
    Atizoram

    CP-80,633

    Phosphodiesterase (PDE) Inflammation/Immunology
    Atizoram (CP-80,633), a cyclic nucleotide phosphodiesterase (PDE4) inhibitor, elevates plasma cyclic AMP levels and decreases tumor necrosis factor-α (TNFα) production in mice.
  • HY-122493
    Illudin M

    DNA Alkylator/Crosslinker Apoptosis Cancer
    Illudin M is a cytotoxic fungal sesquiterpene that can be isolated from the culture medium of Omphalotus olearius mushrooms. Illudin M can alkylate DNA. Illudin M has anti-tumor activities.
  • HY-13603
    Crolibulin

    EPC2407

    Microtubule/Tubulin Apoptosis Cancer
    Crolibulin (EPC2407) is a tubulin polymerization inhibitor, with potent apoptosis induction and cell growth inhibition. Crolibulin has anti-tumor activity. Crolibulin also has cardiovascular toxicity and neurotoxicity.
  • HY-N2490
    Dehydrotrametenolic acid

    Caspase Apoptosis Cancer Inflammation/Immunology
    Dehydrotrametenolic acid is a sterol isolated from the sclerotium of Poria cocos. Dehydrotrametenolic acid induces apoptosis through caspase-3 pathway. Dehydrotrametenolic acid has anti-tumor activity, anti-inflammatory, anti-diabetic effects.
  • HY-150753
    RS6212

    Lactate Dehydrogenase Cancer
    RS6212 is a specific LDH (lactate dehydrogenase) inhibitor with an IC50 value of 12.03 μM . RS6212 inhibits tumor growth and exhibits potent anticancer activity in multiple cancer cell lines.
  • HY-N9339
    Norglaucine

    (+)-Norglaucine

    Others Cancer
    Norglaucine ((+)-Norglaucine), a cytotoxic alkaloid, exhibits cytotoxicity towards the tumor cell lines B16-F10, HepG2, K562 and HL-60 cells.
  • HY-B2230
    Hinokitiol

    β-Thujaplicin

    Keap1-Nrf2 DNA Methyltransferase Virus Protease Cancer Infection
    Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases DNMT1 and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities.
  • HY-16062
    ARQ 621

    Kinesin Cancer
    ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity. ARQ 621 is a kinesin inhibitor.
  • HY-10529
    Betulinic acid

    Lupatic acid; Betulic acid

    Apoptosis Topoisomerase HIV Autophagy Mitophagy NF-κB Endogenous Metabolite Cancer Infection Inflammation/Immunology
    Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties.
  • HY-N0103A
    Sophocarpine monohydrate

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine (monohydrate) significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-123938
    CYH33

    PI3K Cancer
    CYH33 is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 has potent activity against solid tumors.
  • HY-N0103
    Sophocarpine

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-140455
    Azido-PEG10-acid

    PROTAC Linkers Cancer
    Azido-PEG10-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-119109
    Laminaran

    Others Cancer
    Laminaran is an β-1-3-glucan and a typical ligand for Dectin-1 from Eisenia Bicyclis, has potent immunomodulating, radioprotective, and anticancer activities. Laminaran is made up of β (1→3)-glucan with β (1→6)-branches and can be catalyzed by enzymes such as laminarinase (EC 3.2.1.6) that breaks the β (1→3) bonds. Laminaran is a promising immune stimulatory molecule for use in cancer immunotherapy.
  • HY-140802
    Azido-PEG11-alcohol

    PROTAC Linkers Cancer
    Azido-PEG11-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-118620
    Nortriptyline

    Desmethylamitriptyline; Desitriptilina

    Autophagy Drug Metabolite Cancer Neurological Disease
    Nortriptyline (Desmethylamitriptyline), the main active metabolite of Amitriptyline, is a tricyclic antidepressant used to relieve the symptoms of depression. Nortriptyline is a potent autophagy inhibitor.
  • HY-133061
    Fluorescein-thiourea-PEG6-acid

    PROTAC Linkers Cancer
    Fluorescein-thiourea-PEG6-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-133006
    Fluorescein-PEG5-acid

    PROTAC Linkers Cancer
    Fluorescein-PEG5-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-N3023
    3,4-Dihydroxybenzylamine hydrobromide

    NSC 263475 hydrobromide

    DNA/RNA Synthesis Cancer
    3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells. 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity.
  • HY-W000838
    1-Hydroxyanthraquinone

    DNA/RNA Synthesis Cancer
    1-Hydroxyanthraquinone, a naturally occurring compound with oral activity from some plants like Tabebuia avellanedae, exhibits carcinogenic effect.
  • HY-B1417
    Nortriptyline hydrochloride

    Desmethylamitriptyline hydrochloride; Desitriptilina hydrochloride

    Autophagy Drug Metabolite Cancer Neurological Disease
    Nortriptyline hydrochloride (Desmethylamitriptyline hydrochloride), the main active metabolite of Amitriptyline, is a tricyclic antidepressant used to relieve the symptoms of depression. Nortriptyline hydrochloride is a potent autophagy inhibitor.
  • HY-140217
    Azido-PEG10-amine

    PROTAC Linkers Cancer
    Azido-PEG10-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • 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-120773
    Fmoc-PEG3-C2-NHS ester

    PROTAC Linkers Cancer
    Fmoc-PEG3-CH2CH2-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-N2254
    (-)-Oxypeucedanin hydrate

    (-)-Prangol

    Others Cancer
    (-)-Oxypeucedanin hydrate ((-)-Prangol) is a derivative of furocoumarin isolated from Ducrosia anethifolia.
  • HY-122459
    Fmoc-PEG5-NHS ester

    PROTAC Linkers Cancer
    Fmoc-PEG5-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-12419
    BMS-983970

    Notch Cancer
    BMS-983970 is an oral pan-Notch inhibitor for the treatment of multiplecancers.
  • HY-140801
    Azido-PEG10-alcohol

    PROTAC Linkers Cancer
    Azido-PEG10-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140218
    Azido-PEG11-amine

    PROTAC Linkers Cancer
    Azido-PEG11-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-130798
    (S,R,S)-AHPC-amido-C5-acid

    E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-amido-C5-acid incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design XY028-133 (HY-129180).
  • HY-19897
    4SC-203

    FLT3 VEGFR Cancer
    4SC-203 is a potent multikinase inhibitor with potential antineoplastic activity. 4SC-203 selectively FLT3/STK1, FLT3 mutated forms, and VEGFRs.
  • HY-12572
    TIE-2/VEGFR-2 kinase-IN-2

    VEGFR Cancer
    TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC50 values of 8.61 and 8.56, respectively. TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research.
  • HY-18307
    SYN1143

    c-Met/HGFR Cancer
    SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively. SYN1143 has weak inhibitory activity on Lck, Tie2, Src, and BTK with IC50s ranging from 160 to 710 nM. SYN1143 can be used for the research of cancers that RON and c-Met are activated.
  • HY-126881
    Fmoc-PEG2-C2-NHS ester

    PROTAC Linkers Cancer
    Fmoc-PEG2-CH2CH2-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-W013249
    Boc-piperazine-benzoic acid

    PROTAC Linkers Cancer
    Boc-piperazine-benzoic acid is a PROTAC linker and can be used in the synthesis of PROTACs, such as PROTAC androgen receptor (AR) degrader ARD-2128 (HY-13229).
  • HY-W010764
    Biotin-PEG2-Mal

    PROTAC Linkers Cancer
    Biotin-PEG2-Mal is a PEG-based PROTAC linker can be used in the synthesis of PROTAC.
  • HY-122456
    Fmoc-PEG4-NHS ester

    PROTAC Linkers Cancer
    Fmoc-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-130077
    Fmoc-PEG1-CH2CH2-NHS ester

    PROTAC Linkers Cancer
    Fmoc-PEG1-CH2CH2-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140759
    Azido-PEG10-NHS ester

    PROTAC Linkers Cancer
    Azido-PEG10-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-16069A
    Tucatinib hemiethanolate

    Irbinitinib hemiethanolate; ARRY-380 hemiethanolate; ONT-380 hemiethanolate

    EGFR Cancer
    Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
  • HY-D1342
    Coumberol

    Others Cancer
    Coumberol is a fluorescent substrate of AKR1C3 protein. Coumberol can be used for the research of AKR1C3.
  • HY-126882
    Fmoc-PEG6-NHS ester

    PROTAC Linkers Cancer
    Fmoc-PEG6-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-125506
    NP-G2-044

    Others Cancer
    NP-G2-044 is a potent, orally active fascin inhibitor, with an IC50 of ~2 μM. NP-G2-044 blocks tumor metastasis and increases antitumor immune response.
  • HY-N6601
    Pomolic acid

    Randialic acid A

    Apoptosis Cancer
    Randialic acid A (Pomolic acid) is a pentacyclic triterpene isolated from Euscaphis japonica (Tunb.). Randialic acid A (Pomolic acid) inhibits tumor cells growth and induces cell apoptosis. Randialic acid A (Pomolic acid) has a potential for the treatment of prostate cancer (PC).
  • HY-101194
    Tin-protoporphyrin IX

    SnPPIX; Stannous protoporphyrin IX

    Reactive Oxygen Species Cancer
    Tin-protoporphyrin IX (SnPPIX) is a potent Heme oxygenase-1 (HO-1) inhibitor. Tin-protoporphyrin IX (SnPPIX) sensitizes pancreatic ductal adenocarcinoma (PDAC) tumors to chemotherapy in mice model.
  • HY-114244
    USL311

    CXCR Cancer Endocrinology
    USL311 is a selective CXCR4 antagonist, with anti-tumor activity. USL311 prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.
  • HY-137471
    RBPJ Inhibitor-1

    RIN1

    Notch Cancer
    RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.
  • HY-147812
    POLA1 inhibitor 1

    Others Cancer
    POLA1 inhibitor 1 (Compound 12) is an orally active POLA1 inhibitor. POLA1 inhibitor 1 shows antitumor activity against several tumor histotypes and Adarotene-resistant cell line.
  • HY-135145
    CB-103

    Notch Cancer
    CB-103 is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. CB-103 has anti-tumor activity.
  • HY-N6990
    Anhydrosecoisolariciresinol

    Others Cancer
    Anhydrosecoisolariciresinol is from the flower of Wedelia biflora, has anti-tumor activities. Anhydrosecoisolariciresinol decreases the growth of human breast cancer MCF-7 and MDA-MB-231 cell lines.
  • 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-143586
    CDK7-IN-8

    CDK Cancer
    CDK7-IN-8 is a potent CDK7 inhibitor with IC50 of 54.29 nM. CDK7-IN-8 has inhibitory effect on certain cancer cells and in vivo tumor models.
  • HY-B0311A
    Carbidopa monohydrate

    (S)-(-)-Carbidopa monohydrate

    Aryl Hydrocarbon Receptor Cancer Neurological Disease
    Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth.
  • HY-N0250
    Saikosaponin D

    STAT NF-κB Estrogen Receptor/ERR Bacterial Cancer Infection Inflammation/Immunology
    Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.
  • HY-129600
    MYCi361

    NUCC-0196361

    c-Myc Cancer
    MYCi361 (NUCC-0196361) is a MYC inhibitor with the Kd of 3.2 μM for binding to MYC. MYCi361 (NUCC-0196361) suppresses tumor growth and enhances anti-PD1 immunotherapy.
  • HY-77554
    Cephalomannine

    Microtubule/Tubulin Cancer
    Cephalomannine is a Paclitaxel (HY-B0015) alkaloidal analog and isolated from most Cephalotaxus species. Cephalomannine is an orally active anti-tumor agent and can be used as a chemotherapy agent for cancer research.
  • HY-B0311
    Carbidopa

    (S)-(-)-Carbidopa

    Aryl Hydrocarbon Receptor Cancer Neurological Disease
    Carbidopa ((S)-(-)-Carbidopa), a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth.
  • HY-146615
    Axl-IN-6

    TAM Receptor Cancer
    Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model.
  • HY-14949C
    Cevipabulin fumarate

    TTI-237 fumarate

    Microtubule/Tubulin Cancer
    Cevipabulin fumarate (TTI-237 fumarate) is an oral, microtubule-active, antitumor compound and inhibits the binding of [ 3H]NSC 49842 to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line.
  • HY-128595
    MT-4

    Others Cancer
    MT-4 blocks the TG2/FN complex at the interface between cancer cells and the tumor niche. MT-4 inhibits the adhesion of ovarian cancer (OC) cells to the peritoneum.
  • HY-119874
    Alkannin

    Ras Cancer Inflammation/Immunology
    Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2). Alkannin does not inhibit PKM1 and pyruvate kinase-L (PKL). Alkannin acts as a potential anticancer agent.
  • HY-N2357
    Eudesmin

