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Results for "

PD-L1 expression

" in MedChemExpress (MCE) Product Catalog:

82

Inhibitors & Agonists

2

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9

Inhibitory Antibodies

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1

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16141
    Cilengitide
    Maximum Cited Publications
    70 Publications Verification

    EMD 121974

    		 Integrin Autophagy Apoptosis STAT PD-1/PD-L1 Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Cilengitide (EMD 121974) is a BBB-permeable integrins antagonist with IC50s of 0.61 nM (ανβ3), 8.4 nM (ανβ5) and 14.9 nM (α5β1), respectively. Cilengitide inhibits the binding of ανβ3 and ανβ5 to Vitronectin with IC50s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers .
    Cilengitide
  • HY-N3005
    Britannin
    1 Publications Verification

    		 Apoptosis Autophagy NOD-like Receptor (NLR) Pyroptosis Inflammation/Immunology Cancer
    Britannin is an NLRP3 inhibitor with an IC50 of 3.630 μM, exhibiting anti-inflammatory activity. Britannin inhibits the activation and assembly of the NLRP3 inflammasome by blocking the interaction between NLRP3 and NEK7. Additionally, Britannin demonstrates antitumor activity by inhibiting the proliferation of tumor cells through blocking the interaction between HIF-1α and Myc, thereby suppressing PD-L1 expression and enhancing cytotoxic T lymphocyte activity. Britannin can also induce apoptosis and autophagy in liver cancer cells by activating ROS-regulated AMPK. Britannin holds promise for research in the fields of anti-inflammatory and antitumor therapeutics .
    Britannin
  • HY-P9997
    Rosnilimab

    ANB030

    		 PD-1/PD-L1 Inflammation/Immunology
    Rosnilimab (ANB030) is a PD-1 agonist IgG1 monoclonal antibody. Rosnilimab can inhibit T cell proliferation, the secretion of inflammatory cytokines, and reduce CD4 and CD8 T cells with high PD-1 expression. Rosnilimab can be used in the research of inflammatory diseases such as colitis and rheumatoid arthritis .
    Rosnilimab
  • 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-P991628
    SSGJ-707

    PF-08634404

    		 PD-1/PD-L1 VEGFR Cancer
    SSGJ-707 (PF-08634404) is a bispecific antibody targeting VEGF and PD-1. SSGJ-707 exerts dual anti-tumor effects by neutralizing VEGF and blocking the PD-1 signaling pathway. SSGJ-707 can be combined with platinum-based chemotherapy to inhibit advanced non-small cell lung cancer (NSCLC), and its inhibitory effect is not limited by PD-L1 expression levels. In the HARMONi-2 trial, the objective response rate of SSGJ-707 correlates with the PD-L1 tumor proportion score, and the incidence of grade ≥3 adverse events is comparable to that of Inetetamab (HY-P99969). SSGJ-707 is being extensively investigated for a variety of malignancies including advanced NSCLC, colorectal cancer and small cell lung cancer .
    SSGJ-707
  • HY-N0596
    Panaxadiol
    4 Publications Verification

    20(R)-Panaxadiol

    		 PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT Cancer
    Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities .
    Panaxadiol
  • HY-108691
    PF-06465469
    2 Publications Verification

    		 Itk Btk CXCR PD-1/PD-L1 LAG-3 Cancer
    PF-06465469 is a covalent inhibitor of ITK with an IC50 of 2 nM. PF-06465469 also inhibits BTK. PF-06465469 inhibits cell migration in response to CXCL12. PF-06465469 decreases PD-1 and LAG-3 expression. PF-06465469 can be used to study leukemia and T-cell lymphoma .
    PF-06465469
  • HY-124700
    LYPLAL1-IN-1
    1 Publications Verification

