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ADAM inhibitors block the a disintegrin and metalloproteinase (ADAM) sheddases ADAM10 and ADAM17. These zinc-dependent enzymes cut membrane proteins close to the cell surface and release their ectodomains. ADAM17, also called tumor necrosis factor-α converting enzyme (TACE), releases soluble tumor necrosis factor-α (TNF-α) from its membrane-bound precursor. It also sheds ligands of the epidermal growth factor receptor (EGFR) and several cytokine receptors. ADAM10 cleaves Notch receptors after ligand binding, a step that Notch signaling requires during development. GI 254023X is listed as an ADAM10 inhibitor, and KP-457 as an ADAM17 inhibitor. Hydroxamate compounds such as TAPI-2 and TMI-1 inhibit TACE together with related matrix metalloproteinases, which are listed under MMP.
GI 254023X is a selective ADAM10 metalloprotease inhibitor; displays over 100-fold higher potency at ADAM10 compared to ADAM17.
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.
Synonyms: TNF Protease Inhibitor 0
(S,S)-TAPI-0 is an inhibitor of TACE (IC50 = 50-100 nM) as well as other matrix and membrane metalloproteases
Synonyms: TNF Protease Inhibitor 2
TAPI-2 is an inhibitor of TACE, ADAMs, ACE secretase, and other MMPs (metalloproteinases). TAPI-2 blocks release of DCC7, APP, TNFα, L-selectin, NOTCH, TGFα, IL-6R9, erbB2/HER2, and ACE. This inhibitor has been used in tissue culture.
Synonyms: TAPI1
TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors.
TMI-1 is a novel orally active dual inhibitor of ADAM17 (TACE) and MMP.
JG26 is a potent ADAM inhibitor with IC50 values of 12 nM for ADAM8, 1.9 nM for ADAM17, and 150 nM for ADAM10. It also inhibits MMP-12 with an IC50 of 9.4 nM. JG26 suppresses AngII-induced EGFR transactivation and ERK activation, upregulates ACE2 expression, inhibits CD23 shedding, and reduces SARS-CoV-2 infection. Additionally, JG26 demonstrates anti-metastatic effects in colorectal cancer and holds research potential in Hodgkin lymphoma and vascular diseases.
IK-862 is a selective inhibitor of Tumor Necrosis Factor-alpha Converting Enzyme (TACE), which plays a critical role in the release of pro-inflammatory cytokines. As a TACE inhibitor, IK-862 exhibits key biological activity by reducing tumor progression and inflammation, making it valuable in cancer and inflammatory disease research. This compound can be utilized in studies focused on understanding the role of TACE in various pathological processes and therapeutic interventions targeting cytokine regulation.
BMS-566394 is a potent inhibitor of tumor necrosis factor-α (TNF-α) converting enzyme (TACE). By inhibiting TACE, it effectively reduces the production of TNF-α, leading to decreased inflammation and a potential therapeutic approach for immune-mediated disorders. This compound is valuable for research focused on inflammatory and autoimmune diseases.
Synonyms: DPC 333 formate
BMS-561392 formate is a potent inhibitor of TNF alpha-converting enzyme (TACE), also known as ADAM17. This compound selectively blocks TACE activity, resulting in the modulation of inflammatory processes. BMS-561392 formate is particularly useful for investigating the role of TACE in inflammatory bowel disease and other related inflammatory conditions.
TAPI-0 is a potent inhibitor of TACE (TNF-α converting enzyme, ADAM17) with an IC50 of 100 nM, effectively modulating TNF-α processing. This compound also exhibits inhibitory activity against matrix metalloproteinases (MMPs), making it valuable for studying inflammatory processes and the role of TNF-α in various disease states. TAPI-0 is relevant for research applications involving cancer, autoimmune diseases, and tissue remodeling.
INCB3619 is a selective and orally active inhibitor of ADAM metalloproteinases, demonstrating an IC50 of 22 nM for ADAM10 and 14 nM for ADAM17. This compound exhibits notable anti-tumor activity, making it a valuable tool for cancer research. INCB3619 is applicable in studies exploring the roles of ADAM proteases in tumor progression and metastasis.
ADAM17-IN-1 is a selective inhibitor of ADAM17, targeting its enzymatic activity to modulate immune responses. This compound effectively reduces the metabolic activity of dendritic cells, impairing their antigen-presenting function and diminishing allergen-specific Th2 cell polarization, leading to decreased secretion of Th2 cytokines (IL-4, IL-5, IL-13). ADAM17-IN-1 exhibits protective efficacy against house dust mite (HDM)-induced type 2/eosinophilic airway inflammation in murine models, making it valuable for research into type 2-high allergic asthma.
