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cytotoxic agent

" in MCE Product Catalog:

117

Inhibitors & Agonists

1

Screening Libraries

1

Dye Reagents

1

Biochemical Assay Reagents

3

Inhibitory Antibodies

12

Natural
Products

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-144722
    Antitubercular agent-12

    Others Infection
    Antitubercular agent-12 (Compound 2c) is an antitubercular agent (MIC = 1.439 μg/mL). Antitubercular agent-12 shows greatly lower cytotoxicity (CC50: 57.34 μg/mL).
  • HY-147806
    Antiparasitic agent-8

    Parasite Infection
    Antiparasitic agent-8 (Compound 9) is an antiparasitic agent against Hymenolepis nana with low cytotoxicity.
  • HY-146417
    Antiviral agent 19

    Influenza Virus Infection
    Antiviral agent 19 (Compound 3) is a selective inhibitor against Zika virus infection with an EC50 of 1.3 µM. Antiviral agent 19 has low cytotoxicity.
  • HY-146418
    Antiviral agent 20

    Influenza Virus Infection
    Antiviral agent 20 (Compound 17b) is a selective inhibitor against Zika virus infection with an EC50 of 4.5 µM. Antiviral agent 20 has low cytotoxicity.
  • HY-147871
    Antimycobacterial agent-3

    Bacterial Infection
    Antimycobacterial agent-3 (Compound 1h) is an antimycobacterial agent against both drug-sensitive MTB strain H37Rv and drug-resistant clinical isolates (MIC: < 0.029–0.110 μM). Antimycobacterial agent-3 shows low cell cytotoxicity.
  • HY-147006
    MT-VC-ZD02044

    Others Cancer
    MT-VC-ZD02044 is a cytotoxic and anti-mitotic agent.
  • HY-147505
    Antitubercular agent-21

    Bacterial Fungal Infection
    Antitubercular agent-21 (Compound 15) is an antitubercular agent with an MIC of o.4 µg/mL against M. tuberculosis H37Rv. Antitubercular agent-21 exhibits lower activity against other microorganism such as bacteria gram-positive, gram-negative or fungi. Antitubercular agent-21 shows low cytotoxicity.
  • HY-147971
    Anticancer agent 75

    Parasite Topoisomerase Cancer Infection
    Anticancer agent 75 is a potent anticancer agent. Anticancer agent 75 shows cytotoxicity and selectivity in cancer cell lines. Anticancer agent 75 shows cytotoxicity to normal human kidney cell lines is at least 35 times lower than that of the Doxorubicin standard. Anticancer agent 75 shows good activity of antiplasmodial.
  • HY-130083
    Seco-Duocarmycin TM

    ADC Cytotoxin DNA Alkylator/Crosslinker Cancer
    Seco-Duocarmycin TM is a DNA alkylator agent belonging to Duocarmycins family that inhibits DNA synthesis. Seco-Duocarmycin TM is a cytotoxic agent, used as the cytotoxic component in antibody-drug conjugates (ADC)[1].
  • HY-N3741
    Didrovaltrate

    Didrovaltratum

    Others Cancer
    Didrovaltrate (Didrovaltratum), isolated from the roots of Valeriana wallichii D.C, is a cytotoxic and antitumor agent.
  • HY-147883
    Antitubercular agent-27

    Bacterial Infection
    Antitubercular agent-27 (compound 1) is a potent antitubercular agent with an IC50 value of 3.2 µM, an MIC value of 7.8 µM, an IC90 value of 7.0 µM. Antitubercular agent-27 shows antimycobacterial activity for resistant isolates of Mycobacterium tuberculosis H37Rv. Antitubercular agent-27 shows effective intracellular antimycobacterial activity and low cytotoxicity.
  • HY-147884
    Antitubercular agent-28

    Bacterial Infection
    Antitubercular agent-28 (compound 2) is a potent antitubercular agent with an IC50 value of 1.5 µM, an MIC value of 4.5 µM, an IC90 value of 2.5 µM. Antitubercular agent-28 shows antimycobacterial activity for resistant isolates of Mycobacterium tuberculosis H37Rv. Antitubercular agent-28 shows effective intracellular antimycobacterial activity and low cytotoxicity.
  • HY-147968
    Anticancer agent 74

    Cancer
    Anticancer agent 74 is a moderate anticancer agent. Anticancer agent 74 has lower selectivity and cytotoxicity than doxorubicin to normal cell.
  • HY-W028690
    DNMDP

    Phosphodiesterase (PDE) Cancer
    DNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, is a potent and selective cancer cell cytotoxic agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity.
  • 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-139705
    Anticancer agent 12