    		 Cyclic GMP-AMP Synthase STING PD-1/PD-L1 Epoxide Hydrolase Metabolic Disease
    LYPLAL1-IN-1 (compound 11) is a selective, covalent, and irreversible inhibitor of the lysophospholipase-like enzyme LYPLAL1 (IC50 = 6 nM). LYPLAL1-IN-1 shows selectivity against other serine hydrolases such as carboxylesterase CES1 (IC50 > 50 μM for CES1). LYPLAL1-IN-1 inhibits the depalmitoylation function of LYPLAL1, blocking its depalmitoylation modification of cyclic GMP-AMP synthase (cGAS), thereby promoting cGAS dimerization and activation, and initiating the cGAS-STING pathway-mediated innate immune response. LYPLAL1-IN-1 can enhance DNA-induced type I interferon production, upregulate PD-L1 expression in tumor cells, and promote the accumulation of tumor-infiltrating CD8 + T cells, with the core function of strengthening the anti-tumor immune response. LYPLAL1-IN-1 is primarily used in tumor immunology research, especially in combination with PD-1/PD-L1 inhibitors .
    LYPLAL1-IN-1
  • HY-178193
    Chem-0199

    		DNA/RNA Synthesis Akt PD-1/PD-L1 Cancer
    Chem-0199 is an Adipocyte Enhancer-Binding Protein 1 (AEBP1) inhibitor. Chem-0199 can disrupt the interaction between AEBP1 and CKAP4, thereby enhances antitumor immunity. Chem-0199 can inhibit Akt phosphorylation (p-Akt) and downregulates PD-L1 expression. Chem-0199 can be used for the research of cancer, such as colon cancer .
    Chem-0199
  • HY-108693
    β-Tocotrienol

    		Leukotriene Receptor Apoptosis Inflammation/Immunology
    β-Tocotrienol is an isomer of vitamin E. β-Tocotrienol is a less potent antioxidant than α-tocotrienol. β-Tocotrienol can be found in the tocotrienol-rich fraction (TRF) of palm oil, which possesses anti-carcinogenic effects in vitro on human colon carcinoma and prostate cancer cells. β-Tocotrienol inhibits the growth of A549 (GI50 = 1.38 μM) and U87MG (GI50 = 2.53 μM) cells. β-Tocotrienol also induces apoptosis in cancer cells. β-Tocotrienol can inhibit PD-L1 expression and mitigates PD-L1-mediated immune suppression in vitro and in vivo .
    β-Tocotrienol
  • HY-101454
    SR0987
    3 Publications Verification

    		 ROR Inflammation/Immunology Cancer
    SR0987, a SR1078 analog, is a RORγt agonist, with an EC50 of 800 nM. SR0987 increases IL17 expression while repressing the expression of PD-1 .
    SR0987
  • HY-N3431
    Kaempferol-7-O-rhamnoside

    		AMPK PD-1/PD-L1 FXR Reactive Oxygen Species (ROS) Cardiovascular Disease
    Kaempferol-7-O-rhamnoside is a PD-1/PD-L1 inhibitor and farnesoid X receptor (FXR) agonist. Kaempferol-7-O-rhamnoside demonstrates cardioprotective potential targeting the AMPKα1 signaling pathway. Kaempferol-7-O-rhamnoside significantly upregulates the mRNA expression of AMPKα1 in H9c2 cardiomyocytes. Kaempferol-7-O-rhamnoside reverses APAP-induced reduction of glutathione (GSH) content and increase of ROS production in L02 cells. Kaempferol-7-O-rhamnoside has the potential for heart failure .
    Kaempferol-7-O-rhamnoside
  • HY-P3440
    WL12

    		Radionuclide-Drug Conjugates (RDCs) PD-1/PD-L1 Cancer
    WL12 is a specifically targeting programmed death ligand 1 (PD-L1) binding peptide. WL12 can be radiolabeled by different radionuclides, generating radiotracers, which can assess the tumor PD-L1 expression .
    WL12
  • HY-P99914
    Emfizatamab

    GNC-038

    		 PD-1/PD-L1 CD19 TNF Receptor CD3 Interleukin Related IFNAR Inflammation/Immunology Cancer
    Emfizatamab (GNC-038) is a monoclonal antibody against CD19/CD3E/TNFRSF9/PD-L1. Emfizatamab exhibits antitumor activity, being capable of activating CD3 and 4-1BB signals on T cells, as well as targeting the high expression of CD19 or PD-L1 on tumor cells. Emfizatamab functions as a CD19-specific T cell engager by mediating direct antitumor activity. Emfizatamab can also overcome the inhibition of T cells by PD-L1. Emfizatamab can be used in the research of tumors such as R/R non-Hodgkin lymphoma or acute lymphoblastic leukemia .
    Emfizatamab
  • 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-12964
    SGI-7079
    3 Publications Verification

