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Catalog No.
Product Name
Application
Product Information
Citations
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IL-1/β-transferase Inhibitor
Pentenocin A is an inhibitor of IL-1β-transferase, also known as interleukin-1 converting enzyme (ICE). This compound displays weak inhibitory activity against the processing of pro-inflammatory cytokine IL-1β, making it useful for studies related to inflammation and immune response. Its applications can extend to research exploring pathways involved in cytokine maturation and signaling, contributing to the understanding of various inflammatory diseases. -
IL-2 Inhibitor
Digitoxigenin-3-O-β-D-quinovoside is a potent interleukin-2 (IL-2) inhibitor, exhibiting an IC50 value of 52 nM. This cardiac glycoside is derived from the plant Elaeodendron australe var. integrifolium. It is useful in research applications focused on immune modulation and the investigation of IL-2 signaling pathways, providing valuable insights into related therapeutic areas. -
IL-1β Inhibitor
Shegansu B is a potent inhibitor of IL-1β, demonstrating significant inhibition of IL-1β expression in LPS-induced THP-1 cells, achieving an inhibition rate of 64.74%. This compound exhibits noteworthy anti-inflammatory activity, making it a valuable tool for research applications focused on inflammation and immune response modulation. Its selective targeting of IL-1β positions Shegansu B as an important reagent for studies aimed at understanding inflammatory processes and potential therapeutic interventions. -
CD45/CD148 Tyrosine Phosphatase Inhibitor
RWJ-60475 is a selective inhibitor of CD45 and CD148 tyrosine phosphatases, exhibiting an IC50 of 3.3 μM. By inhibiting these phosphatases, RWJ-60475 disrupts the phagocytic activity of macrophages, effectively blocking the invasion of Legionella pneumophila and the subsequent transport of effector proteins. This compound is valuable for research applications focused on anti-infection strategies that target host cellular factors. -
CXCR4/STAT3 Inhibitor
Minecoside is a potent inhibitor of the CXCR4 receptor and STAT3 signaling pathway. It demonstrates significant anticancer and anti-inflammatory activities by downregulating CXCR4 expression and suppressing STAT3 activation, which leads to the inhibition of CXCL12-induced cellular invasion. Minecoside has been shown to effectively hinder cancer metastasis and enhance apoptosis, making it a valuable tool for research in cancer biology and therapeutic development. -
mPGES-2 Inhibitor
SZ0232 is a selective inhibitor of microsomal prostaglandin E synthase-2 (mPGES-2), effectively reducing the production of prostaglandin E2 (PGE2) and downregulating the PGE2-EP4 signaling pathway. This inhibition disrupts the β-catenin/STAT3/c-Myc proliferation cascade, demonstrating significant effects on the abnormal proliferation of cyst epithelial cells. SZ0232 serves as a valuable tool for investigating autosomal dominant polycystic kidney disease (ADPKD) in both in vitro and in vivo research models. -
mTOR Inhibitor
Rapamycin-d3 is a deuterium-labeled analog of Rapamycin, a highly potent and selective inhibitor of the mechanistic target of rapamycin (mTOR), exhibiting an IC50 of 0.1 nM in HEK293 cells. It functions by binding to FKBP12, leading to allosteric inhibition of mTORC1. This compound is notable for its roles in autophagy activation and immunosuppression, making it valuable for various research applications including cancer biology, metabolic disorders, and studies of cellular growth and proliferation. -
COX-2 Inhibitor
COX-2-IN-43 is a selective COX-2 inhibitor with an IC50 of 0.247 μM for COX-2 and 0.983 μM for COX-1. This compound demonstrates significant biological activity by inhibiting cancer cell proliferation and colonization while inducing apoptosis. It is valuable for research applications targeting inflammatory diseases and cancer therapeutics. -
