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combined anticancer

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22

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Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-111373
    RapaLink-1
    10+ Cited Publications

    mTOR Autophagy Cancer
    RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity .
    RapaLink-1
  • HY-159127

    Ras MEK PERK Apoptosis Cancer
    HRS-4642 is a high affinity, selective, long-acting, and non-covalent KRAS G12D inhibitor with a Kd value of 0.083 nM. HRS-4642 inhibits the binding of KRAS G12D to SOS1 or RAF1, thereby blocking the downstream MEK-ERK signaling pathway. HRS-4642 promotes Apoptosis. HRS-4642 alone or combined with Carfilzomib (HY-10455) effectively shapes the tumor microenvironment. HRS-4642 has an anti-cancer effect on pancreatic and colorectal cancers carrying the KRAS G12D mutation[1][2][3].
    HRS-4642
  • HY-114243

    NF-κB JNK Caspase Apoptosis Neurological Disease Cancer
    DpC is a selective, orally active iron chelator with anticancer activity. DpC acts on signaling pathway-related targets such as JNK, NF-κB, and its activity is competitively inhibited by another iron chelator Dp44mT (HY-18973). By chelating intracellular iron and copper ions in tumor cells to form redox-active complexes, DpC induces oxidative stress, activates the JNK, NF-κB pathways and downregulates IκBα, upregulates the expressions of neuroglobin and cytoglobin, activates caspase 3/9 to induce tumor cell apoptosis. It also overcomes P-glycoprotein-mediated multidrug resistance through a lysosome-targeting mechanism, and exhibits broad-spectrum synergistic effects when combined with various chemotherapeutic agents. DpC inhibits tumor metastasis and increases TNF-α levels in the tumor microenvironment to enhance endogenous immune responses. DpC is applicable to the research of various malignancies including neuroblastoma, pancreatic cancer, prostate cancer, lung cancer, and breast cancer .
    DpC
  • HY-N4246

    Aquaporin PKC Akt PI3K Apoptosis Monoamine Oxidase Pregnane X Receptor (PXR) Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Bacopaside I is an orally active aquaporin AQP1 inhibitor and PKC modulator with neuroprotective and anticancer activities. Bacopaside I specifically blocks the water channel and cGMP-gated ion channel activities of AQP1 without affecting AQP4, thereby inhibiting the migration of colon cancer cells expressing AQP1. Bacopaside I activates the Akt pathway by interacting with PI3K, specifically inhibits MAO-A, effectively alleviates neuron necrosis and apoptosis induced by oxygen-glucose deprivation, reduces oxidative stress, and regulates the surface expression of neuroreceptors. When combined with Bacopaside II (HY-N6016), Bacopaside I significantly reduces the viability, proliferation and invasion ability of breast cancer cells, and binds to the pregnane X receptor (PXR). Bacopaside I is applicable to the research of colon cancer, breast cancer, vascular dementia, cerebral ischemia and other related diseases .
    Bacopaside I
  • HY-P990552A

    PAI-1 Integrin Cancer
    huATN-658 is an inhibitor that specifically targets the DIII domain of human urokinase plasminogen activator receptor (uPAR). huATN-658 neutralizes uPAR function by blocking the interaction between uPAR and integrins, without interfering with the binding of uPA or vitronectin to uPAR. huATN-658 inhibits the proliferation and invasion of breast cancer cells, slows the growth of primary breast tumors, reduces breast cancer-induced bone lesions and decreases osteoclast activity. huATN-658 also alters the gene expression of the TGF-β receptor complex signaling pathway. huATN-658 exerts synergistic anticancer effects when combined with Zoledronic Acid (HY-13777), and does not cause physiological or behavioral abnormalities in immunodeficient mice. huATN-658 can be used in research related to breast cancer, metastatic breast cancer and breast cancer-induced bone disease .
    huATN-658
  • HY-148702

    Liposome Cancer
    di-Pal-MTO is a palm oil-based lipid produced by combining the anticancer agent mitoxantrone (MTO) with palmitoleic acid. When nanoparticles of mono-Pal-MTO and di-Pal-MTO are combined in a molar ratio of 1:1, they show effective siRNA cell delivery and enhance anticancer activity .
    di-Pal-MTO
  • HY-18668

    Integrin Cancer
    Integrin antagonist 27 (Compound 27) is a small molecule integrin αvβ3 antagonist with an affinity of 18 nM. Integrin antagonist 27 can be combined with Paclitaxel (HY-B0015) to selectively target αvβ3-positive metastatic cancer cells. Integrin antagonist 27 is used as an anticancer agent .
    Integrin antagonist 27
  • HY-N10159