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

    Ribosomal S6 Kinase (RSK) Cancer Infection Metabolic Disease Inflammation/Immunology
    Eudesmin ((-)-Eudesmin) impairs adipogenic differentiation via inhibition of S6K1 signaling pathway. Eudesmin possesses diverse therapeutic effects, including anti-tumor, anti-inflammatory, and anti-bacterial activities.
  • HY-133141
    DI-87

    Others Cancer
    DI-87 is an orally active and selective deoxycytidine kinase (dCK) inhibitor with an EC50 of 10.2 nM. DI-87 has antitumor activity and is used in combination therapy against tumors expressing dCK.
  • HY-N0405
    Orientin

    Others Cancer Neurological Disease
    Orientin is a naturally occurring bioactive flavonoid that possesses diverse biological properties, including anti-inflammation, anti-oxidative, anti-tumor, and cardio protection. Orientin is a promising neuroprotective agent suitable for therapy for neuropathic pain.
  • HY-111192
    IPR-803

    Ser/Thr Protease Cancer
    IPR-803 is a potent inhibitor of the uPAR•uPA protein-protein interaction (PPI). IPR-803 binds directly to uPAR with sub-micromolar affinity. IPR-803 displays anti-tumor activity.
  • HY-P1404
    R8-T198wt

    Pim Cancer
    R8-T198wt is a cell-permeable carboxyl-terminal p27 Kip1 peptide exhibits anti-tumor activity by inhibiting Pim-1 kinase.
  • HY-N0769
    Isopimpinellin

    DNA/RNA Synthesis Parasite Cancer Infection Inflammation/Immunology
    Isopimpinellin, an orally active compound isolated from the roots of Pimpinella saxifrage. Isopimpinellin blocks DNA adduct formation and skin tumor initiation by 7,12-dimethylbenz[a]anthracene. Isopimpinellin possesses anti-leishmania effect.
  • HY-126379
    CDDO-2P-Im

    Apoptosis Cancer
    CDDO-2P-Im is an analogue of CDDO-Imidazolide with chemopreventive effect. CDDO-2P-Im can reduce the size and the severity of the lung tumors in mouse lung cancer model.
  • HY-108472
    Loxoribine

    7-Allyl-8-oxoguanosine; RWJ 21757

    Toll-like Receptor (TLR) Influenza Virus Cancer Infection
    Loxoribine (7-Allyl-8-oxoguanosine) is a guanosine analog with anti-viral and anti-tumor activities. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist.
  • HY-130803
    5-Methyl-5,6-dihydrouridine

    Others Cancer
    5-Methyl-5,6-dihydrouridine is a minor constituent in the chromosomal RNA of the rat ascites tumor. 5-Methyl-5,6-dihydrouridine can be used for nucleic acid modification.
  • HY-Y0892
    4-Hydroxybenzyl alcohol

    Apoptosis Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    4-Hydroxybenzyl alcohol is a phenolic compound widely distributed in various kinds of plants. Anti-inflammatory, anti-oxidant, anti-nociceptive activity. Neuroprotective effect. Inhibitor of tumor angiogenesis and growth.
  • HY-123691
    7-O-Demethyl rapamycin

    Fungal Cancer Infection Inflammation/Immunology
    7-O-Demethyl rapamycin, a derivative of Rapamycin (HY-10219), has antifungal activity and immunosuppressant properties. 7-O-Demethyl rapamycin has useful tumor cell growth-inhibiting activity.
  • HY-N10265
    Stephacidin B

    Endogenous Metabolite Cancer
    Stephacidin B is a fungal metabolite. Stephacidin B shows in vitro cytotoxicity against a panel of human tumor cell lines. Stephacidin B shows the strongest cytotoxicity against testosterone-dependent prostate LNCaP cancer cells.
  • HY-N1984
    Artemisic acid

    Qing Hao acid; Artemisinic acid; Arteannuic acid

    Bacterial Cancer Infection Metabolic Disease Inflammation/Immunology
    Artemisinic acid (Qing Hao acid), an amorphane sesquiterpene isolated from Artemisia annua L., possesses a variety of pharmacological activity, such as antimalarial activity, anti-tumor activity, antipyretic effect, antibacterial activity, allelopathy effect and anti-adipogenesis effect.
  • HY-U00447
    PK11000

    MDM-2/p53 DNA Alkylator/Crosslinker Cancer
    PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities.
  • HY-100763
    Mcl1-IN-12

    Bcl-2 Family Cancer
    Mcl1-IN-12 (Compound F) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively. Anti-tumor activity.
  • HY-111320
    Chrysomycin B

    Bacterial Antibiotic Cancer
    Chrysomycin B is an antibiotic isolated from a strain of Streptomyces. Chrysomycin B causes DNA damage in the human lung adenocarcinoma A549 cell line and inhibits topoisomerase II. Chrysomycin B suppresses the growth of transplantable tumors in mice.
  • HY-150782
    UNC-CA359

    EGFR Cancer
    UNC-CA359 is a potent epidermal growth factor receptor (EGFR) inhibitor, with an IC50 value of 18 nM. UNC-CA359 exhibits strong anti-tumor activity, can be used to Chordoma research.
  • HY-123938A
    CYH33 methanesulfonate

    PI3K Cancer
    CYH33 methanesulfonate is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 methanesulfonate inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 methanesulfonate has potent activity against solid tumors.
  • HY-144769
    SDOX

    Topoisomerase Cancer
    SDOX is the Doxorubicin (DOX) prodrug. The loaded DOX prodrugs (SDOX) which can release the parent drugs DOX triggered by excessive GSH in tumor cells, minimize the unexpected side effects on normal tissues without compromising the potency.
  • HY-131446
    Chk1-IN-5

    Checkpoint Kinase (Chk) Cancer
    Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.
  • HY-13540
    E7016

    GPI 21016

    PARP Cancer
    E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent.
  • HY-111183
    Neocarzinostatin

    DNA/RNA Synthesis Bacterial Apoptosis Antibiotic Cancer Infection
    Neocarzinostatin, a potent DNA-damaging, anti-tumor antibiotic, recognizes double-stranded DNA bulge and induces DNA double strand breaks (DSBs). Neocarzinostatin induces apoptosis. Neocarzinostatin has potential for EpCAM-positive cancers treatment .
  • HY-115948
    Antitumor agent-46

    Others Cancer
    Antitumor agent-46 (Compound 2h) is an anti-tumor agent. Antitumor agent-46 demonstrates markedly higher antiproliferative activity on MCF-7 cells with an IC50 value of 2.08 µM.
  • HY-N7766
    Rubropunctatin

    Apoptosis Cancer Inflammation/Immunology
    Rubropunctatin, an orange azaphilone pigment, is isolated from the extracts of Monascus pilosus-fermented rice (red-mold rice). Rubropunctatin has anti-inflammatory, immunosuppressive and antioxidative effects, and also exhibits anti-tumor activity.
  • HY-P1687
    Siomycin A

    Bacterial Apoptosis Cancer
    Siomycin A is a thiopeptide antibiotic and is a Forkhead box M1(FOXM1) selective inhibitor without affecting other members of the Forkhead box family. Siomycin A has anti-tumor and promotes apoptosis.
  • HY-135829
    BAY 2416964

    Aryl Hydrocarbon Receptor Cancer
    BAY 2416964 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. BAY 2416964 has the potential for solid tumors treatment.
  • HY-N6772
    Cytochalasin E

    Autophagy Cancer
    Cytochalasin E, an epoxide containing Aspergillus-derived fungal metabolite, inhibits angiogenesis and tumor growth. Cytochalasin E is a potent actin depolymerization agent, and it binds and caps the barbed end of actin filaments to prevent actin elongation.
  • HY-106014
    Tezacitabine

    DNA/RNA Synthesis Nucleoside Antimetabolite/Analog Apoptosis Cancer
    Tezacitabine is a cytostatic and cytotoxic antimetabolite and a nucleoside analogue. Tezacitabine irreversibly inhibits the ribonucleotide reductase and interferes with DNA replication and repair. Tezacitabine effectively induces cells apoptotic. Tezacitabine has the potential for leukemias and solid tumors (carcinomas) treatment.
  • HY-107593
    PS-1145 dihydrochloride

    IKK Inflammation/Immunology
    PS-1145 (dihydrochloride) is a potent IκB kinase-2 inhibitor with an IC50 value of 88 nM. PS-1145 (dihydrochloride) inhibits activity of NF-κB by blocking IκB kinase phosphorylation in tumor-bearing rats.
  • 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-143256
    Enpp-1-IN-12

    Phosphodiesterase (PDE) Cancer
    Enpp-1-IN-12 (compound 43) is a potent and orally active ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor, with a Ki of 41 nM. Enpp-1-IN-12 exhibits anti-tumor activity.
  • HY-N2135
    Puerarin 6''-O-Xyloside

    Apoptosis Cancer Inflammation/Immunology
    Puerarin 6''-O-Xyloside, isolated from radix of Pueraria lobata (Willd.), possesses snti-osteoporotic and anti-tumor activity. Puerarin 6''-O-Xyloside induces the mitochondria-mediated apoptosis pathway..
  • HY-N5106
    (E)-Flavokawain A

    Apoptosis Cancer
    (E)-Flavokawain A, a chalcone extracted from Kava, has anticarcinogenic effect. (E)-Flavokawain A induces apoptosis in bladder cancer cells by involvement of bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice.
  • HY-146048
    Antitumor agent-57

    Apoptosis Reactive Oxygen Species Cancer
    Antitumor agent-57 (Compound 3o) is an NQO1-directed antitumor agent. Antitumor agent-57 inhibits tumor cell growth, triggers ROS generation and induces cell apoptosis.
  • HY-N6782
    Oligomycin

    ATP Synthase Fungal Antibiotic Cancer Infection
    Oligomycin, an antifungal antibiotic, is an inhibitor of H +-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells.
  • HY-100846
    JQEZ5

    Histone Methyltransferase Cancer
    JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitive inhibition of polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects.
  • 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-144217
    SKLB-197

    ATM/ATR Cancer
    SKLB-197 showed an IC50 value of 0.013 μM against ATR but very weak or no activity against other 402 protein kinases. It displayed potent antitumor activity against ATM-deficent tumors both in vitro and in vivo.
  • HY-124778
    SW106065

    Apoptosis Cancer
    SW106065 is an apoptosis inducer in malignant peripheral nerve sheath tumors (MPNST). SW106065 inhibits ATP consumption of sMPNST and other models of MPNST with an EC50 of 1 µM. SW106065 can be used for MPNST research.
  • HY-147699
    FRα-IN-1

    Antifolate Cancer
    FRα-IN-1 (Compound 4) is a tumor-targeting agent. FRα-IN-1 shows selective anticancer activity towards folate receptors (FRα and FRβ) expression cells.
  • HY-111145
    RD162

    Androgen Receptor Cancer
    RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer.
  • HY-N5058
    Dehydroeffusol

    Apoptosis Cancer
    Dehydroeffusol is a phenanthrene from medicinal herb Juncus effuses. Dehydroeffusol inhibits gastric cancer cell growth and tumorigenicity by selectively inducing tumor-suppressive endoplasmic reticulum stress and a moderate apoptosis. It shows very low toxicity.
  • HY-12875
    BQU57

    Ras Cancer
    BQU57 shows selective inhibition for Ral relative to Ras or Rho and inhibit xenograft tumor growth similar to depletion of Ral by siRNA. The IC50 for BQU57 of 2.0 μM in H2122 and 1.3 μM in H358.
  • HY-N1333
    Rubioncolin C

    NF-κB Cancer
    Rubioncolin C exerts anti-tumor activity by inducing apoptotic and autophagic Cell Death and inhibiting the NF-κB and Akt/mTOR/P70S6K Pathway in Human Cancer Cells.
  • HY-W014004
    m-Carboxycinnamic acid bishydroxamide

    CBHA

    HDAC Cancer
    m-Carboxycinnamic acid bishydroxamide is a potent HDAC inhibitor, exhibiting ID50 values of 10 and 70 nM in vitro for HDAC1 and HDAC3, respectively. m-Carboxycinnamic acid bishydroxamide also induces apoptosis and suppresses tumor growth.
  • HY-N3085
    Phellamurin

    P-glycoprotein Apoptosis Cancer Metabolic Disease
    Phellamurin is a plant flavonone glycoside from the leaves of Phellodendron amurense and inhibits intestinal P-glycoprotein. Phellamurin also inhibits egg laying by Papilio protenor. Phellamurin induces cells apoptosis and has anti-tumor activity.
  • HY-107981
    LSN 3213128

    Antifolate Cancer
    LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity.
  • HY-146250
    Antitumor agent-71

    Microtubule/Tubulin Cancer
    Antitumor Agent-71 is an antiproliferative activity antitumor agent and against tumor cell lines with IC50 values ranging from 3.98-15.70 μM. Antitumor Agent-71 is an antitumor agent that can inhibit tubulin polymerization.
  • HY-13326
    ASP3026

