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Catalog No.
Product Name
Application
Product Information
Citations
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TLR7/8 Inhibitor
Enpatoran hydrochloride is a dual inhibitor of Toll-like receptors 7 and 8, demonstrating potent activity with IC50 values of 11.1 nM and 24.1 nM, respectively, in HEK293 cells. This compound is selectively inactive against TLR3, TLR4, and TLR9, effectively blocking both synthetic and natural RNA ligands. Enpatoran hydrochloride exhibits favorable pharmacokinetic profile in vivo, making it a valuable tool for research into innate and adaptive autoimmunity pathways. -
TLR9 Inhibitor
TLR9-IN-1 is a potent and selective inhibitor of Toll-like receptor 9 (TLR9), exhibiting an IC50 value of 7 nM for human TLR9. This compound is valuable for studying diseases linked to aberrant immune responses, making it an important tool in immunological research and therapeutic development. Researchers can utilize TLR9-IN-1 to explore the modulation of TLR9 pathways in various inflammatory and autoimmune conditions. -
TLR7/TLR8 Inhibitor
TLR7/8-IN-1 is a potent inhibitor of Toll-like receptors 7 and 8, which play critical roles in the immune response. This compound exhibits strong potential in modulating inflammatory pathways associated with autoimmune diseases. It serves as a valuable tool for researchers investigating the therapeutic targeting of TLR7 and TLR8 in various immunological studies. -
TLR4 Inhibitor/PROTAC Linker
TLR4-IN-C34-C2-COOH is a TLR4 inhibitor that serves as a PROTAC linker. It demonstrates significant potential in the modulation of inflammatory responses, particularly in studies involving acute myocardial injury. By targeting TLR4 in enterocytes and macrophages, TLR4-IN-C34-C2-COOH effectively reduces systemic inflammation in murine models of endotoxemia and necrotizing enterocolitis, making it a valuable tool for research in inflammation-related pathways. -
Inflammatory Cell Activation Inhibitor
CI-959 is an inhibitor of inflammatory cell activation, primarily targeting signaling pathways involved in immune response modulation. It demonstrates significant anti-inflammatory and anti-allergic properties by reducing the production of reactive oxygen species in neutrophils, inhibiting neutrophil adhesion, and blocking histamine release from mast cells. CI-959 also effectively suppresses the release of inflammatory mediators, including histamine, leukotrienes, and thromboxane, from guinea pig and human lung tissues. This compound is valuable for research focused on inflammatory and allergic diseases, particularly asthma. -
pan-SIK/PAK2/3 Inhibitor
MRIA9 is an ATP-competitive inhibitor targeting pan Salt-Inducible kinases (SIK) as well as PAK2 and PAK3. It exhibits potent biological activity with IC50 values of 516 nM for SIK1, 180 nM for SIK2, and 127 nM for SIK3. MRIA9 is suitable for applications in signaling pathway research and the study of various cellular processes influenced by SIK and PAK kinases. -
GCK/MAP4K2 Inhibitor
TL4-12 is a selective inhibitor of MAP4K2 and GCK, demonstrating a dose-dependent ability to downregulate IKZF1 and BCL-6. This compound effectively inhibits cell proliferation in multiple myeloma with an IC50 of 37 nM, and it also induces apoptosis in cancerous cells. TL4-12 holds potential for overcoming resistance to immunomodulatory agents in the treatment of multiple myeloma. -
PTPN2/1 Dual Inhibitor
PTPN2/1-IN-4 is a potent dual inhibitor of PTPN1 and PTPN2, exhibiting IC50 values of 12.8 nM and 5.8 nM, respectively. This compound effectively modulates the IFNγ-JAK-STAT signaling pathway, resulting in enhanced CD8+ T-cell infiltration into tumors. PTPN2/1-IN-4 demonstrates significant anticancer activity, inhibiting tumor growth both as a standalone treatment and in combination with anti-PD-1 antibodies in B16-OVA syngeneic mouse models, making it a valuable tool for cancer research. -
JAK2 Inhibitor
Tkip is a selective inhibitor of JAK2, targeting the JAK2 autophosphorylation site. It effectively inhibits JAK2 autophosphorylation and the phosphorylation of the IFN-γ receptor subunit IFNGR-1, thereby reducing the antiviral effects of IFN-γ and downregulating MHC Class I molecule expression. Tkip is a valuable tool for investigating the IFN-γ signaling pathway and its implications in various biological processes. -
