Catalog No.
Product Name
Application
Product Information
Citations
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PD-L1/HDAC6 Inhibitor
PD-L1/HDAC6-IN-1 is a dual inhibitor targeting PD-L1 and HDAC6, effectively disrupting the PD-L1/PD-1 interaction with IC50 values of 26.8 nM and 69 nM, respectively. This compound significantly enhances the cytotoxicity of Jurkat T cells against HepG2 cells with an IC50 of 3.4 μM. Additionally, PD-L1/HDAC6-IN-1 demonstrates favorable pharmacokinetics in rat models, achieving a drug exposure level of 871.62 ng·h/mL, and shows promising antitumor efficacy in B16-F10 xenograft models in mice. -
PD-L1/HDAC Inhibitor
PD-L1/HDAC-IN-1 is a dual inhibitor targeting PD-L1, HDAC2, and HDAC3, with IC50 values of 88.10 nM, 27.98 nM, and 14.47 nM, respectively. This compound effectively disrupts the PD-1/PD-L1 interaction and demonstrates minimal cytotoxicity in MCF-7 cells (IC50=19.34 μM). PD-L1/HDAC-IN-1 enhances the expression of PD-L1 and CXCL10, thereby facilitating an anti-tumor immune response through increased T-cell recruitment into the tumor microenvironment (TME). Its unique mechanism positions it as a valuable tool for research in cancer immunotherapy. -
COX-2/HDAC Inhibitor
Andrographidine E is an inhibitor of cyclooxygenase-2 (COX-2) and histone deacetylases (HDAC), with an IC50 of 19 μM for COX-2 and a strong affinity for HDAC1 and HDAC3. This compound selectively binds to macrophages, suggesting its potential as an immunotargeting agent. Andrographidine E is valuable for research applications focused on inflammation and immune modulation. -
Anti-Inflammatory Agent
Triamcinolone acetonide is a potent anti-inflammatory agent that primarily targets fibroblast growth factor (bFGF) signaling pathways. It effectively inhibits bFGF-induced proliferation of retinal endothelial cells, promotes macrophage activation with anti-inflammatory properties, and reduces chondrocyte viability, contributing to cartilage degradation. This compound is valuable for research applications related to various inflammatory conditions, including atopic dermatitis. -
Nrf2 Activator
Dimethyl fumarate is an orally bioavailable Nrf2 activator that enhances the expression of antioxidant genes. This compound has been shown to induce necroptosis in colon cancer cells via mechanisms involving glutathione depletion, reactive oxygen species elevation, and activation of MAPK pathways. Additionally, Dimethyl fumarate promotes autophagy and is applicable in studies focused on multiple sclerosis and related neurodegenerative conditions. -
Anti-inflammatory Agents
Balsalazide disodium is a prodrug that releases mesalamine in the colon, primarily targeting anti-inflammatory pathways. It exhibits significant anti-inflammatory activity in conditions such as colitis and demonstrates potential anticancer effects through modulation of the IL-6/STAT3 signaling pathway. This compound is useful in research focused on gastrointestinal disorders and cancer therapy. -
Anti-inflammatory Agent
Luteolin 5-O-glucoside is a potent anti-inflammatory agent derived from Cirsium maackii. This compound effectively inhibits lipopolysaccharide (LPS)-induced nitric oxide production and tert-butyl hydroperoxide (t-BHP)-induced reactive oxygen species generation. Additionally, Luteolin 5-O-glucoside downregulates the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in macrophages, making it valuable for research in inflammatory pathways and related conditions. -
Anti-inflammatory Agent
Ajugol is an orally active iridoid glycoside that functions as an anti-inflammatory agent. It activates TFEB-mediated autophagy and lysosomal biogenesis, contributing to its protective effects on cellular homeostasis. Ajugol demonstrates significant potential for research in conditions such as asthma, non-alcoholic fatty liver disease (NAFLD), and osteoarthritis due to its dual role in promoting autophagy and mitigating inflammation. -
PDE IV Inhibitor/A1AR Antagonist
