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Checkpoint inhibitor

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18174
    Prexasertib
    Maximum Cited Publications
    33 Publications Verification

    LY2606368

    		 Checkpoint Kinase (Chk) Apoptosis Cancer
    Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity .
    Prexasertib
  • HY-13902
    Berzosertib
    20+ Cited Publications

    VE-822; VX-970; M6620

    		 ATM/ATR Apoptosis STING Caspase Infection Metabolic Disease Cancer
    Berzosertib (VE-822) is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib blocks ATR kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .
    Berzosertib
  • HY-B0097
    Floxuridine
    10+ Cited Publications

    5-Fluorouracil 2'-deoxyriboside

    		 Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Bacterial CMV HSV Apoptosis Infection Cancer
    Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
    Floxuridine
  • HY-10992
    AZD-7762
    20+ Cited Publications

    		 Checkpoint Kinase (Chk) Cancer
    AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
    AZD-7762
  • HY-136270
    Gartisertib
    5 Publications Verification

    VX-803; M4344; ATR inhibitor 2

    		 ATM/ATR Cancer
    Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity .
    Gartisertib
  • 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-100016
    AZD0156
    10+ Cited Publications

    		 ATM/ATR Apoptosis Cancer
    AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis .
    AZD0156
  • HY-16438
    RRx-001
    15+ Cited Publications

    Nibrozetone

    		 CD47 Apoptosis Parasite Infection Inflammation/Immunology Cancer
    RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes agent resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity . RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α . RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity .
    RRx-001
  • HY-15532
    SCH900776
    10+ Cited Publications

    MK-8776

    		 Checkpoint Kinase (Chk) Cancer
    SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively .
    SCH900776
  • HY-107407
    SB-218078
    5 Publications Verification

    		 Checkpoint Kinase (Chk) CDK PKC Apoptosis Cancer
    SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest .
    SB-218078
  • HY-13946
    BML-277
    5+ Cited Publications

    Chk2 inhibitor II

    		 Checkpoint Kinase (Chk) Apoptosis Cancer
    BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM.
    BML-277
  • HY-P9986
    Tiragolumab

    MTIG-7192A; RG-6058

    		 CD28 Cancer
    Tiragolumab is an immune checkpoint inhibitor binding to the T-cell immunoglobulin and ITIM domain (TIGIT). Tiragolumab in combination with Atezolizumab (HY-P9904) and Bevacizumab (HY-P9906) has benefit in unresectable hepatocellular carcinoma. Tiragolumab can be used to study non-small cell lung cancer (NSCLC) and melanoma .
    Tiragolumab
  • HY-18174A
    Prexasertib dihydrochloride
    Maximum Cited Publications
    33 Publications Verification

    LY2606368 dihydrochloride

    		 Checkpoint Kinase (Chk) Apoptosis Cancer
    Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity .
    Prexasertib dihydrochloride
  • HY-135960
    BO-264
    1 Publications Verification

    		 FGFR Apoptosis Cancer
    BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity .
    BO-264
  • HY-102011
    BMS-1166
    5+ Cited Publications

    		 PD-1/PD-L1 Inflammation/Immunology Cancer
    BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation .
    BMS-1166
  • HY-101093
    CA-170
    2 Publications Verification

    		 PD-1/PD-L1 Inflammation/Immunology Cancer
    CA-170 is an orally delivered dual inhibitor of VISTA and PD-L1. CA-170 exhibits potent rescue of proliferation and effector functions of T cells inhibited by PD-L1/L2 and VISTA with selectivity over other immune checkpoint proteins as well as a broad panel of receptors and enzymes .
    CA-170
  • HY-P99777
    Ontorpacept
    1 Publications Verification

    TTI-621

    		 CD47 Cancer
    Ontorpacept (TTI-621) is a soluble fusion protein that consists of the human SIRPα N-terminal (1-118) linked to the Fc region of human IgG1. The N-terminal (1-118)-fragment of ontorpacept is a binding domain for CD47 which is an inhibitor of phagocytosis by macrophages. Ontorpacept is a CD47-blocking checkpoint inhibitor with antitumor activity .
    Ontorpacept
  • HY-P99032
    Monalizumab
    5 Publications Verification

    IPH2201

    		 Checkpoint Kinase (Chk) IFNAR Inflammation/Immunology Cancer
    Monalizumab (IPH2201) is an immune checkpoint inhibitor targeting Natural Killer Group 2A (NKG2A). Monalizumab, a humanized anti-NKG2A blocking mAb, increases IFN-γ production, thereby promoting NK cell effector functions. Monalizumab can be used for the research of head and neck squamous cell carcinoma (HNSCC) .
    Monalizumab
  • HY-P99166
    Vudalimab

    XMAB-20717

    		 PD-1/PD-L1 CTLA-4 Inflammation/Immunology Cancer
    Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cell activation .
    Vudalimab
  • HY-13649
    Indibulin
    1 Publications Verification

    ZIO 301; D 24851

    		 Apoptosis Microtubule/Tubulin Checkpoint Kinase (Chk) Neurological Disease Cancer
    Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis .
    Indibulin
  • HY-P99950
    Evorpacept

