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PD model

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-136927
    MSA-2
    Maximum Cited Publications
    30 Publications Verification

    		 STING Inflammation/Immunology Cancer
    MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models .
    MSA-2
  • HY-N0120A
    Polydatin
    Maximum Cited Publications
    14 Publications Verification

    Piceid

    		 Autophagy Apoptosis Mitophagy Inflammation/Immunology Cancer
    Polydatin (Piceid), extracted from the roots of Reynoutria japonica, a widely used traditional Chinese remedies, possesses anti-inflammatory activity in several experimental models. Polydatin (Piceid) inhibits G6PD and induces oxidative and ER stresses.
    Polydatin
  • HY-16468
    Squalamine
    1 Publications Verification

    MSI-1256; ENT-01 free acid

    		 Bacterial HBV FAK Dengue Virus Infection Neurological Disease Cancer
    Squalamine (MSI-1256) is an aminosterol compound with broad-spectrum antiviral activity. Squalamine makes cells less conducive to certain viral replication by altering the electrostatic interactions in the inner membrane of host cells. Squalamine also has antibacterial and antitumor activities. Squalamine has broad-spectrum antibacterial activity against Gram-negative and Gram-positive bacteria, fungi and protozoa. Squalamine inhibits tumor-related angiogenesis and the growth of human breast cancer cells. Squalamine restores the function of enteric nervous system in Parkinson ,s disease mouse models .
    Squalamine
  • HY-164992
    Trastuzumab vedotin
    2 Publications Verification

    MRG002; Trastuzumab MMAE

    		 Antibody-Drug Conjugates (ADCs) EGFR Microtubule/Tubulin Cancer
    Trastuzumab vedotin (MRG002; Trastuzumab MMAE) is an antibody-drug conjugate and cytotoxin targeting HER2, with a Kd of 7.50E-11 M for human HER2. After binding to HER2, Trastuzumab vedotin undergoes internalization and lysosomal trafficking, delivering a cytotoxic payload to HER2-expressing cells and inducing tumor regression in in vivo xenograft models with HER2-expressing tumors. The anti-tumor activity of Trastuzumab vedotin is enhanced when used in combination with anti-PD-1 antibodies, and it exhibits preclinical anti-tumor activity in drug-resistant breast cancer, gastric cancer, and urothelial carcinoma PDX models. Trastuzumab vedotin has low antibody-dependent cellular cytotoxicity activity and can be used in studies related to HER2-positive breast cancer, HER2-positive gastric cancer, and unresectable locally advanced or metastatic HER2-positive urothelial carcinoma .
    Trastuzumab vedotin
  • HY-145746
    Sulfo-Cy5 azide

    		Fluorescent Dye PD-1/PD-L1 Inflammation/Immunology Cancer
    Sulfo-Cy5 azide is a near-infrared fluorescent probe with favorable click chemistry reactivity. Sulfo-Cy5 azide enables fluorescence imaging, tissue and cellular visualization of PD-L1 in tumors, and site-specific modification of anti-PD-L1 antibodies. Sulfo-Cy5 azide has been employed for RNA labeling and imaging. Sulfo-Cy5 azide can be conjugated to targeting agents for fluorescence imaging in atherosclerosis and breast cancer models (Ex/Em = 645/670 nm) .
    Sulfo-Cy5 azide
  • HY-69019
    7-Nitroindazole
    1 Publications Verification

    		 NO Synthase Cardiovascular Disease Neurological Disease
    7-Nitroindazole is a selective and BBB-penetrable inhibitor of nitric oxide synthase (NOS) (IC50 = 0.47 μM in mouse cerebellum). 7-Nitroindazole does not affect blood pressure or endothelium-dependent relaxation while inhibiting nNOS in experimental animals. 7-Nitroindazole has anti-injurious and neuroprotective properties, and can be studied in research for neurological diseases such as Parkinson’s disease .
    7-Nitroindazole
  • HY-101449
    Adaptaquin
    2 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species (ROS) Neurological Disease Metabolic Disease Inflammation/Immunology
    Adaptaquin is a BBB-penetrable HIF-PHDs inhibitor. Adaptaquin has anti-inflammatory and neuroprotective effects. Adaptaquin can effectively inhibit lipid peroxidation, maintain mitochondrial function, and reduce neuronal death. Adaptaquin can be used in the research of nervous system diseases such as Parkinson's disease .
    Adaptaquin
  • HY-148794
    Risvodetinib