    ALK Apoptosis Cancer
    ASP3026 is a potent, selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 induces apoptosis of tumor cells. ASP3026 can be used for the research of non-small cell lung cancer (NSCLC).
  • HY-15734
    AGI-6780

    Isocitrate Dehydrogenase (IDH) Cancer
    AGI-6780 that potently and selectively inhibits the tumor-associated mutant IDH2 R140Q with IC50 of 23±1.7 nM. AGI-6780 is less potent against IDH2 WT with IC50 of 190±8.1 nM.
  • HY-115722
    (S)-(-)-MRJF22

    Others Cancer
    (S)-(-)-MRJF22 is haloperidol metabolite II valproate ester. (S)-(-)-MRJF22 exhibits the high antimigratory effects in endothelial and tumor cells. (S)-(-)-MRJF22 is a potential multifunctional agent against uveal melanoma.
  • HY-129055
    Isoeleutherin

    Fungal Inflammation/Immunology
    Isoeleutherin is a naphthopyran derivative isolated from E. americana Merr. Et Heyne with anti-fungal, anti-viral, and anti-tumor activities. Isoeleutherin plays an important role in selective modulation of T helper cell-mediated immune responses.
  • HY-112607
    Tubulin inhibitor 1

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.
  • HY-132980
    KRAS G12C inhibitor 19

    Ras Cancer
    KRAS G12C inhibitor 19 is a potent inhibitor of KRAS G12C. KRAS G12C inhibitor 19 significantly inhibits tumor growth (extracted from patent WO2021118877A1).
  • HY-10222
    Ixabepilone

    BMS-247550; Aza-epothilone B

    Microtubule/Tubulin Apoptosis Cancer
    Ixabepilone (BMS-247550) is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
  • HY-N7046
    Silybin B

    Amyloid-β Cancer Neurological Disease
    Silybin B, a flavonolignan separated from Silybum marianum, has anti-tumor activity. Silybin B is the most potent antifibrillogenic and anti-oligomeric component of silymarin and proposes it as a promising anti Alzheimer’s disease drug candidate.
  • HY-116506
    Bigelovin

    RAR/RXR Reactive Oxygen Species Apoptosis Autophagy Cancer
    Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.
  • HY-B1460B
    Sulconazole

    (±)-Sulconazole

    Fungal Cancer
    Sulconazole is a potent antifungal agent in the imidazole class. Sulconazole blocks the NF-κB/IL-8 signaling pathway and CSC (Cancer stem cells) formation. Sulconazole inhibits tumor growth, and can be used for breast cancer research.
  • HY-145289
    Antitumor agent-37

    Apoptosis Cancer
    Antitumor agent-37 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-37 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-37 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-37 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues.
  • HY-100513A
    Dehydroaltenusin

    Apoptosis DNA/RNA Synthesis Antibiotic Cancer
    Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM). Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis. Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo.
  • HY-145288
    Antitumor agent-36

    Apoptosis Cancer
    Antitumor agent-36 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-36 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-36 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-36 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues.
  • HY-124628
    IPI-9119

    Fatty Acid Synthase (FASN) Cancer
    IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models.
  • HY-N4121
    Isocurcumenol

    Estrogen Receptor/ERR Apoptosis Cancer
    Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1µg/mL and 178.2 µg/mL in DLA and KB cells, respectively.
  • HY-106382
    PMEDAP

    HIV CMV Cancer Infection
    PMEDAP is a potent inhibitor of human immunodeficiency virus (HIV) replication. PMEDAP has anti-murine cytomegalovirus (MCMV) activity. PMEDAP is a very potent inhibitor of Moloney murine sarcoma virus (MSV)-induced tumor formation and associated mortality.
  • HY-144655
    IP2

    Others Cancer
    IP2 is an immunomodulatory agent. IP2 increases PTP (Pioneer Translation Product)-derived antigen presentation in cancer cells. IP2 shows non-cytotoxic for cancer cells. IP2 induces tumor growth defects in mouse.
  • HY-13520
    Nocodazole

    Oncodazole; R17934

    Microtubule/Tubulin Bcr-Abl CRISPR/Cas9 Autophagy Apoptosis Cancer
    Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
  • HY-N0222
    Avicularin

    COX NF-κB PPAR ERK GLUT Apoptosis Cancer Infection Inflammation/Immunology Neurological Disease
    Avicularin is an orally active flavonoid. Avicularin inhibits NF κB (p65), COX 2 and PPAR γ activities. Avicularin has anti-inflammatory, anti-infectious anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities.
  • HY-N2463
    Kushenol E

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    Kushenol E is a class of flavonoids isolated from Sophora flavescens and is a non-competitive indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 of 7.7 µM and a Ki of 9.5 µM, has anti-tumor activity.
  • HY-N6674
    Diazepinomicin

    ECO-4601; TLN-4601; BU 4664L

    Ras Apoptosis Cancer
    Diazepinomicin (TLN-4601) is a secondary metabolite produced by Micromonospora sp. Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. An anti-tumor agent for K-Ras mutant models.
  • HY-146416
    Antitumor photosensitizer-2

    Others Cancer
    Antitumor photosensitizer-2 (Compound 11) is a potent photosensitizer. Antitumor photosensitizer-2 has outstanding photodynamic anti-tumor effects without obvious skin photo-toxicity, and can act as new drug candidates for photodynamic research.
  • HY-103018
    Gusacitinib

    ASN-002

    JAK Syk Cancer
    Gusacitinib (ASN-002) is an orally active and potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. Gusacitinib has anti-cancer activity in both solid and hematological tumor types.
  • HY-150979
    Gd-NMC-3

    Others Cancer
    Gd-NMC-3 is a near-infrared fluorescence/magnetic resonance (NIRF/MR) bimodal imaging probe. Gd-NMC-3 shows high resolution and sensitivity in tumor imaging with good biocompatibility, indicating huge application potential.
  • HY-146414
    Antitumor photosensitizer-1

    Others Cancer
    Antitumor photosensitizer-1 (Compound 8) is a potent photosensitizer. Antitumor photosensitizer-1 has outstanding photodynamic anti-tumor effects without obvious skin photo-toxicity, and can act as new drug candidates for photodynamic research.
  • 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-N6884
    Bixin

    Reactive Oxygen Species Cancer Inflammation/Immunology Cardiovascular Disease
    Bixin (BX), isolated from the seeds of Bixa orellana, is a carotenoid, possessing anti-inflammatory, anti-tumor and anti-oxidant activities. Bixin treatment ameliorated cardiac dysfunction through inhibiting fibrosis, inflammation and reactive oxygen species (ROS) generation.
  • HY-N0206
    Ardisiacrispin A

    Deglucocyclamin; LTS-4; Saxifragifolin B

    Others Cancer
    Ardisiacrispin A (Deglucocyclamin) is a common triterpenoid saponin from Ardisia species. Ardisiacrispin A has similar biological properties with some triterpenoid saponins in A. crenata which is one of the species of genus Ardisia and exhibits cytotoxic effect on tumor cells, immunomodulatory and antiviral activities.
  • HY-19792
    Mertansine

    DM1; Maytansinoid DM1

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC).
  • HY-100016
    AZD0156

    ATM/ATR Apoptosis Cancer
    AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis.
  • HY-N2995
    Poricoic acid A

    Poricoic acid A(F)

    Others Cancer
    Poricoic acid A, isolated from Poria cocos, possesses anti-tumor activity. Poricoic acid A enhances melatonin inhibition of AKI-to-CKD transition by regulating Gas6/AxlNFκB/Nrf2 axis.
  • HY-P99013
    Codrituzumab

    GC33; RO5137382

    Others Cancer
    Codrituzumab is a monoclonal antibody targeting GPC3 (glypican-3). GPC3 is an oncofetal protein expressed on the cell surface of hepatocellular carcinoma (HCC). Codrituzumab induces antibody-dependent cellular cytotoxicity (ADCC) and inhibits tumor growth.
  • HY-19542
    C6 Ceramide

    C6-Cer; N-Hexanoylsphingosine

    Apoptosis Cancer
    C6-ceramide, a ceramide pathway activator, shows activity against a variety of cancer cell lines. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects.
  • HY-130628
    PAK4-IN-1

    PAK Cancer
    PAK4-IN-1 (Compound 19) is a potent, selective, orally active PAK4 inhibitor with robust anti-tumor efficacy in vivo. PAK4-IN-1 is stable under both acidic and neutral conditions.
  • HY-147208
    MSC-4106

    YAP Cancer
    MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model.
  • HY-P1149
    Epitalon

    Epithalon; Epithalamin

    Telomerase Cancer Neurological Disease
    Epitalon is an anti-aging agent and a telomerase activator. Epitalon has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon can be used for cancer, old age and Retinitis Pigmentosa.
  • HY-N2040
    (20R)-Protopanaxadiol

    Bacterial Cancer Infection
    (20R)-Protopanaxadiol is a triterpenoid saponin metabolite of 20(R)-ginsenoside Rg3 in black ginseng. (20R)-Protopanaxadiol exhibits anti-tumor activity and cytotoxicity, and potently inhibits the growth of Helicobacter pylori.
  • HY-145261
    hDHODH-IN-8

    Lactate Dehydrogenase Inflammation/Immunology
    hDHODH-IN-8 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 of 16 nM. hDHODH-IN-8 has potent antiproliferative activity and excellent aqueous solubility. hDHODH-IN-8 has the potential for the research of tumor disease, especially lymphoma.
  • HY-130518
    AS-0141

    Cdc7-IN-6

    CDK Cancer
    AS-0141 (Cdc7-IN-6) is a potent Cdc7 kinase inhibitor (IC50=4 nM), extracted from patent WO2019165473A1, compound I- D, has anti-tumor activity.
  • HY-135967
    MTH1-IN-2

    DNA/RNA Synthesis Cancer
    MTH1-IN-2 is a MutT homolog 1 (MTH1) inhibitor extracted from patent WO2016135138A1, Compound (6), MTH1-IN-2 can be used for the research of cancer. Anti-tumor activity.
  • HY-A0037
    Lasofoxifene

    CP-336156

    Estrogen Receptor/ERR Cancer Inflammation/Immunology
    Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis.
  • HY-N0889
    Ginkgetin

    Wnt Apoptosis Autophagy Inflammation/Immunology Cancer
    Ginkgetin, a biflavone, is isolated from Ginkgo biloba leaves. Ginkgetin exhibit anti-tumor, anti-inflammatory, neuroprotective, anti-fungal activities. Ginkgetin is also a potent inhibitor of Wnt signaling, with an IC50 of 5.92 μΜ.
  • HY-103316A
    Ned 19

    Calcium Channel Cancer
    Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca 2+ signaling, with an IC50 of 65 nM. Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice.
  • HY-124036
    DS-7423

    PI3K mTOR Cancer
    DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM, 34.9 nM for PI3Kα and mTOR, respectively. DS-7423 possesses anti-tumor activity.
  • HY-130117
    AlbA-DCA

    Reactive Oxygen Species Apoptosis Cancer
    AlbA-DCA is a conjugate formed by the attachment of Albiziabioside A (AlbA) to a dichloroacetate acid (DCA) subunit. AlbA-DCA can induce a marked increase in intracellular ROS and alleviate the accumulation of lactic acid in tumor microenvironment (TME), and also selectively kills cancer cells and induce apoptosis.
  • HY-N0004
    Oridonin

    NSC-250682; Isodonol

    Akt Bacterial Cancer Infection Inflammation/Immunology
    Oridonin (NSC-250682), a diterpenoid isolated from Rabdosia rubescens, acts as an inhibitor of AKT, with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2; Oridonin possesses anti-tumor, anti-bacterial and anti-inflammatory effects.
  • HY-13675
    ME-143

    NV-143

    Endogenous Metabolite Cancer
    ME-143 is a second-generation tumor-specific inhibitor of NADH oxidase. ME-143 inhibits the WNT/β-catenin pathway in colorectal cancer cells. ME-143 has broadly active against cancers in vitro and in vivo.
  • HY-123055
    Adenosine dialdehyde

    Nucleoside Antimetabolite/Analog Cancer
    Adenosine dialdehyde, a purine nucleoside analogue, is a potent inhibitor of S-Adenosylhomocysteine hydrolase (SAHH) (Ki=3.3 nM). Adenosine Dialdehyde exhibits potent anti-tumor activity in vivo and can be used for the cancer research.
  • HY-114356
    BPI-9016M

    c-Met/HGFR Cancer
    BPI-9016M is a potent, orally active, and selective dual c-Met and AXL tyrosine kinases inhibitor. BPI-9016M suppresses tumor cell growth, migration and invasion of lung adenocarcinoma.
  • HY-135859
    NH2-MPAA-NODA