Doxofylline is an orally active phosphodiesterase IV (PDE IV) inhibitor and adenosine A1 receptor (A1AR) antagonist. It exhibits anti-inflammatory properties by reducing mitochondrial reactive oxygen species (ROS) production and modulating various cellular pathways, including the NLRP3-TXNIP inflammasome activation. This compound is valuable for research related to respiratory diseases such as asthma, chronic obstructive pulmonary disease (COPD), and bronchospasm. -
Nonsteroidal Anti-inflammatory Agent
2-Ethoxybenzamide is a nonsteroidal anti-inflammatory agent that exhibits both analgesic and antipyretic activities. Its mechanism involves the induction of melanin synthesis through the phosphorylation of cAMP response element-binding protein (CREB). This compound is valuable for research focused on hypopigmentation and inflammation-related diseases, providing insights into therapeutic applications and biological pathways involved in these conditions. -
PD-1/PD-L1 Interaction Inhibitor
PD-1/PD-L1-IN 3 is a macrocyclic peptide that acts as a selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions. By binding to PD-L1, it effectively disrupts the binding of PD-L1 to PD-1 and CD80, exhibiting IC50 values of 5.60 nM and 7.04 nM, respectively. This compound is valuable for research in various fields, particularly in cancer immunotherapy and the study of infectious diseases. -
Anti-inflammatory Agent
Salsalate is an anti-inflammatory agent primarily targeting the modulation of cytokine expression without direct cyclooxygenase inhibition. This compound exhibits significant anti-inflammatory effects and has been shown to lower blood glucose levels, enhance insulin sensitivity, and mitigate the effects of metabolic disorders associated with high-fat diets. Salsalate is utilized in research pertaining to type 2 diabetes, atherosclerosis, and non-alcoholic steatohepatitis, demonstrating its potential in the management of metabolic disorders. -
COX-1/cAMP Phosphodiesterase Inhibitor
Triflusal is a dual inhibitor of Cyclooxygenase-1 (COX-1) and cAMP phosphodiesterase, which penetrates the blood-brain barrier. It effectively inhibits platelet aggregation, nuclear factor kappa B (NF-κB) activation, inducible nitric oxide synthase (iNOS) activity, and prostaglandin synthesis in ischemic tissues. Additionally, Triflusal enhances neutrophil nitric oxide production, endothelial nitric oxide synthase (eNOS) expression, and constitutive nitric oxide synthase (cNOS) activity. This compound is valuable for investigating thromboembolic and ischemic diseases of the cardiovascular and cerebrovascular systems, as well as Alzheimer's disease pathology. -
Nrf2 Activator
Raffinose serves as an Nrf2 activator and is known for its ability to modulate intestinal flora. It inhibits the TLR4-MyD88-NF-κB signaling pathway while promoting Nrf2 signaling, contributing to its anti-inflammatory, antioxidant, and immunomodulatory properties. This compound is orally active and is valuable in research applications focusing on inflammation and oxidative stress. -
β/α-1 Blocker
Carvedilol phosphate hemihydrate is a non-selective β/α-1 adrenergic receptor blocker. It demonstrates significant biological activity by inhibiting lipid peroxidation with an IC50 of 5 μM and acts as a multiple-action antihypertensive agent, with potential applications in treating angina and congestive heart failure. Additionally, carvedilol phosphate hemihydrate has been identified as an autophagy inducer that suppresses the NLRP3 inflammasome, making it valuable for research in inflammation and cardiovascular diseases. -
nNOS Inhibitor
NXN-188 is a selective nNOS inhibitor that also acts as an agonist for the 5HT-1B/1D receptors. This compound exhibits potential in modulating neurogenic inflammation and is particularly relevant in research focused on migraine pathophysiology and treatment strategies. Its dual action supports investigations into the intricate mechanisms underlying headache disorders. -
COX Inhibitor