iNOS Inhibitor
iNOS-IN-5 (Compound BN-4) is a potent inhibitor of inducible nitric oxide synthase (iNOS) with an IC50 of 0.1707 μM, effectively reducing nitric oxide levels in LPS-induced RAW264.7 cells. This compound demonstrates protective properties against hypoxic injury by decreasing reactive oxygen species (ROS) and lactate dehydrogenase expression, exhibiting significant anti-necrosis and anti-apoptosis effects. Additionally, iNOS-IN-5 has shown neuroprotective activity and protective effects against cerebral ischemia in SD rat models, while also being capable of penetrating the blood-brain barrier. -
STING Inhibitor
STING-IN-16 is a potent inhibitor of the Stimulator of Interferon Genes (STING) pathway, exhibiting IC50 values of 44 nM in human cells and 32 nM in murine cells. It effectively inhibits STING activation, leading to restoration of renal mitochondrial function, reduction of reactive oxygen species (ROS) production, and decreased cell apoptosis. With demonstrated anti-inflammatory efficacy in vivo, STING-IN-16 is valuable for research focused on autoimmune and autoinflammatory diseases. -
CD73 Inhibitor
BK50164 is a selective inhibitor of CD73, exhibiting an IC50 of 13.089 μM. It demonstrates a binding affinity to CD99 with a KD of 1.5 μM. This compound exhibits antiproliferative effects and is capable of inducing apoptosis, as well as causing cell cycle arrest in the Sub-G1 phase. BK50164 is valuable in studies focused on tumor immunology and metabolic regulation. -
Arginase Inhibitor
Nor-NOHA is a selective and reversible inhibitor of arginase, primarily targeting the regulation of arginine metabolism. It has been shown to induce apoptosis in cells expressing arginase 2 under hypoxic conditions and exhibits anti-leukemic activity. This compound is valuable for research applications related to endothelial dysfunction, immunosuppression, and metabolic studies. -
CXCR-4 Inhibitor
SSB-2548 is a selective inhibitor of the chemokine receptor CXCR-4. It has demonstrated significant efficacy in inhibiting the proliferation and migration of acute myeloid leukemia cells, while also promoting apoptosis. Its favorable gastrointestinal absorption profile makes SSB-2548 a valuable tool for investigating the underlying mechanisms of leukemia and exploring potential therapeutic interventions. -
COX Inhibitor
Metamizole hemimagnesium is a cyclooxygenase (COX) inhibitor with anti-inflammatory and antioxidant properties. This compound effectively reduces body temperature and has been shown to decrease levels of C-reactive protein (CRP) and interleukin 6 (IL-6). Metamizole hemimagnesium also inhibits cell proliferation and promotes apoptosis. It is utilized in research applications focused on inflammation and fever modulation. -
Nucleoside Reverse Transcriptase Inhibitor
Stavudine sodium is a nucleoside reverse transcriptase inhibitor (NRTI) primarily utilized for its efficacy against HIV-1 and HIV-2. This compound demonstrates the ability to inhibit mitochondrial DNA replication, reduce NLRP3 inflammasome activation, and modulate the autophagy of Amyloid-β, contributing to its therapeutic potential. Additionally, Stavudine sodium is associated with inducing apoptosis in targeted cells, making it a valuable tool in HIV research and related cellular studies. -
PD-1/PD-L Complex Inhibitor
BMS-202 hydrochloride is a potent inhibitor of the PD-1/PD-L1 complex, exhibiting an IC50 of 18 nM and a KD of 8 μM. This nonpeptidic molecule selectively binds to PD-L1, effectively blocking the interaction between human PD-1 and PD-L1. BMS-202 hydrochloride demonstrates significant antitumor activity, making it a valuable tool for research in immunotherapy and cancer biology. -
COX Inhibitor
