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4T1

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-162312

    Deubiquitinase Apoptosis Cancer
    LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model .
    LLK203
  • HY-155745

    Apoptosis Cancer
    Antitumor agent-115 (SS-12) is an effective anti-tumor compound with an IC50 value of 0.34 μM-24.14 μM for cell line 4T1. Antitumor agent-115 can block the cell cycle of mouse breast cancer cell line 4T1, reduce the mitochondrial membrane potential, and induce apoptosis, and the IC50 value is 8-25 μmol/L for cell viability. Antitumor agent-115 can be used for breast cancer research .
    Antitumor agent-115
  • HY-170453

    Epigenetic Reader Domain Cancer
    iHAC is an inhibitor HSP90-anchoring chimera, that covalently binds BRD4 ligand (+)-JQ-1 to HSP90, and inhibits the proliferation of cancer cells. iHAC activates the anti-tumor immune response, inhibits the recurrence and metastasis of 4T1 breast cancer in mouse models .
    iHAC
  • HY-162958

    Apoptosis TrxR Cancer
    Photosensitizer-6 (Compound 4) is a gold (I) complex and exhibits inhibitory activity against TrxR. Photosensitizer-6 induces apoptosis in 4T1 cell, targets and eradicates tumors through chemo-phototherapy and immunogenic cell death under light exposure. Photosensitizer-6 can be used for tumor imaging .
    Photosensitizer-6
  • HY-173060

    ERK Apoptosis Autophagy Cancer
    ERK1/2 inhibitor 13 (Compound 21y) is the orally active inhibitor for ERK that inhibits ERK1 and ERK2 with IC50 of 91.71 nM and 97.87 nM. ERK1/2 inhibitor 13 inhibits the proliferation of MCF-7, 4T1, MDA-MB-468, and HCC1970 (IC50 of 0.67, 2.76, 2.15 and 1.68 μM), inhibits the cancer cell migration, induces apoptosis and autophagy in MCF-7. ERK1/2 inhibitor 13 exhibits antitumor and anti-metastatic effect in 4T1 xenograft mouse model .
    ERK1/2 inhibitor 13
  • HY-170989

    Epigenetic Reader Domain Autophagy Cancer
    BRD4 degrader-5 (Compound 23) is a hydrophobic tag (HyTag)-based protein degrader for BRD4 (DC50 = 24.7 μM) through ER stress and autophagy-lysosome pathway. BRD4 degrader-5 inhibits the proliferation of cancer cell 4T1 with an IC50 of 20.6 μM .
    BRD4 degrader-5
  • HY-D2620

    Photosensitizer Reactive Oxygen Species Ferroptosis Cancer
    CAR-2 is a BODIPY-based photosensitizer that induces ferroptosis in photodynamic therapy (PDT) by targeting the endoplasmic reticulum (ER) and lipid droplets (LDs). CAR-2 exhibits phototoxicity in breast cancer cells with IC50 of 0.01-0.02 μM. CAR-2 exhibits antitumor efficacy in 4T1 xenograft mouse models .
    CAR-2
  • HY-161338

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin polymerization-IN-61 (Compound 9a) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-61 destroys the microtubule skeleton, blocks the cell cycle in G2/M phase, induces Apoptosis, and inhibits cancer cell migration and colony formation. Tubulin polymerization-IN-61 shows antitumor activity in vivo against 4T1 xenograft model .
    Tubulin polymerization-IN-61
  • HY-115947

    Drug Derivative Cancer
    Anticancer agent 33 (compound 3), a Squamocin and Bullatacin derivative, is a potent anticancer agent. Anticancer agent 33 shows high potency to inhibit 4T1 breast cancer cell line (A549, HeLa, HepG2 and MCF-7 cells) growth with IC50s of 1.9-5.4 µM .
    Anticancer agent 33
  • HY-155229

    Epigenetic Reader Domain Histone Acetyltransferase Cancer
    CBP/p300-IN-21 (Compound 5d) is a selective CBP/p300 inhibitor (IC50: 0.07 and 1.755 μM for p300 and CBP). CBP/p300-IN-21 decreases H3K18Ac level. CBP/p300-IN-21 inhibits growth of 4T1 tumor growth in mice .
    CBP/p300-IN-21
  • HY-169392