    Others Cancer
    Anticancer agent 12 is unexpectedly devoids of hepatotoxicity while maintaining cytotoxic activity in malignant cells.
  • HY-144632
    Antifungal agent 22

    Fungal Infection
    Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity.
  • HY-146406
    Anticancer agent 52

    Apoptosis Cancer
    Anticancer agent 52 is a potent anticancer agent. Anticancer agent 52 shows in vitro cytotoxicity. Anticancer agent 52 induces apoptosis. Anticancer agent 52 shows antitumor effect. Anticancer agent 52 has the potential for the research of bladder cancer.
  • HY-146197
    Apoptotic agent-1

    Apoptosis Cancer
    Apoptotic agent-1 (Compound 8a) is an apoptotic agent with high antiproliferative activity against cancer cells and low cytotoxic effect. Apoptotic agent-1 induces over-expression of Fas receptor and Cyto C genes.
  • HY-146348
    Tuberculosis inhibitor 5

    Bacterial Infection
    Tuberculosis inhibitor 5 (Compound 11i) is a potent antimycobacterial biphenyl analogue without noticeable cytotoxicity. Tuberculosis inhibitor 5 is an anti-tuberculosis agent.
  • HY-147534
    Antileishmanial agent-6

    Parasite Infection
    Antileishmanial agent-6 (compound 8m) is a potent antileishmanial agent. Antileishmanial agent-6 shows antileishmanial and cytotoxic activity against Leishmania donovani and L-6, with IC50 values of 0.54 and 10.2 μM, respectively.
  • HY-146286
    Anticancer agent 44

    Apoptosis Cancer
    Anticancer agent 44 (compound 2a) is a potent anticancer agent. Anticancer agent 44 shows cytotoxicity activity in cancer cells. Anticancer agent 44 induces apoptosis. Anticancer agent 44 shows low toxicity towards activated lymphocytes of human blood.
  • HY-147538
    Antitumor agent-64

    Apoptosis Cancer
    Antitumor agent-64 (Compound 8d) is a diosgenin derivative. Antitumor agent-64 exhibits potent cytotoxic activity against A549 cell line. Antitumor agent-64 induces A549 cells apoptosis via the mitochondria-related pathway.
  • HY-143641
    Anticancer agent 25

    Others Cancer
    Anticancer agent 25 exhibits the strongest cytotoxicity against PC3 cells with an IC50 value of 0.19 μM.
  • HY-137773
    N-Methyl pemetrexed

    Others Cancer
    N-Methyl pemetrexed is an impurity of Pemetrexed. Pemetrexed is an antifolate cytotoxic agent that can be used for the research of cancer.
  • HY-101127
    SGD-1882

    PBD dimer

    ADC Cytotoxin Cancer
    SGD-1882 is a cytotoxic, DNA minor-groove crosslinking agent pyrrolobenzodiazepine (PBD) dimer, acting as the payload for ADCs.
  • HY-146290
    Anticancer agent 45

    Apoptosis Cancer
    Anticancer agent 46 (compound 2b) is a potent and selective anticancer agent. Anticancer agent 46 shows cytotoxicity activity in cancer cells. Anticancer agent 46 induces apoptosis. Anticancer agent 46 shows low toxicity towards activated lymphocytes of human blood.
  • HY-145908
    Antitumor agent-49

    Others Cancer
    Antitumor agent-49 (Compound 10) is a Harmine derivative-furoxan hybrids containing NO donor, with antitumor activities. Antitumor agent-49 shows cytotoxic activity against HepG2 cells with an IC50 of 1.79 µM. Antitumor agent-49 produces high levels of NO in vitro.
  • HY-146407
    Anticancer agent 53

    Apoptosis Cancer
    Anticancer agent 53 is a potent anticancer agent. Anticancer agent 53 shows in vitro cytotoxicity. Anticancer agent 53 induces apoptosis and cell cycle arrest in S/G2/M phases. Anticancer agent 53 shows antitumor activity with no apparent toxicity.
  • HY-19609
    Calicheamicin

    Calicheamicin γ1

    DNA Alkylator/Crosslinker ADC Cytotoxin Bacterial Apoptosis Antibiotic Cancer Infection
    Calicheamicin, an antitumor antibiotic, is a cytotoxic agent that causes double-strand DNA breaks. Calicheamicin is a DNA synthesis inhibitor.
  • HY-13640
    Rabacfosadine

