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4T1 tumor model

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Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-144088
    ZYF0033

    HPK1-IN-22

    		 MAP4K Inflammation/Immunology Cancer
    ZYF0033 is an orally active inhibitor of the hematopoietic progenitor cell kinase HPK1 with an IC50 of less than 10 nM based on the phosphorylation inhibition of MBP protein. ZYF0033 promotes anti-cancer immune responses and reduces phosphorylation of SLP76 (serine 376). ZYF0033 inhibits tumor growth in the 4T-1 syngeneic mouse model and leads to increased intratumoral infiltration of DCs, NK cells, and CD107a +CD8 + T cells, but not T cells, PD-1 +CD8 + T cells, TIM-3 +CD8 + Infiltration of T cells and LAG3 +CD8 + T cells was reduced .
    ZYF0033
  • HY-175201
    pro-FTY

    		LPL Receptor STAT Cancer
    pro-FTY, a FTY720 (HY-12005) anticancer prodrug, is a sphingosine-1-phosphate (S1P) (HY-108496) inhibitor. pro-FTY specifically inhibits S1P signaling in cancer cells using a drug delivery system (DDS) that reacts with acrolein. pro-FTY significantly inhibits the survival of breast cancer cells, including multidrug-resistant cells and its organoids resistant to Paclitaxel (HY-B0015) or Doxorubicin (HY-15142A). pro-FTY potently suppresses tumor growth in 4T1 cells or organoids xenograft tumors mice model while avoiding lymphocytopenia .
    pro-FTY
  • HY-170453
    iHAC

    		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-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-P991621
    EOS006215

    EOS-215

    		 TREM receptor Cancer
    EOS006215 is a humanized monoclonal antibody inhibitor targeting TREM-2. EOS006215 reprograms TREM2 + macrophages, significantly blocks their pleiotropic pro-tumoral functions and overcomes resistance. EOS215 decreases metastasis burden in orthotopic 4T1 triple negative breast cancer mice model and significantly inhibits tumor growth in anti-PD-1 resistant mice model. EOS006215 can be used to study advanced malignant solid neoplasm, such as triple negative breast cancer (TNBC) .
    EOS006215
  • HY-173433
    JV8

    		Epigenetic Reader Domain Cancer
    JV8 is a BRD4 PROTAC degrader. JV8 promotes the ubiquitination and degradation of BRD4 and induces apoptosis. JV8 has antitumor activity in a mouse 4T1 orthotopic tumor model. (Pink: BRD4 ligand (HY-78695); Blue: E3 ligase VHL ligand (HY-173435); Black: Linker (HY-33366); E3 ligase VHL ligand-linker conjugate (HY-173436)) .
    JV8
  • HY-174811
    PROTAC BRD4 Degrader-33

    		PROTACs Epigenetic Reader Domain PD-1/PD-L1 Inflammation/Immunology Cancer
    PROTAC BRD4 Degrader-33 is an enzyme activated clickable BRD4 PROTAC degrader with favorable tumor microenvironment-response. PROTAC BRD4 Degrader-33 has superior tumor tissue penetration capabilities and efficiently inhibits PD-L1 protein expression. PROTAC BRD4 Degrader-33 shows potent anti-tumoral immunomodulation activity in 4T1 tumor-bearing mice model . Pink: BRD4 ligand (HY-174812); Blue: CRBN ligase ligand (HY-10984); Black: linker
    PROTAC BRD4 Degrader-33
  • 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-172934
    FGT-4

    		Toll-like Receptor (TLR) NO Synthase PROTACs Inflammation/Immunology Cancer
    FGT-4 is a folate receptor β (FR-β) targeting chimeric molecule. FGT-4 is a TLR7 agonist. FGT-4 facilitates the secretion of iNOS and proinflammatory cytokine IL-6 associated with M1 macrophages and enhances the proliferation of cytotoxic CD8 + T cells. FGT-4 has anti-tumor activity in the 4T1 breast cancer mouse model. FGT-4 can be used for the study of cancer immunity. (Pink: target protein TLR7/8 agonist 1 ligand (HY-103698); black: linker (HY-172936); blue: FR-β ligand (HY-172935)) .
    FGT-4
  • HY-122566
    SMU127

    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-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-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-174403
    c-MYC/BCL2 ligand 1 iodide

    		Bcl-2 Family c-Myc Apoptosis Caspase Cancer
    c-MYC/BCL2 ligand 1 iodide is a dual-targeting c-MYC/Bcl-2 G4 ligand with Kd values of 0.90 μM (c-MYC G4) and 0.56 μM (Bcl-2 G4). c-MYC/BCL2 ligand 1 iodide inhibits c-MYC and Bcl-2 gene transcription by binding to G4-forming sequences and downregulates their protein expression. c-MYC/BCL2 ligand 1 iodide inhibits suppresses migration, induces caspase-dependent apoptosis, and triggers cell cycle G1 arrest in MCF-7 cells. c-MYC/BCL2 ligand 1 iodide significantly suppresses tumor growth in a 4T1 syngeneic model with no observable toxicity. c-MYC/BCL2 ligand 1 iodide can be used for the research of breast cancer.
    c-MYC/BCL2 ligand 1 iodide
  • HY-163965
    Antitumor agent-185

    		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-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-N0841
    Bruceine A
    3 Publications Verification

    Dihydrobrusatol; NSC310616

    		 Parasite NF-κB p38 MAPK Phosphatase Apoptosis Infection Cancer
    Bruceine A (Dihydrobrusatol) is a natural quassinoid. Bruceine A is an inhibitor of parasites, NF-κB, and PFKFB4 (Kd: 44 nM). Bruceine A is an activator of P38α MAPK. Bruceine A has antiparasitic activity. Bruceine A has antitumor activity and inhibits cancer cell migration. Bruceine A blocks the cell cycle and induces apoptosis. Bruceine A can be used in parasites, pancreatic cancer, and breast cancer research .
    Bruceine A

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