    Others Cancer
    NH2-MPAA-NODA is a nitroveratryl-based photocleavable linker, it has a NODA motif and a methyl phenyl acetic acid (MPAA) backbone. NH2-MPAA-NODA can be used as a radiolabel by labeling with 18F-fluoride.
  • HY-N0282
    Colcemid

    Demecolcine

    Microtubule/Tubulin Cancer Inflammation/Immunology
    Colcemid (Demecolcine), a derivative of colchicine, is a potent mitotic inhibitor. Colcemid binds to the protein tubulin and arrest cells in metaphase for karyotyping assays. Colcemid incuces cell apoptosis and can be used for cancer research.
  • HY-137813
    PERK-IN-4

    PERK Cancer Metabolic Disease Neurological Disease
    PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states.
  • HY-139458
    MDM2-IN-21

    MDM-2/p53 Cancer
    MDM2-IN-21 is a potent MDM2 inhibitor. MDM2-IN-21 can be used for the research of cancer.
  • HY-130845
    AR antagonist 1

    Ligands for E3 Ligase Cancer
    AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
  • HY-150620
    BI-0282

    MDM-2/p53 Cancer
    BI-0282 (Compound 1) is a potent MDM2-p53 interaction inhibitor.
  • HY-10014
    R547

    CDK GSK-3 Apoptosis Cancer
    R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.
  • HY-144304
    PROTAC EGFR degrader 2

    PROTACs EGFR Cancer
    PROTAC EGFR degrader 2 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC50 of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC.
  • HY-W019939
    Hydroxy-PEG10-Boc

    ADC Linkers Cancer
    Hydroxy-PEG10-Boc is extacted from patent CN108707228 (example 0024). Hydroxy-PEG10-Boc is a uncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Hydroxy-PEG10-Boc can be conjugated to Paclitaxel (HY-B0015) or docetaxel (HY-B0011).
  • HY-17381A
    Idarubicin

    4-Demethoxydaunorubicin

    Topoisomerase Bacterial Fungal Autophagy c-Myc DNA/RNA Synthesis Antibiotic Cancer Infection
    Idarubicin is an orally active and potent anthracycline antileukemic agent. Idarubicin inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin shows induction of DNA damage. Idarubicin inhibits DNA synthesis and of c-myc expression. Idarubicin inhibits the growth of bacteria and yeasts.
  • HY-17381
    Idarubicin hydrochloride

    4-Demethoxydaunorubicin hydrochloride

    Topoisomerase Bacterial Fungal Autophagy Antibiotic DNA/RNA Synthesis c-Myc Cancer Infection
    Idarubicin hydrochloride is an anthracycline antileukemic drug. It inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin hydrochloride inhibits the growth of bacteria and yeasts.
  • HY-108969
    Pyrazoloacridine

    NSC 366140; PD 115934

    Topoisomerase Apoptosis Cancer
    Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment.
  • HY-13896
    PD168393

    EGFR Autophagy Apoptosis Cancer
    PD168393 is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC50=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC.
  • HY-146034
    NOD1/2 antagonist-1

    NOD-like Receptor (NLR) Cancer Inflammation/Immunology
    NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding oligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX).
  • HY-139065
    AMPC

    Others Cancer
    AMPC is a potent and effective TFF3 inhibitor. AMPC inhibits cell proliferation, survival, oncogenicity, and CSC-like behaviour in TFF3-positive CMS4 CRC cells. AMPC acts as a potential anti-cancer agent alone or in combination with 5-FU, and can be used for cancer research.
  • HY-139693
    PTPN22-IN-1

    Others Phosphatase Cancer Inflammation/Immunology
    PTPN22-IN-1 is a potent PTPN22 inhibitor (IC50=1.4 µM; Ki=0.50 µM). PTPN22-IN-1 exhibits >7-10 fold selectivity for PTPN22 over similar phosphatases. PTPN22-IN-1 augments antitumor immune responses. From WO2021007491A1 compound L-1.
  • HY-112294
    TIE-2/VEGFR-2 kinase-IN-1

    VEGFR Cancer Inflammation/Immunology Cardiovascular Disease
    TIE-2/VEGFR-2 kinase-IN-1 is used for the synthesis of TIE-2 and/or VEGFR-2 inhibitors, extracted from patent WO2003022852, example 14. TIE-2/VEGFR-2 kinase-IN-1 is used for the study of diseases associated with inappropriate angiogenesis.
  • HY-115499
    MPC-0767

    HSP Cancer
    MPC-0767 is a potent, selective, and orally active hsp90 inhibitor. MPC-0767 is an L-alanine ester prodrug of MPC-3100 with improved chemical stability.
  • HY-122927
    Symphytine

    Others Cancer
    Symphytine is a pyrrolizidine alkaloid isolated from Symphytum officinale and has carcinogenicity.
  • HY-N7496
    Odoroside A

    Apoptosis Cancer
    Odoroside A is an active ingredient extracted from the leaves of Nerium oleander Linn. Odoroside A has anti-cancer activity. Odoroside A could induce apoptosis and cell cycle arrest through ROS/p53 signaling pathway, leading to the tumor cell death.
  • HY-132302
    Hu7691

    Akt PKA PKC ROCK Ribosomal S6 Kinase (RSK) SGK Cancer
    Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
  • HY-125286
    AB-680

    CD73 Cancer
    AB-680 is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity.
  • HY-N0126
    Xanthone

    Bacterial Influenza Virus Fungal Apoptosis Cancer Infection Inflammation/Immunology
    Xanthone is isolated from Mangosteen and is known to control cell division and growth, apoptosis, inflammation, and metastasis in different stages of carcinogenesis. Xanthone has anti-oxidant, anti-tumor, anti-allergic, anti-inflammatory, anti-bacterial, anti-fungal, and anti-viral activities.
  • HY-139702
    α5β1 integrin agonist-1

    Integrin Cancer
    α5β1 integrin agonist-1, acting as α5β1 integrin agonist, is able to selectively deliver 5-FU into tumor cells, successfully leading to cancer cell death.
  • HY-129179
    Lisaftoclax

    APG-2575; Bcl-2/Bcl-xl inhibitor 1

    Bcl-2 Family Cancer
    Lisaftoclax (compound 6) is a dual Bcl-2 and Bcl-xl inhibitor with anti-tumor activity, extracted from patent WO2018027097A1. Lisaftoclax exhibits IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.
  • HY-124325
    PIP-199

    DNA Alkylator/Crosslinker Cancer
    PIP-199 is a selective inhibitor of RMI (RecQ-mediated genome instability protein) core complex/MM2 interaction, with an IC50 of 36 μM. PIP-199 can be used for the research of sensitizing resistant tumors to DNA crosslinking chemotherapeutics.
  • HY-106588
    Heptaplatin

    SKI 2053R

    Others Cancer
    Heptaplatin (SKI 2053R) is a platinum derivative with anticancer activity against various cancer cell lines, including cisplatin-resistant tumor cell lines. SKI-2053R is active in the research of gastric adenocarcinoma and has favorable toxicity profiles.
  • HY-16261
    Aldoxorubicin

    INNO-206; DOXO-EMCH

    Topoisomerase ADC Cytotoxin Cancer
    Aldoxorubicin (INNO-206) is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
  • HY-136476B
    Cu(II) protoporphyrin IX

    Others Cancer Inflammation/Immunology
    Cu (II) Protoporphyrin IX is used as a negative control for Zn (II) Protoporphyrin (an inihibitor of heme oxygenase). Heme oxygenase has been implicated in tumor cell resistance to chemotherapy, reduction of free radical formation and inflammation, and associated with vascular repair.
  • HY-150591
    20S Proteasome-IN-3

    Proteasome Cancer
    20S Proteasome-IN-3 is a 20S proteasome β5 subunit inhibitor (IC50=1.64 μM). 20S Proteasome-IN-3 shows anti-tumor proliferation activity.
  • HY-144064
    Adenosine receptor antagonist 2

    Adenosine Receptor Cancer
    Adenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC50s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity.
  • HY-N6641
    Monascin

    Others Cancer Inflammation/Immunology
    Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor).
  • HY-Y0445A
    Sodium dichloroacetate

    PDHK Reactive Oxygen Species NKCC Apoptosis Cancer
    Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.
  • HY-13513
    U-104

    SLC-0111

    Carbonic Anhydrase Cancer
    U-104 (SLC-0111) is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki values of 45.1 nM and 4.5 nM, respectively. U-104 shows a significant delay in tumor growth in mice model.
  • HY-147570
    ATR-IN-18

    ATM/ATR Cancer
    ATR-IN-18 (compound 2) is an orally active and potent ATR kinase inhibitor, with an IC50 of 0.69 nM. ATR-IN-18 shows antiproliferative activity in LoVo cells, with an IC50 of 37.34 nM. ATR-IN-18 has anti-tumor activity.
  • HY-129337
    Reveromycin A

    Antibiotic Fungal Apoptosis Cancer Infection
    Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity.
  • HY-14375
    CB 300919

    NAMPT Cancer
    CB 300919 is a quinazoline-based antitumour agent with high activity in the CH1 human ovarian tumour xenograft. CB 300919 has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft.
  • HY-N0289
    Lycorine hydrochloride

    Autophagy Bacterial Virus Protease Cancer Inflammation/Immunology
    Lycorine hydrochloride is the main active ingredient of the herbal medicine derived from Lycoris radia and is also a melanoma vasculogenic inhibitor and has anti-tumor activity. Lycorine hydrochloride effectively inhibits mitotic proliferation of Hey1B cells (IC50 of 1.2 μM).
  • HY-N6623
    Malvidin-3-galactoside chloride

    Apoptosis ROS Kinase Cancer
    Malvidin-3-galactoside chloride, an anthocyanin monomer, induces hepatocellular carcinoma (HCC) cells cycle arrest and apoptosis. Malvidin-3-galactoside chloride inhibits the production and accumulation of ROS. Malvidin-3-galactoside chloride has anti-tumor function.
  • HY-N8213
    Rapanone

    Apoptosis Phospholipase Bacterial Parasite Cancer Infection Inflammation/Immunology
    Rapanone is a natural benzoquinone. Rapanone exhibits a broad spectrum of biological actions, including anti-tumor, antioxidant, anti-inflammatory, antibacterial and antiparasitic. Rapanone also is a potent and selective human synovial PLA2 inhibitor, with an IC50 of 2.6 μM.
  • HY-122312
    BAY-8002

    Monocarboxylate Transporter Cancer
    BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity.
  • HY-120394
    TVB-3166

    Fatty Acid Synthase (FASN) Apoptosis Cancer
    TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.
  • HY-19356A
    Didesmethylrocaglamide

    Eukaryotic Initiation Factor (eIF) Apoptosis Cancer
    Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity.
  • HY-143280
    Topoisomerase II inhibitor 4

    Topoisomerase Cancer
    Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect.
  • HY-136198
    SRX3207

    Syk PI3K Cancer
    SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression.
  • HY-P1149A
    Epitalon TFA

    Epithalon TFA; Epithalamin TFA

    Telomerase Cancer Neurological Disease
    Epitalon TFA is an anti-aging agent and a telomerase activator. Epitalon TFA has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon TFA can be used for cancer, old age and Retinitis Pigmentosa.
  • HY-112642
    9-Methoxycanthin-6-one

    Others Cancer
    9-Methoxycanthin-6-one, a canthin-6-one alkaloid, is present in intact plant parts and in callus tissues of different explants. 9-Methoxycanthin-6-one shows anti-tumor activity.
  • HY-15794
    Nemorubicin

    Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243

    Others Cancer
    Nemorubicin (Methoxymorpholinyl doxorubicin) is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity.
  • HY-12182
    ONO-8711

    Prostaglandin Receptor Cancer
    ONO-8711 is a potent and selective competitive antagonist of EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1 respectively). ONO-8711 effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer.
  • HY-N6679
    (R)-10,11-Dehydrocurvularin

    Others Cancer
    (R)-10,11-Dehydrocurvularin is a secondary metabolite isolated from Curvularia sp.. (R)-10,11-Dehydrocurvularin displays concentration-dependent cytotoxicity towards human tumor cell lines with a mean IC50 value of 1.25 µM.
  • HY-125378
    SBP-0636457

    SBI-0636457; SB1-0636457

    IAP Cancer
    SBP-0636457 (SB1-0636457) is a SMAC mimetic, and as an IAP antagonist. SBP-0636457 binds to the BIR-domains of the IAP proteins, with a Ki of 0.27 μM. SBP-0636457 can be used for the research of solid tumors and hematologic cancers.
  • HY-125286A
    AB-680 ammonium

    CD73 Cancer
    AB-680 ammonium is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity.
  • HY-119515
    Denopamine