    GS-9219; VDC-1101

    Nucleoside Antimetabolite/Analog Cancer
    Rabacfosadine (GS-9219), a novel prodrug of the nucleotide analogue PMEG, is designed as a cytotoxic agent that preferentially targets lymphoid cells.
  • HY-146359
    Influenza A virus-IN-5

    Influenza Virus DNA/RNA Synthesis Infection
    Influenza A virus-IN-5 (Compound 16e) is a potent, orally active anti-influenza A virus (IAV) agent with an IC50 of 1.29 μM. Influenza A virus-IN-5 inhibits the transcription and replication of viral RNA with acceptable cytotoxicity.
  • 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-146496
    Antitubercular agent-20

    Bacterial Infection
    Antitubercular agent-20 (Compound 2d) is an orally active antitubercular agent. Antitubercular agent-20 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: <0.016 µg/ml). Antitubercular agent-20 has low cytotoxicity and good tolerance in BALB/c mice.
  • HY-146495
    Antitubercular agent-19

    Bacterial Infection
    Antitubercular agent-19 (Compound 1c) is an antitubercular agent. Antitubercular agent-19 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: <0.016 µg/ml). Antitubercular agent-19 shows low cytotoxicity and relatively high acute lethal toxicity in BALB/c mice.
  • HY-115949
    Antitumor agent-47

    Others Cancer
    Antitumor agent-47 (Compound 3e) is a silibinin derivative with an antitumor activity. Antitumor agent-47 shows cytotoxic activity against NCI-H1299 and HT29 cells with IC50 values of 8.07 µM and 6.27 µM, respectively.
  • HY-147704
    Antimycobacterial agent-2

    Bacterial Infection
    Antimycobacterial agent-2 (compound 58) is a potent antimycobacterial agent. Antimycobacterial agent-2 shows anti-mycobacterial activities with an MIC99 of 0.8 µM for Mycobacterium tuberculosis (M.tb) H37Rv. Antimycobacterial agent-2 shows cytotoxic activities with an IC50 of48.1 µM for CHO cells.
  • 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-146043
    Antiparasitic agent-5

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

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

    Parasite Infection
    Antiparasitic agent-7 (compound 5d) has selectively antiparasitic activity against Leishmania infantum (L. infantum) with an IC50 value of 2.85 μM. Antiparasitic agent-7 also has certain cytotoxicity against HepG2 (CC50 = 10.61 μM).
  • HY-147970
    Antifungal agent 34

    Fungal Infection
    Antifungal agent 34 (compound 6i) is a potent antifungal agent. Antifungal agent 34 shows a potent antifungal activity against Candida albicans, with a MIC of 4 µg/mL. Antifungal agent 34 shows significant inhibition on Candida albicans hyphae and biofilm development. Antifungal agent 34 exhibits no cytotoxicity to mammalian cells.
  • HY-147536
    Antileishmanial agent-8

    Parasite Infection
    Antileishmanial agent-8 (compound 18) has potent and selective activity against Leishmania donovani (L. donovani) with an IC50 value of 5.64 μM. Antileishmanial agent-8 has relatively low cytotoxicity in L-6 cells (IC50=73.9 μM).
  • HY-142545
    Antibacterial agent 68

    Bacterial Infection
    Antibacterial agent 68 (compound 4d) is an antibacterial agent against drug-resistant Escherichia coli. Antibacterial agent 68 has low cytotoxicity and exerts strong antibacterial activities against multidrug-resistant Escherichia coli at low concentrations as 0.007 mM.
  • HY-146104
    Antimycobacterial agent-1

    Bacterial Infection
    Antimycobacterial agent-1 (compound 33) has selectively antimycobacterial activity against Mycobacterium tuberculosis (M. tuberculosis) H37Ra with a MIC value of 1 μg/ml. Antimycobacterial agent-1 has relatively low cytotoxicity in normal cells (Vero cells IC50 = 143.2 μg/ml).
  • HY-146389
    Anticancer agent 50

    MDM-2/p53 P-glycoprotein Cancer
    Anticancer agent 50 (compound 6) is a potent ABCB1 efflux pump modulator. Anticancer agent 50 shows cytotoxic effects and antiproliferative effects. Anticancer agent 50 decreases the expression of cyclin D1 and induces p53 expression. Anticancer agent 50 has the potential for the research of T-lymphoma.
  • HY-146547
    Anti-inflammatory agent 17

    Inflammation/Immunology
    Anti-inflammatory agent 17 is a potent and orally active anti-inflammatory agent. Anti-inflammatory agent 17 inhibits the release of IL-6 and TNF-α in vitro experiments without cytotoxicity. Anti-inflammatory agent 17 exhibits anti-inflammatory activity in vivo. Anti-inflammatory agent 17 has the potential for the research of Acute lung injury (ALI).
  • HY-12456
    Duocarmycin SA

