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Catalog No.
Product Name
Application
Product Information
Citations
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CD73 Inhibitor
LY-3475070 is a potent and selective CD73 Inhibitor with IC50 of 28 nM. -
IRAK4 inhibitor
IRAK4-IN-4 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM. -
nNOS inhibitor
7-Nitroindazole, a heterocyclic compound, acts as a selective inhibitor for neuronal nitric oxide synthase showing a 10-fold selectivity for neuronal NOS. -
Primates' C3 Inhibitor
Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates' complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively.
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Complement factor C3 inhibitor
POT-4 (AL-78898A), a Compstatin derivative, is a potent inhibitor of complement factor C3 activation. POT-4 can be used for age-related macular degeneration research -
CKLF1/CCL17 inhibitor
CKLF1-C19 is the C-terminal peptide of human chemokine-like factor 1 (CKLF1). CKLF1-C19 interacts with CCR4, and inhibits chemotaxis induced by both CKLF1 and CCL17. CKLF1-C19 can suppress allergic lung inflammation via inhibiting chemotaxis mediated by CCR3 and CCR4. -
FAP Inhibitor
FAPI-4 is a potent inhibitor of fibroblast activation protein (FAP), targeting FAP with high specificity. This compound demonstrates significant potential in cancer research, particularly in improving diagnostic imaging. The use of 68Ga-FAPI-4 in PET/CT scans offers enhanced tumor-to-background contrast ratios, making it an effective tool for visualizing various types of tumors. -
Rab27a-JFC1 Inhibitor
Nexinhib20 is a selective inhibitor of the Rab27a-JFC1 interaction (IC50: 2.6 μM) and Rac-1-GTP signaling. This compound effectively inhibits neutrophil exocytosis, adhesion, and β2 integrin activation, demonstrating significant anti-inflammatory properties. Nexinhib20 is suitable for research applications focused on systemic inflammation and myocardial ischemia-reperfusion injury. -
FKBP12(F36V) Inhibitor
dTAGV-1-NEG is a diastereomer that acts as a heterobifunctional negative control for dTAGV-1, specifically targeted at FKBP12(F36V). This compound is utilized in research to study the selectivity and efficacy of FKBP12(F36V) degraders, helping to elucidate cellular mechanisms and pathways influenced by FKBP12 modulation. Its role as a control reagent makes it essential for validating experimental results in protein degradation studies. -
NO Synthase Inhibitor
L-NAME hydrochloride inhibits NOS with an IC50 of 70 μM. L-NAME is a precursor to NOS inhibitor L-NOARG which has an IC50 value of 1.4 μM. -
PDE Inhibitor
Theophylline, a potent phosphodiesterase (PDE) inhibitor, primarily targets PDE3, leading to relaxation of airway smooth muscle and enhanced bronchodilation. This compound also functions as an adenosine receptor antagonist and exhibits anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation into the nucleus. Additionally, Theophylline has been shown to induce apoptosis in certain cell types. Its applications are particularly relevant in the research of asthma and chronic obstructive pulmonary disease (COPD). -
Topoisomerase IV Inhibitor
Ciprofloxacin is a potent topoisomerase IV inhibitor that demonstrates significant antibacterial activity as a fluoroquinolone antibiotic. It induces both mitochondrial and nuclear DNA damage, leading to mitochondrial dysfunction and increased reactive oxygen species (ROS) production. Ciprofloxacin exhibits anti-proliferative properties and triggers apoptotic pathways, making it a valuable tool for research applications focused on bacterial infections, oxidative stress, and cancer biology. -
TNF Receptor Inhibitor
Muscone, a TNF receptor inhibitor, is derived from the traditional Chinese medicine musk. It effectively inhibits NF-κB signaling and NLRP3 inflammasome activation, resulting in a significant reduction of inflammatory cytokines such as IL-1β, TNF-α, and IL-6. This compound is valuable in research focused on inflammation, cardiac function restoration, and improving survival rates in various pathological conditions. -
IL-1 Inhibitor
Diacerein is a potent IL-1 inhibitor that functions by reducing the production of IL-1 converting enzyme, thereby inhibiting the activation of IL-1β and its downstream signaling pathways. This compound exhibits significant anti-inflammatory and anti-rheumatic properties, making it useful for various research applications, including studies on osteoarthritis and the management of bronchospasm and airway inflammation in asthmatic models. Diacerein is recognized as a slow-acting drug for symptomatic relief of osteoarthritis, facilitating insights into long-term therapeutic strategies. -