    (R)-(-)-Denopamine; TA-064

    Adrenergic Receptor Cardiovascular Disease
    Denopamine ((R)-(-)-Denopamine) is an orally active, selective β1-adrenergic agonist. Denopamine prolongs survival in a murine model of congestive heart failure induced by viral myocarditis: suppression of tumor necrosis factor-α production in the heart. Cardiovascular effects.
  • HY-10619B
    Niraparib tosylate

    MK-4827 tosylate

    PARP Apoptosis Cancer
    Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-109176
    Giredestrant

    GDC-9545

    Estrogen Receptor/ERR Cancer
    Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity.
  • HY-115735
    SKI-I

    SphK Apoptosis Cancer
    SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC50 of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC50=11 μM). SKI-I induces apoptosis in tumor cell lines.
  • HY-147281
    BAY 1135626

    Others Cancer
    BAY 1135626 is used to synthesize BAY 1129980, and use to anti-tumor research. BAY 1129980 is a Auristatin-based anti-C4.4A (LYPD3) antibody–drug conjugate (ADC), is used to non–small cell lung cancer (NSCLC) research.
  • 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-N0848
    Epibrassinolide

    24-Epibrassinolide; B1105; BP55

    Apoptosis Cancer
    Epibrassinolide (24-Epibrassinolide) is a ubiquitously occurring plant growth hormone which shows great potential to alleviate heavy metals and pesticide stress in plants. Epibrassinolide is a potential apoptotic inducer in various cancer cells without affecting the non-tumor cell growth.
  • HY-143617
    photoCORM-1

    Others Cancer
    photoCORM-1 (compound 8) is a combinatorial carbon monoxide releasing molecule (CORM). photoCORM-1 exhibits good cellular uptake and real-time monitoring ability of CO uncaging by a color change approach. photoCORM-1 has anti-tumor antivity.
  • 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-144448
    FAK-IN-2

    FAK Apoptosis Cancer
    FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis.
  • HY-100492
    Fisogatinib

    BLU-554

    FGFR Cancer
    Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 5 nM. Fisogatinib has significant anti-tumor activity in models of hepatocellular carcinoma (HCC) that are dependent on FGFR4 signalling.
  • HY-N6986
    Liquiritigenin-7-O-β-D-glucopyranosyl-(1→2)-β-D-apiofuranoside

    Liquiritigenin-7-apiosylglucoside

    Others Cancer
    Liquiritigenin-7-O-β-D-glucopyranosyl-(1→2)-β-D-apiofuranoside (Liquiritigenin-7-apiosylglucoside) is a flavonoid isolated from the roots of Glycyrrhiza, has weaker cytotoxicity against several tumor cells and normal cells.
  • HY-N0448
    10-Gingerol

    Others Cancer Inflammation/Immunology
    10-Gingerol is a major pungent constituent in the ginger oleoresin from fresh rhizome, with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM.
  • HY-14807S
    Tosedostat-d5

    Aminopeptidase Cancer
    Tosedostat-d5 (CHR-2797-d5) is the deuterium labeled Tosedostat. Tosedostat (CHR-2797) is an orally active aminopeptidase inhibitor. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines.
  • HY-32015
    Cot inhibitor-1

    MAP3K Inflammation/Immunology
    Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM.
  • HY-141510
    myo-Inositol trispyrophosphate hexasodium

    ITPP hexasodium

    Others Cancer
    myo-Inositol trispyrophosphate (ITPP) hexasodium, a modifier of haemoglobin, is an allosteric effector that reduces the oxygen‐binding affinity of haemoglobin and facilitates the release of oxygen by red blood cells. myo-Inositol trispyrophosphate can reverse hypoxia, control tumor growth and improve chemotherapy response.
  • HY-100544
    FLLL32

    STAT JAK Apoptosis Cancer
    FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
  • HY-12522
    PF-06380101

    Aur0101; Auristatin-0101

    Microtubule/Tubulin ADC Cytotoxin Cancer
    PF-06380101 (Aur0101), an auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue. PF-06380101 (Aur0101) shows excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.
  • HY-N1231
    Sophoraflavanone G

    Kushenol F

    Apoptosis Cancer
    Sophoraflavanone G (Kushenol F) is iaolated from Sophora flavescens and shows anti-tumor and anti-inflammatory properties.  Sophoraflavanone G (Kushenol F) induces MDA-MB-231 and HL-60 cells apoptosis through suppression of MAPK-related pathways.
  • HY-143618
    photoCORM-2

    Others Cancer
    photoCORM-2 (compound 3) is a single carbon monoxide releasing molecule (CORM). photoCORM-2 exhibits good cellular uptake and real-time monitoring ability of CO uncaging by a color change approach. photoCORM-2 has anti-tumor activity.
  • HY-135903
    Giredestrant tartrate

    GDC-9545 tartrate

    Estrogen Receptor/ERR Cancer
    Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity.
  • HY-10619E
    Niraparib tosylate hydrate

    MK-4827 tosylate hydrate

    PARP Apoptosis Cancer
    Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-N0368
    Linalool

    iGluR Apoptosis Endogenous Metabolite Cancer Cardiovascular Disease
    Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity.Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome.
  • HY-10619
    Niraparib

    MK-4827

    PARP Apoptosis Cancer
    Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-101667
    LTURM34

    DNA-PK Cancer
    LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines.
  • HY-128775
    JHU395

    Others Cancer
    JHU395 is an orally-bioavailable and a plasma stable lipophilic glutamine antagonists (GA) prodrug. JHU395 delivers 6-diazo-5-oxo-L-norleucine (DON) to malignant peripheral nerve sheath tumor (MPNST) in vitro and in vivo, and has antitumor activity in MPNST.
  • HY-10619A
    Niraparib hydrochloride

    MK-4827 hydrochloride

    PARP Apoptosis Cancer
    Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-130116A
    IACS-8779 disodium

    STING Cancer
    IACS-8779 disodium is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy. IACS-8779 disodium shows robust activation of the STING pathway in vitro and a superior systemic anti-tumor response in the B16 murine model of melanoma.
  • HY-131194
    JAK2/STAT3-IN-1

    Interleukin Related Cancer
    JAK2/STAT3-IN-1 (compound (S)-10a) is a potent GP130 inhibitor with an IC50 of 3.04 µM. JAK2/STAT3-IN-1 shows anti-tumor activity.
  • HY-13767
    Tirapazamine

    SR259075; SR4233; Win59075; SML 0552; SR 259075; Tirazone

    Others Cancer
    Tirapazamine is an anticancer agent that shows selective cytotoxicity for hypoxic cells in solid tumors, thereby inducing single-and double-strand breaks in DNA, base damage, and cell death. Tirapazamine is an anticancer and bioreductive agent. Tirapazamine can enhance the cytotoxic effects of ionizing radiation in hypoxic cells.
  • HY-135336AS
    (S)-Verapamil D7 hydrochloride

    (S)-(-)-Verapamil D7 hydrochloride

    Leukotriene Receptor Calcium Channel Apoptosis Cancer
    (S)-Verapamil D7 hydrochloride ((S)-(-)-Verapamil D7 hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells.
  • HY-123410
    KM-233

    Cannabinoid Receptor Cancer
    KM-233 is a classical cannabinoid with good blood brain barrier penetration. KM-233 possesses a selective affinity for the CB2 receptors relative to THC. KM-233 is effective at reducing U87 glioma tumor burden, and can be used for glioma research.
  • HY-126297
    c-Fms-IN-10

    c-Fms Cancer Inflammation/Immunology
    c-Fms-IN-10 is the derivative of thieno [3,2-d] pyrimidine, an kinase inhibitor of FMS (Colony stimulating factor-1 receptor, CSF-1R) with IC50 of 2 nM. c-Fms-IN-10 has anti-tumor activity.
  • HY-W008253S1
    5-Hydroxyindole-3-acetic acid-d6

    Endogenous Metabolite Cancer Neurological Disease
    5-Hydroxyindole-3-acetic acid-d6 is the deuterium labeled 5-Hydroxyindole-3-acetic acid. 5-Hydroxyindole-3-acetic acid is the main metabolite of serotonin or metanephrines, which can be used as a biomarker of neuroendocrine tumors.
  • HY-145861
    LSD1-IN-14

    Histone Demethylase Apoptosis Cancer
    LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells.
  • HY-W008253S
    5-Hydroxyindole-3-acetic acid-d2

    Endogenous Metabolite Cancer Neurological Disease
    5-Hydroxyindole-3-acetic acid-d2 is the deuterium labeled 5-Hydroxyindole-3-acetic acid. 5-Hydroxyindole-3-acetic acid is the main metabolite of serotonin or metanephrines, which can be used as a biomarker of neuroendocrine tumors.
  • HY-135147
    ONC206

    Dopamine Receptor Cancer Neurological Disease
    ONC206 is an analogue of TRAIL inducer ONC201. ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity.
  • HY-132302A
    Hu7691 free base

    Akt PKA PKC ROCK Ribosomal S6 Kinase (RSK) SGK Cancer
    Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
  • HY-P2316
    Epinecidin-1 TFA

    Bacterial Antibiotic Infection
    Epinecidin-1 TFA is a multi-functional antimicrobial peptide (AMP) from Orange-spotted grouper (Epinephelus coioides). Epinecidin-1 TFA has antibacterial, antifungal, antiviral, anti-tumor, and immunomodulatory effects. Epinecidin-1 TFA has the potential to be an alternative for current antibiotics.
  • HY-N9596
    Stigmasta-4,22-dien-3-one

    Bacterial Cancer Infection
    Stigmasta-4,22-dien-3-one is an antitubercular agent. Stigmasta-4,22-dien-3-one shows cytotoxicity against human HT1080 tumoral cell line with an IC50 of 0.3 mM.
  • HY-10218
    Everolimus

    RAD001; SDZ-RAD

    mTOR FKBP Autophagy Apoptosis Cancer
    Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities.
  • HY-A0038
    Lasofoxifene tartrate

    CP-336156 tartrate

    Estrogen Receptor/ERR Endocrinology Cancer
    Lasofoxifene (CP-336156) tartrate is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene tartrate exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene tartrate can be used for the research of breast cancer and postmenopausal osteoporosis.
  • HY-144361
    Antitumor agent-44

    Apoptosis Cancer
    Antitumor agent-44 (Compound 5n) disrupts the mitochondrial homeostasis, induces cell cycle arrest and apoptosis in human adenocarcinoma cells. Antitumor agent-44 (Compound 5n) possesses good anti-tumor activity in a lung-cancer-cell xenograft mice model.
  • HY-143435
    AG6033

    Apoptosis Others Cancer
    AG6033 is a potential novel CRBN modulator. AG6033 suppresses various tumor cells by modulating the interactions between CRBN and various antitumor target proteins. AG6033 can cause GSPT1 and IKZF1 degradation. AG6033 induces CRBN-dependent cytotoxic effect.
  • HY-78695
    JQ-1 (carboxylic acid)

    Epigenetic Reader Domain Cancer
    JQ-1 carboxylic acid, a type of (+)-JQ-1 derivative, is a potent BET bromodomain inhibitor for downregulating PD-L1 expression on the surface of tumor cells. JQ-1 carboxylic acid can be used as a precursor to synthesize PROTACs, which targets BET bromodomains.
  • HY-147574
    Axl-IN-7

    TAM Receptor Cancer Inflammation/Immunology Cardiovascular Disease
    Axl-IN-7 (Chemie 22) is a potent AXL inhibitor. Axl-IN-7 can be used for Axl-related diseases research, for example cancers (such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors), renal disease, immune system disorders, and cardiovascular disease.
  • HY-N6615
    Aflatoxin B1

    Bacterial Endogenous Metabolite Cancer Infection
    Aflatoxin B1 (AFB1) is a Class 1A carcinogen, which is a secondary metabolite of Aspergillus flavus and A. parasiticus. Aflatoxin B1 (AFB1) mainly induces the transversion of G-->T in the third position of codon 249 of the p53 tumor suppressor gene, resulting in mutation.
  • HY-16590
    X-376

    ALK c-Met/HGFR Cancer
    X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). X-376 is a less potent inhibitor of MET (IC50=0.69 nM). X-376 displays potent anti-tumor activity.
  • HY-13622
    Elomotecan hydrochloride

    BN 80927

    Topoisomerase Cancer
    Elomotecan hydrochloride (BN 80927) is a potent inhibitor of topoisomerases I and II. Elomotecan hydrochloride (BN 80927) is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan hydrochloride (BN 80927) reduces the proliferation of different tumor cells with higher potency than other anticancer drugs of reference targeting topoisomerases I and II.
  • HY-N8432
    Dipyrithione