Pentagamavunon-1 (PGV-1) is a COX-2 inhibitor that modulates multiple molecular pathways to induce apoptosis. This Curcumin analog exhibits notable oral bioactivity and suppresses key angiogenic factors, including vascular endothelial growth factor (VEGF). Additionally, PGV-1 inhibits NF-κB activation, highlighting its potential in cancer research and therapeutic applications targeting inflammation and tumor progression. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-piperazine-Boc is an E3 ligase ligand-linker conjugate that serves as an intermediate in the synthesis of PROTAC targeting B-cell lymphoma 6 protein (BCL6). This compound plays a significant role in targeted protein degradation, facilitating the selective destruction of BCL6 and aiding in research related to cancer therapeutics. Its application is essential for studies focusing on E3 ligase modulation and PROTAC development in oncology. -
CD47-SIRPα axis Inhibitor
DMUP is a potent inhibitor of the CD47-SIRPα axis. This compound promotes apoptosis and enhances macrophage phagocytosis in A549 lung cancer cells, while also reducing the expression of CD47 and SIRPα proteins. DMUP demonstrates significant antitumor activity, making it a valuable tool for research in cancer immunotherapy and macrophage biology. -
PD-1/PD-L1 Inhibitor
PD-1/PD-L1-IN-10 is a potent orally active inhibitor of the PD-1/PD-L1 interaction, with an IC50 value of 2.7 nM. This compound exhibits significant anticancer efficacy by blocking the immune checkpoint pathway, thereby enhancing T-cell activation and promoting anti-tumor responses. PD-1/PD-L1-IN-10 is valuable for research in immunotherapy and cancer treatment studies. -
Anti-inflammatory agent
DHMB (2,3-Dihydroxy-4-methoxybenzaldehyde) is an organic compound known for its anti-inflammatory properties. It exhibits protective effects on intestinal epithelial cells, making it valuable for research related to inflammation and gut health. This reagent is useful in studying the pathways involved in inflammatory responses and exploring therapeutic solutions for inflammatory disorders. -
Anti-inflammatory Agent
Lupeol acetate is a derivative of Lupeol that functions as an anti-inflammatory agent. It exhibits significant biological activity by down-regulating the expression of inflammatory cytokines and inhibiting osteoclast production, thereby improving symptoms of rheumatoid arthritis. Additionally, Lupeol acetate shows antibacterial and anti-trypanosomic properties and has been observed to inhibit spermatogenesis in male rats, potentially leading to infertility. This compound is suitable for research applications related to inflammation, cancer, and reproductive health. -
Anti-inflammatory Agent
β-Amyrin acetate is a triterpenoid recognized for its anti-inflammatory properties. This compound exhibits a range of biological activities, including antifungal, anti-diabetic, and anti-hyperlipidemic effects. Research indicates that β-Amyrin acetate can inhibit HMG-CoA reductase activity by binding to the hydrophobic cleft of the enzyme, making it a valuable candidate for studies related to lipid metabolism and inflammation management. -
EGFR/HER2/CDK9/COX-2 Inhibitor
CDK9-IN-41 is a potent inhibitor of CDK9, EGFR, HER2, and COX-2, exhibiting IC50 values of 192.81 nM, 254.03 nM, 238.81 nM, and 775 nM respectively. This compound demonstrates significant antitumor activity across various cancer cell lines, including leukemia, colon, melanoma, ovarian, and breast cancer. It serves as a valuable tool for exploring the role of these kinases in cancer biology and therapeutic applications. -
HER2-TLR7/8 Conjugate
MC-Val-Cit-PAB-Amide-TLR7 Agonist 4 is a HER2-targeted TLR7 and TLR8 immune agonist conjugate. This compound activates Toll-like receptors, enhancing immune responses through the stimulation of both innate and adaptive immunity. It is primarily utilized in research applications aimed at cancer immunotherapy, particularly in enhancing the immune system's ability to target HER2-expressing tumors. -
Anti-EGFR/CD47 Antibody
Vislarafusp alfa is a humanized IgG1κ antibody targeting both EGFR and CD47. This novel bispecific antibody exhibits potential for modulating tumor immune evasion and promoting anti-tumor responses, making it significant in cancer research applications. Its unique mechanism of action presents valuable opportunities for studying combination therapies and understanding the interplay between immune checkpoint regulators and growth factor signaling pathways. -
Peptide Toxin
