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Results for "

immune microenvironment

" in MedChemExpress (MCE) Product Catalog:

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14

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1

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-107202
    Polyinosinic-polycytidylic acid
    60+ Cited Publications

    Poly(I:C)

    		 RIG-I-like receptor (RLR) Toll-like Receptor (TLR) PKD HSP Bcl-2 Family Interleukin Related Apoptosis Infection Inflammation/Immunology Cancer
    Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid can directly trigger cancer cells to undergo apoptosis .
    Polyinosinic-polycytidylic acid
  • HY-135748
    Polyinosinic-polycytidylic acid sodium
    Maximum Cited Publications
    62 Publications Verification

    Poly(I:C) sodium

    		 RIG-I-like receptor (RLR) Toll-like Receptor (TLR) Apoptosis Inflammation/Immunology Cancer
    Polyinosinic-polycytidylic acid (Poly(I:C)) sodium is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis .
    Polyinosinic-polycytidylic acid sodium
  • HY-156677
    STC-15
    4 Publications Verification

    		 METTL3 Cancer
    STC-15 is an orally active RNA methyltransferase METTL3 inhibitor with the activity of activating anti-tumor immunity and reshaping the tumor microenvironment. STC-15 inhibits tumor growth by activating anti-cancer immune responses associated with increased interferon signaling and synergizes with T-cell checkpoint blockade. STC-15 can be used in the study of proliferative diseases such as cancer and autoimmune diseases .
    STC-15
  • HY-16961
    Sitravatinib
    5+ Cited Publications

    MGCD516; MG-516

    		 VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Inflammation/Immunology Cancer
    Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
    Sitravatinib
  • HY-P6292A
    KS-133 TFA

    		PACAP Receptor Neurological Disease Inflammation/Immunology Cancer
    KS-133 TFA is a highly selective and potent antagonist of the vascular active enteropeptide receptor 2 (VIPR2) with IC50 values for Ca influx measurement and cAMP measurement of 24.8 nM and 500 nM, respectively. KS-133 TFA reverses the tumor-promoting M2 phenotype of tumor-associated macrophages to the anti-tumor M1 phenotype, alters the tumor immune microenvironment, and inhibits tumor growth. KS-133 TFA can be used for research on schizophrenia and cancer immune regulation .
    KS-133 TFA
  • HY-P991097
    Pumitamig

    PM-8002; BNT-327

    		 VEGFR PD-1/PD-L1 Cancer
    Pumitamig (PM-8002, BNT-327) is a bispecific antibody targeting PD-L1 and VEGF-A, with immune activation and anti-angiogenic activities. By binding to PD-L1, Pumitamig restores the function of effector T cells, while neutralizing VEGF-A in the tumor microenvironment to reverse its inhibition on the infiltration and activation of immune cells and normalize tumor blood vessels. Pumitamig can also be combined with various ADCs targeting TROP2, B7H3, HER2, HER3 for the research of advanced/metastatic solid tumors, including non-small cell lung cancer, ovarian cancer, triple-negative breast cancer, cervical cancer, etc. Pumitamig also exhibits potential efficacy in "cold" tumors with low PD-L1 expression that are insensitive to immunotherapy .
    Pumitamig
  • HY-P99144A
    Anti-Mouse PD-1 Antibody (S-5001)
    1 Publications Verification

    		 PD-1/PD-L1 Inflammation/Immunology Cancer
    Anti-Mouse PD-1 Antibody (S-5001) is a selective inhibitor targeting PD-1, blocking the PD-1/PD-L1 immune checkpoint axis through competitive binding to PD-1. Anti-Mouse PD-1 Antibody (S-5001) works by reversing the tumor immunosuppressive microenvironment and reactivating the anti-tumor activity of cytotoxic T lymphocytes. It can be used in research on tumors such as melanoma and HPV-positive oropharyngeal squamous cell carcinoma. Anti-Mouse PD-1 Antibody (S-5001) is often combined with photothermal therapy, chemotherapy, etc., to enhance efficacy .
    Anti-Mouse PD-1 Antibody (S-5001)
  • HY-W075517
    ZIF-8

    2-Methylimidazole zinc salt

    		 MOFs Caspase Pyroptosis Cancer
    ZIF-8 (2-Methylimidazole zinc salt) is a pyroptosis inducer that activates the caspase-1/gasdermin D-dependent pyroptosis pathway. ZIF-8 induces pyroptotic cell death accompanied by necrosis and immunogenic cell death. ZIF-8 initiates in situ immunity, activates anti-tumor immunity, and reprograms the immunosuppressive tumor microenvironment to inhibit tumor growth. ZIF-8 acts as a pH-responsive and stimulus-responsive drug release inducer. ZIF-8 is applicable to cancer-related research .
    ZIF-8
  • HY-148029
    Dazostinag disodium