    Apoptosis Bacterial Fungal Cancer Infection Inflammation/Immunology
    Dipyrithione is a potent antimicrobial agent. Dipyrithione shows antifungal activity and antiproliferative activity. Dipyrithione induces apoptosis and cycle arrest at G1 phase. Dipyrithione shows anti-inflammatory activity in vivo. Dipyrithione shows anti-tumor activity. Dipyrithione has the potential for the research of dermatophytosis.
  • HY-16196
    ENMD-1198

    IRC-110160

    Microtubule/Tubulin HIF/HIF Prolyl-Hydroxylase STAT Cancer
    ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
  • HY-N5020
    Carabrone

    Bacterial Infection
    Carabrone is isolated from the fruits of Carpesium abrotanoides , is a well-known sesquiterpene and exhibits significant anti-bacterial and anti-tumor activities. Carabrone exhibits antifungal activities in vitro and in vivo against Botrytis cinerea, Colletotrichum lagenarium(EC50=7.10 μg/mL) and Erysiphe graminis.
  • HY-N2350
    Cynaropicrin

    MMP NF-κB TNF Receptor Cancer
    Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
  • HY-14444
    Plinabulin

    NPI-2358

    Microtubule/Tubulin Cancer
    Plinabulin (NPI-2358) is a vascular disrupting agen (VDA) against tubulin-depolymerizing with an IC50 of 9.8 nM against HT-29 cells. Plinabulin binds the colchicine binding site of β-tubulin preventing polymerization and has potent inhibitory to tumor cells.
  • HY-147521
    Antitumor photosensitizer-3

    Others Cancer
    Antitumor photosensitizer-3 (Compound I) is a chlorin derivative. Antitumor photosensitizer-3 induces tumor cells apoptosis and necrosis under 650 nm laser irradiation. Antitumor photosensitizer-3 exhibits lower skin photo-toxicity than positive reference m-THPC in vivo.
  • HY-N7422
    Kauran-16,17-diol

    ent-Kauran-16β,17-diol

    Apoptosis Cancer Inflammation/Immunology
    Kauran-16,17-diol (ent-Kauran-16β,17-diol), a natural diterpene, posseses anti-tumor and inducing-apoptosis activity, with a IC50 of 17 μM on inhibiting NO production in LPS-stimulated RAW 264.7 macrophages.
  • HY-13580S
    Budesonide-d8

    Glucocorticoid Receptor Cancer Inflammation/Immunology
    Budesonide-d8 is the deuterium labeled Budesonide. Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
  • HY-146260
    NVP-CLR457

    PI3K Cancer
    NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity.
  • HY-A0020
    Eldecalcitol

    ED-71; 2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3

    VD/VDR Cancer Metabolic Disease Inflammation/Immunology
    Eldecalcitol (ED-71) is an orally active vitamin D3 analogue, inhibits bone resorption and increases bone mineral density. Eldecalcitol (ED-71) displays anti-tumor effect and inhibits cell proliferation, migration and induces apoptosis by suppressing GPx-1.
  • HY-N1517
    Ganoderic acid C2

    Others Cancer
    Ganoderic acid C2 is a bioactive triterpenoid in Ganoderma lucidum. Ganoderic acid C2 possesses the potential anti-tumor bioactivity, antihistamine, anti-aging and cytotoxic effects. Ganoderic acid C2 exhibits high inhibitory activity against the rat lens aldose reductase (RLAR) with an IC50 of 3.8 µM.
  • HY-18959
    CWP232228

    β-catenin Wnt Cancer
    CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs).
  • HY-N9398
    3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol

    Sirtuin Cancer
    3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol, a SIRT1 activator, exhibits significant stimulation of SIRT1 activity. Anti-tumor activity.
  • HY-N5112
    (Rac)-Arnebin 1

    (Rac)-β,β-Dimethylacrylalkannin; (Rac)-β,β-​Dimethylacrylshikonin

    Others Others
    (Rac)-Arnebin 1 ((Rac)-β,β-Dimethylacrylalkannin) is the racemate of β,β-Dimethylacrylalkannin and/or β,β-Dimethylacrylshikonin. β,β-Dimethylacrylalkannin and β,β-Dimethylacrylshikonin are napthoquinones isolated from Arnebia nobilis. β,β-Dimethylacrylshikonin has anti-tumor activity.
  • HY-100431
    IMR-1

    Notch Cancer
    IMR-1 is a novel class of Notch inhibitor 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-135336AS1
    (S)-Verapamil-d6 hydrochloride

    (S)-(-)-Verapamil-d6 hydrochloride

    Leukotriene Receptor Calcium Channel Apoptosis Cancer
    (S)-Verapamil-d6 ((S)-(-)-Verapamil-d6) hydrochloride is the deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells.
  • HY-144127
    AR antagonist 3

    Androgen Receptor Cancer
    AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally.
  • HY-W009156
    Hydroxycitric acid tripotassium hydrate

    Potassium citrate monohydrate

    ATP Citrate Lyase HIF/HIF Prolyl-Hydroxylase Bacterial Cancer Infection Metabolic Disease Inflammation/Immunology
    Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia. Hydroxycitric acid tripotassium hydrate competitively inhibits ATP citrate lyase with weight loss benefits. Hydroxycitric acid tripotassium hydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects.
  • HY-119272
    EF24

    ERK Caspase Cancer
    EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK.
  • HY-119696S
    MTIC-d3

    Drug Metabolite Cancer Neurological Disease
    MTIC-d3 is deuterium labeled MTIC. MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the drug’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane.
  • HY-101519
    BETd-260

    ZBC 260

    PROTACs Epigenetic Reader Domain Apoptosis Cancer
    BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.
  • HY-122705
    RAD51-IN-1

    RAD51 Cancer
    RAD51-IN-1, a derivative of  B02, is a potent inhibitor of RAD51. RAD51-IN-1 can be used for cancer research.
  • HY-134885
    RMC-0331

    RM-023

    Ras Cancer
    RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction.
  • HY-132202
    PD-1/PD-L1-IN-10

    PD-1/PD-L1 Apoptosis Cancer
    PD-1/PD-L1-IN-10 (compound B2) is an orally active PD-1/PD-L1 inhibitor (IC50 of 2.7 nM) with potent anticancer efficacy.
  • HY-143611
    AKT-IN-8

    Akt Cancer
    AKT-IN-8 is a potent AKT inhibitor with IC50s of 4.46, 2.44, and 9.47 nM for AKT1, AKT2, and AKT3, respectively.
  • HY-P2336
    CCZ01048

    Melanocortin Receptor Cancer
    CCZ01048, a α-melanocyte-stimulating hormone (α-MSH) analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma.
  • HY-138540
    1-Dodecylimidazole

    N-Dodecylimidazole

    Fungal Cancer
    1-Dodecylimidazole (N-Dodecylimidazole) is a lysosomotropic detergent and a cytotoxic agent. 1-Dodecylimidazole causes cell death by its acid-dependent accumulation in lysosomes, disruption of the lysosomal membrane, and releaseof cysteine proteases into the cytoplasm. 1-Dodecylimidazole has hypocholesterolaemic activity and broad-spectrum antifungal activity.
  • HY-10406
    Talmapimod

    SCIO-469

    p38 MAPK Cancer
    Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.
  • HY-13007A
    PF-3758309 hydrochloride

    PF-03758309 hydrochloride

    PAK Apoptosis Cancer
    PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-N10183
    Crocin-4

    Reactive Oxygen Species Neurological Disease
    Crocin-4, a carotenoid constituent of saffron, is a potent and brain-penetrant antioxidant agent. Crocin-4 can inhibit the aggregation and the concomitant deposition of Aβ fibrils in the brain. Crocin-4 can be used for the research of Alzheimer's Disease. Crocin-4 also exhibits antitumor and anti-inflammatory activities.
  • HY-136055
    (S,R,S)-AHPC-C5-COOH

    VH032-C5-COOH

    E3 Ligase Ligand-Linker Conjugates HIF/HIF Prolyl-Hydroxylase Cancer
    (S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases.
  • HY-100556
    Tie2 kinase inhibitor 1

    Others Cancer
    Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.
  • HY-13007
    PF-3758309

    PF-03758309

    PAK Apoptosis Cancer
    PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-P2336A
    CCZ01048 TFA

    Melanocortin Receptor Cancer
    CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma.
  • HY-125974
    HM03

    HSP Cancer
    HM03 is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 has anticancer activity.
  • HY-N7038
    Phytohemagglutinin

    PHA-M

    Others Inflammation/Immunology
    Phytohemagglutinin (PHA-M), the major seed lectin of the common bean, Phaseolus vulgaris, accumulates in the parenchyma cells of the cotyledons. Phytohemagglutinin is a T-cell activator. Stimulation of human mononuclear leukocytes by Phytohemagglutinin induces the expression of ChAT mRNA, and potentiated ACh synthesis.
  • HY-122615B
    SPOP-IN-6b dihydrochloride

    Others Cancer
    SPOP-IN-6b dihydrochloride is a potent speckle-type POZ protein (SPOP) inhibitor with an IC50 of 3.58 μM.
  • HY-13007B
    PF-3758309 dihydrochloride

    PF-03758309 dihydrochloride

    PAK Apoptosis Cancer
    PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-14691
    Refametinib

    BAY 869766; RDEA119

    MEK Cancer
    Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
  • HY-125974A
    HM03 trihydrochloride

    HSP Cancer
    HM03 trihydrochloride is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 trihydrochloride has anticancer activity.
  • HY-15338
    TG003

    CDK Cancer
    TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
  • HY-13775
    XL019

    JAK Apoptosis Cancer
    XL019 is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
  • HY-147293
    Nenocorilant

    Relacorilant; CORT125134

    Glucocorticoid Receptor Apoptosis Caspase Cancer
    Nenocorilant (Relacorilant) is a potent, orally activity glucocorticoid receptor (GR) antagonist with Ki value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent. Nenocorilant can be used for cancer research.
  • HY-15338A
    (E/Z)-TG003

    CDK Cancer
    (E/Z)-TG003 is a racemic compound of (Z)-TG003 and (E)-TG003. (Z)-TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
  • HY-116832
    Retrorsine N-oxide

    Others Cancer
    Retrorsine N-oxide, an N-oxide of pyrrolizidine alkaloid, is a carcinogen. Retrorsine N-oxide-derived DNA adducts are common toxicological biomarkers of pyrrolizidine alkaloid N-oxides.
  • HY-131909
    CJ-2360

    ALK Cancer
    CJ-2360 is a potent and orally active ALK inhibitor with IC50s of 2.2, 4.0, 8.8, 6.3, and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively. CJ-2360 displays potent inhibitory activity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated.
  • HY-124131
    DS-437

    Histone Methyltransferase Cancer Inflammation/Immunology
    DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3.
  • HY-10406A
    Talmapimod hydrochloride

    SCIO-469 hydrochloride

    p38 MAPK Cancer
    Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod hydrochloride shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.
  • HY-130851
    HS-27

    HSP Cancer
    HS-27, a fluorescently-tethered Hsp90 inhibitor, assays surface Hsp90 expression on intact tissue specimens. HS-27 is made up of the core elements of SNX-5422, an Hsp90 inhibitor, tethered via a PEG linker to a fluorescein derivative (fluorescein isothiocyanate or FITC), that binds to ectopically expressed Hsp90. HS-27 has potential use in a see-and-treat paradigm in breast cancer.
  • HY-131054
    Cinerubin B

    Antibiotic Bacterial Infection
    Cinerubin B, a glycosylated anthracycline antibiotic, is an anticancer agent from Streptomyces sp. SPB74.
  • HY-16373
    CP-609754

    LNK-754; OSI-754

    Farnesyl Transferase Cancer
    CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL.
  • HY-122615A
    SPOP-IN-6b hydrochloride

    Others Cancer
    SPOP-IN-6b hydrochloride is a potent speckle-type POZ protein (SPOP) inhibitor with an IC50 of 3.58 μM.
  • HY-145899
    PKN1/2-IN-1

    Others Cancer
    PKN1/2-IN-1 is a potent, cell penetrant and selective PKN2 (PRK2) inhibitor (IC50=16 nM; Ki=8 nM).
  • HY-131065
    MET kinase-IN-2

    c-Met/HGFR Cancer
    MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity.
  • HY-106376A
    L-Buthionine-(S,R)-sulfoximine

    L-Buthionine sulfoximine; L-BSO

    Ferroptosis Cancer
    L-Buthionine-(S,R)-sulfoximine is a cell-permeable, potent, fast acting and irreversible inhibitor of g-glutamylcysteine synthetase and depletes cellular glutathione levels. The IC50 value of L-Buthionine-(S,R)-sulfoximine on melanoma, breast and ovarian tumor specimens are 1.9 μM, 8.6 μM, and 29 μM, respectively.
  • HY-134990
    Hematoporphyrin monomethyl ether