    PD-1/PD-L1 Cancer
    D5B is a potent and selective PD-L1 inhibitor. D5B has been modified by DBCO. The EC50 of D5B degrading PD-L1 in 4T1 and B16-F10 tumor cells are 5.4 μM and 6.2 μM, respectively. D5B can block PD-L1/PD-1 interaction and has anti-tumor activity .
    D5B
  • HY-162645

    TAM Receptor Inflammation/Immunology Cancer
    BPR5K230 is a dual inhibitor for the receptor tyrosine kinase MER and AXL, with IC50 of 4.1 nM and 9.2 nM. BPR5K230 inhibits the proliferation of Ba/F3-MER with IC50 of 5 nM. BPR5K230 exhibits good pharmacokinetic characteristics in mice, exhibits anti-inflammatory and antitumor against 4T1, MDA-MB-231, MC38 and Hepa1?6 in mouse models .
    BPR5K230
  • HY-161778

    HDAC VD/VDR Inflammation/Immunology Cancer
    ZG-126 is an agonist for vitamin D receptor (VDR) and an inhibitor for histone deacetylase (HDAC) (IC50=0.63-67.6 μM). ZG-126 exhibits cytotoxicity in cancer cells MDA-MB-231 and 4T1. ZG-126 exhibits antitumor and anti-metastatic efficacy against melanoma and triple-negative breast cancer (TNBC) in mouse models. ZG-126 also exhibits anti-inflammatory activity, through the reduction of macrophage infiltration and immunosuppressive M2-polarization .
    ZG-126
  • HY-161641

    Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
    Tubulin polymerization-IN-62
  • HY-162766

    Apoptosis Cancer
    Antitumor agent-184 (compound 12aa) induces cell apoptosis, with the IC50s of 2.35 μM, 7.32 μM and 10.31 μM in B16-F10 cells, 4T1 cells and CT26 cells, respectively .
    Antitumor agent-184
  • HY-156109

    PDHK Mitochondrial Metabolism Cancer
    PDK-IN-2 (Compound 1F) is a PDK inhibitor (IC50: 68 nM). PDK-IN-2 inhibits the cellular expression of PDK1 and PDK4. PDK-IN-2 enhances mitochondrial bioenergetics, attenuates glycolytic phenotypes, and induces cell apoptosis in the mitochondrial pathway. PDK-IN-2 inhibits tumor growth in 4T1 syngeneic mice model .
    PDK-IN-2
  • HY-P10833

    VEGFR Cardiovascular Disease Cancer
    VGB3 is an antagonist peptide of vascular endothelial growth factor receptor 1 (VEGFR1)/VEGFR2 with antiangiogenic and antitumor effects. VGB3 binds to both VEGFR1 and VEGFR2, thereby inhibits VEGF-driven proliferation, migration and tube formation of endothelial cells, and tumor growth and metastasis in murine 4T1 mammary carcinoma tumor model .
    VGB3
  • HY-170883

    Photosensitizer Cancer
    Type-I/-II Photosensitizer-1 (compound 8b) is a photosensitizer with anticancer activity. Type-I/-II Photosensitizer-1 exhibits significant phototoxicity against both A549 and 4T1 tumor cells. Type-I/-II Photosensitizer-1 shows a strong oxygen-independent antitumor effect under laser irradiation (IC50=1.50-1.76 μM) .
    Type-I/-II Photosensitizer-1
  • HY-116904

    Apoptosis Akt Cancer
    Anticancer agent 253 (Compound 26) has anti-cancer activity against breast cancer cells, with IC50s of 6 μM (MCF-7), 10 μM (MDA-MB-231) and 6.4 μM (4T1 cells). Anticancer agent 253 arrests cell cycle and induces mitochondria-mediated apoptosis in cancer cells. Anticancer agent 253 inhibits Akt phosphorylation in human breast and prostate cancer .
    Anticancer agent 253
  • HY-163709

    PROTACs FAK Cancer
    PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader for focal adhesion kinase (FAK), with DC50 of 27.72 and 60.1 nM, for total FAK and phosphorylated p-FAK. PROTAC FAK degrader 2 inhibits cell viability of cancer cells 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435, with IC50s of 0.73-5.84 μM. PROTAC FAK degrader 2 reverses the multidrug resistance (MDR) through inhibition of AKT and ERK signaling pathway. PROTAC FAK degrader 2 exhibits antitumor efficacy in HCT/8 xenograft mouse model. (Pink: ligand for target protein Ifebemtinib (HY-122844); Black: linker (HY-Y0681); Blue: ligand for E3 ligase Thalidomide (HY-14658))
    PROTAC FAK degrader 2
  • HY-144088