Candidalysin is a cytolytic peptide toxin derived from the pathogenic fungus Candida albicans, primarily targeting epithelial cells. This peptide is known for its ability to activate the EGFR-MAPK signaling pathway, which leads to increased expression of matrix metalloproteinases (MMPs) and calcium influx, as well as modulation of the c-Fos transcription factor through p38 MAPK and ERK1/2. Candidalysin plays a critical role in both mucosal and systemic infections by stimulating NLRP3 inflammasome activation, promoting inflammatory responses, neutrophil recruitment, and Th17 immunity. Additionally, it induces lactate dehydrogenase (LDH) release, resulting in membrane damage and cytotoxicity. -
Molecular Glue
MNN-02-155 is a bivalent molecular glue that binds simultaneously to p300/CBP and BCL6. This compound effectively activates the BCL6-target reporter gene, leading to significant induction of cell death. MNN-02-155 is particularly relevant for research into diffuse large B cell lymphomas (DLBCLs), providing insights into potential therapeutic strategies involving BCL6 modulation. -
Molecular Glue
TCIP3 is a bivalent molecular glue that targets p300/CBP and BCL6. By redirecting p300 and CBP, TCIP3 activates programmed cell death genes that are typically suppressed by the oncogenic driver BCL6, making it a valuable tool for investigating diffuse large B cell lymphomas (DLBCLs). Importantly, TCIP3 demonstrates no toxicity to non-transformed tonsillar lymphocytes or fibroblasts, ensuring the safety of experimental applications. -
RNA Modifying Substance
N4-Acetylcytidine is an RNA-modifying nucleoside metabolite produced during tRNA degradation, primarily via N-acetyltransferase 10 and additional enzymes. This compound has been shown to enhance NLRP3 inflammasome activation through the upregulation and release of HMGB1. N4-Acetylcytidine plays a crucial role in modifying the stability and translation efficiency of mRNA, tRNA, and rRNA, particularly in relation to enterovirus 71 RNA. Its applications extend to research in cancer, neuroinflammatory diseases, viral infections, and obesity. -
NCD38 Enantiomer
(1R,2S)-NCD38 TFA is a selective inhibitor of Lysine-specific demethylase 1 (LSD1). This enantiomeric form of NCD38 TFA exhibits potent biological activity, primarily in the modulation of epigenetic regulation through LSD1 inhibition. It is applicable in research focused on cancer biology, developmental studies, and potential therapeutic interventions targeting LSD1-related pathways. -
Anti-inflammatory Peptide
SAP15 is a synthetic anti-inflammatory peptide derived from human beta-defensin 3, comprising 15 amino acids. This peptide effectively penetrates cells to downregulate intracellular inflammation by inhibiting the phosphorylation of HDAC5, which in turn reduces the phosphorylation of NF-κB p65. In LPS-induced macrophages, SAP15 demonstrates significant anti-inflammatory activity, while also enhancing the expression of aggrecan and type II collagen, and decreasing osteocalcin levels in LPS-induced chondrocytes. SAP15 serves as a valuable tool in the exploration of inflammation regulation and the development of anti-inflammatory therapies for biomaterials. -
SIK Inhibitor
YKL-05-093 is a selective SIK (Salt-Induced Kinase) inhibitor, demonstrating a binding affinity (Kd) of 7.1 nM for SIK2. This compound effectively reduces the phosphorylation levels of HDAC4, HDAC5, and CRTC2, while inhibiting SOST expression and stimulating RANKL expression both in vitro and in vivo. YKL-05-093 is suitable for research applications focusing on bone diseases and related signaling pathways. -
PRMT5 Inhibitor
PRMT5-IN-53 is a potent, orally bioavailable inhibitor of PRMT5, exhibiting pIC50 values of ≥ 9.7 against both human and mouse PRMT5. It demonstrates high affinity for the PRMT5:MEP50 complex with a KD of 11.3 pM. This compound effectively inhibits PRMT5 in the intestines of murine models, leading to a significant reduction in the number and size of polyps while minimizing systemic hematological toxicity. PRMT5-IN-53 is particularly valuable for research in colorectal cancer, especially in the context of familial adenomatous polyposis (FAP). -
Anti-inflammatory