    Apoptosis Cancer
    Hematoporphyrin monomethyl ether, second generation of porphyrin-related photosensitizer, is characterized by its single form, high yield of singlet oxygen, high selectivity, and low toxicity, which has been widely used in the diagnosis and treatment of various tumors, including lung cancer, bladder cancer, and nevus flammeus and brain glioma.
  • HY-121993
    Combretastatin A-1

    Microtubule/Tubulin Cancer
    Combretastatin A-1 is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 exhibits anti-tumor and anti-vascular effects.
  • HY-147943
    PROTAC BTK Degrader-1

    PROTACs Btk Cancer
    PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth.
  • HY-112328
    Fascaplysin

    Apoptosis Autophagy ROS Kinase Cancer Infection
    Fascaplysin is an antimicrobial and cytotoxic red pigment, that can come from the marine sponge (Fascaplysinopsis sp.). Fascaplysin has been synthesized in seven steps from indole (65% yield). Fascaplysin can induces apoptosis and autophagy in human leukemia HL-60 cells. Fascaplysin shows anti-tumor activity.
  • HY-116626
    SM-7368

    NF-κB p38 MAPK MMP Cancer
    SM-7368 is a potent NF-kB inhibitor that targets downstream of MAPK p38 activation. SM-7368 inhibits TNF-α-induced MMP-9 upregulation. SM-7368 can be used for the research of chemotherapies targeting TNF-α-mediated tumor invasion and metastasis .
  • HY-N6950
    Hederacolchiside A1

    PI3K Akt mTOR Parasite Apoptosis Cancer Infection
    Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro.
  • HY-P9920
    Ramucirumab

    VEGFR Cancer
    Ramucirumab is a human VEGFR-2 antagonist for the treatment of solid tumors. Ramucirumab is a recombinant human immunoglobulin G1 monoclonal antibody that binds to the extracellular binding domain of VEGFR-2 and prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D. Ramucirumab is also an angiogenesis inhibitor.
  • HY-19828
    Herboxidiene

    GEX1A

    DNA/RNA Synthesis Cancer
    Herboxidiene (GEX1A) is a potent phytotoxic polyketide from Streptomyces sp. A7847 with a diverse range of activities, including herbicidal, anti-cholesterol, anti-tumor effects. Herboxidiene inhibits the pre-mRNA splicing process by binding to spliceosome-associated protein (SAP) 155, a subunit of SF3b, in the splicesome.
  • HY-N0790
    Lupeol

    Clerodol; Monogynol B; Fagarasterol

    Androgen Receptor Apoptosis Cancer
    Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC).
  • HY-147040
    ABN401

    c-Met/HGFR Cancer
    ABN401 is a highly potent and selective ATP-competitive c-MET inhibitor with an IC50 value of 10 nM. ABN401 has cytotoxic activity against MET-addicted cancer cells. ABN401 can inhibit c-MET phosphorylation in tumor tissues. ABN401 can be used for researching anticancer.
  • HY-137605
    WSF1-IN-1

    Others Cancer
    WSF1-IN-1 (compound 136), an orally active WSF1 inhibitor, can be used in the study for WSF1 (Wolfram syndrome) related tumors, with IC50 values of 0.33 μM and >27 μM in HepG2 parental and HepG2 WFS1 KO cell lines, respectively.
  • HY-105846
    Nogalamycin

    DNA/RNA Synthesis Bacterial Antibiotic Cancer
    Nogalamycin is an anthracyclinone antibiotic. Nogalamycin is a potent antibiotic against Gram-positive bacteria, also has cytotoxicity against certain tumor cells. Nogalamycin is produced by Streptomyces nogalater var. Nogalater. Nogalamycin selectively inhibits RNA synthesis after binding to DNA template. Nogalamycin can be used for researching anticancer.
  • HY-145427
    NU5455

    DNA-PK Cancer
    NU5455 is a potent, selective, and orally active inhibitor of DNA-PKcs. NU5455 administration increases both the efficacy and the toxicity of a parenterally administered topoisomerase inhibitor. NU5455 enhances the activity of Doxorubicin released locally in liver tumor xenografts without inducing any adverse effect.
  • HY-129467S
    (Rac)-Idroxioleic acid-d17

    2-Hydroxyoleic acid-d17; 2-OHOA-d17

    Apoptosis Cancer
    (Rac)-Idroxioleic acid-d17 (2-Hydroxyoleic acid-d17) is the deuterium labeled (Rac)-Idroxioleic acid. (Rac)-Idroxioleic acid (2-Hydroxyoleic acid) is a synthetic oleic acid (OA) derivative that binds to the plasma membrane and alters lipid organization. (Rac)-Idroxioleic acid has anti-tumor effect.
  • HY-13642
    RG108

    N-Phthalyl-L-tryptophan

    DNA Methyltransferase Cancer
    RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.
  • HY-125232
    MS645

    Epigenetic Reader Domain Cancer
    MS645 is a bivalent BET bromodomains (BrD) inhibitor with a Ki of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells.
  • 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-N5112B
    β,β-Dimethylacrylshikonin

    Isoarnebin I

    Others Cancer
    β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative isolated from Arnebia nobilis, promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway.β,β-Dimethylacrylshikonin has anti-tumor activity.
  • HY-144766
    ATX inhibitor 13

    Apoptosis Others Cancer
    ATX inhibitor 13 (10c) is an orally active and potent ATX inhibitor, with an IC50 of 3.4 nM. ATX inhibitor 13 inhibits proliferation and migration, and induces apoptosis and G2 phase arrest in RAW264.7 cells. ATX inhibitor 13 suppresses tumor cell colony formation.
  • HY-W015828
    RGX-202

    3-Guanidinopropionic acid

    Endogenous Metabolite Cancer
    RGX-202 (3-Guanidinopropionic acid) is an oral small-molecule SLC6A8 transporter inhibitor. RGX-202 robustly inhibits creatine import in vitro and in vivo, reduces intracellular phosphocreatine and ATP levels, and induces tumor apoptosis. RGX-202 can be used for the research of cancer.
  • HY-149019
    Antitumor agent-70

    c-Kit Apoptosis Cancer
    Antitumor agent-70 (compound 8b) has anti-tumor activity and can induce cell apoptosis. Antitumor agent-70 inhibits multiple myeloma with an IC50 value of 0.12 μM. Antitumor agent-70 is a potential multi-targeted kinase inhibitor especially for c-Kit.
  • HY-16125
    Carboxyamidotriazole Orotate

    L-651582 Orotate; CAI Orotate

    Calcium Channel Cancer Inflammation/Immunology
    Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects.
  • HY-B0311AS
    Carbidopa-d3 monohydrate

    (S)-(-)-Carbidopa-d3 monohydrate

    Aryl Hydrocarbon Receptor Cancer Neurological Disease
    Carbidopa-d3 ((S)-(-)-Carbidopa-d3) monohydrate is the deuterium labeled Carbidopa monohydrate. Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth.
  • HY-143585
    CDK9-IN-14

    CDK Cancer
    CDK9-IN-14 is a potent and selective CDK9 inhibitor with IC50 of 6.92 nM. CDK9-IN-14 has a relatively strong inhibitory effect on MV4;11 cells and in vivo tumor models, and has a good selectivity and a low toxicity and few side effects.
  • HY-147215
    UC-1V150

    Toll-like Receptor (TLR) Inflammation/Immunology
    UC-1V150 is a specific TLR7 (Toll-like receptor) agonist that stimulates cellular immune responses and has anti-tumor activity. UC-1V150 can be used to synthesize ISAC (Immune-Stimulating Antibody Conjugates) molecule.
  • HY-15615A
    TIC10

    ONC-201

    TNF Receptor Apoptosis Cancer
    TIC10 (ONC-201) is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can cross the blood-brain barrier.
  • HY-N3387
    Licoricidin

    Apoptosis NF-κB Akt MMP Cancer Inflammation/Immunology
    Licoricidin (LCD) is isolated from Glycyrrhiza uralensis Fisch, possesses anti-cancer activities. Licoricidin (LCD) inhibit SW480 cells (IC50=7.2 μM) by inducing cycle arrest, apoptosis and autophagy, and is a potential chemopreventive or chemotherapeutic agent against colorectal cancer. Licoricidin (LCD) inhibits Lung Metastasis by inhibition of tumor angiogenesis and lymphangiogenesis as well as changes in the local microenvironment of tumor tissues the anticarcinogenic effect. Licoricidin enhanced gemcitabine-induced cytotoxicity in Osteosarcoma (OS) cells by inactivation of the Akt and NF-κB pathways in vitro and in vivo. Licoricidin blocks UVA-induced photoaging via ROS scavenging, limits the activity of MMP-1, it can be considered as an active ingredient in new topically applied anti-ageing formulations.
  • HY-B1295
    Lithium citrate tetrahydrate

    Litarex tetrahydrate

    ATP Citrate Lyase Bacterial HIF/HIF Prolyl-Hydroxylase Cancer Infection Metabolic Disease Inflammation/Immunology
    Lithium citrate (Litarex) tetrahydrate is the major active ingredient of Garcinia cambogia. Lithium citrate tetrahydrate competitively inhibits ATP citrate lyase with weight loss benefits. Lithium citrate tetrahydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects.
  • HY-119307
    Apratastat

    MMP TNF Receptor Cancer
    Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) . Apratastat can potently inhibit the release of TNF-α in vitro, ex vivo, and in vivo with IC50s of 144 ng/mL in vitro and 81.7 ng/mL ex vivo, respectively.
  • HY-147663
    hCAIX-IN-6

    Carbonic Anhydrase Cancer
    Compounds 6B and 14g showed significant inhibitory effect on tumor related subtype HCA IX with low nanomolar potency, while 6K was effective on HCA XII. Compounds 6B, 14g and 6K can be considered as the leading molecules for the development of future cancer therapeutic drugs based on new mechanisms of action.
  • HY-146684
    HDAC-IN-36

    HDAC Autophagy Apoptosis Cancer
    HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research.
  • HY-136291
    Sulfo-SPDB-DGN462

    Drug-Linker Conjugates for ADC Cancer
    Sulfo-SPDB-DGN462 is a drug-linker conjugate for ADC. Sulfo-SPDB-DGN462 consists a toxin DGN462 (HY-101150) conjugated to the cleavable Sulfo-SPDB linker. DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML).
  • HY-W008859
    Tetrac

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

    Integrin Endogenous Metabolite Cancer
    Tetrac (Tetraiodothyroacetic acid), a derivative of L-thyroxine (T4), is a thyrointegrin receptor antagonist. Tetrac blocks the actions of T4 and 3,5,3'-triiodo-L-thyronine (T3) at the cell surface receptor for thyroid hormone on integrin αvβ3. Tetra has anti-angiogenic and anti-tumor activities.
  • HY-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-N0192
    Arbutin

    β-Arbutin

    Tyrosinase Cancer
    Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Ki app values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties.
  • HY-P99015
    Dacetuzumab

    TNF Receptor Cancer
    Dacetuzumab (SGN-40) is a humanized IgG1, anti-CD40 monoclonal antibody with anti-lymphoma activity. Dacetuzumab kills tumor cells via immune effector functions (antibody-dependent cellular cytotoxicity and phagocytosis [ADCC/ADCP]). Dacetuzumab ((SGN-40) can be used for multiple myeloma research.
  • HY-N6061
    Ophiopogonin C

    Others Cancer
    Ophiopogonin C, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin C shows cytotoxic activity against two human tumor cell lines MG-63 and SNU387 with IC50s of 19.76 μM and 15.51 μM, respectively.
  • HY-N5077
    Sinapine

    Cholinesterase (ChE) P-glycoprotein Cancer Inflammation/Immunology Neurological Disease
    Sinapine is an alkaloid isolated from seeds of the cruciferous species. Sinapine exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
  • HY-145803
    KIF18A-IN-3

    Microtubule/Tubulin Cancer
    KIF18A-IN-3 is a potent KIF18A inhibitor (IC50=61 nM). KIF18A-IN-3 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-3 can be used for researching cancer.
  • HY-19992
    3-Bromopyruvic acid

    Bromopyruvic acid; Hexokinase II Inhibitor II, 3-BP

    Hexokinase Apoptosis Autophagy Cancer
    3-Bromopyruvate (Bromopyruvic acid) is an analogue of pyruvate and a potent hexokinase (HK)-II inhibitor with high tumor selectivity. 3-Bromopyruvate inhibits cell growth and induces apoptosis through interfering with glycolysis. 3-Bromopyruvate induces autophagy by stimulating ROS formation in breast cancer cells. Antimicrobial activities.
  • HY-N7691
    3,29-O-Dibenzoyloxykarounidiol

    Karounidiol dibenzoate

    Others Cancer Infection
    3,29-O-Dibenzoyloxykarounidiol (Karounidiol dibenzoate) is a triterpene benzoate isolated from the fruit of Momordica grosvenori. 3,29-O-Dibenzoyloxykarounidiol has potent inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) induced by tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA).
  • HY-135671
    AhR modulator-1