    IkT-148009

    		 c-Met/HGFR Bcr-Abl Neurological Disease Cancer
    Risvodetinib (IkT-148009) is an orally active, selective and brain-penetrant protein tyrosine kinase inhibitor, displaying excellent target efficacy against c-Abl1, c-Abl2/Arg with IC50 values of 33 nM, 14 nM, respectively. Risvodetinib suppresses c-Abl activation and substantially protects dopaminergic neurons from degeneration in mouse models of both inherited and sporadic Parkinson’s disease (PD), which is promising for research in the field of PD .
    Risvodetinib
  • HY-131183
    PROTAC PD-1/PD-L1 degrader-1

    		PROTACs PD-1/PD-L1 Inflammation/Immunology
    PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner .
    PROTAC PD-1/PD-L1 degrader-1
  • HY-118144
    PD166326

    		Src Bcr-Abl p38 MAPK Cancer
    PD166326 is an orally active tyrosine kinase inhibitor with a IC50 of 8 nM against abl tyrosine kinase and a IC50 of 6 nM against src tyrosine kinase. PD166326 blocks Bcr/Abl kinase activity. PD166326 inhibits Bcr/Abl-dependent proliferation and cell cycle progression. PD166326 reduces peripheral blood granulocytosis, alleviates splenomegaly and prolongs survival in a mouse model of chronic myeloid leukemia. PD166326 can be used in research related to chronic myeloid leukemia .
    PD166326
  • HY-P10439
    CVRARTR

    		PD-1/PD-L1 Inflammation/Immunology Cancer
    CVRARTR is a programmed cell death ligand-1 (PD-L1) antagonist with a KD of 281 nM. CVRARTR induces the internalization of PD-L1 and downregulates PD-L1 on the cell surface. CVRARTR restores cytokine secretion and T cell proliferation in cell CT26. CVRARTR exhibits antitumor efficacy against in CT26 homograft mouse model. CVRARTR can be used in melanoma research .
    CVRARTR
  • HY-N7526
    Naphthazarin
    1 Publications Verification

    DHNQ; 5,8-Dihydroxy-1,4-naphthoquinone

    		 Apoptosis Autophagy PI3K Akt Neurological Disease Inflammation/Immunology Cancer
    Naphthazarin (DHNQ) is a microtubule depolymerizing agent. Naphthazarin can improve motor function and reduce neuroinflammation in mouse models of Parkinson's disease. Naphthazarin can induce tumor cell apoptosis, autophagy, and cell cycle arrest. Naphthazarin can also induce erythrocyte apoptosis. Naphthazarin can be used in the research of tumors and neurodegenerative diseases .
    Naphthazarin
  • HY-P99943
    Erfonrilimab

    KN-046

    		 PD-1/PD-L1 CTLA-4 Cancer
    Erfonrilimab (KN-046) is a monoclonal antibody targeting PD-L1/CTLA-4. Erfonrilimab blocks the PD-L1 and CTLA-4 pathways, thereby regulating T cell function. Erfonrilimab enhances the secretion of IL-2 in superantigen-stimulated peripheral blood mononuclear cells. Erfonrilimab inhibits tumor growth in xenograft and double gene knock-in mouse models. Erfonrilimab can be used in research related to a variety of advanced solid tumors, including non-small cell lung cancer and nasopharyngeal carcinoma.
    Erfonrilimab
  • HY-138742
    HPK1-IN-7

    		MAP4K Cancer
    HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1 .
    HPK1-IN-7
  • HY-132192
    PD-1/PD-L1-IN-9
    2 Publications Verification

