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Catalog No.
Product Name
Application
Product Information
Citations
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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). -
C1q/MBL inhibitor
PIC1 PA is a 15-amino-acid peptide and a potent analog of PIC1 that inhibits classical pathway–mediated complement activation. It functions by disrupting the interaction between C1s-C1r-C1r-C1s/MASPs and the collagen-like region (CLR) of C1q or MBL. PIC1 PA specifically binds to the CLR of C1q, with a mean equilibrium dissociation constant (K\_D) of 33.3 nM for purified C1q. -
Complement factor B inhibitor
Lanoracopan is a potent inhibitor of complement factor B, with an IC₅₀ of 1.2 μM. It is suitable for research in inflammation- and immunity-related diseases. -
C5a receptor inhibitor
CP-289,503 is an inhibitor of the complement C5a receptor, with an IC₅₀ of 1 μM. The C5a receptor mediates pro-inflammatory signaling by binding to C5a, a complement activation product that stimulates leukocyte and phagocyte activation, upregulates integrins, and induces degranulation of inflammatory cells, contributing to endothelial damage. By blocking C5a signaling, CP-289,503 may be useful in the treatment of various inflammatory diseases. -
Kinases PROTAC/Nek9 Inhibitor
DB0614 is a PROTAC molecule utilizing a cereblon ligand, designed as a selective and potent degrader of NEK9 and other kinases. It induces the degradation of multiple kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1–3, MAP4K5, MAPK14, MAPK7–9, MAPKAPK2/3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1/3, SIK2/3, STK35, TNK2, and ULK1. DB0614 is suitable for research involving diseases or disorders driven by aberrant kinase activity. -
NSUN2 inhibitor
MY-1B is a covalent inhibitor of the RNA methyltransferase NSUN2 (IC50: 1.3 μM), stereoselectively targeting active-site cysteine residues (C271). It also covalently binds to PSME1, disrupting the proteasome regulatory complex and downregulating specific MHC-I subtype presentation. -
CD38 inhibitor
MK-0159 is an orally active, potent, and selective inhibitor of CD38, with IC₅₀ values of 22 nM for human, 3 nM for mouse, and 70 nM for rat CD38. It exhibits good microsomal stability in both human and rodent liver microsomes. MK-0159 effectively increases NAD⁺ (nicotinamide adenine dinucleotide) levels and decreases ADPR (adenosine diphosphate ribose) concentrations in whole blood and heart tissue, making it a promising compound for research in metabolic, cardiovascular, and age-related diseases. -
COX/LOX inhibitor
Phenidone is an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX) pathways, exhibiting anti-inflammatory and immunomodulatory effects. It has been shown to ameliorate paralysis in rat models of experimental autoimmune encephalomyelitis (EAE), a model for multiple sclerosis. Phenidone also acts as a potent hypotensive agent in spontaneously hypertensive rats. Additionally, it has a long-standing application as a photographic developer due to its redox properties. -
COX-1/COX-2 inhibitor
Glafenine is a non-selective, non-steroidal anti-inflammatory drug (NSAID) that inhibits both COX-1 and COX-2 enzymes. It exerts anti-inflammatory, anti-proliferative, and anti-migratory effects by suppressing the arachidonic acid metabolic pathway, thereby reducing prostaglandin production. Additionally, glafenine induces cell cycle arrest in vascular smooth muscle cells and endothelial cells and decreases the synthesis of the extracellular matrix protein tenascin. It is utilized in research related to inflammatory disorders, vascular restenosis, and cystic fibrosis. -
NOS inhibitor
L-NMMA acetate (NG-monomethyl-L-arginine acetate) is a non-selective nitric oxide synthase (NOS) inhibitor that targets all three NOS isoforms: neuronal (nNOS/NOS1), endothelial (eNOS/NOS3), and inducible (iNOS/NOS2). It exhibits Ki values of approximately 0.18 µM for rat nNOS, 0.4 µM for human eNOS, and 6 µM for mouse iNOS, making it a valuable tool for studying nitric oxide–mediated physiological and pathological processes. -
IL-6 inhibitor