    ADC Cytotoxin DNA Alkylator/Crosslinker Cancer
    Duocarmycin SA is a potent antitumor antibiotic with an IC50 of 10 pM. Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro.
  • HY-146078
    Antimicrobial agent-1

    Bacterial Infection
    Antimicrobial agent-1 (compound 6C) possesses potent activity against TolC mutant E. coli with an MIC value of 2 μg/mL. Antimicrobial agent-1 and Colistin exhibit synergistic activity against Gram-negative bacteria. Antimicrobial agent-1 has no cytotoxicity on mammalian cell lines, with MICs > 128 μg/mL in Caco-2 and Vero 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-14769
    Folitixorin

    5,10-Methylenetetrafolate; ANX-510 free acid

    Endogenous Metabolite Cancer
    Folitixorin (5,10-methylenetetrahydrofolate) is a cofactor and an analog of leucovorin. Folitixorin is a promising agent for modulation of 5-FU cytotoxicity in adjuvant cancer research.
  • HY-146057
    Antituberculosis agent-2

    Bacterial Infection
    Antituberculosis agent-2 (Compound 8d) is an antituberculosis agent against drug-sensitive and multidrug-resistant tuberculosis. Antituberculosis agent-2 shows anti-tuberculosis activity with MIC values of 0.454, 1.757 and 1.644 µg/mL against M. tuberculosis H37Rv, 13946 and 14862, respectively. Antituberculosis agent-2 displays favorable mouse and human microsomal stability, low cytotoxicity, and acceptable oral bioavailability.
  • HY-149013
    Anti-MRSA agent 5

    Bacterial Infection
    Anti-MRSA agent 5 (B14) is a potent
    MRSA
    agent with MIC50 values of 0.38 μg/mL and has low hERG activity with an IC50 values of >40 μM. Anti-MRSA agent 5 (B14) also has low cytotoxicity to mammal cells and unlikely to acquire bacterial resistance.
  • HY-146042
    Antiparasitic agent-4

    Parasite Infection
    Antiparasitic agent-4 (compound 4q) has highly antiparasitic activity against Leishmania infantum (L. infantum) and Trypanosoma cruzi (T. cruzi) with IC50s of 8.51 μM and 2.20 μM, respectively. Antiparasitic agent-4 also has certain cytotoxicity against HepG2 (CC50 = 18.97 μM).
  • HY-147514
    Anticancer agent 64

    Apoptosis Caspase PARP Bcl-2 Family Cancer
    Anticancer agent 64 (compound 5m) shows cytotoxic activity in CCRF-CEM cells, with IC50 of 2.4 μM. Anticancer agent 64 shows good anticancer activity through apoptosis induction. Anticancer agent 64 induces caspase 3 and 7 activation and PARP cleavage. Anticancer agent 64 induces significant effect of mitochondria depolarization.
  • HY-146041
    Antiparasitic agent-2

    Parasite Infection
    Antiparasitic agent-2 (compound 8a) has highly antiparasitic activity against Leishmania infantum (L. infantum) and Trypanosoma cruzi (T. cruzi) with IC50s of 7.28 μM and 2.30 μM, respectively. Antiparasitic agent-2 also has certain cytotoxicity against HepG2 (CC50 = 26.79 μM).
  • HY-14907
    Verubulin

    MPC 6827

    Microtubule/Tubulin Apoptosis Cancer
    Verubulin (MPC-6827) is a microtubule-disrupting agent with potent and broad-spectrum in vitro and in vivo cytotoxic activities, and acts as a promising candidate for the treatment of multiple cancer types.
  • HY-116786
    11-Hydroxycanthin-6-one

    Others Cancer
    11-Hydroxycanthin-6-one, a canthin-6-one alkaloid, is an antitumor agent which shows potent cytotoxic activity.
  • HY-146428
    Anti-MRSA agent 4

    Bacterial Infection
    Anti-MRSA agent 4 (compound 7a) is a potent and selective growth inhibitor of Gram-positive Methicillin-resistant Staphylococcus aureus (MRSA), with MIC ≤ 0.26 µM. Anti-MRSA agent 4 exhibits no cytotoxic and no hemolytic activity in HEK293 cells.
  • HY-146421
    Anti-inflammatory agent 21