    		 PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model .
    PD-1/PD-L1-IN-9
  • HY-107428
    PD-166793

    		MMP Cardiovascular Disease
    PD-166793 is a potent, selective, orally active and wide-broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure .
    PD-166793
  • HY-112411
    PD 174265

    		EGFR ERK PDGFR FGFR Neurological Disease Inflammation/Immunology
    PD 174265 is a highly selective, reversible EGFR/ErbB2 tyrosine kinase inhibitor (IC50=0.45 nM) and cell differentiation inducer. By blocking receptor autophosphorylation and the downstream ERK signaling pathway (with an IC50 of 0.45 μM for full-length ERK), PD 174265 effectively inhibits tumor growth and exhibits antitumor activity without obvious toxicity in in vivo models. PD 174265 drives oligodendrocyte precursor cells to switch from a proliferative state to a differentiated state, significantly upregulates the expression of myelin proteins such as CNP, PLP and MBP, and induces neurite branching. PD 174265 shows no inhibitory effect on other kinases including insulin, PDGF and basic FGF receptors, and serves as a crucial tool molecule for investigating the treatment of human epidermoid carcinoma and the mechanism of myelin repair in multiple sclerosis .
    PD 174265
  • HY-P99916
    Emirodatamab

    AMG-427

    		 FLT3 CD3 TNF Receptor Inflammation/Immunology Cancer
    Emirodatamab (AMG-427) is a bispecific T-cell engager (BiTE). Emirodatamab simultaneously binds FLT3 on the surface of acute myeloid leukemia (AML) cells and CD3 on the surface of T cells, thereby precisely recruiting immune effector cells to tumor sites. Emirodatamab potently induces T cell activation, secretion of proinflammatory cytokines (such as IFNγ, TNFα), and specific cytotoxicity, effectively lysing FLT3-positive tumor cells and inhibiting their growth. Emirodatamab not only significantly prolongs survival in mouse xenograft models and eliminates diseased cells in primates, but also exhibits a synergistic enhancement effect when combined with PD-1 blockade therapy. Emirodatamab is used in studies of acute myeloid leukemia, especially relapsed or refractory cases .
    Emirodatamab
  • HY-159838
    Enrupatinib

    EI‐1071

    		 c-Fms Amyloid-β Neurological Disease Cancer
    Enrupatinib (EI‐1071) is a potent, orally active, CNS-penetrant and selective CSF1R inhibitor. Enrupatinib inhibits macrophage proliferation and osteoclast differentiation in vitro. Enrupatinib preserves microglia distal to Aβ plaques. Enrupatinib mitigates Alzheimer's disease (AD)-related pathologies by reducing neuroinflammation, preserving neuronal integrity, lowering disease-associated microglia gene expression, and enhancing cognitive function in 5xFAD and J20 mouse models. Enrupatinib reduces tumor-associated macrophage infiltration and enhances antitumor activity of anti-PD-1 antibody in murine colorectal cancer and breast cancer models. Enrupatinib can be used for the research of AD, colorectal cancer, and breast cancer .
    Enrupatinib
  • HY-P99744
    Modakafusp alfa

    TAK-573

    		 CD38 Inflammation/Immunology Cancer
    Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice .
    Modakafusp alfa
  • HY-145774
    PD-1/PD-L1-IN-23

    		PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-23 is a potent and orally active inhibitor of PD-1/PD-L1. PD-1/PD-L1-IN-23 is an ester proagent of L7. L7 is a benzo[c][1,2,5]oxadiazole derivative and biologically evaluated as inhibitors of PD-L1. PD-1/PD-L1-IN-23 displays significant antitumor effects in tumor models of syngeneic and PD-L1 humanized mice .
    PD-1/PD-L1-IN-23
  • HY-P99922
    Encelimab

    		LAG-3 Cancer
    Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) .
    Encelimab
  • HY-144088
    ZYF0033
    2 Publications Verification

