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microenvironment

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59

Inhibitors & Agonists

1

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1

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4

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7

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2

Natural
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3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-131347

    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-P990042

    ONC-392; BNT 316

    CTLA-4 Cancer
    Gotistobart (ONC-392) is a humanized anti-CTLA-4 antibody that confers immunotherapeutic effect by selective depletion of regulatory T cells (Treg) in the tumor microenvironment .
    Gotistobart
  • HY-139245

    ADC Linker Cancer
    MC-Ala-Ala-Asn-PAB is a linker extracted from patent CN104147612A, page 14. MC-Ala-Ala-Asn-PAB can be used to synthesis the tumor microenvironment specific activated micromolecular targeted conjugate .
    MC-Ala-Ala-Asn-PAB
  • HY-154850

    STING Cancer
    F-CRI1 is a potent STING agonist with a Kd value of 40.62 nM. F-CRI1 is a radioactive probe with 18F-labeled modification. F-CRI1 can be used to study STING visualization in the tumor microenvironment .
    F-CRI1
  • HY-154869

    PD-1/PD-L1 Inflammation/Immunology Cancer
    PD-1/PD-L1-IN-34 (Compound (1S,2S)-A25) inhibits PD-1/PD-L1 interaction (IC50=0.029 μM), with a selected binding affinity with PD-L1 (KD=0.1554 μM). PD-1/PD-L1-IN-34 inhibits tumor growth by activating the immune microenvironment .
    PD-1/PD-L1-IN-34
  • HY-151559

    Checkpoint Kinase (Chk) STAT CXCR CCR Cancer
    Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. Zn-DPA-maytansinoid conjugate 1 induces lasting regression of tumor growth and rejuvenates tumor microenvironment (TME) to an “inflamed hot tumor” .
    Zn-DPA-maytansinoid conjugate 1
  • HY-157157

    Protein Arginine Deiminase Cancer
    PAD4-IN-3 (compound 4B) is a PAD4 inhibitor with antitumor activity in vitro and in vivo. PAD4-IN-3 was covalently linked to RGD sequence peptide-modified chitosan (K-CRGDV), resulting in an enhanced oxidative stress-responsive nanoagent. K-CRGDV-PAD4-IN-3 can actively target tumors, inhibit PAD4 activity, block the formation of neutrophil extracellular traps (NETs), and improve the tumor immune microenvironment in response to the tumor microenvironment .
    PAD4-IN-3
  • HY-135748

    Poly(I:C) sodium

    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-134958

    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-160053

    PDGFR Cancer
    Gint4.T aptamer sodium is a nuclease-resistant RNA aptamer-based antagonist targeting platelet-derived growth factor receptor beta (PDGFRβ) (Kd: 9.6 nM). Gint4.T aptamer sodium inhibits PDGFRβ heterodimerization and EGFR transactivation. It can significantly inhibit cell migration and proliferation, induce differentiation and prevent tumor growth in vivo. Gint4.T aptamer sodium specifically inhibits PDGFRβ-mediated tropism of mesenchymal stem cells (MSCs) toward the tumor microenvironment .
    Gint4.T aptamer sodium
  • HY-146215

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    Hy-146215 is an enzyme that catalyzes the oxidative metabolism of tryptophan. It can immunosuppress tumors in the tumor microenvironment.
    IDO1-IN-20
  • HY-161248

    Microtubule/Tubulin Cancer
    E7130 is a microtubule inhibitor, which ameliorates the tumor microenvironment through suppression of cancer-associated fibroblasts (CAF) and promotion of tumor vasculature remodeling .
    E7130
  • HY-116071

    Autophagy Cancer
    Autophagy-IN-3 (Compound 6k) is an autophagy inhibitor. Autophagy-IN-3 promotes metabolic stress in the tumor microenvironment and enhances the effects of cytostatics in combined treatments .
    Autophagy-IN-3
  • HY-141663

    ADC Linker Cancer
    2',3'-cGAMP-C2-SH is a cyclic di-nucleotide (CDN) that can be conjugated to antibodies or antigen-binding fragments targeting specific antigens in the microenvironment of diseased cells or tissue .
    2',3'-cGAMP-C2-SH
  • HY-160421

    Others Inflammation/Immunology Cancer
    TREM2-IN-1 (OPA) is a TREM2 inhibitor derived from oxaliplatin and artesunate. TREM2-IN-1 is capable of relieving immunosuppressive tumor microenvironment and enhancing chemical anticancer efficiency .
    TREM2-IN-1
  • HY-137206

    Ligands for E3 Ligase Molecular Glues Cancer
    ALV2 is a potent and selective Helios degrader. ALV2 binds CRBN, with an IC50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable Treg cell phenotype in the inflammatory tumor microenvironment .
    ALV2
  • HY-D0074

    Fluorescent Dye Others
    Prodan, a solvatochromic fluorophore, has been used as a microenvironment-sensitive membrane reporter. Based on the chemistry of Prodan, fluorescent nucleosides are designed and synthesized.The fluorescent nucleosides sensitively varied the Stokes shift values depending on the orientational polarizability of the solvent .
    Prodan
  • HY-P99565