LMT-28 is an orally active and the first synthetic interleukin-6 (IL-6) inhibitor that acts by directly binding to gp130, a key signal-transducing component of the IL-6 receptor complex. It selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130, exhibiting low toxicity. LMT-28 is a promising compound for research into IL-6-mediated inflammatory and autoimmune diseases. -
COX inhibitor
Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active, non-selective cyclooxygenase (COX) inhibitor. It exhibits analgesic, anti-inflammatory, and anti-cancer effects. As the active enantiomer of ketoprofen, Dexketoprofen trometamol is commonly used for the management of pain and inflammation, and it is also under investigation for its potential anticancer properties. -
COX-2 inhibitor
SC-58125 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.04 μM. It demonstrates antitumor activity both in vitro and in vivo and is effective in reducing inflammation-related edema. Additionally, SC-58125 possesses analgesic properties, making it a valuable compound for research in cancer, inflammation, and pain management. -
HO-1 inhibitor
Tin protoporphyrin IX dichloride (SnPPIX) is a potent inhibitor of heme oxygenase-1 (HO-1), an enzyme involved in cellular stress responses and tumor progression. SnPPIX has been shown to sensitize pancreatic ductal adenocarcinoma (PDAC) tumors to chemotherapy in mouse models, enhancing therapeutic efficacy and supporting its potential use as a chemosensitizing agent in cancer treatment. -
PGAM1 inhibitor
HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1) that induces apoptosis and suppresses cell migration by inhibiting the formation of invasive pseudopodia. It increases oxidative stress, activates the JNK/c-Jun pathway, and downregulates AKT and ERK signaling. HKB99 is a promising compound for the study of non-small cell lung cancer (NSCLC). -
ALK/ROS1 inhibitor
Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor that effectively blocks tyrosine autophosphorylation of ALK, mutant ALK, and EGFR, with IC50 values ranging from 5.38 to 16.74 nM. Additionally, it inhibits the transport activity of MATE1, MATE2K, P-gp, and BCRP. Iruplinalkib is under investigation for the treatment of non-small cell lung cancer (NSCLC). -
Endoplasmic Reticulum Stress Inhibitor
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects. -
KRASG12C inhibitor
RMC-4998 is an orally active inhibitor that selectively targets the active, GTP-bound state of the KRAS^G12C mutant. It forms a ternary complex with intracellular cyclophilin A (CYPA) and activated KRAS^G12C, exhibiting an IC50 of 28 nM. RMC-4998 suppresses ERK signaling and induces apoptosis in KRAS^G12C-mutant cancer cells, making it a valuable candidate for tumor research. -
NSAID/COX inhibitor
Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory drug (NSAID) that functions primarily by inhibiting cyclooxygenase (COX) enzymes, thereby reducing the synthesis of pro-inflammatory prostaglandins. In addition to its classical NSAID activity, Fenoprofen has been identified as a positive allosteric modulator (PAM) of melanocortin receptors (MCRs), enhancing MCR-mediated signaling. Fenoprofen also promotes ERK1/2 activation in HEK293T cells, suggesting additional modulation of intracellular signaling pathways involved in inflammation and cellular proliferation. -
CD38 inhibitor
RBN013209 is an orally active, small molecule inhibitor of CD38, exhibiting potent inhibitory activity with an IC₅₀ ranging from 0.01 to 0.1 μM against human CD38. It effectively blocks the enzymatic conversion of extracellular NAD⁺ to ADPR and cADPR in both tumor cells and peripheral blood mononuclear cells (PBMCs), thereby modulating the tumor microenvironment. Beyond its direct antitumor potential, RBN013209 also enhances the efficacy of immunotherapies. It preserves the naïve and central memory phenotypes of CAR-T cells, while reducing the expression of activation markers and exhaustion-associated inhibitory receptors. These properties position RBN013209 as a promising agent for both tumor research and the development of combination strategies to improve CAR-T cell persistence and function. -
RAS inhibitor
