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Catalog No.
Product Name
Application
Product Information
Citations
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FLAP inhibitor
GSK2190915 is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM. -
EGFR inhibitor
Olafertinib (CK-101, RX518) is an epidermal growth factor receptor (EGFR) inhibitor.
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CypA Inhibitor
HL001 is an oral small molecule inhibitor targeting Cyclophilin A (CypA) and acting as a receptor antagonist for Lysophosphatidic acid 1 (LPA1). This compound induces cell cycle arrest and apoptosis in tumor cells via p53 stabilization, achieved by down-regulating G3BP1 and promoting reactive oxygen species production and DNA damage. HL001 disrupts the MDM2-p53-72R interaction in a CypA-dependent manner, demonstrating significant antitumor activity. Additionally, HL001 serves as a valuable tool in the investigation of pulmonary fibrosis. -
NADPH Oxidase Inhibitor
VAS 3947 is a selective inhibitor of NADPH oxidase (NOX), demonstrating significant antiplatelet activity. In addition to its role as an NOX inhibitor, VAS 3947 induces apoptosis through the activation of the unfolded protein response (UPR), primarily driven by protein aggregation and misfolding. This compound is valuable for research focused on oxidative stress and its implications in cardiovascular diseases. -
NF-κB Inhibitor/Nrf2/AMPK Activator
Panduratin A is a potent inhibitor of the NF-κB signaling pathway, recognized for its significant anti-inflammatory and antioxidant properties. It demonstrates protective effects against nephrotoxicity induced by Colistin, primarily by mitigating oxidative stress and enhancing mitochondrial function. Additionally, Panduratin A activates autophagy through an AMPK-dependent mechanism and exhibits potential anti-tuberculosis and antiviral activities by inhibiting the methyltransferase of SARS-CoV-2. These diverse biological activities make Panduratin A a valuable tool in various areas of research, including inflammation, cellular stress responses, and infectious diseases. -
FLAP Inhibitor
MK-886 sodium salt is a potent inhibitor of the 5-lipoxygenase-activating protein (FLAP), exhibiting an IC50 of 30 nM. It effectively inhibits leukotriene biosynthesis with IC50 values of 3 nM in intact leukocytes and 1.1 μM in human whole blood. Additionally, MK-886 acts as a non-competitive antagonist of PPARα and can induce apoptosis, making it a valuable tool for research in inflammatory diseases and apoptosis pathways. -
COX Inhibitor
Ketorolac hemicalcium is a non-steroidal anti-inflammatory drug (NSAID) that functions as a nonselective cyclooxygenase (COX) inhibitor, exhibiting IC50 values of 20 nM for COX-1 and 120 nM for COX-2. This compound is utilized in research related to allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain, as well as for its potential applications in cancer research due to its role as a DDX3 inhibitor. -
COX Inhibitor
Metamizole magnesium is an orally active cyclooxygenase (COX) inhibitor known for its key roles in reducing inflammation and pain. It exhibits significant anti-inflammatory and antioxidant activities, along with the ability to inhibit cell proliferation and promote apoptosis. Due to its antipyretic and analgesic properties, Metamizole magnesium is commonly utilized in various research applications aimed at investigating pain mechanisms and inflammatory responses. -
Topo I/COX-2 Inhibitor
Topo I/COX-2-IN-1 is an inhibitor of both Topoisomerase I and Cyclooxygenase-2 (COX-2). It demonstrates significant biological activity, with IC50 values of 0.24 μM for COX-2 and 4.42 μM for Topo I. This compound effectively induces apoptosis and inhibits the migration of cancer cells, showcasing potential applications in cancer research and therapy. -
Topo I/COX-2 Inhibitor