Bacterial Inhibitor
Lactobionic acid is a bionic acid that functions as a bacterial inhibitor, comprising gluconic acid and galactose. It exhibits potent antimicrobial and antioxidant properties, making it valuable in research related to food safety and microbiology. Lactobionic acid is effective against food-borne pathogens and has been shown to inhibit DNA repair, protein synthesis, and key metabolic pathways in methicillin-resistant Staphylococcus aureus (MRSA). Its applications extend to developing new functional products and enhancing food preservation. -
COX2 Inhibitor
Iminostilbene is a well-characterized inhibitor of COX2 (Cyclooxygenase-2) with additional activity against PKM2 (Pyruvate Kinase M2). This compound effectively reduces the expression of COX2 and iNOS, as well as the release of pro-inflammatory cytokines such as IL-1β, IL-6, TNF-α, and MCP-1 in macrophages. Its ability to mitigate macrophage-mediated inflammatory responses makes iminostilbene a valuable reagent for investigating mechanisms of inflammation regulation, cardiovascular disease, including myocardial ischemia/reperfusion injury, and immune-related disorders. -
SIK Inhibitor
GLPG3312 is a potent SIK inhibitor, demonstrating IC50 values of 2.0 nM, 0.7 nM, and 0.6 nM for SIK1, SIK2, and SIK3, respectively. It exhibits significant anti-inflammatory and immunomodulatory activities both in vitro on human primary myeloid cells and in vivo in mouse models. Due to its favorable oral bioavailability, GLPG3312 is an important reagent for research into various inflammatory and immune-related diseases. -
NLRP3 Inhibitor
Tabersonine hydrochloride is a selective NLRP3 inhibitor that targets the NACHT domain of the NLRP3 protein, effectively inhibiting its ATPase activity and oligomerization. This action prevents ASC spot formation and caspase-1 activation, leading to a reduction in pro-inflammatory cytokine release, including IL-1β. Additionally, Tabersonine hydrochloride inhibits K63-linked ubiquitination of TRAF6, interfering with NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Its applications extend to the study of NLRP3-driven inflammatory conditions, such as acute lung injury, sepsis, and peritonitis, as well as in liver cancer research, where it induces apoptosis through mitochondrial and death receptor pathways. -
Pyroptosis Inhibitor
7-Oxogedunin is a potent inhibitor of pyroptosis, acting primarily on protein kinase R (PKR). It effectively protects macrophages from cell death induced by anthrax lethal toxin and inhibits the assembly of various inflammasomes, including NLRP1 and NLRP3, as well as the activation of caspase-1 through its effects on PKR. In addition to its role in cell survival, 7-Oxogedunin exhibits growth inhibitory activity against European corn borer larvae, making it valuable for research in LT toxicity and pest control. -
NLRP3 Inhibitor
NLRP3-IN-81 is a potent inhibitor targeting the NLRP3 inflammasome, effectively preventing NLRP3-dependent pyroptosis with an EC50 of 0.029 μM in cell models using Nigericin. This compound inhibits the activation of caspase-1 and the subsequent release of IL-1β by disrupting the interaction between NLRP3 and the adaptor protein ASC, thereby inhibiting ASC oligomerization. NLRP3-IN-81 is relevant for research into pyroptosis-related conditions, including inflammatory bowel diseases and type 2 diabetes. -
NLRP3 Inhibitor
NLRP3-IN-87 is a selective, orally active inhibitor of the NLRP3 inflammasome, exhibiting a Kd value of 0.23 μM. This compound directly targets the NACHT domain of NLRP3, effectively disrupting its interactions with NEK7 and ASC, thereby inhibiting ASC oligomerization and inflammasome assembly. NLRP3-IN-87 is known to suppress caspase-1 activation and IL-1β secretion, demonstrating significant anti-inflammatory and analgesic effects. It is particularly useful for investigating the pathophysiology of gout as it reduces joint swelling, inflammation, and pain in MSU-induced acute gout models. -
NLRP3 Inflammasome Inhibitor