    ARENEGYR; NGR-TNF; NGR-hTNF

    TNF Receptor Cancer
    Tengonermin (ARENEGYR) is a vascular-targeting agent consisting of the human Tumour Necrosis Factor-α (TNF-α) conjugated with the CNGRCG peptide. Tengonermin increases penetration of intratumoral chemotherapy and T-cell infiltration by modifying the tumour microenvironment .
    Tengonermin
  • HY-160041A

    CXCR Cancer
    Olaptesed pegol sodium A pegylated-based L-oligoribonucleotide aptamer targeting CXCL12. Olaptesed pegol sodium neutralizes CXCL12, and CXCL12 inhibition mobilizes chronic lymphocytic leukemia cells into the circulation and prevents their homing into the protective microenvironment .
    Olaptesed pegol sodium
  • HY-148494

    FLX475

    CCR Cancer
    Tivumecirnon (FLX475) is an orally active CCR4 antagonist that blocks regulatory T cells from entering the tumor microenvironment, thereby reducing their interference with effective anti-tumor immune responses. Tivumecirnon has antitumor activity .
    Tivumecirnon
  • HY-D0067
    7ACC1
    5+ Cited Publications

    DEAC; Coumarin D 1421; D 1421

    Monocarboxylate Transporter Cancer
    7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
    7ACC1
  • HY-130117

    Reactive Oxygen Species Apoptosis Cancer
    AlbA-DCA is a conjugate formed by the attachment of Albiziabioside A (AlbA) to a dichloroacetate acid (DCA) subunit. AlbA-DCA can induce a marked increase in intracellular ROS and alleviate the accumulation of lactic acid in tumor microenvironment (TME), and also selectively kills cancer cells and induce apoptosis .
    AlbA-DCA
  • HY-Y0445A
    Sodium dichloroacetate
    Maximum Cited Publications
    14 Publications Verification

    PDHK Reactive Oxygen Species NKCC Apoptosis Cancer
    Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor .
    Sodium dichloroacetate
  • HY-160041

    CXCR Cancer
    Olaptesed pegol (NOX-A12) L-oligoribonucleotide aptamer targeting CXCL12 based on a pegylated structure. Olaptesed pegol neutralizes CXCL12, and CXCL12 inhibition mobilizes chronic lymphocytic leukemia cells into the circulation and prevents their homing into the protective microenvironment .
    Olaptesed pegol
  • HY-160696

    CD73 Cancer
    ORIC-533 is an orally active, selective CD73 inhibitor with AMP-competition. ORIC-533 restores immunosuppressed CD8+ T cell proliferation and activation, triggers significant lysis and cell death of multiple myeloma cells in the bone marrow microenvironment .
    ORIC-533
  • HY-147204

    Drug-Linker Conjugates for ADC Cancer
    Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE (compound S6) is a potent anticancer agent, which can be specific activated by tumor microenvironment. Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE can suppress tumor growth in mice (extracted from patent CN104147612A) .
    Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE
  • HY-P99039

    MEDI9447

    CD73 Cancer
    Oleclumab (MEDI9447) is a human IgG1λ monoclonal antibody targeting CD73 and inhibits the exonuclease activity of the extracellular enzyme CD73. Oleclumab can adjust the composition of bone marrow and lymphoid infiltrating leukocyte populations in the tumor microenvironment and has anti-tumor activity .
    Oleclumab
  • HY-P99536

    SL-401

    Interleukin Related Cancer
    Tagraxofusp (SL-401) is a potent IL-3 receptor inhibitor to inhibits plasmacytoid dendritic cells (pDCs) growth in multiple myeloma (MM) bone marrow (BM) microenvironment. Tagraxofusp has synergistic effect with Bortezomib (HY-10227) and Pomalidomide (HY-10984) to suppress multiple myeloma (MM) .
    Tagraxofusp
  • HY-15888
    PTC-209
    5+ Cited Publications

    Autophagy Cancer
    PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment .
    PTC-209
  • HY-15888A
    PTC-209 hydrobromide
    5+ Cited Publications

    Autophagy Cancer
    PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment .
    PTC-209 hydrobromide
  • HY-163081

    PARP Cancer
    PARP7-IN-17 is a potent inhibitor of PARP7 with IC50 of 4.5 nM that has oral bioavailability. PARP7-IN-17 displays antitumor effect .
    PARP7-IN-17
  • HY-119367

    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-P3448

    CEND-1; iRGD; LSTA1

    Integrin Complement System Cancer
    Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary agent conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors .
    Certepetide
  • HY-163146

    Fluorescent Dye Cancer
    TME-HYM (PH Probe) is a novel fluorescent probe based on acidic tumor microenvironment (TME) activation and organic anion transporting polypeptide (OATPs, overexpressed on cancer cells), and can be selective uptaken. TME-HYM (PH Probe) can selectively lit up cancer cells and tumor tissues, offering dual tumor selectivity for precise visualization of tumor mass .
    TME-HYM (PH Probe)
  • HY-125836

    CCR Endocrinology Cancer
    CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca 2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively .
    CCR4 antagonist 2
  • HY-P99742