    HPK1-IN-22

    MAP4K Inflammation/Immunology Cancer
    ZYF0033 is effective in inhibiting hematopoietic progenitor cells HPK1, basically inhibiting MBP protein oxidation IC50 10 nM . ZYF0033 promotes anti-cancer immune response, lowers SLP76 (acid 376) oxidation. ZYF0033 Suppression 4T-1 Small mouse model with the same underlying cause, medium bulge growth length expansion DC, NK 细细和 CD107a + CD8 + T Cells, PD-1 +CD8 + T Cells, TIM-3 +CD8 + T Cells LAG3< sup>+CD8 + T Cellular immersion decreases.
    ZYF0033
  • HY-162103

    TAM Receptor Apoptosis Cancer
    Axl-IN-18 (compound 25c) is a potent and selective type II AXL inhibitor. Axl-IN-18 shows excellent AXL inhibitory activity (IC50=1.1 nM) and 343-fold selectivity over the highly homologous kinase MET in biochemical assays (IC50=377 nM). Axl-IN-18 significantly inhibits AXL-driven cell proliferation, dose-dependently suppresses 4T1 cell migration and invasion, and induces apoptosis. Axl-IN-18 shows noticeable antitumor efficacy in a BaF3/TEL-AXL xenograft model .
    Axl-IN-18
  • HY-163757

    PROTACs PD-1/PD-L1 Inflammation/Immunology Cancer
    PROTAC PD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with a notable PD-L1 protein degradation capability. PROTAC PD-L1 degrader-1 shows potent PD-L1 degradation in 4T1 cells with a DC50 of 0.609 μM. PROTAC PD-L1 degrader-1 can be used for the study of breast cancer. (Blue: CRBN ligand (HY-150839), Black: linker; Pink: PD-L inhibitor (HY-19745)) .
    PROTAC PD-L1 degrader-1
  • HY-122566

    ZINC666243

    Toll-like Receptor (TLR) TNF Receptor Cancer
    SMU127 is an agonist of the toll-like receptor 1/2 (TLR1/2) heterodimer. It induces NF-κB signaling in cells expressing human TLR2 (EC50=0.55 μM) but not cells expressing human TLR3, -4, -5, -7, or -8 when used at concentrations ranging from 0.1 to 100 μM. SMU127 induces the production of TNF-α in isolated human peripheral blood mononuclear cells (PBMCs) when used at concentrations ranging from 0.01 to 1 μM. In vivo, SMU127 (0.1 mg/animal) reduces tumor volume in a 4T1 murine mammary carcinoma model.
    SMU127
  • HY-156296

    CDK Apoptosis Cancer
    CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective CDK9-Cyclin T1 protein-protein interaction (PPI) inhibitor. CDK9-Cyclin T1 PPI-IN-1 inhibits cell proliferation in TNBC MDA-MB-231 cells (IC50: 0.044 μM), and induces apoptosis. CDK9-Cyclin T1 PPI-IN-1 inhibits CDK9 transcription activity, reduces the phosphorylation of RNA Pol II CTD ser2. CDK9-Cyclin T1 PPI-IN-1 inhibits tumor growth in a TNBC 4T1 mouse model .
    CDK9-Cyclin T1 PPI-IN-1
  • HY-156096

    HDAC Histone Methyltransferase Caspase Apoptosis DNA/RNA Synthesis Cancer
    HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .
    HDAC3-IN-2
  • HY-123715

    Apoptosis Cancer
    Anticancer agent 255 is a monocarbonylated curcumin-1,2,3-oxazole conjugate with significant anticancer activity. The IC50 values of Anticancer agent 255 in prostate cancer cells PC-3 and DU-145 are 8.8μM and 9.5μM respectively. The IC50 values of Anticancer agent 255 against breast cancer cells MCF-7, MDA-MB-231 and 4T1 are 6μM, 10μM and 6.4μM, showing good anti-cancer activity Effect. Anticancer agent 255 can induce mitochondria-mediated apoptosis in cancer cells and prevent cell cycle progression. Anticancer agent 255 down-regulated the cell proliferation marker PCNA and inhibited the activation of cell survival proteins. Anticancer agent 255 up-regulated the pro-apoptotic protein Bax and down-regulated the anti-apoptotic protein Bcl-2 .
    Anticancer agent 255
  • HY-153546

