Catalog No.
Product Name
Application
Product Information
Citations
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HMGB1 release inhibitor
Ethyl pyruvate is a simple derivative of the endogenous metabolite, pyruvic acid. Ethyl pyruvate is an anti-inflammatory agent. -
anti-infective agent
Tizoxanide is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide has anti-HIV-1 activities. -
NF-κB Inhibitor
Micheliolide is a sesquiterpene lactone that functions as an NF-κB inhibitor. It exhibits significant anti-cancer and anti-inflammatory properties by attenuating high glucose-induced NF-κB activation and reducing the expression of inflammatory mediators such as MCP-1, TGF-β1, and FN in mouse mesangial cells. Additionally, Micheliolide inhibits LPS-induced NF-κB activation and the PI3K/Akt/p70S6K pathways, making it a valuable tool for studying inflammatory disease models, including colitis-associated cancer and rheumatic arthritis. -
Fluorometric HDAC Substrate
Boc-Lys(Ac)-AMC is a cell-permeable fluorometric substrate for histone deacetylases (HDACs). When cleaved by HDAC enzymes, it releases a fluorescent signal with excitation and emission maxima at 355 nm and 460 nm, respectively. This compound is valuable for studying HDAC activity in various biological contexts and can be utilized in high-throughput screening assays to evaluate enzyme inhibitors. -
NF-κB Inhibitor
Aristolochic acid A is a potent NF-κB inhibitor derived from the plant extracts of Aristolochia and Asarum species. This compound effectively diminishes the activities of activator protein 1 (AP-1) and NF-κB, making it a valuable tool for studying signaling pathways related to inflammation and cancer. Additionally, Aristolochic acid A has been shown to downregulate BLCAP gene expression in human cell lines, highlighting its potential for investigating gene regulation mechanisms. -
Endogenous Metabolite
Ergothioneine is an endogenous metabolite that acts as a potent antioxidant. It functions primarily as a specific inhibitor of p38 MAPK and Akt, which are critical signaling pathways involved in cellular stress responses. Ergothioneine is utilized in research focused on neuroprotection, cell apoptosis, and oxidative stress, making it a valuable compound for investigations into cellular resilience and health. -
VUBI1 Analogue
VUBI1 analogue-1 is an analogue of VUBI1, functioning as a selective activator of the SOS1 pathway with a Kd of 44 nM. This compound is valuable for studying SOS1 activation mechanisms and provides a basis for the synthesis of (4S)-PROTAC SOS1 degrader-1. Its applications include investigations into targeted degradation and modulation of cellular pathways involving SOS1, offering insights into cellular signaling and potential therapeutic strategies. -
TBK1 Degrader
PROTAC TBK1 Degrader-2 is a targeted protein degrader designed to selectively degrade the serine/threonine kinase TANK-binding kinase 1 (TBK1) with a DC50 of 15 nM and Kd of 4.6 nM, exhibiting a maximum efficiency of 96%. Additionally, this compound also influences IkB kinase IKKε, demonstrating an IC50 of 8.7 nM, and displays a low selectivity over TBK1 with an IC50 of 1.3 nM. This reagent is suitable for investigating TBK1-related signaling pathways and potential therapeutic applications in various diseases. -
PROTAC IRAK Degrader
Zomiradomide is an orally bioavailable PROTAC degrader targeting IRAK4, with a DC50 of 6 nM, which effectively inhibits the NF-κB signaling pathway. In addition to its suppression of IRAK4, Zomiradomide functions as a molecular glue, facilitating the degradation of Ikaros with a DC50 of 1 nM and consequently activating the type I IFN signaling pathway. This dual action positions Zomiradomide as a valuable tool in research focused on immune modulation and inflammatory responses. -
STAT3/NF-κB Inhibitor