    TAK-676

    		 STING Cancer
    Dazostinag disodium (TAK-676) is an agonist of STING, triggering the activation of STING signaling pathway and type I interferons. Dazostinag disodium is also a modulator of immune system, resulting complete regressions and durable memory T-cell immunity. Dazostinag disodium promotes durable IFN-dependent antitumor immunity .
    Dazostinag disodium
  • HY-119367
    ODM-203

    		FGFR VEGFR Cancer
    ODM-203 is an orally active and selective FGFR/VEGFR inhibitor with IC50 values of 6, 11, 16, 5, 9, 26 and 35 nM for FGFR3/1/2 and VEGFR3/2/1/4, respectively. ODM-203 has strong anti-tumour activity and activates immune responses in the tumour microenvironment .
    ODM-203
  • HY-151427
    TGFβ1-IN-1
    3 Publications Verification

    		 TGF-β Receptor Inflammation/Immunology
    TGFβ1-IN-1 (compound 42) is a potent, orally active TGF-β1 inhibitor. TGFβ1-IN-1 inhibits the upregulation of TGF-β1-induced fibrosis markers (α-SMA and fibronectin) and can be used in liver fibrosis disease studies .
    TGFβ1-IN-1
  • HY-N6985
    Baccatin III
    2 Publications Verification

    		 Others Cancer
    Baccatin III is an orally available, selective inhibitor of the TGF-β1 signaling pathway and myeloid-derived suppressor cell (MDSC) activation. Baccatin III targets the AKT/STAT6 and Smad2/3 pathways, blocking TGF-β1-induced fibroblast differentiation and MDSC-mediated immunosuppression. Baccatin III exerts anti-inflammatory and anti-fibrotic effects by inhibiting macrophage activation and extracellular matrix deposition, and shows potential in the treatment of pulmonary fibrosis and cancer in terms of regulating the tumor immune microenvironment .
    Baccatin III
  • HY-152830
    Adrixetinib

    Q702

    		 c-Fms TAM Receptor MHC Cancer
    Adrixetinib (Q702) is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma .
    Adrixetinib
  • HY-176786
    MCB-36

    		PROTACs Ras Apoptosis PERK p38 MAPK Caspase TNF Receptor Cancer
    MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities Kd ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)) .
    MCB-36
  • HY-P991621
    EOS006215

    EOS-215

    		 TREM receptor Cancer
    EOS006215 (EOS-215) is a humanized monoclonal antibody targeting TREM-2. EOS006215 competes with TREM2 ligands, prevents TREM2 multimerization, and blocks downstream signaling. EOS006215 inhibits efferocytosis, reprograms transcriptomic profiles of monocyte-derived macrophages, alters metabolism and immune response genes, and increases pro-inflammatory marker secretion. EOS006215 reduces metastasis burden, delays tumor growth, and reprograms the tumor microenvironment to overcome anti-PD-1 resistance. EOS006215 can be used for the research of triple negative breast cancer and colorectal cancer .
    EOS006215
  • HY-153358
    TNG260

    		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-114243
    DpC

    		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-124447
    BTYNB

    		IGF-1R c-Myc Apoptosis TGF-beta/Smad Cancer
    BTYNB is a structure-specific nucleic acid binder and IGF2BP1 inhibitor (with an IC50 of 5 μM against hBTYNB). BTYNB disrupts the IGF2BP1-RNA interaction and blocks its binding to oncogenic mRNAs such as c-Myc, MDM2, PD-L1. BTYNB completely blocks the INHBA-Smad2/3 pathway, disrupts the MYCN/IGF2BP1 loop, and thereby induces apoptosis and cell cycle arrest, effectively inhibiting the proliferation and survival of cancer cells. In addition, BTYNB acts as an immune activator and tumor microenvironment modulator, enhances T cell-mediated tumor killing, and produces significant synergistic effects with inhibitors of PD-1, BRD and BIRC5. BTYNB can be used in relevant research on various malignant tumors including ovarian cancer, neuroblastoma, leukemia and melanoma .
    BTYNB
  • HY-13032B
    Molibresib besylate
    20+ Cited Publications