    ALX148

    		 CD47
    Evorpacept (ALX148) is a high-affinity CD47-blocking fusion protein with an inactive human immunoglobulin Fc region. Evorpacept binds to CD47, blocks the interaction of the CD47-SIRPα immune checkpoint, and inhibits the binding of wild-type SIRPα to CD47. Evorpacept is applicable to research related to acute myeloid leukemia .
    Evorpacept
  • HY-18175
    CCT244747
    5 Publications Verification

    		 Checkpoint Kinase (Chk) Cancer
    CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
    CCT244747
  • HY-145034
    KIF18A-IN-1
    1 Publications Verification

    		 Kinesin Cancer
    KIF18A-IN-1 is an inhibitor of the mitotic kinesin KIF18A with anti-tumor activity. KIF18A targeted inhibitors may activate mitotic checkpoints and selectively kill chromosomally unstable cancer cells .
    KIF18A-IN-1
  • HY-149874
    BMS-502
    1 Publications Verification

    		 DGK Inflammation/Immunology Cancer
    BMS-502 (Compound 22) is a potent dual inhibitor of diacylglycerol kinase (DGK) α and ζ with IC50 of 4.6 nM and 2.1 nM. BMS-502 enhanced T cell immune responses in mice. BMS-502 can be used in tumor immunity related research .
    BMS-502
  • HY-153450
    JBI-589

    		Protein Arginine Deiminase Cancer
    JBI-589 is a non-covalent PAD4 isoform-selective inhibitor with oral bioavailability. JBI-589 reduces CXCR2 expression and blocks neutrophil chemotaxis. JBI-589 reduces primary tumor and metastases, and enhances the anti-tumor effect of checkpoint inhibitors. JBI-589 can be used in cancer research .
    JBI-589
  • HY-120635
    BMS-1001 hydrochloride

    		PD-1/PD-L1 Inflammation/Immunology Cancer
    BMS-1001 is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 exhibits low-toxicity in cells. The IC50 value of BMS-1001 in a homogeneous time-resolved fluorescence (HTRF) binding assay is 2.25 nM .
    BMS-1001 hydrochloride
  • HY-18174E
    Prexasertib dimesylate
    Maximum Cited Publications
    33 Publications Verification

    LY2606368 dimesylate

    		 Checkpoint Kinase (Chk) Apoptosis Cancer
    Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity .
    Prexasertib dimesylate
  • HY-156649
    Vorbipiprant

    CR6086

    		 Prostaglandin Receptor Interleukin Related MMP PD-1/PD-L1 Cardiovascular Disease Inflammation/Immunology Cancer
    Vorbipiprant (CR6086) is an orally active EP4 receptor antagonist with high selectivity for the human EP4 receptor (Ki: 16.6 nM). Vorbipiprant has immunomodulatory, anti-inflammatory, antitumor, and anti-angiogenic activities. Vorbipiprant can inhibit the expression of multiple pro-inflammatory cytokines and the activation of immune cells, and convert "cold" tumors unresponsive to immune checkpoint inhibitors into "hot" tumors. Vorbipiprant is used in the research of diseases such as rheumatoid arthritis and colon cancer .
    Vorbipiprant
  • HY-150879
    BMS-37

    		PD-1/PD-L1 Ligands for Target Protein for PROTAC Cancer
    BMS-37 is a PD-1/PD-L1 immune checkpoint inhibitor with an IC50 towards the PD-L1/PD-1 complex in the range of 18 to 200 nM. BMS-37 shows unspecific toxicity against modified Jurkat T cells with an EC50 between 3 and 6 µM. BMS-37 can be used for the study of the PD-L1-induced exhaustion of T-cells or as PD-L1 ligand to synthesize PROTAC molecules .
    BMS-37
  • HY-100341
    M2I-1

    		Checkpoint Kinase (Chk) Others
    M2I-1 is a Mad2 inhibitor targeting the binding of Mad2 to Cdc20, an essential protein-protein interaction (PPI) within the spindle assembly checkpoint (SAC) .
    M2I-1
  • HY-112162
    BOS-172722
    2 Publications Verification

    		 Mps1 Cancer
    BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1) checkpoint with an IC50 of 11 nM and 63 nM for MPS1 (1 mM ATP) and P-MPS1, respectively. BOS-172722 also has potential for the study of various forms of breast cancer .
    BOS-172722
  • HY-10992A
    AZD-7762 hydrochloride
    20+ Cited Publications

    		 Checkpoint Kinase (Chk) Cancer
    AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
    AZD-7762 hydrochloride
  • HY-15532B
    SCH900776 (S-isomer)

    MK-8776 S-isomer

    		 Drug Isomer Cancer
    SCH900776 S-isomer is the S-isomer of SCH900776. SCH900776 is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with IC50 of 3 nM.
    SCH900776 (S-isomer)
  • HY-P99895
    Rulonilimab