    E1/E2/E3 Enzyme Cancer
    1-Benzyl-I3C is a NEDD4-1 inhibitor with significant anticancer activity. 1-Benzyl-I3C can directly inhibit the ubiquitination activity of NEDD4-1 with an IC50 of 12.3μM, which is significantly better than its precursor compound I3C of 284μM. 1-Benzyl-I3C and its analogs showed good effects in inhibiting the proliferation of human melanoma cells, which is roughly related to their potency as NEDD4-1 enzyme inhibitors. By combining in vitro ubiquitination experiments and thermal stability analysis, 1-Benzyl-I3C was shown to be able to bind to the catalytic HECT domain of NEDD4-1 .
    1-Benzyl-I3C
  • HY-117884

    Apoptosis Cancer
    (Rac)-CCT 250863 (compound rac-21) is a selective and reversible NEK 2 inhibitor with an IC50 of 0.073 µM. (Rac)-CCT 250863 shows good effects of inducing cell cycle arrest and also can antiproliferative in cells (Pomalidomide sensitive/resistant). (Rac)-CCT 250863 induces apoptosis when combines with Pomalidomide .
    (Rac)-CCT 250863
  • HY-117720

    PKC Apoptosis Cancer
    OSU-2S is a potent PKCδ activator. OSU-2S inhibits cell proliferation and migration. OSU-2S decreases the expression of p-ERK1/2, increases the expression of PKCδ (38 kDa) when combined with Sorafenib (HY-10201). OSU-2S induces Apoptosis. OSU-2S slao is a non-immunosuppressive analogue of FTY720. OSU-2S shows anticancer activity .
    OSU-2S
  • HY-N2492

    Methyl trans-p-coumarate

    Apoptosis Interleukin Related GSK-3 Parasite Infection Cancer
    (E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate) is a phenolic compound and derivative of Cinnamic acid (HY-N0610A). (E)-Methyl 4-coumarate can be found in several plants, such as the leaves of Allium cepa and Morinda citrifolia L. (E)-Methyl 4-coumarate, when combined with Carnosic acid (HY-N0644), induces Apoptosis. (E)-Methyl 4-coumarate inhibits GSK3β activity and modulates inflammatory cytokine levels (increasing IL-10 and decreasing IL-4). (E)-Methyl 4-coumarate combined with Carnosic acid exhibits anticancer effects against acute myeloid leukemia. (E)-Methyl 4-coumarate ameliorates Plasmodium berghei NK65 infection .
    (E)-Methyl 4-coumarate
  • HY-173116

    Carbonic Anhydrase Cancer
    DOTA-XYIMSR-01 is a molecular probe targeting CAIX that can be labeled with 177Lu for the inhibition and localization of malignant gliomas. The uptake of [177Lu] Lu-XYIMSR-01 in U87MG tumors is 6.19 % of the injected dose per gram (% ID/g), and the tumor-to-muscle uptake ratio is 20.14. In the orthotopic glioma model, combined injection with Temozolomide (HY-17364) can significantly improve the survival rate of mice and inhibit tumor growth. DOTA-XYIMSR-01 shows promise for research in the field of anti-cancer therapy .
    DOTA-XYIMSR-01
  • HY-179418

    Apoptosis Cancer
    Ceritinib-platinum(IV)-4-phenylbutyrate (complex 7) is a Ceritinib (HY-15656)-conjugated Platinum(IV) prodrug with anticancer activity. Ceritinib-platinum(IV)-4-phenylbutyrate induces S-phase arrest, DNA damage responses, and apoptosis. Ceritinib-platinum(IV)-4-phenylbutyrate combines cytotoxicity with immune and anti-invasive activation in cancer cell models. Ceritinib-platinum(IV)-4-phenylbutyrate can be used for cancer research, such as non-small cell lung cancer (NSCLC) .
    Ceritinib-platinum(IV)-4-phenylbutyrate
  • HY-176220

    AUTACs Autophagy Glutathione Peroxidase Ferroptosis Cancer
    GPX4-AUTAC is a GPX4-targeting autophagy-mediated degrader (AUTAC). GPX4-AUTAC consists of an inhibitor ML162-yne (HY-153748), a degradation tag FBnG (HY-W073762) and a glycol linker (HY-W021401). GPX4-AUTAC promotes the ubiquitination of GPX4 by E3 ligase TRAF6, and enhances the binding with GPX4 and p62, leading to the selective autophagy-dependent degradation of GPX4. GPX4-AUTAC significantly induces ferroptosis and shows a potent anti-cancer activity in breast cancer cells, breast cancer-derived organoids (PDOs) and MDA-MB-231 tumor xenograft mice model, with potent synergistic effects when combined with Sulfasalazine (SAS) (HY-14655) or chemotherapy drugs (Paclitaxel (HY-B0015) or Cisplatin (HY-17394)) .
    GPX4-AUTAC
  • HY-148701

    Liposome Cancer
    mono-Pal-MTO is a palm oil-based lipid produced by combining the anticancer agent mitoxantrone (MTO) with palmitoleic acid. When nanoparticles of mono-Pal-MTO and di-Pal-MTO are combined in a molar ratio of 1:1, they show effective siRNA cell delivery and enhance anticancer activity .
    mono-Pal-MTO
  • HY-129909