    NO Synthase NF-κB Reactive Oxygen Species Inflammation/Immunology
    Anti-inflammatory agent 21 (compound 9o) is an orally active and low cytotoxic anti-inflammatory agent, with an IC50 value of 0.76 μM for NO. Anti-inflammatory agent 21 acts via accumulation ROS and blocks the NF-κB/MAPK signaling pathway. Anti-inflammatory agent 21 can ameliorate cartilage destruction and inflammatory cell infiltration in arthritis rats model.
  • HY-115905
    Antimalarial agent 9

    Others Infection
    Antimalarial agent 9 (Compound 11) is a potent antimalarial agent. Antimalarial agent 9 is a quinoline-imidazole derivative compound. Antimalarial agent 9 exhibits significant antimalarial efficacy in-vitro against both CQ-sensitive (IC50-0.14 μM) and MDR strain (IC50-0.41 μM) with minimal cytotoxicity and high selectivity.
  • HY-15579S
    D8-MMAF

    Monomethylauristatin F D8

    Microtubule/Tubulin ADC Cytotoxin Cancer
    D8-MMAF hydrochloride is a deuterated form of MMAF hydrochloride. MMAF Hydrochloride, a potent tubulin polymerization inhibitor, is used as a antitumor agent and a cytotoxic component of antibody-drug conjugates (ADCs).
  • HY-19118
    KP1019

    FFC14A

    Apoptosis Cancer
    KP1019 (FFC14A) is a Ru(III)-based anti-metastatic and cytotoxic anti-cancer agent. KP1019 induces DNA damage and apoptosis in cancer cells.
  • HY-143232
    Antibacterial agent 73

    Fungal Bacterial Cancer Infection
    Antibacterial agent 73 (compound 7a) is a potent antimicrobial agent. Antibacterial agent 73 exhibits very good antitubercular activity (MIC=0.65 µg/mL) against Mtb H37Rv. Antibacterial agent 73 shows good activity against fungal and bacterial. Antibacterial agent 73 also shows cytotoxicity in MCF-7 breast cancer cell lines, with IC50 of 8.20 μM.
  • HY-146557
    Antitubercular agent-16

    Bacterial Infection
    Antitubercular agent-16 (Compound 5q) is an antitubercular agent with MIC90 values of 0.40, 20.11, 23.51, 19.62, 10.93 and 13.62 μg/mL against M. tuberculosis H37Rv, CF16, CF61, CF76, CF152 and CF161, respectively. Antitubercular agent-16 shows low cytotoxicity against macrophages and pulmonary fibroblasts.
  • HY-146556
    Antitubercular agent-15

    Bacterial Infection
    Antitubercular agent-15 (Compound 5n) is an antitubercular agent with MIC90 values of 0.73, 7.69, 9.38, 18.80, 7.53 and 7.31 μg/mL against M. tuberculosis H37Rv, CF16, CF61, CF76, CF152 and CF161, respectively. Antitubercular agent-15 shows low cytotoxicity against macrophages and pulmonary fibroblasts.
  • HY-115950
    Antitumor agent-48

    Others Cancer
    Antitumor agent-48 (Compound 4a) is a 2,3-dehydrosilybin derivative with an antitumor activity. Antitumor agent-48 shows cytotoxic activity against MCF-7, NCI-H1299, HepG2 and HT29 cells with IC50 values of 8.06 µM, 13.1 µM, 16.51 µM and 12.44 µM, respectively.
  • HY-147816
    Anticancer agent 70

    Mitochondrial Metabolism Cancer
    Anticancer agent 70 (Compound 21), an anticancer agent, exhibits remarkable cytotoxic activity against numerous human cancer cell lines. Anticancer agent 70 results in the G0/G1-cell cycle arrest with a concomitant increase in p53 and p21 protein levels. Anticancer agent 70 leads to ATP depletion and disruption of the mitochondrial membrane potential.
  • 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-N6997
    Ceratamine A

    Microtubule/Tubulin Cancer
    Ceratamine A is an antimitotic heterocyclic alkaloid isolated from the marine sponge Pseudoceratina sp., acts as a microtubule-stabilizing agent. Ceratamine A exhibits cytotoxicity against human cancer cell lines.
  • HY-N2877
    Annonacin

    Potassium Channel Sodium Channel Na+/K+ ATPase Calcium Channel Neurological Disease
    Annonacin is an Acetogenin and promotes cytotoxicity via a pathway inhibiting the mitochondrial complex. Annonacin is the active agent found in Graviola leaf extract to act as an inhibitor of sodium/potassium (NKA) and sarcoplasmic reticulum (SERCA) ATPase pumps.
  • HY-144822
    Anti-MRSA agent 2