Triacetylresveratrol is an acetylated analog of Resveratrol that functions as an inhibitor of STAT3 and NF-κB signaling pathways. It effectively reduces the phosphorylation levels of STAT3 and NF-κB in a dose- and time-dependent manner in PANC-1 and BxPC-3 cancer cell lines. Its promising anticancer activity makes it a valuable tool for research in cancer biology and therapeutic development. -
HDAC Inhibitor
HC-Toxin is a potent histone deacetylase (HDAC) inhibitor with an IC50 of 30 nM. This cyclic tetrapeptide effectively induces apoptosis in tumor cells, demonstrating significant anticancer activity. Its mechanism of action makes it valuable for research in cancer therapy and the modulation of gene expression. -
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). -
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. -
Apoptosis Inducer
Sanguinarine chloride is a benzophenanthridine alkaloid that functions as an apoptosis inducer primarily through the generation of reactive oxygen species (ROS). This compound is known to activate key signaling pathways, specifically JNK and NF-κB, facilitating programmed cell death. Sanguinarine chloride is widely utilized in cancer research and studies investigating apoptotic mechanisms. -
Anti-asthmatic Agent
Verproside, a catalpol derivative iridoid glycoside isolated from the genus Pseudolysimachion, represses TNF-α -induced MUC5AC expression by inhibiting NF-κB activation via the IKK/IκB signaling cascade. Verproside has potent anti-inflammatory, antioxidant, antinociceptive and anti-asthmatic activities. Verproside has the potential for the study of chronic obstructive pulmonary disease (COPD). -
Non-steroidal Anti-inflammatory Agent
Gaultherin is an orally active non-steroidal anti-inflammatory agent that selectively inhibits key inflammatory pathways, including NF-κB, MAPK, COX-2 (IC50 = 0.35 mg/mL), LOX (IC50 = 0.56 mg/mL), and HYAL (IC50 = 28.58 μg/mL). This compound demonstrates anti-inflammatory, antipyretic, and analgesic activities, making it suitable for research into inflammation-related conditions. Additionally, Gaultherin exhibits modest direct antioxidant capacity, particularly in cell-based models, while sparing COX-1, thus reducing the likelihood of gastrointestinal side effects commonly associated with traditional non-steroidal anti-inflammatory drugs. -
NF-κB Inhibitor
Sciadopitysin is a biflavonoid that serves as a potent NF-κB inhibitor. Its primary mechanism involves the inhibition of RANKL-induced osteoclastogenesis, contributing to the prevention of bone loss. By suppressing NF-κB activation and lowering the expression levels of c-Fos and NFATc1, Sciadopitysin demonstrates significant potential for research applications focused on bone metabolism and related disorders. -
Anti-inflammatory Agent
Darutoside is an orally active diterpene compound that functions primarily as an anti-inflammatory agent. It exhibits notable analgesic properties and enhances wound healing by inhibiting COX-2 expression and the migration of inflammatory cells. Additionally, Darutoside modulates macrophage polarization towards the M2 phenotype through NF-κB pathway inhibition, thereby reducing inflammation. This compound has been shown to significantly alleviate acute gouty arthritis by regulating metabolic networks involved in inflammatory responses. -
GR Agonist
Flumethasone is a highly selective and potent glucocorticoid receptor (GR) agonist. It effectively activates GR, leading to the inhibition of nuclear factor kappa B (NF-κB) and subsequent reduction of pro-inflammatory cytokine production, such as TNF-α and IL-1β. Additionally, Flumethasone upregulates anti-inflammatory gene expression, particularly IL-10, and modulates metabolic enzyme activity, including tyrosine aminotransferase. This compound is valuable for research into inflammatory diseases, cancer, and endocrine regulation. -
Bacterial Inhibitor