    		 TAM Receptor Cancer
    SGI-7079 is a selective, ATP-competitive, orally active inhibitor of the receptor tyrosine kinase Axl. SGI-7079 blocks Axl-mediated signaling pathways such as NF-κB activation and MMP-9 expression, thereby inhibiting tumor cell proliferation, migration and invasion. SGI-7079 is mainly used in the research of malignant tumors such as inflammatory breast cancer and bladder cancer, as well as in combination with immunization (used in combination with PD-1 therapy)[1][2][3].
    SGI-7079
  • HY-148511
    Vidutolimod

    CMP-001

    		 Toll-like Receptor (TLR) IFNAR PD-1/PD-L1 Indoleamine 2,3-Dioxygenase (IDO) Cancer
    Vidutolimod (CMP-001) is a virus-like particle containing a TLR9 activator . Vidutolimod induces human peripheral blood mononuclear cells to secrete IFNα, and upregulates the gene expression of CXCL10, PDL1, IDO and CD80. Vidutolimod activates TLR9, which in turn triggers plasmacytoid dendritic cell activation, production of IFNγ and TNFα, induction of CXCL10, and recruitment of antitumor T cells. Vidutolimod causes influenza-like symptoms, hypotension and tumor regression, and its activity depends on the presence of anti-Qβ antibodies. Vidutolimod modulates monocyte function, promotes CD4 T cell proliferation, and activates multiple immune cell types in an environment with anti-Qβ antibodies. Vidutolimod prolongs the survival of tumor-bearing mice. Vidutolimod is used in research related to advanced melanoma, head and neck squamous cell carcinoma, and advanced non-small cell lung cancer .
    Vidutolimod
  • HY-168530
    PDL1 degrader-1

    		PD-1/PD-L1 Cancer
    PDL1 degrader-1 (compound PMT-O9-1A) is a potent PD-L1 degrader. PDL1 degrader-1 decreases the protein expression of PD-L1. PDL1 degrader-1 shows cytotoxicity. PDL1 degrader-1 shows anticancer activity .
    PDL1 degrader-1
  • HY-149830
    PD-L1-IN-2
    1 Publications Verification

    		 PD-1/PD-L1 Cancer
    PD-L1-IN-2 is a potential tumor immunological agent by inhibiting PD-L1. PD-L1-IN-2 is a Naamidine J derivative and exerts antitumor effects in vivo by reducing PD-L1 expression and enhancing tumor-infiltrating T-cell immunity. PD-L1-IN-2 is used for colorectal cancer research .
    PD-L1-IN-2
  • HY-160768
    OTUB2-IN-1

    		Deubiquitinase Inflammation/Immunology Cancer
    OTUB2-IN-1, a specific inhibitor of OTUB2 (KD: ~12 μM), reduces PD-L1 protein expression in tumor cells and inhibits tumor growth by promoting robust intra-tumor infiltration of cytotoxic T lymphocytes (CTL) .
    OTUB2-IN-1
  • HY-156850
    ITF 3756

    		HDAC NF-κB Cancer
    ITF 3756 is a selective, orally active HDAC6 inhibitor. ITF 3756 antagonizes TNF-α-induced activation of the NF-κB pathway. ITF 3756 reduces PD-L1 expression on human monocytes and CD8 + T cells, and exhibits antitumor activity. ITF 3756 can be used in colon cancer-related research .
    ITF 3756
  • HY-144501
    D18

    		Toll-like Receptor (TLR) PD-1/PD-L1 Inflammation/Immunology Cancer
    D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC50 = 24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases PD-L1 expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2 (HY-144497). D18 has strong immune activation and anti-tumor activity. D18 commonly used in cancer research, such as colon cancer .
    D18
  • HY-N8389
    Globulol

