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MC38 mice

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14

Inhibitors & Agonists

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-160421

    Apoptosis Inflammation/Immunology Cancer
    TREM2-IN-1 (OPA) is a TREM2 inhibitor derived from oxaliplatin and artesunate. TREM2-IN-1 can relieves immunosuppressive tumor microenvironment and enhancing chemical anticancer efficiency. TREM2-IN-1 deters the tumor growth in mice models bearing MC38 colorectal tumor by reducing the number of CD206 + and CX3CR1 + immunosuppressive macrophages. TREM2-IN-1 also promotes the expansion and infiltration of immunostimulatory dendritic, cytotoxic T and natural killer cells .
    TREM2-IN-1
  • HY-171572

    Antibody-Drug Conjugates (ADCs) Microtubule/Tubulin Apoptosis Inflammation/Immunology Cancer
    Atezolizumab-MMAE is an anti-PD-L1 antibody-drug conjugate (ADC) with an EC50 of 1.1 nM. Atezolizumab-MMAE is composed of a humanized anti-PD-L1 antibody (Atezolizumab) (HY-P9904), a lysosomally cleavable dipeptide linker (valine-citrulline), a tubulin inhibitor (MMAE) (HY-15162), and the drug-linker conjugate for ADC is VcMMAE (HY-15575). Atezolizumab-MMAE has a potent cytotoxicity (EC50: 9.75-11.94 nM) and immune activation effect. Atezolizumab-MMAE has a significantly anti-tumor activity in MC38 xenograft PD-1-humanized immune system mice model .
    Atezolizumab-MMAE
  • HY-153358

    HDAC Cancer
    TNG260 is a selective, orally effective inhibitor of HDAC1 and CoREST complex, with a 10-fold selectivity for HDAC1 over HDAC3 and a 500-fold selectivity for CoREST complex over NuRD and Sin3 complex. TNG260 reshapes the tumor immune microenvironment, reduces immunosuppressive neutrophil infiltration, promotes effector T cell recruitment, and reverses anti-PD-1 resistance caused by STK11 deficiency by inhibiting the activity of the CoREST-HDAC1 complex. TNG260 induces durable tumor regression in combination with α-PD1 in MC38 tumor-bearing mice with STK11 mutations, and has lower toxicity to bone marrow cells than non-selective HDAC inhibitors .
    TNG260
  • HY-172930

    Molecular Glues IKZF Family Potassium Channel Inflammation/Immunology Cancer
    PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC50  of  0.7 nM and a Dmax of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC50 of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn 391V C57BL/6 mice .
    PVTX-405
  • HY-149208

    HDAC Apoptosis Cancer
    HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC50>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer .
    HDAC-IN-53
  • 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-169478

    Liposome Cancer
    Lipid N2-3L is an ionizable cationic lipid (pKa = 8.99) that can be used to generate supramolecular lipid nanoparticles (SMLNPs) for mRNA delivery. Lipid nanoparticles formed by encapsulating a luciferase reporter gene with Lipid N2-3L were detected to accumulate in the lymph nodes of mice, indicating that they can effectively enter the mouse immune system. Lipid nanoparticles formed by encapsulating ovalbumin mRNA and the TLR7/8 agonist Resiquimod (HY-13740) with Lipid N2-3L were able to reduce tumor volume and increase survival in the MC-38-OVA mouse colon cancer model. Lipid N2-3L can be used in the research of drug delivery for cancer-related therapies .
    Lipid N2-3L
  • HY-176256

    STING Cancer
    endo-S-cGAFMP (Compound 3) is a STING agonist. endo-S-cGAFMP induces the production of interferon regulatory factors and proinflammatory cytokines by activating the cGAS-STING pathway, thereby enhancing innate and adaptive immune responses. endo-S-cGAFMP has potent immunostimulatory capacity in THP1 monocytes and RAW macrophages (EC50 values of 2.45 μM and 5.54 μM, respectively). endo-S-cGAFMP has significant antitumor activity. endo-S-cGAFMP can be used as a potential cancer immunotherapeutic agent, especially for studies of systemic administration .
    endo-S-cGAFMP
  • HY-176482

    TAM Receptor
    MerTK-IN-3 (compound 11) is an orally active and selectivity MerTK inhibitor with IC50 values of 21.5 nM and 991.3 nM for MerTK and Tyro3, respectively. MerTK-IN-3 can be used for study of colon cancer .
    MerTK-IN-3
  • HY-151153

    HDAC Microtubule/Tubulin Caspase Apoptosis Cancer
    HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice .
    HDAC1-IN-5
  • HY-162357

    PD-1/PD-L1 Cancer
    PD-L1-IN-5 (X22) is an orally active PD-L1 inhibitor, with the IC50 value of 785.6 nM. PD-L1-IN-5 has anti-tumor activity in vivo .
    PD-L1-IN-5
  • HY-172133

    HDAC PD-1/PD-L1 Apoptosis Reactive Oxygen Species (ROS) Inflammation/Immunology Cancer
    HDAC3-IN-6 (Compound SC26) is a selective HDAC3 inhibitor with an IC50 of 53 nM. HDAC3-IN-6 dose-dependently induces the expression of PD-L1. HDAC3-IN-6 induces more pronounced Apoptosis and production of ROS. HDAC3-IN-6 exhibits high antitumor efficacy against colorectal cancer .
    HDAC3-IN-6
  • HY-N15169

    IFNAR CD74 NO Synthase Arginase Cancer
    BG-136 is an innate immune stimulant isolated from Durvillaea Antarctica that can simultaneously stimulate the activation of both innate and adaptive immune cells in the tumor microenvironment (TME), exerting a broad-spectrum antitumor effect .
    BG-136
  • HY-174301

    Deubiquitinase DNA Methyltransferase MDM-2/p53 Cancer
    USP7-IN-18 is a naphthalene derivative. USP7-IN-18 is a selective USP7 inhibitor (IC50 : 130.9 nM), with no or very weak inhibition of the other 8 DUBs including USP47. USP7-IN-18 specifically binds to the catalytic domain of USP7, blocking its deubiquitinase activity. USP7-IN-18 causes degradation of the oncogenic proteins MDM2 and DNMT1, and also degrades the novel target PCLAF. USP7-IN-18 activates the p53-p21 pathway. USP7-IN-18 exerts anti-tumor effects in colon cancer animal models and reshapes the tumor immune microenvironment. USP7-IN-18 achieves both direct cytotoxic and immune-synergistic anti-tumor actions[1].
    USP7-IN-18

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