    Bacterial Infection
    Anti-MRSA agent 2 (compound 14) has highly inhibitory activity against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 0.098 μg/ml, and relatively low cytotoxicity in normal cells. Anti-MRSA agent 2 has strong ability to destroy bacterial membrane and bind to genomic DNA.
  • HY-15579A
    MMAF hydrochloride

    Monomethylauristatin F hydrochloride

    Microtubule/Tubulin ADC Cytotoxin Cancer
    MMAF (Monomethylauristatin F) hydrochloride is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF hydrochloride is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A.
  • HY-135901
    Py-MPB-amino-C3-PBD

    ADC Cytotoxin Bacterial Cancer
    Py-MPB-amino-C3-PBD is a cytotoxic agent comprised non-alkylating group. Py-MPB-amino-C3-PBD acts as the payload for ADCs. Antimicrobial activity.
  • HY-105019A
    Melflufen hydrochloride

    Melphalan flufenamide hydrochloride

    DNA Alkylator/Crosslinker Apoptosis Cancer
    Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells.
  • HY-105019
    Melflufen

    Melphalan flufenamide

    DNA Alkylator/Crosslinker Apoptosis Cancer
    Melflufen (Melphalan flufenamide), a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells.
  • HY-128941
    CCK2R Ligand-Linker Conjugates 1

    Drug-Linker Conjugates for ADC Cancer
    CCK2R Ligand-Linker Conjugates 1 is a ligand-linker conjugate, which conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) via a hydrophilic peptide linker.
  • HY-139882
    Anticancer agent 16

    Others Cancer
    Anticancer agent 16 exhibits good cytotoxic activity against HCT-116, NCI-H460, and SKOV3 cell lines with IC50 8.55 μΜ, 5.41 μΜ, and 6.4 μΜ, respectively.
  • HY-144823
    Anti-MRSA agent 3

    Bacterial Infection
    Anti-MRSA agent 3 (compound 18) has highly inhibitory activity against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 0.098 μg/ml, and low cytotoxicity in normal cells. Anti-MRSA agent 3 has relatively strong ability to destroy bacterial cell wall and membrane, high binding affinity to bacterial genomic DNA.
  • HY-135900
    Aniline-MPB-amino-C3-PBD

    ADC Cytotoxin Bacterial Cancer
    Aniline-MPB-amino-C3-PBD is a cytotoxic agent comprised non-alkylating group. Aniline-MPB-amino-C3-PBD is a sequence-selective DNA minor-groove binding agent. Aniline-MPB-amino-C3-PBD acts as the payload for ADCs. Antimicrobial activity.
  • HY-15579B
    MMAF sodium

    Monomethylauristatin F sodium

    Microtubule/Tubulin ADC Cytotoxin Cancer
    MMAF sodium (Monomethylauristatin F sodium) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF sodium (Monomethylauristatin F sodium) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A.
  • HY-15579
    MMAF

    Monomethylauristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    MMAF (Monomethylauristatin F) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF (Monomethylauristatin F) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin and SGN-CD19A.
  • 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-147933
    Antitrypanosomal agent 8

    Parasite Infection
    Antitrypanosomal agent 8 (compound 3b) has potent antitrypanosomal activity against Trypanosoma brucei with an IC50 value of 0.79 μM and exhibits certain cytotoxicity in L6 cells (IC50=80.95 μM).
  • HY-146226
    Viral 2C protein inhibitor 1

    Enterovirus Infection
    Viral 2C protein inhibitor 1 (compound 6aw) is a potent and broad-spectrum enterovirus antiviral agent, inhibiting viral 2C protein. Viral 2C protein inhibitor 1 inhibits multiple strains of EV-D68, EV-A71 and CVB3 with EC50s of 0.1~3.6 µM, and exhibits high selectivity index and relatively low cytotoxicity.
  • HY-128952
    Tesirine

    SG3249

    Drug-Linker Conjugates for ADC DNA Alkylator/Crosslinker Cancer
    Tesirine (SG3249) is an antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload. Tesirine combines potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics. SG3199 (HY-101161) is the released warhead component of the ADC payload Tesirine. SG3199 retains picomolar activity in a panel of cancer cell lines. PBD dimers are highly efficient DNA minor groove cross-linking agents with potent cytotoxicity.
  • HY-122751
    (R)-DNMDP

    Phosphodiesterase (PDE) Cancer
    (R)-DNMDP is a potent and selective cancer cell cytotoxic agent. (R)-DNMDP, the R-form of DNMDP, binds PDE3A directly. (R)-DNMDP has a 500-fold lower EC50 compared to the (S)-enantiomer in HeLa cell line.
  • HY-121300
    Kendomycin

