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Catalog No.
Product Name
Application
Product Information
Citations
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PGK1 Inhibitor
CBR-470-1 is a selective inhibitor of phosphoglycerate kinase 1 (PGK1), a key enzyme in the glycolytic pathway. This compound also acts as a non-covalent activator of Nrf2, enhancing the cellular defense mechanisms against oxidative stress. In cellular models, CBR-470-1 has demonstrated protective effects against MPP+-induced cytotoxicity in SH-SY5Y neuronal cells by activating the Keap1-Nrf2 signaling pathway. This dual functionality makes CBR-470-1 a valuable tool for research in metabolic regulation and neuroprotection. -
Keap1-Nrf2 PPI Inhibitor
NXPZ-2 is an orally active inhibitor of the Keap1-Nrf2 protein-protein interaction with a Ki value of 95 nM and EC50 values of 120 and 170 nM. It has demonstrated the ability to dose-dependently mitigate Aβ[1-42]-induced cognitive dysfunction and improve brain tissue pathology in Alzheimer's disease models by enhancing neuronal quantity and function. NXPZ-2 functions by inhibiting oxidative stress through increased expression of Nrf2 and promoting its translocation from the cytoplasm to the nucleus, supporting research into Keap1-Nrf2 interactions and Alzheimer’s disease. -
Keap1-Nrf2 PPI Inhibitor
Keap1-Nrf2-IN-13 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI), exhibiting an IC50 of 0.15 μM. This compound effectively disrupts the binding of Keap1 to Nrf2 by establishing hydrogen bonds with critical polar residues such as Asn414, Arg415, Arg483, and Gln530. Keap1-Nrf2-IN-13 is valuable for research focused on oxidative stress-related conditions and inflammatory diseases, including pulmonary fibrosis, chronic obstructive pulmonary disease (COPD), and various cancers. -
Keap1-Nrf2 Inhibitor
Toralactone is a selective inhibitor of the Keap1-Nrf2 pathway, which plays a crucial role in cellular antioxidant defense mechanisms. Originating from Cassia obtusifolia, Toralactone exhibits significant hepatoprotective effects mediated through Nrf2 activation. This compound is suitable for research applications focused on oxidative stress, hepatotoxicity, and the modulation of antioxidant responses in various biological systems. -
Keap1-Nrf2 Inhibitor
Nrf2 activator-12 is a potent activator of the Keap1-Nrf2 pathway, with an EC50 value of 83.5 nM. This compound demonstrates significant pharmacological effects, including the ability to reverse disease progression and mitigate demyelination in an experimental autoimmune encephalomyelitis mouse model. Nrf2 activator-12 is valuable for studies exploring oxidative stress responses and potential neuroprotective strategies in various neurological disorders. -
Keap1-Nrf2 PPI Inhibitor
Keap1-Nrf2-IN-9 is a selective inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI) with a reported IC50 of 0.575 μM. This compound enhances the expression of Nrf2 target genes, including heme oxygenase 1 (Hmox1), glutathione S-transferase P (GstP), and the modulatory and catalytic subunits of glutamate-cysteine ligase (Gclc and Gclm). Keap1-Nrf2-IN-9 exhibits low cytotoxicity in ARPE19 cells, making it a valuable tool for studies focused on oxidative stress and cellular defense mechanisms. -
FAP-PI3K Inhibitor
FAP-PI3KI1 is a fibroblast-activated protein (FAP) inhibitor that selectively targets the phosphoinositide 3-kinase (PI3K) pathway in FAP-expressing human cells. This compound effectively inhibits collagen synthesis and reduces collagen deposition, making it a valuable tool for research in idiopathic pulmonary fibrosis (IPF) and related fibrotic conditions. Its targeted action facilitates investigating the role of the PI3K signaling pathway in fibrosis and offers potential insights into therapeutic strategies for IPF. -