Ceftiofur is a cell wall synthesis inhibitor targeting bacterial penicillin-binding proteins (PBPs). It demonstrates bactericidal activity by interfering with the peptidoglycan synthesis in bacterial cell walls, resulting in cell lysis. Additionally, Ceftiofur exhibits anti-inflammatory properties by inhibiting the activation of NF-κB and MAPKs, which decreases the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6. This makes Ceftiofur a valuable reagent in research investigating bacterial infections and inflammation processes. -
Pro-apoptotic Compound
Dracorhodin perchlorate is a pro-apoptotic compound that targets multiple signaling pathways, inhibiting PI3K/Akt and NF-κB activation. This natural product derived from Dragon's blood upregulates p53 expression, activates caspases, and induces reactive oxygen species (ROS), leading to programmed cell death. It is also known to regulate TLR4, thereby promoting wound healing and offering therapeutic potential in diabetes management. Additionally, Dracorhodin perchlorate exhibits anti-tumor activity against various cancers, including prostate, breast, and cervical cancer, making it a valuable tool for cancer research. -
Insecticide
Azadirachtin is a triterpenoid compound with potent insecticidal properties. It induces apoptosis in insect cells via the mitochondrial pathway, acting through the modulation of the Bcl-2/Bax ratio and activation of Apaf-1 and caspase-3. Additionally, Azadirachtin has demonstrated anti-inflammatory effects by inhibiting the NF-κB signaling pathway, and exhibits a range of other biological activities, including anticancer and antimalarial effects. This compound is widely utilized in research applications focused on pest control and the study of apoptotic mechanisms. -
NF-κB Inhibitor
Cardamonin is a potent NF-κB inhibitor derived from cardamom. It exerts broad biological activity by targeting key signaling pathways, including mTOR, Akt, STAT3, Wnt/β-catenin, and COX-2. This compound has demonstrated significant anticancer, anti-inflammatory, antimicrobial, and antidiabetic properties, making it valuable for various research applications in cancer biology and inflammation studies. -
GRPR Antagonist
Aurantiamide is a selective antagonist of the Gastrin-Releasing Peptide Receptor (GRPR), demonstrating significant anti-inflammatory and neuroprotective properties. It effectively mitigates inflammation and oxidative stress in renal tissues by targeting GRPR-mediated pathways, including RIPK3/MLKL signaling and NF-κB activation, thereby providing protection against acute kidney injury and promoting endothelial function. Additionally, Aurantiamide inhibits M1 microglial polarization and NLRP3 activation, showcasing efficacy in improving outcomes in Alzheimer's disease mouse models. Its notable in vivo effectiveness extends to various acute kidney injury contexts, including ischemia/reperfusion, sepsis, and hypertension models. -
RIPK1 PROTAC Degrader
LD4172 is a selective RIPK1 PROTAC degrader that exhibits a Ki of 4.8 nM. It facilitates RIPK1 protein degradation through the formation of a ternary complex with RIPK1 and VHL E3 ligase, leading to ubiquitination and proteasomal degradation. LD4172 effectively inhibits TNF-induced classical NF-κB signaling in TRAF2-deficient cells, significantly reducing IκBα phosphorylation and IL-8 production. Additionally, it promotes apoptosis and immunogenic cell death in tumor cells, enhances tumor-infiltrating lymphocyte responses, and sensitizes tumors to anti-PD1 therapy, making it a valuable chemical probe for studying RIPK1-related functions in melanoma and colon cancer research. -
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. -
Anti-inflammatory/anti-cancer/anti-viral/anti-tuberculosis Agent
4-Methoxycinnamic acid ethyl ester is a bioactive natural compound that functions primarily as an anti-inflammatory, anti-cancer, anti-viral, and anti-tuberculosis agent. It demonstrates potent anti-inflammatory activity by inhibiting cyclooxygenases (COX-1 and COX-2) and NF-κB, resulting in reduced cytokine production. Additionally, 4-Methoxycinnamic acid ethyl ester effectively inhibits tumor cell proliferation, migration, and angiogenesis through the downregulation of VEGF expression. It also exhibits significant antiviral properties against dengue virus and antimicrobial activity against Mycobacterium tuberculosis, along with notable analgesic effects in preclinical models. -