    (-)-TAN2162

    Antibiotic Bacterial Endothelin Receptor CGRP Receptor Cancer Infection
    Kendomycin ((−)-TAN 2162) is a polyketide antibiotic with remarkable antibacterial and cancer cells cytotoxic activities. Kendomycin tends to be bacteriostatic rather than bactericidal and inhibits the growth of the methicillin-resistant Staphylococcus aureus (MRSA) strain COL at a low concentration (MIC of 5 μg/mL). Kendomycin is a potent antagonist of the endothelin receptor and a calcitonin receptor agonist which plays its role as an anti-osteoporotic agent.
  • HY-108391
    C8-Ceramide

    N-Octanoyl-D-erythro-sphingosine

    Apoptosis PKC Autophagy Cancer Inflammation/Immunology
    C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro.
  • HY-W011762
    VK3-OCH3

    Others Cancer
    VK3-OCH3 is a potent antitumor agent. VK3-OCH3 shows cytotoxicity for neuroblastoma cell lines and low cytotoxicity for normal cell lines. VK3-OCH3 induces apoptosis and cell cycle arrest at G2/M phase in IMR-32 cells. VK3-OCH3 shows antitumor activity.
  • HY-U00279
    Nitracrine

    DNA/RNA Synthesis Cancer
    Nitracrine inhibits RNA synthesis and covalently, reversibly binds to DNA but also forms covalent adducts with DNA in vivo. Nitracrine, a 1-nitroacridine derivative, is a potent hypoxia-selective agent in vitro and antitumor drug. Nitracrine has cytotoxicity towards most cells.
  • HY-N4278
    Huangjiangsu A

    Reactive Oxygen Species Inflammation/Immunology
    Huangjiangsu A, pseudoprotodioscin, methyl protobioside, protodioscin, and protodeltonin, isolated from D. villosa. Huangjiangsu A has hepatoprotective potential against H2O2-induced cytotoxicity and ROS generation and could be promising as potential therapeutic agents for liver diseases.
  • HY-P9985
    Disitamab vedotin

    RC48

    Antibody-Drug Conjugates (ADCs) EGFR Cancer
    Disitamab vedotin (RC48) is an antibody-drug conjugate (ADC) comprising a monoclonal antibody against human epidermal growth factor receptor 2 (HER2) conjugated via a cleavable linker to the cytotoxic agent Monomethyl auristatin E (MMAE). Disitamab vedotin enhances antitumor immunity.
  • 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-P9921
    Trastuzumab emtansine

    Ado-Trastuzumab emtansine; PRO132365; T-DM 1

    Antibody-Drug Conjugates (ADCs) EGFR Cancer
    Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer.
  • HY-147881
    Anti-Influenza agent 3

    Influenza Virus Infection
    Anti-Influenza agent 3 (compound 11h) is a potent anti-influenza agent with EC50 values of 3.29, 2.45 µM for A/HK/68 (H3N2, M2-WT), A/WSN/33 (H1N1, M2-S31N) strain, respectively. Anti-Influenza agent 3 shows low cytotoxicity for MDCK epithelial cells. Anti-Influenza agent 3 inhibits the M2 WT and S31N ion channel conductivity.
  • 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-112732
    Sparfosic acid

    Apoptosis Cancer Metabolic Disease
    Sparfosic acid, a DNA antimetabolite agent, is a potent inhibitor of aspartate transcarbamoyl transferase, the enzyme catalyzing the second step of de novo pyrimidine biosynthesis. Sparfosic acid synergistically enhances the cytotoxicity of a combination of 5-fluorouracil (5-FU) and interferon-alpha (IFN) against human colon cancer cell lines.
  • 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-15311
    Avermectin B1

    Abamectin; Avermectin B1a-Avermectin B1b mixt.

    Parasite Autophagy Apoptosis Reactive Oxygen Species Infection Inflammation/Immunology
    Avermectin B1 (Abamectin) is a mixture of two similar segments of avermectin. Avermectin B1 is an orally anti-infection agent, which can be used in the research of parasitic worms, insect pests, agriculture and animal husbandry. Avermectin B1 can also induce the production of ROS and induces cytotoxicity, apoptosis and autophagy.
  • 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-112732B
    Sparfosic acid trisodium

    Apoptosis Cancer Metabolic Disease
    Sparfosic acid trisodium is a DNA antimetabolite agent and a potent inhibitor of aspartate transcarbamoyl transferase. Aspartate transcarbamoyl transferase catalyzes the second step of de novo pyrimidine biosynthesis. Sparfosic acid trisodium synergistically enhances the cytotoxicity of a combination of 5-fluorouracil (5-FU) and interferon-alpha (IFN) against human colon cancer cell lines.
  • HY-P99107
    Brentuximab vedotin