    GSK 525762C; I-BET 762 besylate

    		 Epigenetic Reader Domain ERK Cancer
    Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT. By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between BET proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2. When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, small-cell lung cancer and various advanced refractory solid tumors .
    Molibresib besylate
  • HY-175035
    HK-2-IN-1

    		Hexokinase Inflammation/Immunology Cancer
    HK-2-IN-1 is a Hexokinase 2 (HK-2) inhibitor. HK-2-IN-1 exhibits a non-activating effect on human recombinant HK-2 enzyme. HK-2-IN-1 has anti-tumor activity, affecting immune cells in the tumor microenvironment. HK-2-IN-1 has immunomodulatory effects and is potentially useful in the study of cancers such as colon cancer, liver cancer, and breast cancer .
    HK-2-IN-1
  • HY-145601
    Tinengotinib

    TT 00420

    		 Aurora Kinase FGFR VEGFR Cancer
    Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B (IC50=1.2-3.3 nM), FGFR1/2/3 (IC50=1.5-3.5 nM), VEGFRs, JAK1/2 and CSF1R. Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK-dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis, inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment .
    Tinengotinib
  • HY-107202A
    Poly (I:C):Kanamycin (1:1)
    5+ Cited Publications

    		 Toll-like Receptor (TLR) RIG-I-like receptor (RLR) PKD HSP Bcl-2 Family Interleukin Related Apoptosis Infection Inflammation/Immunology Cancer
    Poly(I:C):Kanamycin (1:1) is a mixture of Poly(I:C) (HY-107202) and Kanamycin (HY-16566). Poly(I:C) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Poly(I:C) can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Poly(I:C) can directly trigger cancer cells to undergo apoptosis. Kanamycin stabilizes Poly(I:C) .
    Poly (I:C):Kanamycin (1:1)
  • HY-162080
    METTL1-WDR4-IN-1
    1 Publications Verification

    		 DNA Methyltransferase Pyruvate Kinase Cancer
    METTL1-WDR4-IN-1 (Compound 1) is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50 = 144 μM). METTL1-WDR4-IN-1 inhibits the m 7G methyltransferase activity of the METTL1-WDR4 complex, blocking m 7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8 + T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy .
    METTL1-WDR4-IN-1
  • HY-P1181A
    Pam2CSK4 TFA
    1 Publications Verification

    		 Toll-like Receptor (TLR) NO Synthase IKK Akt PKC NF-κB p38 MAPK Interleukin Related Cardiovascular Disease Infection Inflammation/Immunology Cancer
    Pam2CSK4 TFA is a TLR2 agonist. Pam2CSK4 TFA induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 TFA activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 TFA expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 TFA acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 TFA can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis .
    Pam2CSK4 TFA
  • HY-W002199
    6:2 Fluorotelomer alcohol

    6:2 FTOH; 1H,1H,2H,2H-Perfluoro-1-octanol; 2-(Perfluorohexyl)ethanol

    		 Bacterial Apoptosis ERK TNF Receptor Infection Neurological Disease
    6:2 Fluorotelomer alcohol (6:2 FTOH) is an orally active, blood-brain barrier-permeable modulator of cyclin D1 and ETS1. 6:2 Fluorotelomer alcohol downregulates cyclin D1 expression, upregulates ETS1 via the TNF-α/ERK 1/2 pathway, impairs mitochondrial membrane potential and respiratory function, increases reactive oxygen species levels, disrupts calcium homeostasis and activates endoplasmic reticulum stress markers, and induces cell proliferation inhibition and endothelial-mesenchymal transition. Furthermore, 6:2 Fluorotelomer alcohol induces morphological abnormalities in zebrafish embryos and liver developmental damage, while disrupting the brain immune microenvironment in mice, causing systemic toxicity and delayed pup maturation in CD-1 mice. 6:2 Fluorotelomer alcohol also induces cortical neuron apoptosis, glial cell activation, synaptic abnormalities, colonic barrier damage, intestinal dysbiosis and autism spectrum disorder-like symptoms in mice. 6:2 Fluorotelomer alcohol shows no mutagenic, clastogenic, primary skin/eye irritation or skin sensitizing effects, exhibits no selective reproductive toxicity in CD-1 mice, and is classified as GHS Category 4 for acute oral toxicity. 6:2 Fluorotelomer alcohol can be used in studies of neurodevelopmental disorders and autism spectrum disorders .
    6:2 Fluorotelomer alcohol
  • HY-176785S
    MCB-294