Ketorolac hydrochloride is a non-steroidal anti-inflammatory drug (NSAID) that acts as a nonselective inhibitor of cyclooxygenase (COX), with IC50 values of 20 nM for COX-1 and 120 nM for COX-2. It is utilized in the study of various ophthalmic conditions, including allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Additionally, Ketorolac hydrochloride functions as a DDX3 inhibitor, making it relevant for cancer research applications. -
Neddylation Inhibitor
Keap1-Nrf2-IN-4 is a potent neddylation inhibitor that targets the Keap1-Nrf2 pathway. It exhibits significant anti-proliferative activity against MGC-803 gastric cancer cells, with an IC50 value of 2.55 µM. Additionally, Keap1-Nrf2-IN-4 effectively inhibits cell migration and induces apoptosis in these cancer cells, contributing to tumor growth suppression while exhibiting minimal toxicity. This compound is valuable for research into cancer therapies and the regulation of oxidative stress responses. -
COX Inhibitor
Meloxicam sodium is a selective cyclooxygenase (COX) inhibitor, primarily targeting COX-2 with an IC50 of 0.49 μM while exhibiting a higher IC50 of 36.6 μM for COX-1. This non-steroidal anti-inflammatory agent is capable of crossing the blood-brain barrier, making it suitable for research applications involving central nervous system inflammation and pain management. Meloxicam sodium is widely utilized in studies assessing the efficacy of anti-inflammatory therapies. -
COX-1/2 Inhibitor
Taraxerol acetate is an inhibitor of COX-1 and COX-2, exhibiting IC50 values of 116.3 μM and 94.7 μM, respectively. This compound demonstrates notable anticancer properties and has been shown to induce apoptosis in cancer cells. Taraxerol acetate is valuable for research applications focusing on inflammation, pain relief, and cancer treatment mechanisms. -
TLR9 Inhibitor
ODN 20844 is a TLR9 inhibitor designed to disrupt Toll-like receptor-mediated immune responses. As a guanine-modified inhibitory oligonucleotide, it specifically targets TLR7 and TLR9, leading to a reduction in immune cell activation. This compound is useful for research applications focused on modulating immune pathways and studying immune-related diseases. The sequence of ODN 20844 is 5'-TCCTGGCGc7GGGAAGT-3'. -
TLR7/TLR8 Inhibitor
BMS905 is a potent dual inhibitor of Toll-like receptors 7 and 8, exhibiting IC50 values of 0.7 nM and 3.2 nM, respectively. This compound effectively inhibits IL-6 production induced by TLR7 or TLR8 activation in both human and mouse whole blood. BMS905 serves as a valuable tool for investigating the role of these receptors in autoimmune diseases, particularly lupus. -
TLR Inhibitor
ODN 24991, a guanine-modified inhibitory oligonucleotide, functions as an inhibitor of Toll-like receptors TLR3, TLR7, and TLR9. By disrupting TLR-mediated immune cell signaling, ODN 24991 serves as a valuable tool for investigating immune responses. The compound is particularly useful in research aimed at understanding the role of these TLRs in inflammation and immune regulation. ODN 24991 sequence: 5'-C-C-T-G-G-C-c7rGm-G-G-G-3'. -
TLR4/NF-κB Inhibitor
TLR4/NF-κB-IN-1 is a selective inhibitor of the TLR4/NF-κB signaling pathway, demonstrating significant anti-inflammatory properties. This compound exhibits the ability to penetrate the blood-brain barrier, making it suitable for studies involving neuroinflammation. In murine models, TLR4/NF-κB-IN-1 effectively reduces acute neuroinflammation induced by lipopolysaccharides (LPS) while downregulating the expression of TLR4, phosphorylated NF-κB, and phosphorylated IκB-α proteins, providing a valuable tool for researching neuroinflammatory processes and their therapeutic modulation. -
TLR4 Inhibitor
M62812 is a selective toll-like receptor 4 (TLR4) inhibitor that attenuates endothelial and leukocyte activation. By inhibiting TLR4 signaling, M62812 effectively diminishes LPS-induced coagulation and inflammatory responses, offering protective effects against lethal septic shock in murine models. This reagent serves as a valuable tool for research focused on the mechanisms of sepsis and related inflammatory disorders. -