Topo I/COX-2-IN-2 is a potent dual-target inhibitor of Topoisomerase I (Topo I) and Cyclooxygenase-2 (COX-2), exhibiting inhibitory concentrations (IC50) of 0.90 μM and 2.31 μM, respectively. This compound induces apoptosis in cancer cells via the mitochondrial pathway, making it a valuable agent for research in cancer therapeutics and cell death mechanisms. Its dual activity supports investigations into the interplay between topoisomerase inhibition and inflammatory pathways in cancer progression. -
Complement Inhibitor
Dextran sulfate sodium salt (DSS, MW 5000) primarily functions as a complement inhibitor, derived from a polymer of dehydrated glucose. This compound exhibits significant biological activities, including anticoagulation, antiviral properties, and anti-lipemic effects. Its mechanisms involve blocking HIV-1 adsorption to host cells, preventing natural killer (NK) cell-mediated cytotoxicity, and inhibiting instant blood-mediated inflammatory reactions (IBMIR). Dextran sulfate sodium salt (MW 5000) is valuable in research related to immunology, virology, and cardiovascular studies. -
Autophagy Inducer, NLRP3 Inhibitor
Britannin is an autophagy inducer and NLRP3 inflammasome inhibitor with an IC50 of 3.630 μM. It exhibits significant anti-inflammatory effects by disrupting the interaction between NLRP3 and NEK7, effectively preventing NLRP3 activation and assembly. Additionally, Britannin shows antitumor properties by inhibiting tumor cell proliferation through interference with the interaction of HIF-1α and Myc, leading to reduced PD-L1 expression and enhanced activity of cytotoxic T lymphocytes. This compound also promotes apoptosis and autophagy in liver cancer cells via activation of ROS-regulated AMPK, making it a valuable tool for research in anti-inflammatory and oncology studies. -
COX-1 Inhibitor
Ibuprofen sodium is a selective inhibitor of cyclooxygenase-1 (COX-1), exhibiting an IC50 value of 13 μM. This compound demonstrates significant biological activities, including inhibition of cell proliferation, angiogenesis, and induction of apoptosis. As a nonsteroidal anti-inflammatory agent and nitric oxide (NO) donor, ibuprofen sodium is valuable in research areas such as pain, inflammation, infection, immunology, and oncology. -
MARK/SIK/AMPK Inhibitor
MRT199665 is a potent, ATP-competitive inhibitor targeting MARK, SIK, and AMPK pathways, exhibiting IC50 values of 2 nM for MARK1, 10 nM for AMPKα1, and 110 nM for SIK1. This compound induces apoptosis in MEF2C-activated human acute myeloid leukemia (AML) cells by effectively inhibiting the phosphorylation of the SIK substrate CRTC3 at S370. MRT199665 serves as a valuable tool for investigating the roles of MARK, SIK, and AMPK in cellular signaling and cancer biology. -
TLR2/4 Inhibitor
Robinin is a flavonoid that acts as an inhibitor of Toll-like receptors 2 and 4 (TLR2/4), modulating the TGF-β, TLR4/NF-κB, and TLR2-PI3k-AKT signaling pathways. This compound demonstrates significant anti-inflammatory and anti-tumor properties. Additionally, Robinin has been shown to enhance the anti-inflammatory effects of Methotrexate in experimental arthritis models and may mitigate cardiac toxicity induced by Doxorubicin. These attributes make Robinin a valuable reagent for research applications in inflammation and cancer therapy. -
ACE/IKK-β/PKC Inhibitor
Plantainoside D is a phenylethanoid glycoside that functions primarily as an inhibitor of IKK-β, with additional inhibitory effects on angiotensin-converting enzyme (ACE) and protein kinase C (PKC). It exhibits significant biological activities, including the reduction of glutamate release in the rat cerebral cortex, alleviating cell apoptosis through the inhibition of reactive oxygen species (ROS) and NF-κB activation. Additionally, Plantainoside D has been shown to improve outcomes in acute lung injury induced by sepsis via modulation of the Sirt3/NLRP3 signaling pathway. This compound is applicable in studies of neuroprotection, antioxidant activity, anti-inflammatory responses, and antihypertensive effects. -