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ADAMTS-5-IN-2 is an inhibitor of ADAMTS-5 and botulinum neurotoxin A light chain (BoNT/A LC), with IC50 values of 9.6 μM and 0.71 μM respectively. This compound serves as a valuable tool in research concerning osteoarthritis, botulism, and other related pathologies. Its ability to selectively inhibit these targets makes it suitable for investigating therapeutic strategies in diseases associated with extracellular matrix degradation and neurotoxic disorders.
Synonyms: (R)-TNF Protease Inhibitor 2
(R)-TAPI-2 is a potent inhibitor targeting matrix metalloproteinases (MMPs), tumor necrosis factor alpha-converting enzyme (TACE), and a disintegrin and metalloproteinase (ADAM), exhibiting an IC50 value of 20 μM for MMP activity. This compound is utilized in research focused on inflammation, cancer progression, and cell signaling due to its ability to modulate proteolytic processes. Additionally, (R)-TAPI-2 has demonstrated efficacy in preventing viral entry, specifically in the context of SARS-CoV infections, making it valuable for virology studies.
TACE-IN-1 is a selective inhibitor of tumor necrosis factor-α converting enzyme (TACE) that exhibits oral bioactivity. This compound effectively reduces TNF-α production in human whole blood, making it a valuable tool for studying inflammatory processes. TACE-IN-1 is stable in its neutral form and has applications in anti-inflammatory research, aiding in the exploration of therapeutic interventions for inflammatory diseases.
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Synonyms: GLPG1972; S201086
Aldumastat is a selective, orally active inhibitor of ADAMTS-5, exhibiting an IC50 value of 19 nM and demonstrating eight-fold selectivity over ADAMTS-4 with an IC50 of 156 nM. This compound displays significant anticatabolic activity, making it a valuable tool for researching osteoarthritis and related degenerative conditions. Its specificity and potency provide a robust platform for understanding the role of ADAMTS-5 in matrix degradation and cartilage pathology.
ADAMTS-5 Inhibitor is a potent inhibitor of ADAMTS-5 (aggrecanase-2), exhibiting an IC50 of 1.1 µM. This compound demonstrates greater than 40-fold selectivity over ADAMTS-4 (aggrecanase-1). It is utilized in research applications focused on cartilage degradation, osteoarthritis, and the role of aggrecanases in extracellular matrix remodeling.
ADAMTS-5-IN-3 is a potent inhibitor of the metalloproteinases ADAMTS-5 and ADAMTS-4, exhibiting IC50 values of 8 nM and 12 nM, respectively. This compound is relevant in the study of diseases characterized by cartilage degradation and disruptions in cartilage homeostasis, such as osteoarthritis and rheumatoid arthritis. Researchers can utilize ADAMTS-5-IN-3 to investigate potential therapeutic strategies aimed at modulating the activity of these enzymes in various pathological conditions.
Synonyms: PF-5212371
AGG-523 is a selective, reversible inhibitor of the aggrecanases ADAMTS4 and ADAMTS5, demonstrating IC50 values of
TAPI-1 is a specific inhibitor of TACE (ADAM17) and also exhibits inhibitory activity against metalloproteinases (MMPs). By blocking the shedding of various cell surface proteins, TAPI-1 plays a critical role in modulating cellular signaling and processes. It is widely utilized in research applications related to inflammation, cancer, and tissue remodeling, providing valuable insights into the roles of proteolytic enzymes in disease mechanisms.
Synonyms: INCB007839; INCB7839
Aderbasib is a selective inhibitor of ADAM10 and ADAM17, designed for targeted intervention in cancer research. This orally bioavailable hydroxamate compound displays significant antineoplastic activity, making it suitable for investigating various malignancies, including diffuse large B-cell non-Hodgkin lymphoma, HER2+ breast cancer, and gliomas. Its potent inhibitory effects enable detailed studies into the role of ADAM proteases in tumor biology and therapeutic strategies.
Synonyms: BK-1361
Cyclo(RLsKDK) is a potent inhibitor of the metalloproteinase ADAM8, exhibiting an IC50 value of 182 nM. This compound demonstrates significant anti-inflammatory properties and may serve as a valuable tool in the study of inflammatory diseases and cancer progression. Its selective inhibition of ADAM8 positions cyclo(RLsKDK) as a promising candidate for further research in therapeutic applications targeting these pathways.
Ro 32-7315 is a selective inhibitor of TNF-α converting enzyme (TACE), which plays a critical role in the processing of pro-inflammatory cytokine TNF-α. This compound has demonstrated significant anti-inflammatory activity, making it valuable for studying the role of TNF-α in various inflammatory diseases. Ro 32-7315 is applicable in research focused on novel therapeutic strategies for conditions such as rheumatoid arthritis, cancer, and other TNF-α-mediated pathologies.