    Apoptosis Infection Cancer
    Anticancer agent 173 (compound 19) is a potent thioxodihydroquinazolinone analogs when combined with platinum drugs in inducing apoptotic cancer cells death .
    Anticancer agent 173
  • HY-W699643

    BNP-7787-d8

    Isotope-Labeled Compounds Drug Metabolite Cancer
    Dimesna-d8 (BNP-7787-d8) is the deuterium labeled Dimesna (HY-B1022). Dimesna combined with anticancer chemotherapeutic agents to reduce nephrotoxicity.
    Dimesna-d8
  • HY-114527

    Apoptosis Stearoyl-CoA Desaturase (SCD) Cancer
    TPMP-I-2 is an anticancer agent that induces cancer cell lines Apoptosis and decreases protein levels of stearoyl-CoA desaturase. TPMP-I-2 prolongs the survival time of nude rats in a simulated micrometastatic cervical cancer model and reduces tumor growth in a breast cancer model in nude mice combined with immunotoxins .
    TPMP-I-2
  • HY-N2492R

    Methyl trans-p-coumarate (Standard)

    Reference Standards Apoptosis Parasite Interleukin Related GSK-3 Infection Cancer
    (E)-Methyl 4-coumarate (Standard) is the analytical standard of (E)-Methyl 4-coumarate (HY-N2492). This product is intended for research and analytical applications. (E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate) is a phenolic compound and derivative of Cinnamic acid (HY-N0610A). (E)-Methyl 4-coumarate can be found in several plants, such as the leaves of Allium cepa and Morinda citrifolia L. (E)-Methyl 4-coumarate, when combined with Carnosic acid (HY-N0644), induces Apoptosis. (E)-Methyl 4-coumarate inhibits GSK3β activity and modulates inflammatory cytokine levels (increasing IL-10 and decreasing IL-4). (E)-Methyl 4-coumarate combined with Carnosic acid exhibits anticancer effects against acute myeloid leukemia. (E)-Methyl 4-coumarate ameliorates Plasmodium berghei NK65 infection .
    (E)-Methyl 4-coumarate (Standard)
  • HY-N4246R

    Reference Standards PKC Akt PI3K Apoptosis Pregnane X Receptor (PXR) Monoamine Oxidase Aquaporin Neurological Disease
    Bacopaside I (Standard) is the analytical standard of Bacopaside I. This product is intended for research and analytical applications. Bacopaside I is an orally active aquaporin AQP1 inhibitor and PKC modulator with neuroprotective and anticancer activities. Bacopaside I specifically blocks the water channel and cGMP-gated ion channel activities of AQP1 without affecting AQP4, thereby inhibiting the migration of colon cancer cells expressing AQP1. Bacopaside I activates the Akt pathway by interacting with PI3K, specifically inhibits MAO-A, effectively alleviates neuron necrosis and apoptosis induced by oxygen-glucose deprivation, reduces oxidative stress, and regulates the surface expression of neuroreceptors. When combined with Bacopaside II (HY-N6016), Bacopaside I significantly reduces the viability, proliferation and invasion ability of breast cancer cells, and binds to the pregnane X receptor (PXR). Bacopaside I is applicable to the research of colon cancer, breast cancer, vascular dementia, cerebral ischemia and other related diseases .
    Bacopaside I (Standard)
  • HY-162816

    PROTACs MAP4K Cancer
    PROTAC HPK1 Degrader-3 (compound C3) is an orally effective PROTAC targeting HPK1 (DC50=21.26 nM). HPK1 is a negative regulator of T cell receptors, which can lead to T cell dysfunction after abnormal activation. PROTAC HPK1 Degrader-3 can inhibit SLP76 and NF-κB signaling pathways and inhibit MAPK signal transduction, and has anticancer activity and immune activation. PROTAC HPK1 Degrader-3 has a certain oral bioavailability and can be combined with PD-L1 antibody therapy to achieve a tumor growth inhibition rate of 65.58%. PROTAC HPK1 Degrader-3 is composed of E3 ligase ligand Thalidomide (HY-14658; blue part), PROTAC linker tert-Butyl 3-oxoazetidine-1-carboxylate (HY-40146; black part), and target protein ligand HPK1-IN-51 (HY-162842; red part); the activity control of the target protein ligand can be HPK1 ligand 1 (HY-162841) [1] .
    PROTAC HPK1 Degrader-3
  • HY-181932

    MAP4K Cancer
    HDM2004 is a selective, orally active, blood-brain barrier-penetrant HPK1 inhibitor with an IC50 of 1.89 nM. HDM2004 exhibits anticancer activity against colon cancer. HDM2004 shows synergistic activity when combined with anti-PD-L1 in syngeneic mouse models. HDM2004 can be used for the research of colon cancer .
    HDM2004

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