TREM-1 Inhibitor
Nangibotide is a synthetic peptide that serves as a TREM-1 receptor inhibitor. By inhibiting NF-κB and NLRP3 inflammasome activation, Nangibotide effectively reduces the release of pro-inflammatory cytokines such as IL-1β and IL-8 and mitigates apoptosis. This reagent is valuable for research applications related to excessive inflammatory responses, including studies on myocardial ischemia-reperfusion injury, septic shock, acute lung injury, osteoarthritis, and acute liver failure. Additionally, Nangibotide offers protective effects on tissues, such as the liver and lung, during inflammatory conditions. -
Keap1-Nrf2 Protein-Protein Inhibitor
CPUY192018 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, exhibiting an IC50 of 0.63 µM. This compound demonstrates significant anti-inflammatory and antioxidant properties by activating the Nrf2-dependent pathway and inhibiting the NF-κB-related inflammatory response. CPUY192018 is ideal for research applications focused on inflammation-related diseases and the modulation of oxidative stress. -
FKBP51-Hsp90 Interaction Inhibitor
FKBP51-Hsp90-IN-1 is a selective inhibitor targeting the FKBP51-Hsp90 protein-protein interaction, exhibiting an IC50 value of 0.1 μM against FKBP51. This compound is valuable for research into stress-related diseases, Alzheimer's disease, and various metabolic disorders, owing to its ability to modulate protein interactions critical for cellular stress responses and stability. Its specificity makes it a potent tool for elucidating the role of FKBP51 in disease mechanisms. -
FKBP51-Hsp90 Inhibitor
FKBP51-Hsp90-IN-2 is a selective inhibitor of the FKBP51-Hsp90 protein-protein interaction, demonstrating IC50 values of 0.4 µM for FKBP51 and 5 µM for FKBP52. This compound has been shown to enhance cellular energy metabolism and promote neurite growth. Its efficacy makes FKBP51-Hsp90-IN-2 a valuable tool in research focused on neurodegenerative diseases and cancer. -
KRAS(Q61H) Inhibitor
RM-046 is a selective inhibitor targeting the KRAS(Q61H) mutant, functioning through the formation of a ternary complex with cyclophilin A. This compound non-covalently binds to activated KRASQ61H, obstructing effector binding and thereby inhibiting downstream signal transduction pathways. RM-046 has demonstrated efficacy in suppressing ERK phosphorylation, stalling cancer cell proliferation, and promoting anti-tumor activity, including tumor regression in preclinical xenograft studies. It serves as a valuable tool for investigating KRASQ61H-associated malignancies. -
FAP Inhibitor
BR103354 is a selective inhibitor of fibroblast activation protein (FAP) with an IC50 of 14 nM against human FAP. It effectively restores levels of phosphorylated ERK and Glut1, reduces non-fasting blood glucose concentrations, and enhances glucose tolerance, while also decreasing hepatic triglyceride content. This compound demonstrates potential in alleviating hepatic steatosis and fibrosis, making it a valuable tool for research into type 2 diabetes and non-alcoholic steatohepatitis. -
PIKfyve Inhibitor
AS2677131 is a potent and orally active inhibitor of PIKfyve, targeting the PIKfyve-c-Rel signaling pathway. It effectively inhibits the production of pro-inflammatory cytokines, including IL-12p40, IL-6, and IL-1β, by selectively blocking the DNA-binding activity of c-Rel to their respective promoters. Additionally, AS2677131 reduces MHC class II expression on B cells. This compound is valuable for research in the fields of inflammation and immunology, particularly in studies related to arthritis. -
IL-23 Inhibitor
IL-23 cyclic peptide inhibitor 105 targets the interleukin-23 (IL-23) pathway, serving as a specific inhibitor of this pro-inflammatory cytokine. It exhibits significant potential in modulating inflammatory responses associated with disorders such as inflammatory bowel disease (IBD). This compound is a valuable tool for researchers investigating the role of IL-23 in various inflammatory conditions and developing therapeutic strategies targeting IL-23 signaling. -