    		Bacterial Fungal PAK Akt STAT PD-1/PD-L1 Apoptosis CCR Infection Cancer
    Globulol is a terpenoid metabolite and Antimicrobial agent. Globulol can be isolated from Alpinia oxyphylla Miq. Globulol binds to PAK4, reduces the expression level of PAK4 in cancer cells, decreases the phosphorylation of AKT, and downregulates the expressions of STAT3, phosphorylated STAT3, and PD-L1. Globulol promotes the secretion of CCL4 by cancer cells. Globulol reduces the viability and proliferation ability of cancer cells, induces G0/G1 cell cycle arrest and Apoptosis in cancer cells, and inhibits cancer cell migration and the integrity of 3D tumor spheres. Globulol enhances the relevant effects of anti-PD-1 agents in the cancer cell microenvironment. Globulol exhibits anticancer activity against liver cancer. Globulol inhibits the mycelial growth of phytopathogenic fungi and the growth of phytopathogenic bacteria. Globulol can be used in studies related to hepatocellular carcinoma .
    Globulol
  • HY-P3342
    [D-Leu-4]-OB3

    		PD-1/PD-L1 Apoptosis Inflammation/Immunology
    [D-Leu-4]-OB3 inhibits expressions of pro-inflammatory, proliferative and metastatic genes and PD-L1 expression. [D-Leu-4]-OB3 stimulates expression of pro-apoptotic genes .
    [D-Leu-4]-OB3
  • HY-P991193
    NGM-438

    		TNF Receptor Cancer
    NGM-438 is a humanized monoclonal antibody antagonist of LAIR1, with a Ka of 0.26 nM for human LAIR1 and 4.28 nM for cynomolgus monkey LAIR1. NGM-438 blocks the binding of LAIR1 to its Collagen ligand and antagonizes the Collagen-induced LAIR1 signaling pathway. NGM-438 reverses FcγR signaling inhibition in myeloid cells, induces dendritic cells to secrete TNFα, promotes T cell proliferation, and triggers myeloid inflammation and allogeneic T cell responses. NGM-438 sensitizes refractory mouse lung cancer to PD-1 blockade, increases the content of intratumoral CD8 + T cells and the expression of inflammatory genes. NGM-438 is applicable to research related to solid tumors, refractory solid tumors and non-small cell lung cancer .
    NGM-438
  • HY-155847
    LYP-IN-3

    		Phosphatase PD-1/PD-L1 Inflammation/Immunology Cancer
    LYP-IN-3 is a selective, orally active and reversible lymphoid-tyrosine phosphatase (LYP) inhibitor (IC50 = 2.55 μM, Ki = 0.93 μM). D34 exhibits high selectivity of PTP1B, PTPN12, PTPN5 and SSH2. LYP-IN-3 regulates the T-cell receptor (TCR) signaling by specifically inhibiting LYP. LYP-IN-3 does not significantly inhibit MC38 cell viability; its anti-tumor effect stems from immune regulation. LYP-IN-3 can significantly upregulate PD-L1 or PD-1 expression in different immune cells. LYP-IN-3 facilitates T-cell infiltration and enhances T-cell functions. LYP-IN-3 synergizes with PD-L1 blockade can significantly improve colorectal tumor regression. LYP-IN-3 can be used for the study of colorectal cancer .
    LYP-IN-3
  • HY-155848
    LYP-IN-4

    		Phosphatase Cancer
    LYP-IN-4 (compound D14) is a reversible and selective inhibitor of lymphotyrosine phosphatase (LYP) (Ki=1.34 μM, IC50=3.52μM). LYP-IN-4 inhibits LYP to regulate TCR signaling, up-regulates PD-1/PD-L1 expression, and enhance anti-tumor immunity. LYP-IN-4 activates T cells and inhibits M2 macrophage polarization, inhibits tumor growth in MC38 isogenic mouse models.
    LYP-IN-4
  • HY-172200
    PD-L1/HDAC6-IN-1

    		PD-1/PD-L1 HDAC Inflammation/Immunology Cancer
    PD-L1/HDAC6-IN-1 is an orally active dual inhibitor of PD-L1 and HDAC6, with IC50 values of 26.8 nM and 78 nM, respectively. PD-L1/HDAC6-IN-1 binds to human and murine PD-L1 proteins with high affinity, while it reduces STAT3 phosphorylation and downregulates PD-L1 expression by inhibiting HDAC6, thus blocking the PD-1/PD-L1 interaction. PD-L1/HDAC6-IN-1 exhibits potent anti-tumor activity in a mouse melanoma model. PD-L1/HDAC6-IN-1 is suitable for research on tumor immune regulation related to melanoma .
    PD-L1/HDAC6-IN-1
  • HY-P99844
    Davoceticept