    Aryl Hydrocarbon Receptor VEGFR Estrogen Receptor/ERR Cancer Endocrinology
    AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus.
  • HY-15045
    INO-1001

    PARP Cancer
    INO-1001 is a potent and selective poly (ADP-ribose) polymerase (PARP) inhibitor. INO-1001 is a potent enhancer of radiation sensitivity and enhances radiation-induced cell killing by interfering with DNA repair mechanisms, resulting in necrotic cell death. INO-1001 has anti-tumor effects.
  • HY-112698
    CA-5f

    Autophagy Apoptosis Cancer
    CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity.
  • HY-N7526
    Naphthazarin

    DHNQ; 5,8-Dihydroxy-1,4-naphthoquinone

    Apoptosis Cancer Neurological Disease
    Naphthazarin (DHNQ) is a naturally occurring compound. Naphthazarin is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. Naphthazarin triggers apoptosis and has anti-tumor effects.
  • HY-B0109S
    Dorzolamide-d5

    Carbonic Anhydrase Cancer
    Dorzolamide-d5 (L671152-d5) is the deuterium labeled Dorzolamide. Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
  • HY-114657A
    Benproperine phosphate

    Arp2/3 Complex Cancer Inflammation/Immunology
    Benproperine phosphate is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppresses cancer cell migration and tumor metastasis.
  • 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-102051
    XIAP/cIAP1 antagonist-1

    IAP Cancer
    XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo.
  • HY-N10354
    27-Methyl withaferin A

    Apoptosis Cancer
    27-Methyl withaferin A (comppund 26) is an apoptosis inducer with anticancer effects. 27-Methyl withaferin A shows antiproliferative effects against HeLa, A-549 and MCF-7 human tumor cell lines with IC50 values of 3.2 μM, 4.2 μM and 1.4 μM, respectively.
  • HY-112037
    IACS-010759

    IACS-10759

    Mitochondrial Metabolism Apoptosis Cancer
    IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 has the potential for relapsed/refractory AML and solid tumors research.
  • HY-147298
    Plogosertib

    CYC140

    Polo-like Kinase (PLK) Cancer
    Plogosertib (CYC140) is a selective, potent, and orally active ATP-competitive PLK1 inhibitor (IC50: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lung cancer, ovarian, and squamous cell cancers.
  • HY-144366
    P-gp inhibitor 3

    P-glycoprotein Cancer
    P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel.
  • HY-N0392
    Polygalasaponin F

    Toll-like Receptor (TLR) PI3K Akt NF-κB Inflammation/Immunology
    Polygalasaponin F, an oleanane-type triterpenoid saponin extracted from Polygala japonica, decreases the release of the inflammatory cytokine tumor necrosis factor a (TNFa). Polygalasaponin F reduces neuroinflammatory cytokine secretion through the regulation of the TLR4-PI3K/AKT-NF-kB signaling pathway .
  • HY-W008253S3
    5-Hydroxyindole-3-acetic acid-13C6

    Endogenous Metabolite Cancer Neurological Disease
    5-Hydroxyindole-3-acetic acid-13C6 is the 13C-labeled 5-Hydroxyindole-3-acetic acid. 5-Hydroxyindole-3-acetic acid is the main metabolite of serotonin or metanephrines, which can be used as a biomarker of neuroendocrine tumors.
  • HY-120574
    TH1338

    Others Cancer
    TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile.
  • HY-104037
    Cintirorgon

    LYC-55716

    ROR Cancer
    Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival.
  • HY-122181
    OTS186935

    Histone Methyltransferase Cancer
    OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells.
  • HY-N4042
    Hirsutenone

    PI3K ERK Cancer Inflammation/Immunology
    Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects. Hirsutenone attenuates adipogenesis by binding directly to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone can be used for the study of obesity.
  • HY-100950
    ABC1183

    GSK-3 CDK Cancer Inflammation/Immunology
    ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities.
  • HY-N0047
    Polyphyllin I

    JNK mTOR Akt PDK-1 Autophagy Apoptosis Cancer
    Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis.
  • HY-144394
    Antitumor agent-45

    Apoptosis c-Met/HGFR Cancer
    Antitumor agent-45 (Compound 21) could induce and stimulate A549 cells apoptosis in G0/G1 and G2/M phase. Antitumor agent-45 (Compound 21) inhibits c-Met expression to regulate the growth of tumor cells.
  • HY-124066
    RU-302

    TAM Receptor Cancer
    RU-302 is a pan TAM inhibitor that blocks the interface between the TAM Ig1 ectodomain and the Gas6 Lg domain. RU-302 effectively blocks Gas6-inducible Axl receptor activation with a low micromolar IC50in cell assays, and suppresses lung cancer tumor growth.
  • 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-D1468
    Phototherapeutic agent-1

    Others Cancer
    Phototherapeutic agent-1 is a multi-modal light diagnosis agent with aggregation-induced emission properties. have certain Phototherapeutic agent-1 has certain reactive oxygen species (ROS) generation capacity in illumination condition. Phototherapeutic agent-1 can effectively kill cancer cells and tumor tissue.
  • HY-N8211
    Gypenoside L

    p38 MAPK ERK NF-κB Cancer Inflammation/Immunology
    Gypenoside L is a saponin that can be found in Gynostemma pentaphyllum. Gypenoside L increases the SA-β-galactosidase activity, promotes the production of senescence-associated secretory cytokines. Gypenoside L also can activate p38 and ERK MAPK pathways and NF-κB pathway to induce senescence. Gypenoside L exhibits anti-tumor and anti-inflammatory activities.
  • HY-111614
    Melengestrol acetate

    Progesterone Receptor Cancer Metabolic Disease
    Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity. Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research.
  • HY-145820
    Tubulin inhibitor 14

    Apoptosis Thrombin Microtubule/Tubulin Cancer
    Tubulin inhibitor 14 is a potent NQO2 (quinone oxidoreductase 2) inhibitor with an IC50 of 1.0 μM. Tubulin inhibitor 14 also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. Tubulin inhibitor 14 is a microtubule-destabilizing agent with potential tumor-selectivity and antiangiogenic and vascular disrupting features.
  • HY-145802
    KIF18A-IN-2

    Microtubule/Tubulin Cancer
    KIF18A-IN-2 is a potent KIF18A inhibitor (IC50=28 nM). KIF18A-IN-2 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-2 can be used for researching cancer.
  • HY-128643
    FAPI-4

    Others Cancer
    FAPI-4 is a potent fibroblast activation protein (FAP) inhibitor for the targeting FAP. FAPI-4 can be used in cancer research. 68Ga-FAPI-4 PET/CT is a promising new diagnostic method for imaging various kinds of cancer, with good tumor-to-background contrast ratios.
  • HY-12458
    Pyrindamycin A

    DNA/RNA Synthesis Cancer Infection
    Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml.
  • HY-122181B
    OTS186935 hydrochloride

    Histone Methyltransferase Cancer
    OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells.
  • HY-100753
    STAT3-IN-1

    STAT Apoptosis Cancer
    STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis.
  • HY-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-119347
    Cirsilineol

    IFNAR STAT Cancer Inflammation/Immunology
    Cirsilineol, a natural flavone compound, selectively inhibits IFN-γ/STAT1/T-bet signaling in intestinal CD4 + T cells. Cirsilineol has potent immunosuppressive and anti-tumor properties. Cirsilineol significantly ameliorates trinitro-benzene sulfonic acid (TNBS)-induced T-cell-mediated experimental colitis in mice.
  • HY-101119
    GLL398

    Estrogen Receptor/ERR Cancer
    GLL398, an orally active selective estrogen receptor degrader (SERD), competitively binds to the estrogen receptor with an IC50 value of 1.14 nM. GLL398 exhibits a strong dose-dependent binding profile for the ER with a Y537S point mutation (IC50= 29.5 nM). GLL398 blocks tumor growth in xenograft breast cancer models.
  • HY-150505
    DC-U4106

    Deubiquitinase Apoptosis Cancer
    DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer.
  • HY-131088
    N3-PEG8-Phe-Lys-PABC-Gefitinib

    Drug-Linker Conjugates for ADC Cancer
    N3-PEG8-Phe-Lys-PABC-Gefitinib is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-tumor agent, Gefitinib (orally active EGFR tyrosine kinase inhibitor), linked via the cleavable linker N3-PEG8-Phe-Lys-PABC.
  • HY-13755
    Sulforaphane

    HDAC Keap1-Nrf2 Apoptosis Cancer Inflammation/Immunology
    Sulforaphane is an isothiocyanate present naturally in widely consumed vegetables. Sulforaphane increases tumor suppressor protein transcription and inhibits histone deacetylase activity. Sulforaphane activates Nrf2 and inhibits high glucose-induced progression of pancreatic cancer via AMPK dependent signaling. Sulforaphane has shown anti-cancer and anti-inflammatory activities.
  • HY-17364
    Temozolomide

    NSC 362856; CCRG 81045; TMZ

    DNA Alkylator/Crosslinker Autophagy Apoptosis Cancer
    Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects.
  • HY-117596
    UNC569

    TAM Receptor Cancer
    UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors research
  • HY-N0108
    Physcion

    Parietin; Rheochrysidin

    Bacterial Cancer Infection Inflammation/Immunology
    Physcion (Parietin) is an anthraquinone isolated from traditional Chinese medicine Radix et Rhizoma Rhei, acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively. Physcion (Parietin) exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects.
  • HY-100789
    ON1231320

    Polo-like Kinase (PLK) Apoptosis Cancer
    ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC50 of 0.31 µM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity.
  • HY-113314
    AFMK

    Endogenous Metabolite Cancer
    AFMK, antioxidant metabolite of Melatonin, attenuates X-ray-induced oxidative damage to DNA, proteins and lipids in mice. AFMK is a poorer scavenger. The pKa of AFMK at physiological pH is 8.7. Antioxidant capacity. AFMK improves the anti-tumor effect of Gemcitabine in PANC-1 cells through the modulation of apoptotic pathway.
  • HY-119198
    NSC745885

    Apoptosis Histone Methyltransferase Cancer
    NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers.
  • HY-139920A
    Oritinib mesylate

    SH-1028 mesylate

    EGFR Cancer
    Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation.
  • HY-103479
    GOAT-IN-1

    Acyltransferase Cancer Metabolic Disease Neurological Disease Cardiovascular Disease
    GOAT-IN-1 is an inhibitor of ghrelin O-acyltransferase (GOAT), which could be useful for the prophylaxis or treatment of obesity, diabetes, hyperlipidemia, metabolic, non-alcoholic fatty liver, steatohepatitis, sarcopenia, appetite control, alcohol/narcotic dependence, Alzheimer’s disease, Parkinson’s disease, cerebrovascular dementia, cerebral apoplexy, cerebral infarction, cardic disease, some kind of tumors.
  • HY-104077
    Remdesivir

    GS-5734

    DNA/RNA Synthesis SARS-CoV Infection
    Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity, has EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro.
  • HY-129189
    RAS GTPase inhibitor 1

    Ras Cancer
    RAS GTPase inhibitor 1 (example 51) is a RAS GTPase inhibitor with anti-tumor activity, extracted from patent WO2018212774A1. RAS GTPase inhibitor 1 (example 51) exhibits an EC50 less than 1 μM for at least one nucleotide exchange and an IC50 less than 1 μM in H727 cells.
  • HY-N5077B
    Sinapine hydroxide

    Cholinesterase (ChE) P-glycoprotein Cancer Inflammation/Immunology Neurological Disease
    Sinapine hydroxide is an alkaloid isolated from seeds of the cruciferous species. Sinapine hydroxide exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine hydroxide is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
  • HY-147308
    PCLX-001

    DNA/RNA Synthesis Cancer
    PCLX-001 is an orally acitve, small-molecule, dual N-myristoyltransferase (NMT) inhibitor, with IC50s of 5 nM (NMT1) and 8 nM (NMT2), respectively. PCLX-001 exhibits anti-tumor activity and inhibits early B-cell receptor (BCR) signaling, can be used to B-cell malignancies research.
  • HY-17406
    Tolcapone

    Ro 40-7592

    COMT Amyloid-β Apoptosis Cancer Neurological Disease
    Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma.
  • HY-112037A
    IACS-010759 hydrochloride

    IACS-10759 hydrochloride

    Mitochondrial Metabolism Apoptosis Cancer
    IACS-010759 hydrochlorideis an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 hydrochlorideinhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 hydrochloride has the potential for relapsed/refractory AML and solid tumors research.
  • HY-147414
    Vamotinib

    PF-114

    c-Met/HGFR Cancer
    Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia.
  • HY-P2268
    RAGE antagonist peptide