RMC-7977 is an orally bioavailable, triple-complex RAS inhibitor that functions by simultaneously binding to cyclophilin A (CypA; K_d = 195 nM) and KRAS^G12V (K_d = 292 μM), facilitating the formation of a stable inhibitory complex. It exhibits broad-spectrum activity against RAS isoforms—including KRAS, NRAS, and HRAS—across both wild-type and mutant variants. RMC-7977 suppresses key oncogenic signaling pathways by inhibiting the phosphorylation of ERK, CRAF, and RSK, while promoting apoptosis through enhanced PARP cleavage. This dual mechanism results in significant tumor regression and reduced acquired resistance in KRAS^G12C-driven cancer models. It also shows favorable tolerability across a range of RAS-mutant tumor models, positioning it as a promising therapeutic candidate for RAS-driven malignancies. -
KRAS-G12C(ON) Inhibitor
Elironrasib is an orally active, covalent inhibitor specifically targeting the active GTP-bound form of KRAS^G12C (KRAS^G12C(ON)). It uniquely functions by forming a stable tri-complex with KRAS^G12C(ON) and cyclophilin A (CypA) within tumor cells, leading to steric hindrance that blocks the interaction between KRAS and its downstream effectors. This mechanism effectively suppresses RAS-mediated signaling, particularly the ERK pathway. Elironrasib induces apoptosis in KRAS^G12C-mutant H358 non-small cell lung cancer cells and demonstrates potent antiproliferative activity across KRAS^G12C-mutant cell lines, with a median IC₅₀ of 0.11 nM. Its high specificity and novel mechanism make it a promising therapeutic candidate for cancers driven by KRAS^G12C mutations. -
COX-1/HDAC/Tyrosinase Inhibitor
Gnetol is a bioactive phenolic compound isolated from the root of *Gnetum montanum* with diverse pharmacological properties. It potently inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 0.78 μM and exhibits histone deacetylase (HDAC) inhibitory activity. Gnetol is also a strong tyrosinase inhibitor, with an IC₅₀ of 4.5 μM against murine tyrosinase, leading to suppression of melanin biosynthesis. In addition to its antioxidant, antiproliferative, anticancer, and hepatoprotective effects, Gnetol modulates metabolic enzymes in a concentration-dependent manner, including α-amylase, α-glucosidase, and adipogenesis pathways, making it a promising candidate for research in oncology, dermatology, and metabolic disorders. -
NF-κB p65 Inhibitor
Licochalcone D is a naturally occurring flavonoid primarily found in the root of *Glycyrrhiza uralensis* (Chinese licorice). It functions as a potent and orally active inhibitor of the NF-κB p65 subunit, a key regulator of inflammation and cancer-related signaling pathways. Licochalcone D exhibits broad pharmacological properties, including antioxidant, anti-inflammatory, and anticancer activities, making it a promising candidate for research in inflammation-related diseases and oncology. -
SIK1/2 Inhibitor
SIK2-IN-4 is a highly selective inhibitor of SIK1 and SIK2, exhibiting IC50 values of 0.143 μM and 0.076 μM, respectively. By targeting SIK1/2, SIK2-IN-4 reduces the phosphorylation of transcription coactivator 3 (CRTC3), thereby modulating cAMP response element binding protein (CREB)-dependent transcriptional activity. This compound demonstrates inhibitory effects on pro-inflammatory cytokines such as TNF, IL-12/23 p40, and IL-23, while promoting the expression of the anti-inflammatory cytokine IL-10. SIK2-IN-4 is a valuable tool for investigating intestinal inflammation and other chronic inflammatory conditions. -
TNFα/IL-2 Inhibitor
Immuno modulator-1 is a potent inhibitor of TNFα and IL-2, displaying IC50 values of 4.7 nM and 26 nM, respectively, in human peripheral blood mononuclear cells (hPBMC). This compound is valuable for investigating immune response modulation and inflammatory pathways. Additionally, Immuno modulator-1 demonstrates a hERG potassium channel blocking effect, exhibiting a 20% inhibitory percentage at a concentration of 3 μM, making it relevant for studies involving cardiac safety profiles. -
COX-1/2 Inhibitor
Cudraflavone B is a prenylated flavonoid that functions as a dual inhibitor of COX-1 and COX-2, demonstrating significant anti-inflammatory and anti-tumor activity. This compound inhibits the translocation of nuclear factor κB (NF-κB) in macrophages, leading to decreased tumor necrosis factor α (TNFα) gene expression and secretion. Additionally, Cudraflavone B induces the mitochondrial apoptotic pathway while activating MAPK signaling pathways, including p38 and ERK, and upregulating SIRT1 expression. These mechanisms contribute to its efficacy in attenuating the growth of human oral squamous cell carcinoma cells, making it a valuable tool for cancer research. -