TNF-α Inhibitor
TNF-α-IN-11 is a selective inhibitor of tumor necrosis factor alpha (TNF-α) with a dissociation constant (KD) of 12.06 μM. This compound effectively binds to TNF-α, preventing the activation of downstream caspase and NF-κB signaling pathways, as well as inhibiting the phosphorylation of IκBα and the subsequent nuclear translocation of NF-κB p65. TNF-α-IN-11 is suitable for research into TNF-α-mediated autoimmune conditions and the associated inflammatory processes. -
HDAC3 Inhibitor
HDAC3-IN-2 is a potent inhibitor of histone deacetylase 3 (HDAC3), with an IC50 value of 14 nM. This pyrazinyl hydrazide compound exhibits cytotoxicity against triple-negative breast cancer cell lines, demonstrating an IC50 of 0.55 μM for 4T1 cells and 0.74 μM for MDA-MB-231 cells. In in vivo studies using tumor-bearing mouse models, HDAC3-IN-2 effectively enhances histone acetylation levels at H3K9, H3K27, and H4K12 while promoting apoptosis through increased caspase-3, caspase-7, and cytochrome c levels, alongside a decrease in proliferation markers such as Bcl-2, CD44, EGFR, and Ki-67. -
TLR4 Agonist
GlcNAc-MurNAc is a disaccharide that acts as a TLR4 agonist, exhibiting a binding affinity (Kd) of 383 μM for murine TLR4. This compound directly interacts with TLR4, subsequently activating the downstream NF-κB and IRF signaling pathways. Research indicates that GlcNAc-MurNAc ameliorates dextran sulfate sodium salt (DSS)-induced colitis in mice via a TLR4-dependent mechanism, making it a valuable tool for the investigation of inflammatory bowel disease. -
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. -
PROTAC IKKβ/NR4A1 Degrader
PROTAC IKKβ/NR4A1 degrader-1 is a novel dual-PROTAC degrader designed to selectively target and degrade IKKβ and NR4A1, utilizing the E3 ligase cereblon. This compound effectively increases the levels of caspase 3 and cleaved caspase 3 proteins, indicating a potential to induce apoptosis without affecting the necroptosis marker RIP kinase. It is a valuable tool for investigating the mechanisms underlying Acute Myeloid Leukemia (AML) and offers insights into therapeutic strategies targeting these pathways. -
RIPK2 Inhibitor
RIPK2-IN-6 is a selective inhibitor of RIPK2, effectively blocking its phosphorylation and subsequently inhibiting the NF-κB and MAPK signaling pathways. This compound exhibits significant anti-inflammatory and anti-fibrotic properties, demonstrated in Dextran sodium sulfate-induced colitis models in mice. RIPK2-IN-6 is valuable in research exploring therapeutic strategies for inflammatory and fibrotic diseases. -
Anti-inflammatory Agents
(±)-Naringenin is an orally bioavailable anti-inflammatory agent that modulates both acute and chronic inflammatory responses. Its biological activities include antioxidant, neuroprotective, hepatoprotective, and potential anti-cancer effects. (±)-Naringenin enhances vasodilation in endothelial cells via the activation of BKCa channels and demonstrates protective effects against experimental colitis by inhibiting the Toll-like receptor 4/NF-κB signaling pathway. This compound is relevant for research applications in sepsis, fulminant hepatitis, fibrosis, and cancer. -
Saturated Fatty Acid
10-Hydroxydecanoic acid (10-HDAA) is a saturated fatty acid that possesses notable anti-inflammatory properties. It exhibits a range of biological activities including anti-malarial, anti-Leishmania, and insecticidal effects, while also enhancing antigen-specific immune responses. Mechanistically, 10-HDAA inhibits NF-κB activation and interferon regulatory factor 1 (IRF-1) translation, leading to reduced levels of interleukin 6 (IL-6) and nitric oxide (NO) in inflammatory cells. Additionally, it plays a role in mitigating neuroinflammatory responses through the p53-autophagy and p53-NLRP3 pathways, making it a valuable reagent for studies in immunology and inflammation research. -
