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4T1

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59

Inhibitors & Agonists

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1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-155745
    Antitumor agent-115

    		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-162958
    Photosensitizer-6

    		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-161338
    Tubulin polymerization-IN-61

    		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
    Anticancer agent 33

    		Others 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
    CBP/p300-IN-21

    		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-162312
    LLK203

    		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-162645
    BPR5K230

    		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
    ZG-126

    		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
    Tubulin polymerization-IN-62

    		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
    Antitumor agent-184

    		Others 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
    PDK-IN-2

    		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-163709
    PROTAC FAK degrader 2

    		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-116904
    Anticancer agent 253

    		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-144088
    ZYF0033

    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
    Axl-IN-18

    		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
    PROTAC PD-L1 degrader-1

    		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
    SMU127

    ZINC666243

    		 Others 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
    CDK9-Cyclin T1 PPI-IN-1

    		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
    HDAC3-IN-2

    		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
    Anticancer agent 255

    		Others 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 agonist-31

    		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
    Enpp-1-IN-20

    		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-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-163307
    PD-1/PD-L1-IN-39

    		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-162502
    WZU-13

    		Carboxylesterase 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
    Antitumor agent-185

    		Others 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-158317
    SFB-AMD3465

    		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-120797
    CRT0273750

    		LPL Receptor Cancer
    CRT0273750 is an autotaxin (ATX) inhibitor and modulates LPA levels in plasm (IC50 = 0.014 μM). CRT0273750 can be used in ATX/LPA-dependent models of cancer .
    CRT0273750
  • HY-161821
    Antitumor agent-173

    		Others 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-159112
    AW01178

    		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-161518
    PD-1/PD-L1-IN-44

    		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
    Setomimycin

    		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-136552
    β-Bisabolene

    		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-151904
    AXL-IN-13

    		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
    Anticancer agent 221

    		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
    WRX606

    		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-13513
    U-104
    5 Publications Verification

    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 .
    U-104
  • 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 .
    STING agonist-9
  • 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-101466A
    E7090 succinate

    		FGFR Cancer
    E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively .
    E7090 succinate
  • HY-101466
    E7090

    		FGFR Cancer
    E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively .
    E7090
  • HY-116705
    2-Deoxy-2-fluoro-L-fucose

    		Others Cancer
    2-Deoxy-2-fluoro-L-fucose, an L-fucose analog, is a fucosylation inhibitor. 2-Deoxy-2-fluoro-L-fucose inhibits de novo synthesis of GDP-fucose in mammalian cells. Fucosylation is a relatively well-defined biomarker for progression in many human cancers; for example, pancreatic and hepatocellular carcinoma .
    2-Deoxy-2-fluoro-L-fucose
  • HY-151464
    SHP2/HDAC-IN-1

    		SHP2 Phosphatase HDAC Inflammation/Immunology Cancer
    SHP2/HDAC-IN-1 is a dual allosteric SHP2/HDAC inhibitor with IC50 values of 20.4 nM (SHP2) and 25.3 nM (HDAC1) respectively. SHP2/HDAC-IN-1 triggers efficient antitumor immunity by activating T cells, enhancing the antigen presentation function and promoting cytokine secretion. SHP2/HDAC-IN-1 can be used in the research of cancer immunoresearch .
    SHP2/HDAC-IN-1
  • HY-150158
    TMX-201

    		Toll-like Receptor (TLR) Cancer
    TMX-201 is a TLR7 ligand-phospholipid conjugate. TMX-201 shows potent immune stimulatory activity. TMX-201 can be used for breast cancer and melanoma research .
    TMX-201
  • HY-147165
    VT02956

    		YAP Cancer
    VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    VT02956
  • HY-155686
    Tubulin polymerization-IN-44

    		Microtubule/Tubulin Cancer
    Tubulinpolymer-in-44 (compound 7w) is a strong and effective Tubulin inhibitor, with an IC50 value of 0.21 μM. Tubulinpolymer-in-44 induces apoptosis by arresting G2/M phase, which can be used for cancer research.
    Tubulin polymerization-IN-44
  • HY-N12603
    Typhatifolin B

    		Apoptosis Cancer
    Typhatifolin B (Compd 2), an anti-cancer agent, could remarkably induce cell apoptosis and G0/G1 cycle arrest, as well as block cell migration and invasion .
    Typhatifolin B
  • HY-157913
    PKM2-IN-6

    		Pyruvate Kinase Apoptosis Cancer
    PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer .
    PKM2-IN-6
  • HY-115997
    PROTAC HSP90 degrader BP3

    		PROTACs HSP Cancer
    PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain degradation effect on HSP90 protein in MCF-7 cells (DC50=0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell . PROTAC HSP90 degrader BP3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC HSP90 degrader BP3
  • HY-146516
    Anticancer agent 42

    		MDM-2/p53 Apoptosis Reactive Oxygen Species Cancer
    Anticancer agent 42 (compound 10d) is an orally active anticancer agent, and shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 0.07 μM. Anticancer agent 42 can exert its anticancer activity by activating apoptotic pathway and p53 expression. Anticancer agent 42 can be used to study metastatic breast cancer .
    Anticancer agent 42

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