    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-120553
    B-355252
    1 Publications Verification

    		 Apoptosis Neurological Disease
    B355252, a phenoxy thiophene sulfonamide small molecule, is a potent NGF receptor agonist. B355252 potentiates NGF-induced neurite outgrowth. B355252 protects ischemic neurons from neuronal loss by attenuating DNA damage, reducing ROS production and the LDH level, and preventing neuronal apoptosis. B355252 has anti-apoptotic effects in glutamate-induced excitotoxicity, as well as in a murine hippocampal cell line (HT22) model of Parkinson disease (PD) .
    B-355252
  • HY-155457
    Enpp-1-IN-19

    		Phosphodiesterase (PDE) STING Cancer
    Enpp-1-IN-19 (compound 29f) is an orally active ENPP1 inhibitor that inhibits cGAMP hydrolysis by ENPP1 (IC50=68 nM). Enpp-1-IN-19 increases anti-PD-L1 responses and inhibits tumor growth in CT26 syngeneic models. Enpp-1-IN-19 also enhances STING-mediated type I interferon responses, induces immune memory, and prevents tumor recurrence .
    Enpp-1-IN-19
  • HY-125287
    (Rac)-Minzasolmin

    (Rac)-UCB0599; NPT200-11

    		 α-synuclein Neurological Disease
    (Rac)-Minzasolmin ((Rac)-UCB0599; NPT200-11) is a blood-brain barrier penetrated alpha-synuclein (ASYN) misfolding inhibitor. (Rac)-Minzasolmin acts on the early stage of ASYN aggregation process, by replacing the membrane-bound oligomers ASYN, allowing them to revert to the monomeric form, while preventing pathological aggregation. (Rac)-Minzasolmin effectively improves the ASYN deposition in the retina and the neuro-pathological indicators in two α-synuclein transgenic mouse models. (Rac)-Minzasolmin can be used for the studies of Parkinson's disease (PD) and dementia with Lewy bodies (DLB) .
    (Rac)-Minzasolmin
  • HY-100032
    PD 117519

    CI947

    		 Adenosine Receptor Neurological Disease
    PD 117519 (CI947) is an A2A adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models .
    PD 117519
  • HY-171572
    Atezolizumab-MMAE

    		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-174830
    GJ19

    		PD-1/PD-L1 Cancer
    GJ19 is a PD-L1 inhibitor with an IC50 of 32.06 nM. GJ19 can effectively bind to human/murine PD-L1 protein with Kd values of 171 and 290 nM, respectively. GJ19 concentration-dependently promotes HepG2 cell mortality in a co-culture model of HepG2/hPD-L1 and Jurkat T/hPD-1 cells. GJ19 effectively suppresses tumor growth in a B16-F10 melanoma mouse model. GJ19 can be used for the study of tumor immunotherapy .
    GJ19
  • HY-N0120AR
    Polydatin (Standard)
    Maximum Cited Publications
    14 Publications Verification

    Piceid (Standard)

    		 Reference Standards Autophagy Apoptosis Mitophagy Inflammation/Immunology Cancer
    Polydatin (Standard) is the analytical standard of Polydatin. This product is intended for research and analytical applications. Polydatin (Piceid), extracted from the roots of Reynoutria japonica, a widely used traditional Chinese remedies, possesses anti-inflammatory activity in several experimental models. Polydatin (Piceid) inhibits G6PD and induces oxidative and ER stresses.
    Polydatin (Standard)
  • HY-172930
    PVTX-405

    		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-159643
    NDI-101150

    		MAP4K IFNAR Interleukin Related Inflammation/Immunology Cancer
    NDI-101150 is an orally active, potent and selective hematopoietic progenitor cell kinase 1 (HPK1) inhibitor with an IC50 of 0.7 nM. NDI-101150 blocks HPK1-mediated negative regulation of immune receptor signaling, inhibits immunosuppression of T cell activation, enhances antigen-specific antibody production and augments B-cell activation. NDI-101150 inhibits tumor growth in syngeneic tumor models, establishes durable antitumor immune memory, and synergizes with anti-PD1 to enhance exhausted T cell activity and drive tumor regressions. NDI-101150 can be used for the research of cancer, such as breast cancer and colon cancer .
    NDI-101150
  • 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-164576
    NCS-MP-NODA