Anti-inflammatory/Anti-tumor/Anti-fungal/Neuroprotective Agent
(+)–Magnoflorine chloride is an aporphine alkaloid that exhibits potent anti-inflammatory, anti-tumor, anti-fungal, and neuroprotective properties. This compound facilitates Parkin/PINK1-mediated mitochondrial autophagy and modulates the NLRP3/Caspase-1 pathway, demonstrating essential immunomodulatory effects. Additionally, it inhibits the JNK and TLR4/NF-κB signaling pathways while activating the Sirt1/AMPK pathway to reduce neuronal oxidative stress and apoptosis. The ability to regulate miR-410-3p and suppress HMGB1/NF-κB signaling further underscores its potential in therapeutic applications across various diseases. -
Fatty Acid
10-Hydroxy-2-decenoic acid (10-HDA) is a bioactive unsaturated medium-chain fatty acid that modulates various physiological processes. It induces reactive oxygen species (ROS)-mediated apoptosis in A549 cells and inhibits VEGF-induced angiogenesis in human venous endothelial cells. Additionally, 10-HDA activates the AMPK-α signaling pathway to alleviate non-alcoholic fatty liver disease (NAFLD) and protects against bone loss by downregulating NF-κB signaling via FFAR4. It also exhibits antimicrobial properties against multiple bacteria and fungi, including Staphylococcus aureus, while demonstrating potential longevity-promoting effects in C. elegans. Furthermore, 10-HDA mitigates osteoarthritis by targeting aspartyl β-hydroxylase to inhibit chondrocyte senescence. -
Antibiotic
Acetoxycycloheximide is an antibiotic with potent antitumor properties, primarily functioning as a protein synthesis inhibitor. It effectively induces procaspase-3 activation, leading to apoptosis through the release of cytochrome c from mitochondria via the JNK signaling pathway. Additionally, acetoxycycloheximide downregulates cell surface TNF-R1 by activating the ERK and p38 MAPK pathways, thereby inhibiting TNF-α-mediated NF-κB signaling. This reagent is valuable for research related to inflammatory and immune diseases as well as cancer. -
Cathepsin B Inhibitor
(Rac)-Z-FA-FMK is a potent inhibitor of cathepsin B, exhibiting a Ki value of 1.5 μM. This compound also inhibits multiple caspases, specifically caspases 2, 3, 6, 7, and 9, with IC50 values ranging from 6.147 to 110.7 μM. Additionally, (Rac)-Z-FA-FMK demonstrates antiviral activity by inhibiting the main protease involved in SARS-CoV-2 replication with an IC50 of 11.39 μM. It further attenuates the increase in IL-1β levels induced by LPS and represses NF-κB transactivation in macrophages, making it useful for research in inflammation and viral pathogenesis. -
MDM2 Inhibitor
LQFM030 is a novel small molecule inhibitor of MDM2, primarily targeting the MDM2-p53 interaction to promote cellular apoptosis. It demonstrates concentration-dependent cytotoxicity in K562 cells with an IC50 value of 0.28 mM, inducing G0/G1 phase cell cycle arrest and enhancing Caspase activity. LQFM030 also downregulates the expression of key oncogenes and proteins, including MDM2, MDMX, p73, MYC, and NF-κB. This compound is particularly valuable in cancer research, especially in the study of leukemia. -
Epoxy Diterpene Lactone
Triptolidenol is an epoxy diterpene lactone derived from the traditional Chinese medicinal plant Tripterygium wilfordii. It exhibits anti-inflammatory and anticancer properties, significantly inhibiting tumor cell proliferation and migration. Triptolidenol induces S phase cell cycle arrest and apoptosis through the activation of the cytochrome c/caspase cascade signaling pathway, while disrupting the NF-κB/COX-2 pathway via IKKβ inhibition at ATP-binding sites. This compound is pertinent for research in chronic nephritis and various forms of kidney cancer, including clear cell renal cell carcinoma (ccRCC). -
Hsp90 Inhibitor