CD28 Inhibitor
CD28-IN-3 is a selective CD28 inhibitor that effectively interrupts the CD28-B7 interaction, with an IC50 of 7.80 μM and a Kd of 52.45 μM. This compound significantly suppresses the production of key proinflammatory cytokines, including IFN-γ, IL-2, and TNF-α. CD28-IN-3 is valuable for research focused on checkpoint-resistant cancers, providing insights into immune modulation and potential therapeutic strategies. -
CD28 Inhibitor
CD28-IN-1 is a selective inhibitor of CD28 with a dissociation constant (KD) of 12.48 μM. It effectively disrupts the CD28-B7 interactions, leading to a significant reduction in CD28-mediated immune activation. This compound has been shown to suppress cytokine production, including IFN-γ, IL-2, and TNF-α, in primary human T cells when co-cultured with tumor spheroids and human epithelial tissues. CD28-IN-1 is suitable for research focused on tumor immunity and T cell modulation. -
COX Inhibitor
Oxaprozin is a potent, orally active cyclooxygenase (COX) inhibitor, demonstrating IC50 values of 2.2 μM for human platelet COX-1 and 36 μM for IL-1-stimulated human synovial cell COX-2. This compound exhibits significant anti-inflammatory activity and is known to inhibit the activation of NF-κB, promoting cell apoptosis. The inhibition of the Akt/IKK/NF-κB signaling pathway is a key mechanism underlying its anti-inflammatory properties, making Oxaprozin valuable for research in inflammation and related disorders. -
Dual COX-2/EGFR Inhibitor
Melafolone is a potent dual inhibitor of COX-2 and EGFR, displaying IC50 values of 13.2 μM for COX-2 and 17.4 μM for EGFR. This compound enhances the efficacy of anti-PD-1 therapy by promoting vascular normalization and downregulating PD-L1 through the PI3K/Akt signaling pathway in Lewis lung carcinoma (LLC) and CMT167 models. Melafolone is suitable for applications in lung cancer research. -
COX Inhibitor
Oxaprozin potassium is a potent cyclooxygenase (COX) inhibitor, demonstrating IC50 values of 2.2 μM for human platelet COX-1 and 36 μM for IL-1-stimulated human synovial cell COX-2. It not only exhibits anti-inflammatory activity but also inhibits the activation of NF-κB, inducing cell apoptosis. The inhibition of the Akt/IKK/NF-κB pathway is a key mechanism contributing to its anti-inflammatory effects, making it a valuable tool for research in inflammation and related cellular processes. -
PD-1/PD-L1 Inhibitor
PD-1/PD-L1-IN-54 is an inhibitor of the PD-1/PD-L1 interaction, targeting immune checkpoints critical for tumor immune evasion. With a KD of 55.8 μM for PD-1 and 46.4 μM for PD-L1, and an IC50 of 88.6 μM, this compound enhances CD8+ T cell activation and promotes the secretion of key cytokines such as IFN-γ and IL-2. Furthermore, PD-1/PD-L1-IN-54 exhibits anticancer properties by inhibiting tumor cell proliferation and inducing apoptosis, while also modulating T cell immunity via the PI3K/Akt signaling pathway. -
IL-13 Inhibitor
IL13Rα2 D1 is a potent inhibitor of the IL-13/IL13Rα2 signaling pathway. It effectively suppresses IL-13-induced cellular processes, including adhesion, migration, invasion, and proliferation. Additionally, IL13Rα2 D1 inhibits the phosphorylation of key signaling proteins such as FAK, Src, AKT, and ERK1/2, as well as the expression of matrix metalloproteinases (MMPs). This compound is valuable for research focused on cancer biology, particularly in the context of colorectal cancer. -
CXCR4 Inhibitor
Hit 14 is a selective inhibitor of C-X-C chemokine receptor type 4 (CXCR4), demonstrating an IC50 value of 254 nM. This compound effectively inhibits the migration and invasion of MDA-MB-231 cells, highlighting its potential in cancer research. Furthermore, Hit 14 modulates Akt phosphorylation and exhibits anti-inflammatory properties, demonstrating efficacy in reducing ear swelling and damage in mouse models. Its diverse biological activities make it a valuable tool for studies related to cancer metastasis and inflammation. -