    ADC-1013; JNJ-64457107

    TNF Receptor Cancer
    Mitazalimab (ADC-1013; JNJ-64457107) is FcγR-dependent CD40 agonist with tumor-directed activity. Mitazalimab activates antigen-presenting cells, e.g. dendritic cells (DC), to initiate tumor-reactive T cells. Therefore, Mitazalimab induces tumor-specific T cells to infiltrate and kill tumors. Mitazalimab remodels the tumor-infiltrating myeloid microenvironment .
    Mitazalimab
  • HY-16938
    5'-Methylthioadenosine
    3 Publications Verification

    5'-(Methylthio)-5'-deoxyadenosine; 5'-Deoxy-5'-(methylthio)adenosine; 5'-S-Methyl-5'-thioadenosine

    Endogenous Metabolite Apoptosis Parasite Metabolic Disease Cancer
    5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
    5'-Methylthioadenosine
  • HY-P99963

    HS636

    PD-1/PD-L1 Cancer
    Sudubrilimab (HS636) is an Ig G1-kappa monoclonal antibody against PDL1. Sudubrilimab is fused at the C terminus of the heavy chain to a TGF-β1 receptor Ⅱ ectodomain (TGFBR2-ECD), and which can sequester the PD-1/PD-L1 pathway and TGF-β bioactivity in the immunosuppressive tumor microenvironment .
    Sudubrilimab
  • HY-107202
    Polyinosinic-polycytidylic acid
    10+ Cited Publications

    Poly(I:C)

    Toll-like Receptor (TLR) PKD HSP Bcl-2 Family Interleukin Related 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-144274

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO1-IN-14 (compound 4a) is a potent IDO1 inhibitor with an IC50 of 396.9 nM. IDO1-IN-14 has cellular IDO1 inhibition (HeLa EC50=3393 nM) .
    IDO1-IN-14
  • HY-144273

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO1-IN-13 (compound 27a) is a potent IDO1 inhibitor with an IC50 of 61.6 nM. IDO1-IN-13 has cellular IDO1 inhibition (HeLa EC50= 30 nM). IDO1-IN-13 decreases 51% of the kyn/trp ratio in SK-OV-3 xenograft tumor tissues .
    IDO1-IN-13
  • HY-158057

    Adenosine Receptor Cancer
    A2AR/A2BR antagonist 1 (compound 7ai) has a dual antagonistic effect on A2AR/A2BR, with the IC50 values of 11.2 nM and 6.4 nM for A2AR and A2BR, respectively. A2AR/A2BR antagonist 1 promotes T cell-mediated cancer cell death .
    A2AR/A2BR antagonist 1
  • HY-A0183

    Phospholipids, phosphatidylserines; Serine glycerophosphatides

    Phosphatidylserine is a conserved anti-inflammatory and immunosuppressive signal that is highly dysregulated in the tumor microenvironment and autoimmune diseases. During apoptosis and cellular stress,the related disrupting enzymes Xkr8 and TMEM16 mediate Phosphatidylserine externalization. Phosphatidylserine externalization produces a "eat me" signal that initiates endocytosis and helps clear the body of apoptotic cells. When pathogens use Phosphatidylserine and apoptotic mimicry to evade host immune responses,targeting Phosphatidylserine strategies can stimulate immune activity .
    Phosphatidylserine
  • HY-151427

    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-16961
    Sitravatinib
    1 Publications Verification

    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-16961A

    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-16938S

    -(Methylthio)-5'-deoxyadenosine-13C6; 5'-Deoxy-5'-(methylthio)adenosine-13C6; 5'-S-Methyl-5'-thioadenosine-13C6

    Endogenous Metabolite Apoptosis Metabolic Disease Cancer
    5'-Methylthioadenosine- 13C6 is the 13C-labeled 5'-Methylthioadenosine. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis[1]. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2].
    5'-Methylthioadenosine-13C6
  • HY-128946
    CL2A-SN-38
    1 Publications Verification

    Drug-Linker Conjugates for ADC Inflammation/Immunology Cancer
    CL2A-SN-38 is a agent-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody agent conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A-SN-38 uses hydrolyzable linker to deliver active agents within tumor cells and in the tumor microenvironment, resulting in bystander effects .
    CL2A-SN-38
  • HY-144746

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-26 (Compound II-14) is a potent inhibitor of PD-1/PD-L1 with an IC50 of 0.0380 μM. PD-1/PD-L1-IN-26 activates the immune microenvironment by promoting the infiltration of CD4+ T cells into tumor tissues. PD-1/PD-L1-IN-26 has the potential for the research of cancer diseases .
    PD-1/PD-L1-IN-26
  • HY-16938S1

    5'-(Methylthio)-5'-deoxyadenosine-d3; 5'-Deoxy-5'-(methylthio)adenosine-d3; 5'-S-Methyl-5'-thioadenosine-d3

    Apoptosis Parasite Endogenous Metabolite
    5'-Methylthioadenosine-d3 is the deuterium labeled 5'-Methylthioadenosine[1]. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2][3][4].
    5'-Methylthioadenosine-d3

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