    ALPN-202; CD80 vIgD-Fc

    		 CTLA-4 Cancer
    Davoceticept (ALPN-202; CD80 vIgD-Fc) is a variant CD80 vIgD-Fc fusion protein targeting CTLA-4 and PD-L1. Davoceticept consists of the (1-107) fragment of CD80 linked to IGHG1 Fc via a peptidyl linker. The expression system of Davoceticept is usually CHO (Chinese Hamster Ovary) cells .
    Davoceticept
  • HY-173070
    TLR7 agonist 29

    		Toll-like Receptor (TLR) IFNAR PD-1/PD-L1 ADC Payload Inflammation/Immunology Cancer
    TLR7 agonist 29 (Compound 1) is the agonist for TLR7 with an EC50 of 5.2 nM for human TLR7 (EC50 for mouse TLR7 is 48.2 nM). TLR7 agonist 29 activates bone marrow-derived macrophages (BMDMs), stimulates myeloid cells in the tumor microenvironment, promotes the expression of PD-L1, CD86 and IFN-α. TLR7 agonist 29 can be used as payload for synthesis of ADC .
    TLR7 agonist 29
  • HY-178193A
    (Rac)-Chem-0199

    		DNA/RNA Synthesis Akt PD-1/PD-L1 Cancer
    (Rac)-Chem-0199 is the racemic mixture of Chem-0199 (HY-178193). Chem-0199 is an Adipocyte Enhancer-Binding Protein 1 (AEBP1) inhibitor. Chem-0199 can disrupt the interaction between AEBP1 and CKAP4, thereby enhances antitumor immunity. Chem-0199 can inhibit Akt phosphorylation (p-Akt) and downregulates PD-L1 expression. Chem-0199 can be used for the research of cancer, such as colon cancer .
    (Rac)-Chem-0199
  • 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-179557
    iMQT_020

    		Glutathione Peroxidase Reactive Oxygen Species (ROS) Apoptosis Ferroptosis PD-1/PD-L1 Cancer
    iMQT_020 is a selective allosteric SLC1A5_var inhibitor. iMQT_020 disrupts the trimeric assembly of SLC1A5_var, causing metabolic crisis in cancer cells and selectively suppressing their growth. iMQT_020 reduces glutamine anaplerosis and oxidative phosphorylation, resulting in a broad disruption of cancer metabolism. iMQT_020 reduces GSH levels and increases cellular ROS and mitochondrial ROS. iMQT_020 induces apoptosis and ferroptosis. iMQT_020 can epigenetically upregulate PD-L1 expression. iMQT_020 can be used for the study of pancreatic cancer, lung cancer, and colon cancer .
    iMQT_020
  • HY-145769
    N2S2-CBMBC

    		PD-1/PD-L1 Cancer
    N2S2-CBMBC, an N2S2 bromo-benzyl ether derivative, acts as a ligand and use 99mTc-labelled complexes 99mTc-N2S2-CBMBC can be used as an imaging agent to be applied to the aspect of detecting PD-L1 expression, realize the real-time, comprehensive and convenient detection of the PD-L1 level of tumors, and overcome the defects of an immunohistochemical method .
    N2S2-CBMBC
  • HY-175604
    SCL-1

    		PD-1/PD-L1 Cancer
    SCL-1 is an orally active anti-PD-1/PD-L1 inhibitor. SCL-1 can inhibit PD-1/PD-L1 binding. SCL-1 increases T cells, B cells and natural killer cells. SCL-1 exerts strong tumor growth inhibitory effects that were mediated by effector T-cell induction inside tumors and the up-regulated expression of long non-coding RNAs as neoantigens leading to cytotoxic T lymphocyte activation. SCL-1 can be used for the research of cancer, such as triple-negative breast cancer .
    SCL-1
  • HY-169363
    PDL1 degrader-2

    		PD-1/PD-L1 Autophagy AUTACs Cancer
    PD-L1 degrader-2 (Compound B3) is an orally active AUTAC degrader, that degrades PD-L1 through autophagy-lysosome pathway with a DC50 of 0.5 μM. PD-L1 degrader-2 exhibits inhibitory activity against PD-1/PD-L1 interaction with an IC50 of 22.8 nM. PD-L1 degrader-2 upregulates the expressions of Atg9b, Lamp1 and Mitf, and activates the autophagy lysosome system. PD-L1 degrader- exhibits antitumor efficacy in CT26 mouse model . (Pink: autophagy-lysosome activator (HY-159894); Black: linker (HY-W015088); Blue: PD-L1 ligand (HY-169365))
    PDL1 degrader-2
  • HY-175014
    LGT-1