TLR4/MyD88/NF-κB Inhibitor
SjDX5-271 is a small peptide inhibitor targeting the TLR4/MyD88/NF-κB signaling pathway. It is known to induce cell polarization and mitigate hepatic inflammation, demonstrating protective effects against liver ischemia-reperfusion injury in mouse models. This compound is valuable for research in immunology and liver-related inflammation studies. -
TLR9 Inhibitor
ODN 21158 is a selective inhibitor of Toll-like receptors 3 (TLR3) and 9 (TLR9). It effectively reduces interferon-alpha (IFN-α) secretion in a dose-dependent manner without exhibiting cytotoxic effects. This reagent is valuable for research applications involving immune modulation and the study of innate immune responses. -
TLR3 inhibitor
SMU-CX1 is a selective TLR3 inhibitor with an IC50 of 0.11 μM, demonstrating effective inhibition across various influenza A virus subtypes, with IC50 values ranging from 0.14 to 0.33 μM. Additionally, SMU-CX1 shows antiviral activity against SARS-CoV-2, targeting viral PB2 and NP proteins with an IC50 of 0.43 μM. Furthermore, SMU-CX1 modulates the inflammatory response in host cells by inhibiting key factors such as IFN-β, IP-10, and CCL-5, making it a valuable tool for research in virology and innate immune response. -
TLR4 Inhibitor
Stepharine is a natural alkaloid that functions as a toll-like receptor 4 (TLR4) inhibitor by directly interacting with the TLR4/MD2 complex. This compound exhibits significant biological activities, including anti-aging, anti-viral, and anti-hypertensive effects. It is of value in research applications focused on immune modulation and the treatment of inflammatory diseases. -
TLR7/TLR9 Inhibitor
ODN 24888 is a guanine-modified inhibitory oligonucleotide (INH-ODN) that specifically targets TLR7 and TLR9 signaling pathways. It effectively inhibits interferon-alpha (IFN-α) secretion and NF-κB activation, while also reducing interleukin-6 (IL-6) release. ODN 24888 is valuable for studying immune and inflammatory responses and can be utilized as a vaccine adjuvant in various research applications. -
TLR Inhibitor
TIC10g is a dual inhibitor of toll-like receptors 7 and 9 (TLR7 and TLR9). It effectively decreases TNF-α release in mouse macrophages and human B lymphocytes, with IC50 values of 14.5 μM and 6.5 μM for TLR7, and 7.69 μM and 11.5 μM for TLR9, respectively. TIC10g also inhibits the activation of NF-κB and MAPK pathways, demonstrating potential as an anti-inflammatory agent in conditions such as systemic lupus erythematosus and rheumatoid arthritis. -
Pan-TLR Inhibitor
TSI-13-57 is a pan-toll-like receptor (TLR) inhibitor that effectively targets TLR9, TLR7, TLR2, and TLR4 with IC50 values of 2.7 μM, 6.03 μM, 7.37 μM, and 6.38 μM, respectively. It functions by inhibiting the homodimerization of the TIR domains within the MyD88 pathway, thereby modulating immune responses. TSI-13-57 has been shown to significantly reduce systemic inflammatory responses in LPS-induced murine models, making it a valuable tool for research in inflammation and immune signaling pathways. -
TLR4 Signaling Inhibitor
NCI126224 is a TLR4 signaling inhibitor that modulates immune responses by suppressing lipopolysaccharide (LPS)-induced production of key inflammatory mediators, including NF-κB, TNF-α, IL-1β, and nitric oxide. This compound demonstrates biological activity in the low nanomolar to low micromolar range, making it a valuable tool for research into inflammatory diseases and their mechanisms. Its ability to interfere with TLR4 signaling pathways positions NCI126224 as a significant reagent for exploring potential therapeutic strategies in inflammation-related studies. -
Toll-like Receptor (TLR) Inhibitor