GUT-70 is a tricyclic coumarin that functions as a potent Hsp90 inhibitor. It activates caspases 2, 3, 8, and 9, leading to apoptosis in leukemic cells. Additionally, GUT-70 effectively inhibits HIV-1 replication in chronically infected cells by targeting the NF-κB signaling pathway. This compound is suitable for research applications involving leukemia, mantle cell lymphoma (MCL), and HIV-1 infection studies. -
Proteasome Inhibitor
TP-110 is a selective proteasome inhibitor that targets the protease-like activity of the 20S proteasome, leaving trypsin-like and peptidyl-glutamyl peptide hydrolysis activities unaffected. This compound effectively disrupts the NF-κB signaling pathway, leading to activation of caspases 3, 8, and 9, and subsequent PARP cleavage, while decreasing levels of anti-apoptotic proteins cIAP-1 and XIAP. TP-110 induces G2/M phase cell cycle arrest and promotes apoptosis in cancer cells, making it a valuable tool for researching various malignancies, including prostate cancer and multiple myeloma. -
HDAC1/6 Inhibitor
HDAC1/6-IN-3 is a potent inhibitor of histone deacetylases 1 and 6 (HDAC1 and HDAC6). It demonstrates strong inhibitory activity, with IC50 values of 1.1 nM for HDAC1 and 2.7 nM for HDAC6. This compound effectively induces cell cycle arrest in the G0/G1 phase and promotes both apoptosis and pyroptosis in HepG2 cells. Additionally, HDAC1/6-IN-3 exhibits significant antitumor effects in the HepG2 xenograft model and is valuable for research focused on various types of cancer, including liver, lung, colon, and breast cancers. -
Stable Isotope
Aspirin-d3 is a deuterium-labeled derivative of aspirin (acetylsalicylic acid) that serves as a stable isotope for research applications. This compound acts as a potent and irreversible inhibitor of cyclooxygenases COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin-d3 is utilized to investigate its apoptotic effects and to study the inhibition of NF-κB activation. Additionally, it plays a role in exploring the inhibition of platelet prostaglandin synthetase, contributing to research on coronary artery and cerebrovascular thrombosis. -
Anti-inflammatory/Anti-tumor/Anti-fungal/Neuroprotective Agent
(+)-Magnoflorine is an orally active aporphine alkaloid that serves as an anti-inflammatory, anti-tumor, anti-fungal, and neuroprotective agent. It promotes mitochondrial autophagy through Parkin/PINK1 mechanisms and inhibits the NLRP3/caspase-1 signaling pathway, demonstrating significant immunomodulatory effects. Additionally, (+)-Magnoflorine modulates JNK and TLR4/NF-κB pathways, activates Sirt1/AMPK, and alleviates oxidative stress and apoptosis in neuronal cells. Its capacity to upregulate miR-410-3p and inhibit the HMGB1/NF-κB pathway further supports its anti-tumor activity. Furthermore, (+)-Magnoflorine exhibits marked antifungal properties, making it a versatile reagent in chemical research. -
PROTAC
TD1092 is a PROTAC that functions as a pan-IAP degrader, effectively targeting cIAP1, cIAP2, and XIAP. By promoting the degradation of IAPs, TD1092 activates Caspase 3/7, leading to apoptosis in cancer cells. Additionally, it inhibits the TNFα-mediated NF-κB signaling pathway, reducing the phosphorylation of IKK, IkBα, p65, and p38. This compound is primarily used in cancer research to explore mechanisms of apoptosis and therapeutic resistance. -
CD206 Targeting Peptide
RP-182 is a synthetic immunomodulatory peptide that targets the mannose receptor CD206 on tumor-associated macrophages (TAMs), exhibiting a dissociation constant (Kd) of 8 μM. By inducing a conformational change in the CD206 receptor, RP-182 activates NF-κB signaling, promoting TNFα secretion and phagocytosis in CD206high TAMs, ultimately leading to apoptosis via caspase 8 activation. This compound is valuable for research in pancreatic cancer and melanoma, providing insights into therapeutic strategies that enhance anti-tumor immunity. -
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.