(2R)-Octyl-α-hydroxyglutarate sodium is the sodium salt derivative of (2R)-Octyl-α-hydroxyglutarate, functioning primarily as an anti-inflammatory agent. This compound demonstrates significant biological activity in modulating inflammatory responses, making it valuable in various research applications focused on inflammation and related pathways. -
DR4 Ligand
SC-67655 is a potent pentapeptide ligand targeting the MHC class II haplotype DR4 (DR4 Dw4 or DRB 1*0401) with an IC50 of 50 nM. This stable compound is suitable for research applications focusing on autoimmune diseases, facilitating the exploration of immune responses and potential therapeutic interventions. -
Anti-inflammatory Agent
NPB-1575 is a potent, orally bioavailable anti-inflammatory agent that effectively targets neuroinflammation. It functions by activating the IRS2/Nrf2/NF-κB signaling axis, thereby combating ferroptosis and providing neuroprotection. NPB-1575 demonstrates efficacy in mitigating cerebral ischemic injury and enhancing neurological outcomes, making it a valuable tool for research focused on ischemic stroke and related neurodegenerative conditions. -
Nrf2 Activator/ROS Inhibitor
L-Cystine disodium monohydrate primarily functions as an Nrf2 activator and ROS inhibitor. It elevates Nrf2 protein expression and activates the Nrf2 transcription factor, leading to reduced reactive oxygen species (ROS) generation and protection against apoptosis caused by oxidants and Doxorubicin. Additionally, when combined with L-theanine, it enhances the production of antigen-specific IgG by increasing glutathione levels and promoting T helper 2-mediated responses in mice. This compound is valuable for research into cystinuria and the molecular mechanisms underlying kidney stone formation. -
Nrf2 Inhibitor
Nrf2-IN-4 is a potent Nrf2 inhibitor that induces ferroptosis through the inhibition of the Nrf2 pathway. By disrupting iron homeostasis and facilitating ferritin degradation, Nrf2-IN-4 triggers ferroptotic cell death. Additionally, it promotes lysosome activation by enhancing iron-dependent reactive oxygen species (ROS) production and acidification. Due to its significant antitumor efficacy, Nrf2-IN-4 is a valuable tool for studying breast cancer and exploring therapeutic strategies targeting the Nrf2 pathway. -
Nrf2 Activator/ROS Inhibitor
L-Cystine is an effective Nrf2 activator and reactive oxygen species (ROS) inhibitor. This extracellular form of L-Cysteine elevates Nrf2 protein expression and facilitates its transcriptional activity, thereby reducing ROS generation and providing protection against oxidant- or Doxorubicin-induced apoptosis. Additionally, L-Cystine has been shown to enhance antigen-specific IgG production and T helper 2 mediated responses through increased glutathione levels in murine models. This makes L-Cystine a valuable reagent for research in cystinuria and kidney stone formation. -
Nrf2-Gpx4 Activator
Gingerenone A is an Nrf2-Gpx4 activator that triggers ferroptosis in liver tissue, demonstrating significant potential for therapeutic intervention in liver damage. This compound exhibits notable anti-inflammatory, anti-diabetic, anti-tumor, and pro-aging properties observed in murine models, making it valuable for research in oxidative stress regulation and associated diseases. Its oral bioactivity further enhances its applicability in in vivo studies. -
Nox2 Inhibitor
gp91 ds-tat is a specific inhibitor of NADPH oxidase 2 (Nox2), effectively blocking the production of superoxide generated by this enzyme. This bioactive peptide has demonstrated the ability to reduce reactive oxygen species (ROS), lipid peroxidation, and iron levels induced by high glucose conditions. Additionally, gp91 ds-tat inhibits homocysteine-induced activation of NLRP3 inflammasomes and restores the activity of lysosomal TRPML1 channels. Research applications include studies on Alzheimer's disease, glomerular inflammation, and cardiovascular disease, with implications for improving cerebrovascular and cognitive functions in APP/PS1 mouse models. -
Endogenous Metabolite; Nrf2 Activator; ROS Inhibitor