COX-2 Specific Inhibitor
SC-236 is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 10 nM and also acts as a PPARγ agonist. It effectively suppresses activator protein-1 (AP-1) through the inhibition of c-Jun NH2-terminal kinase, demonstrating significant anti-inflammatory effects. SC-236 has been shown to reduce ERK phosphorylation in murine models, highlighting its potential for investigating inflammatory pathways and therapeutic interventions. -
Arginase Inhibitor
Nor-NOHA dihydrochloride is a selective and reversible inhibitor of arginase, particularly impacting the activity of ARG2 under hypoxic conditions. This compound has been shown to induce apoptosis in ARG2-expressing cells and demonstrates anti-leukemic properties. Nor-NOHA dihydrochloride is useful for research applications related to endothelial dysfunction, immunosuppression, and metabolic studies. -
COX-2 Inhibitor
Humulone, a prenylated phloroglucinol derivative, is a selective inhibitor of cyclooxygenase-2 (COX-2). It demonstrates significant anti-inflammatory properties and serves as a positive modulator of GABAA receptors at low micromolar concentrations. Additionally, Humulone is known to inhibit bone resorption and exhibits antioxidant, anti-angiogenic, and pro-apoptotic activities, making it valuable for various research applications in inflammation and cancer studies. -
PD-L1 Inhibitor
PD-L1-IN-1 is a potent inhibitor targeting programmed cell death ligand 1 (PD-L1) with an IC50 of 115 nM. It effectively disrupts the PD-L1 and PD-1 interaction, enhancing antitumor immune responses in co-cultures of PD-L1 expressing cancer cells and peripheral blood mononuclear cells. Additionally, PD-L1-IN-1 demonstrates low cytotoxicity towards healthy cells, making it a valuable tool for immunological research and therapeutic applications in cancer treatment. -
COX-2 Inhibitor
DuP-697 is a potent, irreversible, and selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 of 10 nM for human COX-2 and 800 nM for COX-1. This compound demonstrates significant antiproliferative effects on HT29 colorectal cancer cells with an IC50 of 42.8 nM, as well as antiangiogenic and pro-apoptotic activities. By inhibiting prostaglandin synthesis, DuP-697 offers potential applications in studies related to inflammation, cancer, and fever reduction. -
Keap1-Nrf2 PPI Inhibitor
Tricetin is a competitive inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI). This compound exhibits neuroprotective effects by activating the Nrf2/HO-1 signaling pathway, which mitigates 6-OHDA-induced neurotoxicity in models of Parkinson's disease. Its mechanism of action helps to prevent apoptosis through mitochondrial pathways, making it a valuable reagent for research into neurodegenerative diseases and oxidative stress response. -
ADAM-17 Inhibitor
ZLDI-8 is an inhibitor of the metalloproteinase enzyme ADAM-17, targeting the cleavage of Notch protein. This compound effectively reduces the expression of proteins associated with pro-survival pathways and epithelial-mesenchymal transition (EMT). Additionally, ZLDI-8 functions as a competitive and irreversible inhibitor of the tyrosine phosphatase Lyp, exhibiting an IC50 of 31.6 μM and a Ki of 26.22 μM. Notably, ZLDI-8 demonstrates potent growth inhibition of MHCC97-H cells with an IC50 of 5.32 μM, making it valuable for research into cellular signaling and cancer biology. -
MALT1 Inhibitor
SGR-1505 is a small molecule inhibitor targeting MALT1, effectively modulating the NF-κB signaling pathway. This compound demonstrates significant anti-proliferative and antitumor activities by inhibiting MALT1 enzymatic activity, leading to alterations in cell cycle progression, DNA damage response, and apoptosis-related gene expression in in vivo tumor models. SGR-1505 exhibits both tumorostatic and regressive effects in activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) xenograft models. It is a valuable tool for research into activated B-cell-like diffuse large B-cell lymphoma, non-Hodgkin B-cell lymphomas, chronic lymphocytic leukemia, and mature B cell neoplasms. -
COX Inhibitor