Cavrotolimod is a Toll-like Receptor 9 (TLR9) agonist that enhances immune responses through its structure as a spherical nucleic acid (SNA) modified with type B CpG oligonucleotides. This compound plays a crucial role in oncology research by stimulating the immune system, potentially leading to improved anti-tumor activity. Its application in cancer immunotherapy positions Cavrotolimod as a valuable research tool for understanding immune mechanisms and developing novel therapeutic strategies. -
TLR4/NF-kB/MAPK Inhibitor
TLR4/NF-κB/MAPK-IN-1 is an inhibitor targeting the TLR4/NF-κB/MAPK signaling pathways. It exhibits significant anti-neuroinflammatory activity by suppressing the activation of these pathways, leading to reduced inflammatory responses. This compound is particularly useful for research applications focusing on neuroinflammation and related neurodegenerative diseases. -
TLR4/NF-κB Inhibitor
Ligusticum cycloprolactam is a potent TLR4/NF-κB inhibitor with significant anti-inflammatory properties. It has been shown to alleviate renal injury by effectively disrupting the TLR4/NF-κB signaling pathway in both in vivo and in vitro models. In studies, Ligusticum cycloprolactam reduces serum uric acid levels, diminishes tubular damage, and decreases inflammatory infiltration and interstitial collagen deposition, leading to improved renal function. This compound serves as a valuable reagent for research into hyperuricemic nephropathy. -
TLR Inhibitor
AN-3485 hydrochloride is a benzoxaborole analogue that acts as an antagonist of the Toll-like receptor (TLR) pathway. This compound effectively inhibits TLR-mediated secretion of inflammatory cytokines, demonstrating significant anti-inflammatory properties. Additionally, AN-3485 hydrochloride exhibits potential anti-tumor activity, making it a valuable reagent for research applications focused on inflammation and cancer biology. -
TLR7/8 Inhibitor
KBD4466 is a potent inhibitor of Toll-like receptors 7 and 8 (TLR7/8), demonstrating IC50 values of 0.9 nM and 2.8 nM, respectively. This compound effectively reduces the expression of inflammatory cytokines such as IL-6 and IFN-α. KBD4466 has shown promise in improving disease progression and survival in the BXSB/MpJ mouse model of Systemic Lupus Erythematosus (SLE), making it a valuable tool for research in autoimmune diseases. -
TLR7 Inhibitor
TLR7-IN-1 is a selective inhibitor of Toll-like receptor 7 (TLR7) with an EC50 value of 0.001 µM. This compound effectively modulates TLR7 signaling pathways, making it valuable for research in autoimmune diseases and antiviral responses. Its potency and specificity offer potential for studying the role of TLR7 in various biological contexts. -
TLR4 Inhibitor
M62812 free base acts as a toll-like receptor 4 (TLR4) signal transduction inhibitor. It is effective in suppressing activation of endothelial cells and leukocytes and has demonstrated the ability to prevent lethal septic shock in murine models. This compound is valuable for research applications related to sepsis and its underlying mechanisms. -
Toll-like Receptor (TLR) Inhibitor
Tilsotolimod sodium is a synthetic agonist of Toll-like receptor 9 (TLR9), primarily involved in modulating immune responses. It has exhibited significant antitumor activity in preclinical models, making it a valuable reagent for cancer research. Tilsotolimod’s ability to enhance immune system engagement with tumor cells is particularly relevant for studies focused on immunotherapy and tumor immunology. -
Stx2a/TLR4 Interaction Inhibitor
NAB815 is a selective inhibitor of the Stx2a/TLR4 interaction, exhibiting a Kd of 0.01 μM. It effectively inhibits neutrophil/Stx2a interactions with an IC50 of 0.057 μg/mL and decreases the formation of Stx2-containing extracellular vesicles from leukocytes and platelets, mitigating their toxic effects in both cellular and animal models. Additionally, NAB815 significantly reduces bacterial loads in the kidneys, urine, and bladders of Escherichia coli-infected mice, making it a valuable tool for investigating hemolytic uremic syndrome (HUS). -