    STING Cancer
    STING agonist-31 is a STING agonist, with EC50 values of 0.24 and 39.51 μM for h-STING and m-STING. STING agonist-31 has antitumor efficiency .
    STING agonist-31
  • HY-163343

    Phosphodiesterase (PDE) STING Cancer
    Enpp-1-IN-20 (Compound 31) is an ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) inhibitor, with an IC50 of 0.09 nM. Enpp-1-IN-20 has strongest inhibitory activity in the cell-based assay, with an IC50 of 8.8 nM. Enpp-1-IN-20 has significant potency in both ENPP1 inhibition and STING pathway stimulation in vitro. Enpp-1-IN-20 can be used for the research of cancer .
    Enpp-1-IN-20
  • HY-19891A

    PG545 free acid

    Toll-like Receptor (TLR) SARS-CoV Infection Inflammation/Immunology Cancer
    Pixatimod free acid (PG545 free acid) is a mimetic of Heparan Sulfate (HY-101916), and exhibits inhibitory activity against heparanase. Pixatimod free acid binds to the S1 receptor binding domain (RBD) of the SARS-CoV-2 virus, that inhibits SARS-CoV-2 isolate strains with EC50 of 2.4-13.8 µg/mL. Pixatimod free acid is an agonist for TLR9 signaling pathway, enhances the activity of dendritic cells (DCs), activates natural killer cells, and exhibits immunomodulatory and anti-tumor activities .
    Pixatimod free acid
  • HY-170436

    Photosensitizer Apoptosis Cancer
    NFh-NMe-2 is a photosensitizer, that interacts with nitroreductase, generates singlet oxygen in tumor cells, exhibits cytotoxicity in cancer cells, and induces apoptosis. NFh-NMe-2 exhibits antitumor efficacy in mouse models .
    NFh-NMe-2
  • HY-141652

    Drug Intermediate Cancer
    N-2-Azidoethyl betulonamide is the building block, that could generate cytotoxic triazole derivative through click chemistry .
    N-2-Azidoethyl betulonamide
  • HY-162502

    Carboxylesterase (CES) Wnt Cancer
    WZU-13 is an inhibitor for Carboxylesterase (CES). WZU-13 inhibits 77% CES activity at a dose of 100 μM .
    WZU-13
  • HY-163965

    Toll-like Receptor (TLR) Cancer
    Antitumor agent-185 (compound 3) shows antitumor activity that could effectively reduce the growth of tumors and prolong the survival time of mice in vivo .
    Antitumor agent-185
  • HY-163307

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-39 (X 14) is an orally active PD-1/PD-L1 inhibitor with a IC50 value of 15.73 nM. PD-1/ PD-L1-in-39 has a good binding affinity for human and mouse PD-L1, with KD values of 14.62 nM and 392 nM, respectively. PD-1/PD-L1-IN-39 has antitumor activity .
    PD-1/PD-L1-IN-39
  • HY-128972
    Purpurin 18
    2 Publications Verification

    Reactive Oxygen Species Apoptosis Others
    Purpurin 18, a derivative of chlorophyll and a type of dihydroporphyrin, is used to produce photosensitizers. Purpurin 18 photodynamic therapy can induce cell apoptosis and has anti-tumor activity .
    Purpurin 18
  • HY-158317

    CXCR Biochemical Assay Reagents Others
    SFB-AMD3465 is an AMD3465 (HY-15971A) derivative. SFB-AMD3465 is utilized as positron emission tomography (PET) tracer for CXCR4, when labeled with radioactive Fluorine .
    SFB-AMD3465
  • HY-159112

    HDAC Cancer
    AW01178 is a Class I HDAC inhibitor. AW01178 induces the upregulation of E-cadherin at both mRNA and protein levels and inhibits the EMT of breast cancer cells .
    AW01178
  • HY-161821

    Interleukin Related TNF Receptor MMP Cancer
    Antitumor agent-173 (Compound 4b) is a prodrug of Cycloicaritin (HY-N1940). Antitumor agent-173 is a substrate for OATP2B1. Antitumor agent-173 selectively inhibits the growth of tumor Antitumor agent-173 significantly increases the oral bioavailability of Cycloicaritin and exerts good antitumor activity and safety .
    Antitumor agent-173
  • HY-170402