    Antibody-Drug Conjugates (ADCs) Apoptosis Cancer
    Brentuximab vedotin (cAC10-vcMMAE) is an antibody-drug conjugate (ADC) comprising an anti- CD30 antibody and the cytotoxic agent Monomethyl auristatin E (MMAE). Brentuximab vedotin inhibits CD30-positive cells with an IC50 of 2.5 ng/mL. Brentuximab vedotin can be used for the research of relapsed and refractory Hodgkin lymphoma.
  • HY-15142
    Doxorubicin hydrochloride

    Hydroxydaunorubicin hydrochloride

    Topoisomerase ADC Cytotoxin AMPK Autophagy Apoptosis HIV HBV Mitophagy Antibiotic Bacterial Cancer Infection
    Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy.
  • HY-12098
    Verubulin hydrochloride

    MPC-6827 hydrochloride

    Microtubule/Tubulin Cancer
    Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types.
  • HY-15142A
    Doxorubicin

    Hydroxydaunorubicin

    Topoisomerase ADC Cytotoxin AMPK Autophagy Mitophagy Apoptosis Antibiotic Bacterial HBV HIV Cancer Infection
    Doxorubicin (Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy. Doxorubicin inhibits human DNA topoisomerase I with an IC50 of 0.8 μM.
  • HY-133147
    HDAC3/6-IN-2

    HDAC Apoptosis Cancer
    HDAC3/6-IN-2 (compound 15) is a potent HDAC6 and HDAC3 inhibitor, with IC50 values of 0.368 and 0.635 μM, respectively. HDAC3/6-IN-2 shows antitumor activity, and induces cancer cell apoptosis. HDAC3/6-IN-2 decreases the levels of HDAC6 and HDAC3, associated with upregulation of acetylated H3 and α-tubulin.
  • HY-146087
    Autophagy inducer 4

    Autophagy Cancer
    Autophagy inducer 4 is a Magnolol-based Mannich base derivatives, which can be used as an anticancer agent. Autophagy inducer 4 suppresses cancer cells via inducing autophagy. Autophagy inducer 4 has 76-fold improvement in cytotoxicity against T47D cells compared with Magnolol. Autophagy inducer 4 also possesses suppressive effects on migration of T47D and Hela cancer cells.
  • HY-143755
    Cap-dependent endonuclease-IN-9

    Influenza Virus Infection
    Cap-dependent endonuclease-IN-9 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-9 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-9 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent CN112521386A, compound VI-1).
  • HY-D0190
    2-Thenoyltrifluoroacetone

    HTTA; TTA; TTFA

    Others Cancer Infection Others
    2-Thenoyltrifluoroacetone is a chelating agent. 2-Thenoyltrifluoroacetone can be used for the complexation of various metal ions including Mn(II), Co(III), Ni(II), et al.. 2-Thenoyltrifluoroacetone possesses antitubercular and cytotoxic activities. 2-Thenoyltrifluoroacetone is also used as common inhibitor of mitochondrial electron flux and to analyze the endothelial cell dysfunction. Besides, copper (II) complex of 2-Thenoyltrifluoroacetone has anticancer activity against K562.
  • HY-143743
    Cap-dependent endonuclease-IN-2

    Influenza Virus Infection
    Cap-dependent endonuclease-IN-2 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-2 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-2 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent WO2019052565A1, compound 28).
  • HY-143744
    Cap-dependent endonuclease-IN-3

    Influenza Virus Infection
    Cap-dependent endonuclease-IN-3 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-3 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-3 has the potential for the research of influenza A and influenza B infection (extracted from patent WO2019141179A1, compound VI-1).
  • HY-114778
    Fluzoparib

    SHR3162; Fuzuloparib

    PARP Cancer
    Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell‐free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)‐deficient cells, and sensitizes both HR‐deficient and HR‐proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research.
  • HY-124623
    DNDI-8219

    Parasite Infection
    DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.
  • HY-146158
    WX-081

    Bacterial Potassium Channel Antibiotic Infection
    WX-081, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity. WX-081 exhibits potent activity with MIC50s of 0.083 and 0.11 μg/mL for drug susceptible tuberculosis (DS-TB) and multidrug resistant tuberculosis (MDR-TB) strains. WX-081 also inhibits hERG channel with the IC50 of 1.89 μM.
  • HY-101287
    MPT0B392

    Microtubule/Tubulin JNK Apoptosis Caspase Cancer
    MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line.
  • 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.