Metamizole sodium is a potent cyclooxygenase (COX) inhibitor that exhibits significant anti-inflammatory, analgesic, and antipyretic properties. This compound not only inhibits cell proliferation but also promotes apoptosis in various cell types. Additionally, Metamizole sodium serves as a spasmolytic agent, making it a valuable tool for research applications aimed at pain relief and the study of inflammatory processes. Its multifunctional activities contribute to its utility in diverse areas of biomedical research. -
iNOS Inhibitor
1400W is a selective inhibitor of inducible nitric-oxide synthase (iNOS) with a Kd value of ≤ 7 nM, demonstrating slow and tight binding characteristics. This compound effectively inhibits iNOS induction in microglial cells, leading to reduced nitric oxide production, which in turn helps alleviate oxidative stress and neuronal apoptosis in the rat cerebral cortex. 1400W's ability to ameliorate spatial memory dysfunction associated with acute hypobaric hypoxia-reoxygenation makes it a valuable tool for research in neuroprotection and neurodegenerative disease studies. -
xanthine oxidase inhibitor
Allopurinol is a structural isomer of hypoxanthine (a naturally occurring purine in the body) and is an inhibitor of the enzyme xanthine oxidase. -
COX-2 inhibitor
Celecoxib is a sulfa non-steroidal anti-inflammatory drug (NSAID) and selective COX-2 inhibitor used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, and to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis.
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Dihydropyrimidinase Inhibitor
Dihydromyricetin (Ampelopsin (flavanol); Ampeloptin) is a natural antioxidant with good prospects. -
COX inhibitor
Diclofenac Sodium is a non-selective COX inhibitor with IC50 of 0.5 μg/ml and 0.5 μg/ml for COX-1 and -2 in intact cells, respectively, used as a nonsteroidal anti-inflammatory drug (NSAID) to relieve pain and reduce swelling in flammation. -
xanthine oxidase inhibitor
Febuxostat is a non-purine inhibitor of xanthine oxidase (Ki = 1.2 nM). -
COX-1 inhibitor
Ibuprofen Lysine(Motrin) is a non-steroidal anti-inflammatory drug. -
NLRP3 inflammasome inhibitor
Isoliquiritigenin is a licorice chalconoid, a type of natural phenols that is currently under experimentation phase testing for use as a cancer treatment as well as an aide for cocaine addiction. -
COX-1/COX-2 inhibitor
Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively. -
IMPDH inhibitor
Mycophenolate mofetil is a reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH) in purine biosynthesis (specifically guanine synthesis) which is necessary for the growth of T cells and B cells. -
COX inhibitor
Naproxen sodium is a non-selective cyclooxygenase (COX) inhibitor that displays anti-inflammatory, antipyretic and analgesic effects. Has a neuroprotective role against colchicine-induced cognitive impairment and oxidative stress. -
COX inhibitor
Phenylbutazone is a compound of research interest as an anti-inflammatory and anti-proliferative agent. -
COX inhibitor
Piroxicam is an effective and potent inhibitor of prostaglandin synthesis and a Cox-1 and Cox-2 inhibitor. -
COX inhibitor
Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions -
NFAT5 inhibitor
KRN2 (bromide) is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 0.1 μM. -
IFN-α and IFNAR interaction inhibitor
IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR; inhibit MVA-induced IFN-α responses by BM-pDCs (IC50=2-8 uM). -
Arginase inhibitor
nor-NOHA acetate is a specific and reversible arginase inhibitor, induces apoptosis in ARG2-expressing cells under hypoxia but not normoxia. -
tubulin polymerisation inhibitor
Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulin polymerisation inhibitor with IC50 of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. -
cyclophilin inhibitor
Alisporivir (DEB-025; Debio-025) is a cyclophilin inhibitor molecule with potent anti-hepatitis C virus (HCV) activity. -
COX-2 inhibitor
Etoricoxib D4 (MK-0663 D4) is a deuterium labeled Etoricoxib. Etoricoxib is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood. -
IL-12/IL-23 inhibitor
Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. -
NADPH oxidase inhibitor
APX-115 free base (Ewha-18278 free base) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with Ki values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. -
TLR4 inhibitor
TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis. -
ROS1/NTRK inhibitor
Taletrectinib (DS-6051b) is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor.