L-Cystine hydrochloride is an endogenous metabolite that serves as a potent Nrf2 activator and reactive oxygen species (ROS) inhibitor. It enhances Nrf2 protein expression, facilitating transcriptional responses that combat oxidative stress. Research indicates that L-Cystine hydrochloride reduces ROS generation and protects cells from apoptosis induced by oxidants or Doxorubicin. Additionally, its combination with L-theanine has been shown to boost antigen-specific IgG production by elevating glutathione levels and promoting T helper 2 (Th2) responses. This compound has significant potential for studying cystinuria and kidney stone formation. -
Nucleoside Reverse Transcriptase Inhibitor
Stavudine is an orally active nucleoside reverse transcriptase inhibitor (NRTI) that selectively targets HIV-1 and HIV-2. In addition to its antiviral properties, Stavudine inhibits mitochondrial DNA replication and has been shown to reduce NLRP3 inflammasome activation while modulating Amyloid-β autophagy. Furthermore, Stavudine is associated with the induction of apoptosis, making it a valuable tool for research in HIV treatment and cellular apoptosis mechanisms. -
Keap1/Nrf2 Activator
Sweroside, a potent Keap1/Nrf2 activator, is an iridoid glycoside that enhances Nrf2 nuclear translocation by competing with Keap1. This compound exhibits diverse biological activities, including antioxidant, anti-inflammatory, and anti-apoptotic effects, while regulating lipid metabolism. Sweroside's ability to inhibit oxidative stress and NLRP3-mediated pyroptosis, alongside its activation of the SIRT1 and AMPK/mTOR pathways, makes it valuable for investigating conditions such as myocardial ischemia-reperfusion injury, leukemia, acute lung injury, and non-alcoholic fatty liver disease. -
Anti-inflammatory Agent
Ligustrazine, an alkylpyrazine derived from Ligusticum chuanxiong, functions primarily as an anti-inflammatory agent. This compound has demonstrated notable anti-inflammatory and potential nootropic activities in preclinical studies with rat models. It is utilized in research focused on inflammatory pathways and cognitive enhancement, providing valuable insights into therapeutic applications in neuroprotection and inflammation modulation. -
Anti-inflammatory Agent
Lutein, a xanthophyll carotenoid, acts as a potent anti-inflammatory agent. It demonstrates significant biological activities, including antioxidant and anti-apoptotic effects, primarily by modulating reactive oxygen species (ROS) levels. Lutein is particularly noted for its protective benefits on ocular health and exhibits neuroprotective and antidepressant-like effects in the brain. This compound is biologically active when administered orally, making it a valuable reagent for studies in inflammation and neuroprotection. -
Keap1-Nrf2 Agonist
Methyl 3,4-dihydroxybenzoate functions as a Keap1-Nrf2 agonist, promoting the activation of the Nrf2 pathway. This compound exhibits significant antioxidant and anti-inflammatory properties, making it valuable in research focused on oxidative stress and cellular defense mechanisms. It is primarily utilized in studies investigating the neuroprotective effects of polyphenols and their potential therapeutic applications in various diseases. -
COX Inhibitor
[8]-Shogaol is a potent inhibitor of cyclooxygenase (COX), specifically targeting COX-2 with an IC50 of 17.5 μM. This compound exhibits significant antiplatelet properties (IC50=5 μM) and demonstrates anti-cancer and anti-inflammatory activities. Additionally, [8]-Shogaol modulates key signaling pathways by inhibiting TAK1, IKK, and Akt, thereby influencing MAPK signaling and alleviating synovitis. Its unique pharmacological profile makes it a valuable reagent for research in cancer, inflammation, and cardiovascular diseases. -
COX Inhibitor
Diclofenac potassium is a potent nonselective inhibitor of cyclooxygenase (COX) enzymes, demonstrating IC50 values of 4 nM for human COX-1 and 1.3 nM for human COX-2 in CHO cells, along with 5.1 μM and 0.84 μM for ovine COX-1 and COX-2, respectively. This reagent exhibits significant anti-inflammatory properties and is particularly effective in inducing apoptosis in neural stem cells through the activation of the caspase cascade. It is widely used in research studies focusing on inflammatory pathways and neural stem cell biology.