Tyrosinase Inhibitor, Glutathione Reductase Inhibitor, Dopachrome Tautomerase Cofactor, Melanocortin Receptor 1 and 4 Modulator, Eumelanogenesis Inhibitor, Hair Hypopigmentation Inducer, Hair Cycle Modulator, Antioxidant, Healing Accelerator, Tensile Strength Enhancer, Anti-inflammatory Agent
Zinc sulphate functions primarily as an inhibitor of tyrosinase and glutathione reductase, exhibiting significant modulation of melanocortin receptors 1 and 4. Its biological activities include inducing hair hypopigmentation, enhancing wound healing, and exhibiting antioxidant and anti-inflammatory properties. This compound is valuable for research applications focused on eumelanogenesis, hair follicle cycling, and the investigation of conditions such as benign gastric ulcers and rheumatoid arthritis. -
iNOS Inhibitor
Glycylglycine hydrochloride hydrate is an iNOS inhibitor that acts as a non-selective dipeptidase substrate. This compound is capable of passive diffusion across cell membranes, where it is hydrolyzed to glycine, playing a role in energy metabolism and antioxidant activities. Glycylglycine hydrochloride hydrate promotes the proliferation of spermatogonial stem cells and mitigates astrocyte overactivation while decreasing nitric oxide release. Additionally, it upregulates the expression of neurotrophic factors, aiding in nerve myelin repair. This reagent is suitable for research into male reproductive biology and the neuroprotective mechanisms in neurodegenerative diseases. -
AXL Inhibitor
Denfivontinib hydrochloride is an AXL inhibitor that exerts synergistic antitumor effects when used in combination with the PD-1 inhibitor Pembrolizumab. This compound enhances the NOD-like receptor pathway, facilitating the formation of the NLRP3 inflammasome. Its unique mechanism of action makes it a valuable tool for cancer research, particularly in studying immune modulation and tumor progression. -
CRBN Inhibitor
EM12-SO2F is a potent covalent inhibitor of the E3 ubiquitin ligase cereblon (CRBN), specifically binding to the histidine residue at position 353. This compound serves as a valuable chemical probe for studying CRBN-mediated pathways. EM12-SO2F effectively inhibits the lenalidomide-induced degradation of IKZF1 in MOLT4 cells, making it a useful tool for research in cancer biology and drug resistance. -
COX-1 Inhibitor
FR122047 (hydrochloride) is a selective inhibitor of cyclooxygenase-1 (COX-1) with an IC50 value of 28 nM. This compound exhibits antiplatelet, analgesic, and anti-inflammatory activities, making it a valuable tool for research in the fields of pain management and cardiovascular studies. Its ability to modulate COX-1 offers insights into the therapeutic targeting of inflammatory pathways. -
nNOS Inhibitor
2-Thiouracil is a selective inhibitor of neuronal nitric oxide synthase (nNOS), exhibiting a Ki value of 20 μM. It effectively antagonizes BH4-induced nNOS dimerization, thereby modulating nitric oxide synthesis in neuronal tissues. In addition to its role as an nNOS inhibitor, 2-Thiouracil also has antithyroid properties and serves as a specific marker for melanoma detection. Furthermore, it promotes root growth in pea and corn, making it a valuable tool for various agricultural and biochemical research applications. -
COX Inhibitor
Zaltoprofen is a non-steroidal anti-inflammatory drug (NSAID) that acts as a preferential inhibitor of cyclooxygenase-2 (COX-2), exhibiting IC50 values of 1.3 μM for COX-1 and 0.34 μM for COX-2. It demonstrates significant anti-inflammatory and analgesic properties, making it beneficial for the management of inflammatory pain. Zaltoprofen is utilized in research settings to explore mechanisms of inflammation and pain pathways. -
COX-1/COX-2 Inhibitor
6-Methoxy-2-naphthoic acid is a potent inhibitor of COX-1 and COX-2 enzymes. It effectively inhibits the synthesis of gastric mucosal prostaglandin E2, making it relevant in studies related to inflammation and pain-related conditions. Additionally, 6-Methoxy-2-naphthoic acid serves as an impurity in Naproxen and can be utilized in the synthesis of various active compounds, contributing to diverse research applications in pharmaceutical development. -