COX-2 Inhibitor
Withangulatin A is a selective inhibitor of cyclooxygenase-2 (COX-2), demonstrating significant potential in the modulation of inflammatory and tumorigenic processes. This compound also interferes with the MAPK, NF-κB, and Akt/mTOR/p70S6K signaling pathways, thereby exhibiting notable antitumor and anti-inflammatory activities. Additionally, Withangulatin A has been shown to possess trypanocidal effects, making it useful for research in cancer, inflammation, and parasitic diseases. -
PI3K/Akt/mTOR signaling pathway Inhibitor, TLR4 signaling Inhibitor
25(R,S)-Ruscogenin is a potent inhibitor of the PI3K/Akt/mTOR and TLR4 signaling pathways. This compound effectively suppresses hepatocellular carcinoma (HCC) metastasis by decreasing the expression of matrix metalloproteinases (MMP-2 and MMP-9), uPA, VEGF, and HIF-1α. Additionally, 25(R,S)-Ruscogenin mitigates LPS-induced apoptosis in pulmonary endothelial cells, highlighting its potential for applications in cancer research and inflammatory disease studies. -
COX-2 Inhibitor
Ataquimast is a selective COX-2 inhibitor that effectively suppresses the release of leukotrienes, TNF-α, and GM-CSF. Its mechanism supports research into inflammatory responses and has potential applications in the study of advanced estrogen receptor-positive breast cancer. This compound may aid in elucidating the role of COX-2 in tumor progression and therapeutic resistance. -
COX-2 Inhibitor
COX-2-IN-60 is a potent and selective inhibitor of cyclooxygenase-2 (COX-2), demonstrating an IC50 of 0.06 μM and approximately 100-fold selectivity over COX-1. This compound significantly reduces oxidative stress and neuroinflammatory cytokines, effectively counteracting epileptogenesis. In preclinical studies utilizing a pilocarpine-induced seizure mouse model, COX-2-IN-60 exhibited substantial anticonvulsant effects while protecting against hippocampal injury. Its application in research relates to neuroinflammatory pathways and epilepsy mechanisms. -
TLR Inhibitor
ETI60 is a selective Toll-like receptor (TLR) inhibitor that primarily targets the nucleoside-binding Site I on TLR7 and TLR9, with IC50 values of 0.68 μM and 0.12 μM, respectively. This compound effectively inhibits endosomal TLR-mediated pro-inflammatory signaling, demonstrating nanomolar activity in cellular, biophysical, and in vivo assays. ETI60 modulates the expression of inflammation-related genes and has shown efficacy in alleviating symptoms in mouse models of psoriasis and systemic lupus erythematosus (SLE). This reagent is valuable for research involving autoimmune and inflammatory diseases. -
Proinflammatory Cytokine Inhibitor
Semapimod is a potent inhibitor of proinflammatory cytokine production, targeting Toll-like receptor 4 (TLR4) signaling with an IC50 of approximately 0.3 μM. It effectively inhibits the production of key cytokines such as TNF-α, IL-1β, and IL-6, as well as p38 MAPK activity and nitric oxide production in macrophages. This compound holds promise for research in various inflammatory and autoimmune disorders. -
NO、TNF-α、IL-12 Inhibitor
(R)-5,7-Dimethoxyflavanone acts as an inhibitor of nitric oxide (NO), tumor necrosis factor-alpha (TNF-α), and interleukin-12 (IL-12), demonstrating significant anti-inflammatory properties. In biological assays, this compound exhibits potent antimutagenic activity, effectively reducing MeIQ-induced mutagenesis in the Ames test using S. typhimurium strains TA100 and TA98. Its capacity to modulate inflammatory mediators makes it a valuable tool in research focused on inflammation and mutagenesis. -
TLR Inhibitor
ETI41 is a selective Toll-like receptor (TLR) inhibitor that targets the nucleoside-binding Site I on TLR7 and TLR9, demonstrating IC50 values of 0.63 μM and 0.16 μM, respectively, while sparing surface TLRs. This compound effectively inhibits endosomal TLR-mediated pro-inflammatory signaling, displaying potent nanomolar activity across cellular, biophysical, and in vivo assays. ETI41 suppresses the expression of inflammation-associated genes and improves symptoms in murine models of psoriasis and systemic lupus erythematosus (SLE). It is valuable for research into autoimmune and inflammatory diseases.