    		Ras Apoptosis p38 MAPK Caspase TNF Receptor Cancer
    MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .
    MCB-294
  • HY-158045
    PROTAC PARP1 degrader-1

    		PROTACs PARP Cancer
    PROTAC PARP1 degrader-1 is a PARP1 PROTAC degrader with a DC50 value of 252.5 nM. PROTAC PARP1 degrader-1, combined with Daunorubicin (HY-13062A), induces the accumulation of cytoplasmic DNA fragments, activates the cGAS/STING innate immune pathway, and remodels the tumor microenvironment. PROTAC PARP1 degrader-1 can be used in research related to breast cancer .
    PROTAC PARP1 degrader-1
  • HY-P990704
    Rilvegostomig

    AZD-2936

    		 PD-1/PD-L1 Transmembrane Glycoprotein Cancer
    Rilvegostomig (AZD-2936) is a bispecific humanized IgG1 antibody targeting PD-1 and TIGIT. Rilvegostomig induces tumor growth inhibition and modulates the tumor immune microenvironment. Rilvegostomig exhibits anti-tumor activity in metastatic non-small cell lung cancer (without prior immune checkpoint inhibitor treatment). Rilvegostomig can be used in research related to metastatic non-small cell lung cancer and endometrial cancer .
    Rilvegostomig
  • HY-134958
    Polyinosinic-polycytidylic acid potassium

    Poly(I:C) potassium

    		 Toll-like Receptor (TLR) Apoptosis Inflammation/Immunology Cancer
    Polyinosinic-polycytidylic acid potassium (Poly(I:C) potassium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid potassium can directly trigger cancer cells to undergoApoptosis .
    Polyinosinic-polycytidylic acid potassium
  • HY-177086
    IDO1/TDO-IN-9

    		Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO1/TDO-IN-9 (Compound 66) is a potent dual inhibitor targeting indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) with IC50s of <1 μM. IDO1/TDO-IN-9 inhibits the activity of IDO1 and TDO, blocking tryptophan degradation to kynurenine, restoring immune activity in the tumor microenvironment, and suppressing tumor growth. IDO1/TDO-IN-9 is promising for research of cancers .
    IDO1/TDO-IN-9
  • HY-P991061
    Tagmokitug

    CHS-114; SRF-114

    		 CCR Cancer
    Tagmokitug (CHS-114; SRF-114) is a fully human IgG1 antibody targeting CCR8. Tagmokitug selectively binds to human CCR8 (Kd = 502 pM) and mediates the death of CCR8-expressing cells via antibody-dependent cellular cytotoxicity and antibody-dependent cellular phagocytosis. Tagmokitug selectively eliminates intratumoral regulatory T cells, induces tumor growth inhibition, remodels the tumor immune microenvironment, and promotes the differentiation of cytotoxic CD8 + T cell subsets. Tagmokitug can be used for the research of solid tumors .
    Tagmokitug
  • HY-N14001
    Naamidine J

    		TNF Receptor Interleukin Related Arginase PD-1/PD-L1 Inflammation/Immunology Cancer
    Naamidine J is an imidazole-type alkaloids discovered in a sponge. Naamidine J inhibits inflammation by binding to the protein CSE1L (KD = 5.41 μM). Namidine J significantly inhibits the expression of pro-inflammatory factors such as TNF-α, IL-1β, and IL-6, and upregulates anti-inflammatory factors such as CD206 and Arg-1. Namidine J inhibits PD-L1 and shows antitumor activity. Namidine J significantly reduces pulmonary tissue edema, inflammatory cell infiltration and cytokine storm in mice. Namidine J can be used for the research on the immune microenvironment of acute lung injury and tumors .
    Naamidine J
  • HY-160696
    ORIC-533

    		CD73 Cancer
    ORIC-533 is an orally active, highly selective, AMP-competitive CD73 inhibitor that potently blocks adenosine production with sub-nanomolar affinity (Ka=0.03 nM). In multiple myeloma, ORIC-533 restores and enhances the cytotoxicity of the immune system against tumor cells through multiple immunological mechanisms, including reversing the immunosuppressive microenvironment, inducing immunogenic cell death, and activating dendritic cells, T cells and NK cells, with no direct toxicity to normal cells. The combination of ORIC-533 with Daratumumab (HY-P9915) synergistically enhances anti-tumor efficacy, significantly increases intratumoral CD8 + T cell infiltration and inhibits tumor growth in vivo .
    ORIC-533
  • HY-P1181
    Pam2CSK4

