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ADAM17 Inhibitors

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製品番号 製品名 Target 研究分野 構造式
  • HY-16657
    TAPI-1
    Maximum Cited Publications
    15 Publications Verification

    		 MMP NF-κB Apoptosis TNF Receptor Inflammation/Immunology Cancer
    TAPI-1 is a broad-spectrum MMP inhibitor and NF-κB p65 inhibitor that targets ADAM17/TACE, ADAM10 and other proteins. TAPI-1 reduces the proteolytic cleavage of membrane-bound TNF-α, decreases TNF-α levels, inhibits NF-κB pathway activation, and downregulates profibrotic markers. TAPI-1 reduces the proportion of proinflammatory immune cells, alleviates cardiac and airway fibrosis, and improves cardiac function after myocardial infarction. Meanwhile, TAPI-1 inhibits the viability, migration and invasion of esophageal squamous cell carcinoma cells, enhances the chemosensitivity of Cisplatin (HY-17394), induces apoptosis, and shows low toxicity to normal esophageal epithelial cells. TAPI-1 can be widely used in studies related to myocardial infarction-induced heart failure, severe traumatic tracheal stenosis, esophageal squamous cell carcinoma and other conditions .
    TAPI-1
  • HY-115670
    GW280264X
    5+ Cited Publications

    		 MMP Inflammation/Immunology Cancer
    GW280264X is the mixed ADAM10/TACE (ADAM17) metalloproteinases inhibitor. GW280264X potently blocks TACE (ADAM17) and ADAM10 with IC50s of 8.0 nM and 11.5 nM, respectively . ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells .
    GW280264X
  • HY-110397
    KP-457
    3 Publications Verification

    		 MMP Cardiovascular Disease
    KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC50s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.
    KP-457
  • HY-10293
    Aderbasib
    1 Publications Verification

    INCB007839; INCB7839

    		 MMP Cancer
    Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 + breast cancer, gliomas, et al .
    Aderbasib
  • HY-101984
    N6,N6-Dimethyladenosine
    4 Publications Verification

    		 Nucleoside Antimetabolite/Analog Adenosine Receptor Akt SARS-CoV Infection Cancer
    N6,N6-Dimethyladenosine, a modified ribonucleoside, is an endogenous A3 adenosine receptor ligand. N6,N6-Dimethyladenosine is an AKT inhibitor with antitumor effects. N6, N6-Dimethyladenosine targets SARS-CoV-2 entry protein ADAM17. N6, N6-Dimethyladenosine robustly inhibits AKT signaling in a variety of non-small cell lung cancer cell lines .
    N6,N6-Dimethyladenosine
  • HY-16657A
    (S,S)-TAPI-1

    		MMP mAChR Neurological Disease Inflammation/Immunology Cancer
    (S,S)-TAPI-1 is an isomer of TAPI-1. TAPI-1 is a TACE (ADAM17) inhibitor and blocks the shedding of several cell surface proteins. TAPI-1 is also a metalloproteinase (MMP) inhibitor .
    (S,S)-TAPI-1
  • HY-101448
    TMI-1
    1 Publications Verification

    WAY-171318

    		 MMP Apoptosis Interleukin Related TNF Receptor Caspase Infection Neurological Disease Inflammation/Immunology Cancer
    TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC50 of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions .
    TMI-1
  • HY-20070
    BMS-566394

    		TNF Receptor Inflammation/Immunology
    BMS-566394 is a selective, orally active TACE (ADAM17) inhibitor. BMS-566394 inhibits LPS-induced TNF-α production in whole blood. BMS-566394 selectively inhibits TACE activity .
    BMS-566394
  • HY-123931
    ZLDI-8
    1 Publications Verification

    		 Notch Phosphatase Apoptosis Cancer
    ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM .
    ZLDI-8
  • HY-19667A
    BMS-561392 formate
    2 Publications Verification

    DPC 333 formate

    		 TNF Receptor NF-κB Apoptosis p38 MAPK Neurological Disease Inflammation/Immunology
    BMS-561392 formate (DPC 333 formate) is a selective ADAM17(TACE) inhibitor. BMS-561392 formate inhibits TNF-α secretion by regulating signaling pathways such as p44 MAPK and NF-κB. BMS-561392 formate also affects the survival of central nervous system-related cells including oligodendrocytes and microglia. BMS-561392 formate promotes microglial apoptosis, enlarges the injury area and exacerbates astrogliosis in a mouse spinal cord injury model. BMS-561392 formate can be used in research related to spinal cord injury and inflammatory diseases .
    BMS-561392 formate
  • HY-120852
    JG26
    1 Publications Verification

    		 Angiotensin-converting Enzyme (ACE) MMP EGFR ERK SARS-CoV Infection Cardiovascular Disease Cancer
    JG26 is an ADAM inhibitor with IC50 values of 12 nM, 1.9 nM, and 150 nM for ADAM8, ADAM17, and ADAM10, respectively. JG26 inhibits MMP-12 with an IC50 value of 9.4 nM. JG26 inhibits AngII (HY-13948)-induced EGFR transactivation and ERK activation. JG26 increases the expression of ACE2, inhibits the cleavage of CD23, reduces the infection of SARS-CoV-2. JG26 inhibits colorectal cancer metastasis. JG26 can be used for research on Hodgkin lymphoma and vascular diseases .
    JG26
  • HY-12636
    INCB3619