    		PD-1/PD-L1 Biochemical Assay Reagents Cancer
    LGT-1 is a PD-L1 ligand. LGT-1 labeled with 18F has an excellent specific uptake in B16-F10 tumor cells, and shows a high tumor uptake but a low liver uptake with good stability in B16-F10 tumor-bearing mice model. LGT-1 can be used as a radiotracer for PET imaging of PD-L1 expression in tumors .
    LGT-1
  • HY-159601
    CSN5-IN-1

    		PD-1/PD-L1 E1/E2/E3 Enzyme Cancer
    CSN5-IN-1 (compound Ac-11) is an inhibitor of CSN5, with IC50 values of 12.56 μM and 19 μM as measured by FP assay and fluorescence assay, respectively. CSN5-IN-1 can also downregulate the expression of PD-L1 and upregulate the expression of NEDD8-Cul1 in cells .
    CSN5-IN-1
  • HY-155115
    LSD1-IN-27
    1 Publications Verification

    		 Histone Demethylase PD-1/PD-L1 Cancer
    LSD1-IN-27 is an orally active LSD1 inhibitor (IC50: 13 nM). LSD1-IN-27 inhibits the stemness and migration of gastric cancer cells. LSD1-IN-27 also reduces the expression of PD-L1 in BGC-823 and MFC cells. LSD1-IN-27 can enhance T cell immune response in gastric cancer .
    LSD1-IN-27
  • HY-155580
    MAO A/HSP90-IN-2

    		Monoamine Oxidase HSP Cancer
    MAO A/HSP90-IN-2 (compound 4-C) is a dual inhibitor of HSP90and MAO A with the IC50 values of 0.016 and 4.58 μM, respectively. MAO A/HSP90-IN-2 increases HSP70 expression and reduces HER2 and phospho-Akt expression, and decreases IFN-γ induced PD-L1 expression in GL26 cells. MAO A/HSP90-IN-2 inhibits the growth of Temozolomide (HY-17364) -sensitive and -resistant GBM cells, colon cancer, leukemia, non-small cell lung and other cancers, and has potential to inhibit tumor immune escape [1].
    MAO A/HSP90-IN-2
  • HY-146293
    HDAC6/HSP90-IN-1

    		HDAC HSP Cancer
    HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice .
    HDAC6/HSP90-IN-1
  • HY-16141R
    Cilengitide (Standard)

    EMD 121974 (Standard)

    		 Integrin Autophagy Apoptosis STAT PD-1/PD-L1 Reference Standards Cancer
    Cilengitide (Standard) is the analytical standard of Cilengitide. This product is intended for research and analytical applications. Cilengitide (EMD 121974) is a BBB-permeable integrins antagonist with IC50s of 0.61 nM (ανβ3), 8.4 nM (ανβ5) and 14.9 nM (α5β1), respectively. Cilengitide inhibits the binding of ανβ3 and ανβ5 to Vitronectin with IC50s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers .
    Cilengitide (Standard)
  • HY-175369
    PI3Kδ-IN-25

    		PI3K Akt PD-1/PD-L1 Interleukin Related CD3 Inflammation/Immunology Cancer
    PI3Kδ-IN-25 is an orally active selective PI3Kδ inhibitor (IC50 = 2.1 nM). PI3Kδ-IN-25 has IC50s of 272, 285, and 1171 nM for PI3Kα, PI3Kγ, and PI3Kβ, respectively. PI3Kδ-IN-25 inhibits AKT Ser473 phosphorylation, suppresses Treg cell proliferation, and downregulates PD-L1 expression in B16F10 cells. PI3Kδ-IN-25 exhibits anticancer effects in B16F10 melanoma and Lewis lung cancer mouse models by reducing tumor-infiltrating Treg cells and enhancing immune responses. PI3Kδ-IN-25 is potentially useful in the study of melanoma, lung cancer, and other cancers .
    PI3Kδ-IN-25
  • HY-149213
    LSD1/TLK1-IN-1