NP3-146 sodium is a selective inhibitor of the NLRP3 inflammasome, effectively binding to the NACHT domain of NLRP3. This compound demonstrates significant inhibition of IL-1β release, achieving an IC50 value of 0.171 μM in LPS/Nigericin-stimulated bone marrow-derived macrophages (BMDM). NP3-146 sodium modulates the levels of cleaved Caspase-1 and cleaved IL-1β in cell supernatants, making it a valuable tool for research into inflammatory diseases. -
STING Inhibitor
STING-IN-17 is a potent inhibitor of STING (Stimulator of Interferon Genes), with human STING IC50 of 29 nM and mouse STING IC50 of 15 nM. This compound effectively inhibits the phosphorylation of STING, TBK1, and IRF3, leading to a dose-dependent reduction in the mRNA expression of key inflammatory markers such as IP10, IFNB1, and ISG56. STING-IN-17 also decreases reactive oxygen species (ROS) levels and inhibits the activation of apoptosis-related proteins cleaved-PARP and caspase-3. Its potential applications make it valuable for research into inflammatory conditions, particularly acute kidney injury. -
NLRP3 Inhibitor
GDC-2394 sodium is a selective NLRP3 inhibitor that exhibits potent activity against IL-1β, with IC50 values of 0.4 μM for human IL-1β and 0.1 μM for mouse IL-1β. This compound effectively inhibits NLRP3-induced caspase-1 activity while leaving NLRC4-dependent inflammasome activation unaffected. GDC-2394 sodium is particularly relevant for research into gouty arthritis and may serve as a valuable tool in the study of inflammatory diseases linked to NLRP3 activation. -
COX Inhibitor
Aspirin lithium is a potent, orally active, irreversible inhibitor of cyclooxygenase COX-1 and COX-2, exhibiting IC50 values of 5 and 210 μg/mL, respectively. This compound promotes apoptosis and inhibits the activation of NF-κB, making it valuable for studies on inflammation and cell death. Additionally, Aspirin lithium effectively inhibits platelet prostaglandin synthetase, providing potential protective effects against coronary artery and cerebrovascular thrombosis. -
NLRP3 Inhibitor
NP3-146 is a potent inhibitor of the NLRP3 inflammasome, acting by locking the NACHT domain of NLRP3. It effectively reduces IL-1β release, with an IC50 value of 0.171 μM in LPS/Nigericin-stimulated bone marrow-derived macrophages (BMDM). Additionally, NP3-146 modulates the levels of cleaved Caspase-1 and cleaved IL-1β in cell supernatants, making it a valuable tool in the study of inflammatory diseases. -
B3GAT3 Inhibitor
TMLB-C16 is a selective B3GAT3 inhibitor with a dissociation constant (KD) of 3.962 μM. This compound effectively suppresses cell proliferation and migration while inducing cell cycle arrest and apoptosis in hepatocellular carcinoma cell lines MHCC-97H and HCCLM3, exhibiting IC50 values of 6.53 μM and 6.22 μM, respectively. In vivo studies demonstrate that TMLB-C16 inhibits tumor growth in MHCC-97H and HCCLM3 xenograft models without significant toxicity. TMLB-C16 is a valuable tool for research in hepatocellular carcinoma. -
NLRP3 Inhibitor
GDC-2394 is a selective NLRP3 inhibitor that acts orally, demonstrating inhibitory effects on IL-1β with IC50 values of 0.4 μM for human IL-1β and 0.1 μM for mouse IL-1β. This compound effectively inhibits NLRP3-induced caspase-1 activity while sparing NLRC4-dependent inflammasome activation. GDC-2394 is valuable for research into inflammatory conditions such as gouty arthritis. -
NLRP3 Inhibitor
1,2,4-Trimethoxybenzene is a selective inhibitor of the NLRP3 inflammasome, exerting its effects orally. It significantly suppresses NLRP3 activation induced by Nigericin or ATP, leading to reduced caspase-1 activation and IL-1β secretion. This compound specifically targets the NLRP3 inflammasome without influencing AIM2 inflammasome activation, and it prevents the oligomerization of ASC and the interaction between NLRP3 and ASC, thus inhibiting inflammasome assembly. 1,2,4-Trimethoxybenzene is valuable for researching autoimmune disorders such as experimental autoimmune encephalomyelitis, multiple sclerosis, and metabolic conditions like type 2 diabetes. -
IL-1β Converting Enzyme Inhibitor
SDZ 224-015 is a potent inhibitor of the interleukin-1 beta (IL-1β) converting enzyme and caspase-1, demonstrating significant inhibitory activity. This compound exhibits anti-COVID-19 properties through its interaction with the main protease (Mpro), with an IC50 value of 30 nM. SDZ 224-015 is suitable for research applications focusing on inflammation, cytokine signaling, and viral pathogenesis. -
NLRP3 Inhibitor