    		Toll-like Receptor (TLR) NO Synthase IKK Akt PKC NF-κB p38 MAPK Interleukin Related Cardiovascular Disease Infection Inflammation/Immunology Cancer
    Pam2CSK4 is a TLR2 agonist. Pam2CSK4 induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis .
    Pam2CSK4
  • HY-P990961
    Palverafusp alfa

    IMM-2510; SYN-2510

    		 VEGFR PD-1/PD-L1 Cardiovascular Disease Inflammation/Immunology Cancer
    Palverafusp alfa (IMM-2510; SYN-2510) is a PD-L1/VEGF-targeting IgG1κ type humanized antibody. Palverafusp alfa blocks PD-1/PD-L1 binding, relieves immune suppression, mediates PD-L1-directed antibody-dependent cellular cytotoxicity (ADCC). Palverafusp alfa blocks VEGF/VEGFR binding, inhibits angiogenic signaling, relieves VEGF-induced immune suppression. Palverafusp alfa reduces endothelial cell proliferation, enhances ADCC and antibody-dependent cellular phagocytosis (ADCP), inhibits tumor growth, reverses T cell immune suppression. Palverafusp alfa exhibits immune stimulatory, antiangiogenic, and anti-tumor activity in the tumor microenvironment. Palverafusp alfa can be used for the research of cancer, such as solid tumors, non-small cell lung cancer .
    Palverafusp alfa
  • HY-107202GL
    Polyinosinic-polycytidylic acid (GMP Like)

    Poly(I:C) (GMP Like)

    		 Toll-like Receptor (TLR) PKD HSP Bcl-2 Family Interleukin Related Apoptosis Infection Inflammation/Immunology Cancer
    Polyinosinic-polycytidylic acid (Poly(I:C)) (GMP Like) is the GMP Like class Polyinosinic-polycytidylic acid (HY-107202), and can be used as pharmaceutical excipients. Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid can directly trigger cancer cells to undergo apoptosis .
    Polyinosinic-polycytidylic acid (GMP Like)
  • HY-P991444
    IPH5201

    		NTPDase ATP Synthase Inflammation/Immunology Cancer
    IPH5201 is a selective CD39 inhibitor and a humanized IgG1 monoclonal antibody. IPH5201 selectively binds to and inhibits the enzymatic activity of both membrane-bound and soluble CD39, blocking ATP hydrolysis. IPH5201 enhances the phenotypic maturation and activation of dendritic cells and macrophages. IPH5201 potentiates the anti-tumor effect of Oxaliplatin (HY-17371). IPH5201 shows preliminary evidence of disease stabilization in advanced solid tumor models when used as a single agent or in combination with Durvalumab (HY-P9919). IPH5201 can be used for the research of advanced solid tumors .
    IPH5201
  • HY-131347
    PD-1/PD-L1-IN-NP19

    		PD-1/PD-L1 Inflammation/Immunology Cancer
    PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects .
    PD-1/PD-L1-IN-NP19
  • HY-168887
    ZSA-51

    		STING Cancer
    ZSA-51 is a potent and orally active STING agonist. ZSA-51 shows anticancer activity. ZSA-51 remodeles immune microenvironment both in tumor and lymph node .
    ZSA-51
  • HY-P991309
    ZM-008

    		C-type Lectin-like Receptors (CTLRs) Cancer
    ZM-008 is an anti-LLT1 monoclonal antibody. ZM-008 blocks the interaction between LLT1 and CD161 on the surface of NK cells and T cells. ZM-008 restores anti-tumor immune activity, shifts the tumor microenvironment to an immune-responsive state, and recovers NK cell-mediated cytotoxicity against tumor cells, thereby reversing immunosuppression in immune-resistant "cold" tumors. ZM-008 is applicable to the research of immune-resistant solid tumors .
    ZM-008
  • HY-16961A
    Sitravatinib malate

    MGCD516 malate; MG-516 malate

    		 VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Inflammation/Immunology Cancer
    Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
    Sitravatinib malate
  • HY-179228
    AN02

    		CTLA-4 TGF-beta/Smad Cancer
    AN02 is a derivative of Curcumin (HY-N0005). AN02 inhibits the proliferation and clonogenicity, migration and invasion of ovarian cancer cells. AN02 dose-dependently upregulates the expression of APC and mediates the degradation of CTLA-4 through SMAD4. In the small xenograft model, AN02 significantly inhibits tumor growth and reverses the tumor immune-suppressive microenvironment. AN02, when combined with Ipilimumab (HY-P9901), can enhance efficacy and inhibit epithelial-mesenchymal transition. AN02 can be used for the study of ovarian cancer .
    AN02
  • HY-175660
    KCL-HO-1i