    NODA-Bz-SCN

    		 Radionuclide-Drug Conjugates (RDCs) Cancer
    NCS-MP-NODA (NODA-Bz-SCN) is a bifunctional chelator that can be used to bind to the labeled peptide DK222 with high specificity for PD-L1. The corresponding fluorinated radioactive is synthesized by the aluminum fluoride method, and NCS-MP-NODA targets DK222 to obtain the radioactive analog [18/19F]DK222. [18F]DK222 can quantify PD-L1 in vivo via PET tracking in xenograft models of multiple cancer types.
    NCS-MP-NODA
  • HY-120419
    PF9601N

    		Monoamine Oxidase Neurological Disease
    PF9601N, an monoamine oxidase B (MAO-B) inhibitor, possesses neuroprotective properties in several in vitro and in vivo models of Parkinson's disease (PD). PF9601N can be used for the research of neurodegenerative diseases mediated by excitotoxicity . PF9601N is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PF9601N
  • HY-149667
    BMS-332

    		DGK Cancer
    BMS-332 is a dual DGKα/ζ lipid kinase inhibitor, with IC50s of 5 and 1 nM against DGKα and DGKζ, respectively. BMS-332 enhances the antigen-specific T cell response. BMS-332 reduces the viral load in the liver and spleen when combined with anti-PD-1 in chronic infection models. BMS-332 can be used for the study of T cell immune checkpoint strategy .
    BMS-332
  • HY-145239
    PD-1/PD-L1-IN-13

    		PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-13 (Compound 43) is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC50 value of 10.2 nM. PD-1/PD-L1-IN-13 promots CD8 + T cell activation and delays the tumor growth in the Hepa1-6 syngeneic mouse model .
    PD-1/PD-L1-IN-13
  • HY-132192A
    PD-1/PD-L1-IN-9 hydrochloride
    2 Publications Verification

    		 PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-9 hydrochloride is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 hydrochloride can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 hydrochloride also exhibits significant in vivo antitumor activity in a CT26 mouse model .
    PD-1/PD-L1-IN-9 hydrochloride
  • 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-P990778
    Xirestomig

    ATG-101

    		 TNF Receptor PD-1/PD-L1 Inflammation/Immunology Cancer
    Xirestomig (ATG-101) is a tetravalent "2+2″ PD-L1×4-1BB bispecific antibody. Xirestomig binds PD-L1 and 4-1BB concurrently, with a greater affinity for PD-L1, and potently activated 4-1BB+ T cells when cross-linked with PD-L1-positive cells. Xirestomig activates exhausted T cells upon PD-L1 binding. Xirestomig displays potent antitumor activity in numerous in vivo tumor models, including those resistant or refractory to immune checkpoint inhibitors (ICIs) .
    Xirestomig
  • HY-155126
    LZWL02003

    		Reactive Oxygen Species (ROS) Neurological Disease
    LZWL02003 is an anti-neuroinflammatory agent. LZWL02003 has protective effect on MPP +-induced neuronal damage, and reduces the expression of ROS. LZWL02003 improves cognition, memory, learning, and athletic ability in a Rotenone (HY-B1756)-induced PD rat model. LZWL02003 can be used for research of neurodegenerative disease .
    LZWL02003
  • 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-178716
    PTPN2/1-IN-4

    		Phosphatase IFNAR STAT JAK Cancer
    PTPN2/1-IN-4 (Compound WS35) is an orally active, dual-functional inhibitor of PTPN1 and PTPN2 with IC50s of 12.8 and 5.8 nM for PTPN1 and PTPN2, respectively. PTPN2/1-IN-4 modulates the IFNγ-JAK-STAT signaling pathway and significantly augments CD8+ T-cell tumor infiltration. PTPN2/1-IN-4 has potent anticancer activity, robustly inhibiting tumor growth both as a monotherapy and in combination with an anti-PD-1 antibody in B16-OVA syngeneic mouse models .
    PTPN2/1-IN-4
  • HY-105362
    PD 155080