    		PD-1/PD-L1 Inflammation/Immunology Cancer
    Rulonilimab is a human IgG1 monoclonal antibody against PD-1 that targets, binds and inhibits PD-1 and its downstream signalling pathways with potential immune checkpoint inhibition and anti-tumour activity .
    Rulonilimab
  • HY-18961
    PD 407824

    		Checkpoint Kinase (Chk) Wee1 Inflammation/Immunology Cancer
    PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC50s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4 .
    PD 407824
  • HY-144894
    AM-5308

    		Kinesin Microtubule/Tubulin Cancer
    AM-5308 is the inhibitor for KIF18A (IC50=47 nM) that inhibits KIF18A-mediated microtubule ATPase activity. AM-5308 activates mitotic checkpoints, regulates cell division processes, including chromosome segregation and spindle assembly. AM-5308 exhibits antitumor activity .
    AM-5308
  • HY-125018
    QM31

    SVT016426

    		 Caspase Cancer
    QM31 (SVT016426), a cytoprotective agent, is a selective inhibitor of Apaf-1. QM31 inhibits the formation of the apoptosome (IC50=7.9μM), the caspase activation complex composed by Apaf-1, cytochrome c, dATP and caspase-9. QM31 exerts mitochondrioprotective functions and interferes with the intra-S-phase DNA damage checkpoint .
    QM31
  • HY-15883
    GNE-900

    		Checkpoint Kinase (Chk) Apoptosis Cancer
    GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 μM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. Gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity .
    GNE-900
  • HY-131446
    Chk1-IN-5
    1 Publications Verification

    		 Checkpoint Kinase (Chk) Cancer
    Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model .
    Chk1-IN-5
  • HY-156871
    CAMK1D-IN-1

    		CaMK Cancer
    CAMK1D-IN-1 (compound I) is an inhibitor of CAMK1D, targeting cytotoxic T lymphocyte (CTL)-resistant tumor cells. CAMK1D impairs CTL-induced death receptor signaling and apoptosis by inhibiting caspases, making it a key and effective target for PD-L1-refractory tumors .
    CAMK1D-IN-1
  • HY-161865
    Antitumor agent-180

    		Apoptosis Cancer
    Antitumor agent-180 (Compound 13a) is an inhibitor for BUB1 mitotic checkpoint serine/threonine kinase B (BUB1B). Antitumor agent-180 inhibits the proliferation of ccRCC cell Caki-1 with IC50 of 2.047 µM. Antitumor agent-180 induces necrosis and apoptosis in Caki-1 .
    Antitumor agent-180
  • HY-B0097R
    Floxuridine (Standard)

    5-Fluorouracil 2'-deoxyriboside (Standard)

    		 Reference Standards Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Bacterial CMV HSV Apoptosis Infection Cancer
    Floxuridine (Standard) is the analytical standard of Floxuridine. This product is intended for research and analytical applications. Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
    Floxuridine (Standard)
  • HY-155798
    CHK1-IN-8

    		Checkpoint Kinase (Chk) Cancer
    CHK1-IN-8 (example 3-2) is a Chk1 inhibitor with an IC50 of <10 nM for human Chk1. CHK1-IN-8 can be used for the study of cancer .
    CHK1-IN-8
  • HY-136220
    AHR antagonist 5

    		Aryl Hydrocarbon Receptor Cancer
    AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 μΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 .
    AHR antagonist 5
  • 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-132884
    TTK inhibitor 3

    		Mps1 Cancer
    TTK inhibitor 3 is a potent and selective TTK (an essential spindle assembly checkpoint enzyme) inhibitor with an IC50 value of 3.0 nM.
    TTK inhibitor 3
  • HY-164955
    TTK/PLK1-IN-1

    		Mps1 Polo-like Kinase (PLK) Cancer
    TTK/PLK1-IN-1 (Formula I) is the inhibitor for threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1) with IC50 of 7 nM and 72 nM. TTK/PLK1-IN-1 regulates spindle assembly checkpoint (SAC), and exhibits antitumor efficacy against TNBC .
    TTK/PLK1-IN-1
  • HY-120647
    BMS-1001

    		PD-1/PD-L1 Inflammation/Immunology Cancer
    BMS-1001 is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 exhibits low-toxicity in cells. The IC50 value of BMS-1001 in a homogeneous time-resolved fluorescence (HTRF) binding assay is 2.25 nM .
    BMS-1001
  • HY-145240
    eIF4E-IN-1

    		Eukaryotic Initiation Factor (eIF) Infection Cancer
    eIF4E-IN-1 is a potent inhibitor of eIF4E. eIF4E-IN-1 inhibits immunosuppression components such as immune checkpoint proteins PD-1, PD-L1, LAG3, TIM3, and/or IDO, in order to inhibit or release immune suppression in certain diseases, such as cancer and infectious disease (extracted from patent WO2021003194A1, compound Y) .
    eIF4E-IN-1
  • HY-148305
    PD-1/PD-L1-IN-28

    		PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-28 (compound 3) is an immune checkpoint inhibitor of PD-1/PD-L1 signaling pathway (IC50=0.744 µM). PD-1/PD-L1-IN-28 shows good research potential in tumor immunity .
    PD-1/PD-L1-IN-28

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