Tabersonine is a selective and orally active inhibitor of the NLRP3 inflammasome, targeting the NACHT domain to modulate its ATPase activity and prevent oligomerization. This mechanism effectively inhibits ASC speck formation and blocks caspase-1 activation, leading to reduced secretion of pro-inflammatory cytokines, including IL-1β. Additionally, Tabersonine interferes with K63-linked ubiquitination of TRAF6, disrupting NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. It is primarily utilized in research on NLRP3-mediated inflammatory diseases, such as acute lung injury, sepsis, and peritonitis, as well as in studies related to liver cancer. -
COX Inhibitor
(E)-Ethyl p-methoxycinnamate is a COX inhibitor that exhibits significant anti-inflammatory properties. Isolated from Kaempferia galangal, this compound demonstrates both anti-neoplastic and anti-microbial activities. In vitro studies reveal that (E)-Ethyl p-methoxycinnamate inhibits COX-1 and COX-2 with IC50 values of 1.12 μM and 0.83 μM, respectively, making it a valuable reagent for research in inflammatory and cancer-related studies. -
PCSK9 Inhibitor
Inclisiran is a double-stranded small interfering RNA (siRNA) that specifically targets and inhibits the transcription of proprotein convertase subtilisin/kexin type 9 (PCSK9). By reducing PCSK9 levels, Inclisiran effectively modulates lipid metabolism and demonstrates anti-inflammatory properties, including the inhibition of pyroptosis and a decrease in NLRP3, cleaved caspase-1, IL-1β, and IL-18. This reagent is valuable for research applications focused on hyperlipidemia and cardiovascular diseases (CVD), as it supports studies aimed at understanding lipid regulation and atherosclerosis. -
NLRP3 Inhibitor
Magnesium isoglycyrrhizinate hydrate is a potent NLRP3 inflammasome inhibitor derived from the licorice plant (Glycyrrhiza glabra). It displays significant anti-inflammatory properties, making it a valuable compound for research into inflammatory diseases. Its efficacy in attenuating conditions such as chronic obstructive pulmonary disease in preclinical rat models highlights its potential applications in respiratory research and therapeutic development. -
RAS-G12V inhibitor
RMC-5127 is an orally active, brain-penetrant, mutant-selective tri-complex inhibitor targeting RASG12V. It non-covalently binds to cyclophilin A (CypA), forming a binary complex that engages active RASG12V to create a high-affinity tri-complex, thereby sterically blocking RAS-effector interactions. RMC-5127 inhibits RAS signaling in KRASG12V-mutant cancer cells, suppressing proliferation and inducing apoptosis. It holds promise for the study of RAS-mutant cancers, including non-small cell lung cancer. -
COX-2/MMP-7/TLR4 Inhibitor
Isofraxidin is a coumarin compound derived from *Acanthopanax senticosus* that exhibits anti-invasive and anti-inflammatory properties. It inhibits MMP-7 expression and suppresses cell invasion in human hepatoma cells by reducing ERK1/2 phosphorylation. Isofraxidin also downregulates the expression of iNOS and COX-2 and inhibits the formation of the TLR4/myeloid differentiation protein-2 (MD-2) complex. -
NRP1 inhibitor
EG01377 dihydrochloride is a potent, bioavailable, and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM and IC₅₀ values of 609 nM for both NRP1-a1 and NRP1-b1 domains. It exhibits antiangiogenic, antimigratory, and antitumor activities. -
Perforin inhibitor
Perforin-IN-2 (Compound 1) is a perforin inhibitor that blocks perforin-mediated cell lysis. It has potential to reduce graft rejection in the context of allogeneic bone marrow or stem cell transplantation. -
complement factor D inhibitor
Vemircopan (ALXN2050) is an orally active inhibitor of complement factor D (FD). It is being investigated for the treatment of complement-mediated diseases, including myasthenia gravis, lupus nephritis, IgA nephropathy, and paroxysmal nocturnal hemoglobinuria (PNH). -
Complement factor D inhibitor
Pelecopan (BCX9930) is a potent, selective, and orally active inhibitor of complement factor D, with an IC₅₀ value of 14.3 nM. It targets factor D to prevent both intravascular and extravascular hemolysis in paroxysmal nocturnal hemoglobinuria (PNH) and is also applicable to other diseases mediated by the alternative complement pathway. -
complement factor D (CFD) inhibitor
Zoracopan is a selective inhibitor of complement factor D (CFD). Upon systemic administration (oral or intravenous), it preferentially accumulates in ocular tissues and is released in a sustained manner, primarily targeting the choroid–retinal pigment epithelium (C-RPE) and/or iridociliary body (I-CB).