    		Endothelin Receptor Cardiovascular Disease
    PD 155080 is a selective endothelin A receptor (ETA receptor) antagonist. PD 155080 reduces coronary resistance in the isolated rat heart model. PD 155080 improves myocardial systolic function and diastolic function in the ischemia/reperfusion model. PD 155080 can be used for the study of cardiovascular diseases .
    PD 155080
  • HY-105365
    PD 175069

    		Calcium Channel Neurological Disease
    PD 175069 is a potent and selective N-type calcium channel antagonist with an IC50 of 0.32 μM. PD 175069 is efficacious in an audiogenic seizure model using DBA/2 mice. PD 175069 can be used for research on neurological conditions such as neuropathic pain and stroke .
    PD 175069
  • HY-162972
    PROTAC PD-L1 degrader-2

    		PROTACs PD-1/PD-L1 Cancer
    PROTAC PD-L1 degrader-2 (Compound 9i) is a PROTAC degrader for PD-L1, that inhibits PD-L1 with an IC50 of 197.4 nM and exhibits an affinity with PD-L1 with a Kd of 301 nM. PROTAC PD-L1 degrader-2 promotes the internalization of PD-L1 on the cell membrane, and induces PD-L1 degradation via the synergistic effect of the proteasome and lysosomal pathways. PROTAC PD-L1 degrader-2 can activate the immune system, and exhibits antitumor efficacy in MC38 C57BL/6 mouse model .
    PROTAC PD-L1 degrader-2
  • 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-151066
    BMS-1233

    		PD-1/PD-L1 Cancer
    BMS-1233 is an orally active inhibitor for programmed cell death-ligand 1 (PD-L1), with IC50 of 14.5 nM. BMS-1233 promotes cell death of HepG2 in a Jurkat T cell and HepG2 cell co-culture model, exhibits antitumor activity against melanoma in mouse model .
    BMS-1233
  • HY-175236
    SF-9-2

    		PD-1/PD-L1 Apoptosis ERK JNK Cadherin p38 MAPK GSK-3 IFNAR Caspase Bcl-2 Family Cancer
    SF-9-2 is a PD-L1/PD-1 binding inhibitor (IC50 = 24.9 nM). SF-9-2 inhibits epithelial-mesenchymal transition, migration, invasion, and proliferation of SK-N-SH cells, and also induces apoptosis and cell cycle arrest. SF-9-2 blocks PD-L1-induced SK-N-SH cell growth through the MAPK signaling pathway. SF-9-2 restores GSK-3β activity and enhances PD-L1 degradation through the ubiquitin-proteasome pathway. SF-9-2 inhibits tumor growth in the SK-N-SH NOG mouse model without significant toxicity. SF-9-2 also acts as an immune checkpoint inhibitor, blocking PD-L1 to restore T cell function. SF-9-2 can be used in neuroblastoma research .
    SF-9-2
  • HY-19500
    SC-75416

    		COX Others
    SC-75416 is a selective cyclooxygenase-2 inhibitor. Its pharmacokinetic/pharmacodynamic (PK/PD) model was used for development and clinical trial simulation to design a study protocol to verify its analgesic effect in a post-oral surgery pain model. The simulation results showed that 360 mg of SC-75416 may provide better pain relief than 400 mg of ibuprofen. The actual clinical trial results confirmed this hypothesis, and 360 mg of SC-75416 was indeed superior to 400 mg of ibuprofen in pain relief. The PK/PD model of SC-75416 showed good predictive performance and successfully predicted its clinical effect. These research results show that SC-75416, as a new selective COX-2 inhibitor, has potential clinical application value in the management of post-oral surgery pain.
    SC-75416

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