    J54; J3-54

    		 Histone Demethylase TLK Cancer
    LSD1/TLK1-IN-1 is an orally active LSD1, TLK1, TLK2, TTK inhibitor with an LSD1 IC50 of 0.247 μM. LSD1/TLK1-IN-1 suppresses phosphorylation of Nek1 at T141 and Rad9 at S328, abrogates the TLK1>Nek1>ATR>Chk1 axis, protects H3K4me1/2 from demethylation, and does not affect LSD2, MAO-A, or MAO-B. LSD1/TLK1-IN-1 induces apoptosis, bypasses cell-cycle arrest, suppresses tumor growth, acts as a weak D4R antagonist, downregulates PD-L1 expression, enhances T-cell killing response, inhibits gastric cancer cell proliferation, shows minimal toxicity, and has no significant effect on normal prostate cells. LSD1/TLK1-IN-1 can be used for the research of prostate cancer and gastric cancer .
    LSD1/TLK1-IN-1
  • HY-162463
    Ir-UA

    		PD-1/PD-L1 Cancer
    Ir-UA is an usnic acid-derived iridium(III) complex that enhances PD-L1 expression and converts "cold tumors" into "hot tumors." Ir-UA stimulates PD-L1 expression by explicitly regulating the PD-L1 transcription factor .
    Ir-UA
  • HY-155577
    MAO A/HSP90-IN-1

    		Monoamine Oxidase HSP Cancer
    MAO A/HSP90-IN-1 (4-b) is a MAO A/HSP90 dual inhibitor with IC50 value of 1.77 μM and 0.019 μM in Glioblastoma (GBM) GL26 cells and HSP90α, respectively. MAO A/HSP90-IN-1 (4-b) can inhibit MAO A activity, HSP90 binding and the expression of HER2 and phospho-Akt to inhibit the growth of GBM, they also reduce PD-L1 expression, which inhibits T cell activation. MAO A/HSP90-IN-1 (4-b) have potential to inhibit tumor immune escape. MAO A/HSP90-IN-1 (4-b) can be used for brain tumor-related diseases research .
    MAO A/HSP90-IN-1
  • HY-162399
    PD-L1-IN-6

    		PD-1/PD-L1 STAT Inflammation/Immunology
    PD-L1-IN-6 (Compound 16) is an orally active inhibitor for PD-L1 expression in neutrophil by targeting STAT3 with KD of 90.5 nmol/L. PD-L1-IN-6 promotes neutrophil-mediated antifungal immunoresponse .
    PD-L1-IN-6
  • HY-172167
    PD-L1/HDAC-IN-1

    		PD-1/PD-L1 HDAC Inflammation/Immunology Cancer
    PD-L1/HDAC-IN-1 (Compound 14) is the inhibitor for PD-L1 and HDAC that inhibits PD-1/PD-L1 interaction, HDAC2 and HDAC3 with IC50 of 88.10, 27.98 and 14.47 nM, respectively. PD-L1/HDAC-IN-1 exhibits slight cytotoxicity in MCF-7 (IC50=19.34 μM). PD-L1/HDAC-IN-1 upregulates the expression of PD-L1 and CXCL10, promoting anti-tumour immune response by recruiting T-cell infiltration into TME .
    PD-L1/HDAC-IN-1
  • HY-157569
    PD1-PDL1-IN 2

    		PD-1/PD-L1 Cancer
    PD1-PDL1-IN 2 (ZE132) is a potent and selective PD-1/PD-L1 inhibitor, which has robust anti-tumour activity in vivo. PD1-PDL1-IN 2 promotes cytotoxic T-cell tumour infiltration and induces IL-2 expression. In addition, PD1-PDL1-IN 2 elicits strong inhibitory effects on the mRNA expression of TGF-β .
    PD1-PDL1-IN 2
  • HY-159101
    EP26

    		EGFR PD-1/PD-L1 Cancer
    EP26 is a potent and orally active EGFR and PD-L1 inhibitor with IC50 values of 48.6 nM, 1.77 µM, respectively. EP26 decreased the protein expression of p-EGFR. EP26 induces cell cycle arrest at G0/G1 phase. EP26 has the potential for the research of glioblastoma .
    EP26

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