    		Heme Oxygenase (HO) Cancer
    KCL-HO-1i is an orally active heme oxygenase-1 (HO-1) inhibitor (rat HO-1: IC50 = 123 nM) and human HO-1: IC50 = 128 nM). KCL-HO-1i targets immunosuppressive LYVE-1 + perivascular tumor-associated macrophages (PvTAMs) in the tumor microenvironment (TME), reduces PvTAM-mediated immune exclusion. KCL-HO-1i demonstrates synergistic anti-tumor efficacy with chemotherapy in MMTV-PyMT spontaneous breast cancer mice or C57Bl/6 mice bearing subcutaneous MN-MCA1 sarcomas. KCL-HO-1i can be used for the study of cancer .
    KCL-HO-1i
  • HY-168088
    DNMT1/HDAC-IN-1

    		HDAC DNA Methyltransferase Cancer
    DNMT1/HDAC-IN-1 (compound (R)-23a) is a DNMT1/HDAC dual inhibitor (HDAC1:IC50=0.05 μM), HDAC1 is a major HDAC isoform that interacts with DNMT1 in multiple protein complexes for transcriptional silencing of TSGs. DNMT1/HDAC-IN-1 can reshape the tumor immune microenvironment and induce tumor regression, and effectively reverse cancer-specific epigenetic abnormalities .
    DNMT1/HDAC-IN-1
  • HY-172396
    PD-L1/VISTA-IN-2

    		PD-1/PD-L1 VISTA Cancer
    PD-L1/VISTA-IN-2 (Compound S8) is an orally active bifunctional PD-L1/VISTA inhibitor with an IC50 of 1.4 μM for PD-L1 and a KD of 2.1 μM for VISTA. PD-L1/VISTA-IN-2 can activate the tumor immune microenvironment and exert anti-cancer effects .
    PD-L1/VISTA-IN-2
  • HY-134920
    LW106

    		Indoleamine 2,3-Dioxygenase (IDO) Apoptosis SWI/SNF Complex Cancer
    LW106 is a selective IDO1 inhibitor with an IC50 of 1.57 μM. LW106 has no inhibitory effect on IDO2 and TDO. LW106 inhibits tumor outgrowth by limiting stroma-immune crosstalk and CSC enrichment in the tumor microenvironment. LW106 reduces subpopulation of cancer stem cells (CSCs) in xenografted tumors in which less proliferative/invasive tumor cells and more tumor cells apoptosis. LW106 can be used for the studies of lung cancer and melanoma .
    LW106
  • HY-174301
    USP7-IN-18

    		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.
    USP7-IN-18
  • HY-179288
    TPST2-IN-1

    		Transmembrane Glycoprotein STAT Cancer
    TPST2-IN-1 is a potent and selective TPST2 inhibitor with an IC50 of 946 nM and a Ka of 19.4 μM. TPST2-IN-1 increases the phosphorylation of Stat1 and upregulates the IFNγ-responsive gene CXCL10 by inhibiting TPST2 activity.TPST2-IN-1 exhibits anti-tumor activity and enhances T cell-mediated antitumor immunity characterized by increased infiltration of effector CD8 + T cells. TPST2-IN-1 can be used for the research of cancer, such as colon cancer .
    TPST2-IN-1
  • HY-175294
    PD-L1/Nampt-IN-1

    		PD-1/PD-L1 NAMPT Cancer
    PD-L1/Nampt-IN-1 is an orally active inhibitor that simultaneously target PD-L1 and NAMPT (nicotinamide phosphoribosyltransferase) with IC50s value of 63 nM and 582 nM. PD-L1/Nampt-IN-1 demonstrates cross-species affinity with comparable KD values for hPD-L1 (52.6 nM) and mPD-L1 (49.1 nM), respectively. PD-L1/Nampt-IN-1 effectively inhibits tumor growth by activating the tumor immune microenvironment. PD-L1/Nampt-IN-1 can be used for the study of melanoma .
    PD-L1/Nampt-IN-1
  • HY-152830A
    Adrixetinib TFA

    Q702 TFA

    		 c-Fms TAM Receptor MHC Cancer
    Adrixetinib (Q702) TFA is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib TFA acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib TFA increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib TFA upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib TFA shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib TFA is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma .
    Adrixetinib TFA

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