IL-17 Inhibitor
IL-17-IN-4 is a potent IL-17 inhibitor with an IC50 of less than 0.1 μM, making it a valuable tool for investigating the role of IL-17 in inflammatory diseases. This compound can facilitate research aimed at understanding the mechanisms of inflammation and the therapeutic potential of IL-17 modulation in conditions such as rheumatoid arthritis and psoriasis. Its high potency enables effective studies of IL-17 signaling pathways in various biological contexts. -
IL-1β Secretion Inhibitor
K-832 is an orally active inhibitor of IL-1β secretion, targeting the interleukin-1 pathway. This compound demonstrates significant biological activity by reducing inflammatory responses associated with autoimmune disorders. K-832 is applicable in the research of rheumatoid arthritis and other conditions linked to elevated IL-1β levels, making it a valuable tool for studying inflammation and immune response modulation. -
Keap1-Nrf2 Inhibitor
Keap1-Nrf2-IN-25 is a potent inhibitor of the Keap1-Nrf2 interaction, exhibiting an IC50 of 0.55 μM and a binding affinity (Kd) of 0.50 μM. This compound effectively activates the Nrf2 pathway, leading to the reduction of reactive oxygen species (ROS) and pro-inflammatory cytokines such as IL-1β and IL-6. Keap1-Nrf2-IN-25 has demonstrated protective effects in models of colitis, particularly against DSS-induced inflammation, making it a valuable tool for research in oxidative stress and inflammatory diseases. -
IL-1 Inhibitor
E5090 is an orally active inhibitor of IL-1 generation, acting through its conversion in vivo to the active deacetylated form, DA-E5090. This compound exhibits significant anti-inflammatory properties, making it valuable for studies related to inflammation and immune response modulation. E5090 is useful in various immunology research applications, particularly in understanding the role of IL-1 in disease states. -
IL-17A Inhibitor
Acetyl zingerone is an IL-17A inhibitor that exhibits potent anti-inflammatory and antioxidant activities. This compound plays a crucial role in protecting melanocytes from DNA damage by inhibiting matrix metalloproteinases and downregulating IL-17A target gene expression. Acetyl zingerone is valuable for research focused on inflammatory skin conditions and mechanisms of cellular protection. -
Inflammatory Cytokine Inhibitor
JTE-607 free base is a selective inhibitor of inflammatory cytokine synthesis, targeting the Cleavage and Polyadenylation Specificity Factor 3 (CPSF3). This compound effectively reduces the production of key inflammatory cytokines, including TNF-α, IL-1β, IL-6, IL-8, and IL-10, in LPS-stimulated human peripheral blood mononuclear cells (PBMCs), achieving IC50 values of 11, 5.9, 8.8, 7.3, and 9.1 nM, respectively. JTE-607 free base demonstrates potential utility in research aimed at understanding and mitigating inflammatory responses, particularly in the context of endotoxin shock. -
IL-1/β-transferase Inhibitor
Pentenocin B is an IL-1/β-transferase inhibitor that selectively targets the interleukin-1 signaling pathway. This compound exhibits weak inhibitory activity against IL-1 and β-transferase, which are crucial in mediating inflammatory responses. Pentenocin B is useful for research applications focused on inflammation and related signaling mechanisms. -
IL-2 secretion inhibitor
BC12-4 is a potent inhibitor of interleukin-2 (IL-2) secretion, primarily acting on immune cell signaling pathways. This compound exhibits immunomodulatory activity, making it valuable in the study of cytokine regulation and immune responses. BC12-4 is suitable for research applications focused on autoimmune diseases, transplantation, and cancer immunotherapy. -
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.