TLR9 Inhibitor
TLR9-IN-2 is a selective inhibitor of Toll-like receptor 9 (TLR9), with an IC50 of 25 nM, demonstrating significant selectivity over TLR7 and TLR8 (1400 nM and > 50,000 nM, respectively). This compound is valuable for investigating the role of TLR9 in various biological contexts, particularly in studies related to fibrosis, autoimmune conditions, and inflammatory diseases. Its specificity makes it an important tool for elucidating TLR9-mediated signaling pathways and potential therapeutic interventions. -
Toll-like Receptor (TLR) Inhibitor
Tilsotolimod is a synthetic agonist of Toll-like receptor 9 (TLR9) involved in modulating immune responses. It has exhibited significant antitumor activity in preclinical models, making it a valuable reagent for cancer immunotherapy research. This compound is utilized in studies focused on enhancing the immune system's ability to target and eradicate tumors. -
TLR4/JNK/NF-κB Inhibitor
TLR4-IN-2 is an inhibitor targeting TLR4, JNK, and NF-κB pathways. It demonstrates anti-inflammatory properties by reducing nitric oxide production in LPS-stimulated RAW264.7 cells, with an IC50 of 23.2 µM. By inhibiting TLR4 expression and diminishing JNK phosphorylation, TLR4-IN-2 effectively suppresses NF-κB activation and the transcription of inflammation-related genes, leading to lower levels of iNOS, COX-2, and various inflammatory mediators. This compound shows potential for investigating therapeutic strategies in inflammatory diseases such as rheumatoid arthritis and other inflammatory disorders. -
TLR Inhibitor
IMG-2005 is a Toll-like receptor (TLR) inhibitor that disrupts TLR signaling by mimicking the Toll/interleukin-1 receptor (TIR) domain of MyD88. This mechanism prevents the homodimerization of MyD88, mitigating damage to tracheal epithelial cells and reducing the onset of pulmonary immune diseases. IMG-2005 is valuable for research into TLR-related pathways and the development of therapeutic strategies for respiratory inflammation. -
NLRP3 Inflammasome Inhibitor
(rac)-NDT-19795 is a potent inhibitor of the NLRP3 inflammasome, exhibiting an IC50 value of 66 nM in peripheral blood mononuclear cells (PBMCs) and 4.7 μM in Western blot assays. This racemic compound is derived from NT-0796 and possesses carboxylic acid activity, facilitating intracellular conversion. (rac)-NDT-19795 is valuable for investigating the mechanisms of inflammation and neurological disorders. -
NLRP3/AIM2 Inhibitor
NLRP3/AIM2-IN-3 is a selective inhibitor targeting the NLRP3 and AIM2 inflammasomes. This compound exhibits potent inhibitory activity against pyroptosis in THP-1 macrophages induced by LPS and nigericin, demonstrating an IC50 value of 0.077 ± 0.008 μM. NLRP3/AIM2-IN-3 disrupts the interactions between NLRP3 or AIM2 and the adaptor protein ASC, thereby preventing ASC oligomerization and subsequent inflammasome activation. This reagent is suitable for studies investigating inflammasome-mediated processes and pyroptotic cell death. -
NLRP1/3 Inhibitor
ADS032 is a sulfonylurea compound that functions as an inhibitor of the NLRP1 and NLRP3 inflammasomes. This compound effectively reduces the secretion of pro-inflammatory cytokines and inhibits the oligomerization of ASC, thereby exhibiting anti-inflammatory properties. ADS032 can be utilized in various research applications related to inflammatory diseases, making it a valuable tool for studying inflammasome-mediated pathways. -
NLRP3 Inhibitor
Selnoflast (RO7486967) is a highly selective and reversible small molecule inhibitor of the NLRP3 inflammasome. It effectively inhibits the release of IL-1β in response to NLRP3 activation in human monocyte-derived macrophages associated with Alzheimer's disease. Selnoflast is a valuable reagent for research into Alzheimer's disease and systemic inflammatory conditions, including ulcerative colitis and chronic obstructive pulmonary disease.