    		MMP Apoptosis Cancer
    INCB3619 is a selective and orally active ADAM inhibitor with IC50 of 22 nM and 14 nM for ADAM10 and ADAM17, respectively. INCB3619 has anti-tumor activity .
    INCB3619
  • HY-118694
    TAPI-0

    		TNF Receptor MMP Bacterial Infection Cancer
    TAPI-0 is a TACE (TNF-α converting enzyme; ADAM17) inhibitor with an IC50 of 100 nM. TAPI-0 is a MMP inhibitor and also attenuates TNF-α processing .
    TAPI-0
  • HY-19667
    BMS-561392

    DPC 333

    		 TNF Receptor NF-κB Apoptosis p38 MAPK Neurological Disease Inflammation/Immunology
    BMS-561392 (BMS-561392) is a selective ADAM17(TACE) inhibitor. BMS-561392 inhibits TNF-α secretion by regulating signaling pathways such as p44 MAPK and NF-κB. BMS-561392 also affects the survival of central nervous system-related cells including oligodendrocytes and microglia. BMS-561392 promotes microglial apoptosis, enlarges the injury area and exacerbates astrogliosis in a mouse spinal cord injury model. BMS-561392 can be used in research related to spinal cord injury and inflammatory diseases .
    BMS-561392
  • HY-175876
    ADAM17-IN-1

    		MMP Interleukin Related Inflammation/Immunology
    ADAM17-IN-1 is a selective inhibitor of ADAM17. ADAM17-IN-1 inhibits ADAM17 activity to reduce metabolic activity of dendritic cells (DCs), impair DC antigen-presenting function, suppress allergen-specific Th2 cell polarization, and reduce Th2 cytokine (IL-4, IL-5, IL-13) secretion. ADAM17-IN-1 demonstrates protective efficacy against house dust mite (HDM)-induced type 2/eosinophilic airway inflammation in mice. ADAM17-IN-1 can be used for the study of type 2-high allergic asthma .
    ADAM17-IN-1
  • HY-172394
    ZSNI-21

    		HDAC ADAMTS Apoptosis Bcl-2 Family Cyclin G-associated Kinase (GAK) Cancer
    ZSNI-21 is a ADAM17/HDAC2 inhibitor with ADAM17 IC50 0.939 μM and HDAC2 IC50 0.844 μM. ZSNI-21 regulates the expression of apoptosis-related proteins (Bax, Bcl-2) and Cyclin D1, and induces apoptosis.. ZSNI-21 can be used for the research of hepatocellular carcinoma, breast cancer, and non-small cell lung cancer .
    ZSNI-21
  • HY-101984R
    N6,N6-Dimethyladenosine (Standard)

    		Reference Standards Nucleoside Antimetabolite/Analog Adenosine Receptor Akt SARS-CoV Infection Cancer
    N6,N6-Dimethyladenosine (Standard) is the analytical standard of N6,N6-Dimethyladenosine (HY-101984). This product is intended for research and analytical applications. N6,N6-Dimethyladenosine, a modified ribonucleoside, is an endogenous A3 adenosine receptor ligand. N6,N6-Dimethyladenosine is an AKT inhibitor with antitumor effects. N6, N6-Dimethyladenosine targets SARS-CoV-2 entry protein ADAM17. N6, N6-Dimethyladenosine robustly inhibits AKT signaling in a variety of non-small cell lung cancer cell lines.
    N6,N6-Dimethyladenosine (Standard)
  • HY-110397G
    KP-457

    		MMP Cardiovascular Disease
    KP-457 (GMP) is KP-457 (HY-110397) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture.KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC50s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively .
    KP-457
  • HY-W703549
    Aderbasib-d3

    INCB007839-d3; INCB7839-d3

    		 Isotope-Labeled Compounds MMP Cancer
    Aderbasib-d3 (INCB007839-d3) is deuterium labeled Aderbasib. Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 +?breast cancer, gliomas, et al .
    Aderbasib-d3
  • HY-P992341
    D8P1C1

    		MMP Cancer
    D8P1C1 is a high-affinity ADAM17 inhibitor (with a Kd of 180 pM targeting ADAM17-ECD) that reduces the shedding and phosphorylation of EGFR ligands. D8P1C1 inhibits cancer cell proliferation in vitro and tumor growth in xenograft models. 89Zr-DFO-D8P1C1 radioimmunological PET imaging shows its substantial accumulation in ovarian tumor xenografts, serving as a platform for generating bispecific T-cell engager derivatives. D8P1C1 can be applied to research on related diseases including triple-negative breast cancer, various types of ovarian cancer, lung adenocarcinoma, glioma, and colon cancer .
    D8P1C1
  • HY-10293R
    Aderbasib (Standard)

    INCB007839 (Standard); INCB7839 (Standard)

    		 Reference Standards MMP Cancer
    Aderbasib (Standard) is the analytical standard of Aderbasib (HY-10293). This product is intended for research and analytical applications. Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2+ breast cancer, gliomas, et al .
    Aderbasib (Standard)
  • HY-101448R
    TMI-1 (Standard)

    WAY-171318 (Standard)

    		 MMP Reference Standards Apoptosis Interleukin Related TNF Receptor Caspase Infection Neurological Disease Inflammation/Immunology Cancer
    TMI-1 (Standard) is the analytical standard of TMI-1 (HY-101448). This product is intended for research and analytical applications. TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC50 of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions .
    TMI-1 (Standard)

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