    Sirtuin Apoptosis Cancer
    SIRT6-IN-4 (Compound 10d) is a selective inhibitor for SIRT6 with an IC50 of 5.68 μM. SIRT6-IN-4 inhibits the proliferation of MCF-7 with an IC50 of 8.30 μM. SIRT6-IN-4 arrests the cell cycle at G2/M phase, inhibits thecell migration and invasion of MCF-7, and induces apoptosis. SIRT6-IN-4 exhibits antitumor efficacy in mouse models .
    SIRT6-IN-4
  • HY-168877

    MDM-2/p53 Reactive Oxygen Species Apoptosis Caspase PARP Bcl-2 Family Cancer
    FMP is a Platinum(IV) complexe. FMP significantly upregulates the expression of γ-H2AX and p53. FMP increases the production of ROS. FMP markedly upregulates the expressions of Apoptosis-related proteins (DR5, Fas, caspase-8, Cyt-c, caspase-3, cleaved-PARP1, Bax). FMP shows antiproliferative activity against breast cancer .
    FMP
  • HY-161518

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-44 (Compound 22) selectively inhibits PD-1/PD-L1 proteins (IC50=1.21 nM). PD-1/PD-L1-IN-44 inhibits tumor growth without toxicity in animal models and increases CD8 + cell infiltration .
    PD-1/PD-L1-IN-44
  • HY-124439

    Antibiotic Bacterial SARS-CoV Infection Cancer
    Setomimycin is a potent antibiotic. Setomimycin inhibits the SARS-CoV-2 Mpro enzyme with an IC50 value of 12.02 µM. Setomimycin shows anti-inflammatory and antioxidant properties. Setomimycin shows antiproliferative and antitumor activity .
    Setomimycin
  • HY-151904

    TAM Receptor FLT3 PDGFR Cancer
    AXL-IN-13 is a potent and orally active AXL inhibitor (IC50: 1.6 nM, Kd: 0.26 nM). AXL-IN-13 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion .
    AXL-IN-13
  • HY-163616

    Apoptosis Cancer
    Anticancer agent 221 (Compound 4h) is an orally active anticancer agent and an antioxidant agent. Anticancer agent 221 exhibits cytotoxicity to cancer cells A549 (IC50=22.09 µg/mL) and MCF-7 (IC50=6.40 µg/mL), and induces apoptosis. Anticancer agent 221 exhibits antioxidant efficacy with an IC50 of 42.46 μM in DPPH experiment. Anticancer agent 221 exhibits antitumor efficacy against breast cancer in mouse models .
    Anticancer agent 221
  • HY-W348485

    mTOR Cancer
    WRX606 is an inhibitor for mTOR complex 1 (mTORC1). WRX606 inhibits the phosphorylation of mTORC1 substrate S6 kinase 1 S6K1 (IC50=10 nM), and the phosphorylation of the eukaryotic translation initiation factor 4E binding protein (p-4E-BP1) (IC50=0.27 μM) in MCF-7. WRX606 exhibits cytotoxicity to HepG2 with IC50 of 17 nM. WRX606 exhibits antitumor efficacy in mouse models .
    WRX606
  • HY-136552

    Others Cancer
    β-Bisabolene is a sesquiterpene isolated from opoponax (Commiphora guidotti). β-Bisabolene, an anti-cancer agent, can be used for the study of breast cancer .
    β-Bisabolene
  • HY-173075

    RIP kinase Mixed Lineage Kinase Necroptosis Cancer
    Anticancer agent 267 (Compound 5q) is the activator for RIPK3 and MLKL. Anticancer agent 267 inhibits the proliferation in a variety of cancer cell lines (IC50 for MDA-MB-231, MDA-MB-486 and MCF-7 is 9.79, 10.77 and 5.94 μM, respectively), arrests cell cycle at subG1 phase, and induces necroptosis in cell MDA-MB-231. Anticancer agent 267 exhibits antitumor activity in mouse xenograft models .
    Anticancer agent 267
  • HY-122844
    Ifebemtinib
    1 Publications Verification

    BI-853520; IN-10018

    FAK Cancer
    Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1?nM). Ifebemtinib shows anti-proliferative activity against cancer cells. Ifebemtinib inhibits FER Kinase and FES Kinase with IC50s of 900?nM and 1040?nM, respectively .
    Ifebemtinib
  • HY-147834

    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 .
    STING agonist-9

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