COX-2 Inhibitor
Parecoxib Sodium is a selective COX-2 inhibitor that effectively penetrates the blood-brain barrier and serves as a proagent for Valdecoxib. This nonsteroidal anti-inflammatory drug (NSAID) inhibits prostaglandin synthesis, making it suitable for the relief of acute postoperative pain as well as for managing symptoms associated with chronic inflammatory conditions, including osteoarthritis and rheumatoid arthritis. It has important applications in both clinical and preclinical research focused on pain management and inflammation. -
COX Inhibitor
Tolmetin sodium dihydrate is a potent non-steroidal anti-inflammatory drug (NSAID) that primarily targets cyclooxygenase (COX) enzymes, exhibiting IC50 values of 0.35 μM for human COX-1 and 0.82 μM for COX-2. This compound is commonly utilized in research related to inflammation and pain modulation. Its ability to effectively inhibit COX activity makes it valuable for studying various inflammatory pathways and developing new therapeutic strategies in pain management. -
iNOS Inhibitor
Glycylglycine, an iNOS inhibitor, is a dipeptide that serves as a non-selective glycylglycine dipeptidase substrate. It effectively crosses cell membranes through passive diffusion and is subsequently hydrolyzed to glycine, which participates in energy metabolism and antioxidant defense. This compound promotes the proliferation of spermatogonial stem cells (SSCs), mitigates astrocyte overactivation, and reduces nitric oxide (NO) release while enhancing the expression of neurotrophic factors such as PDGFA, FGF2, and CNTF, thereby supporting nerve myelin repair. Glycylglycine is valuable in research on male reproductive biology and neurodegenerative diseases, including the investigation of neuroprotective mechanisms in conditions like multiple sclerosis. -
COX Inhibitor
Hamaudol is a chromone derived from Saposhnikovia divaricata, acting as a potent inhibitor of cyclooxygenase (COX)-1 and COX-2, with IC50 values of 0.30 mM and 0.57 mM, respectively. This compound exhibits significant analgesic and anti-inflammatory properties, making it a valuable tool in research focused on pain relief and inflammation modulation. Hamaudol is suitable for investigations into COX inhibition and related biological pathways. -
Anti-inflammatory and Protein-Binding Inhibitor
4-Acetylaminoantipyrine is a derivative of antipyrine that functions primarily as an anti-inflammatory agent and a protein-binding inhibitor. It acts as a PGE2-dependent blocker and inhibits cyclooxygenase (COX), thereby modulating inflammatory pathways. Additionally, 4-acetylaminoantipyrine has the capability to inhibit Cu/Zn superoxide dismutase (Cu/ZnSOD) and can spontaneously bind with bovine serum albumin (BSA), resulting in conformational changes. This compound is valuable for research applications in inflammation and protein interaction studies. -
CCR5/CXCR4 Chemotaxis Inhibitor
Catenarin, an anthraquinone compound, serves as an inhibitor of CCR5 and CXCR4-mediated chemotaxis. It effectively reduces the phosphorylation of mitogen-activated protein kinases (p38 and JNK) and their upstream kinases (MKK6 and MKK7), as well as calcium mobilization. Catenarin demonstrates anti-inflammatory properties and inhibits leukocyte migration, contributing to its potential in diabetes research. Additionally, it exhibits significant antibacterial activity against Gram-positive bacteria and has been shown to prevent type 1 diabetes in nonobese diabetic mice. -
Pro-inflammatory Mediator Inhibitor
Heparin disaccharide III-S (trisodium) is a heparin-derived disaccharide that serves as a pro-inflammatory mediator inhibitor. It effectively inhibits the spontaneous secretion of interleukin-8 (IL-8) and interleukin-1 beta (IL-1β) in intestinal epithelial cells by acting at the post-translational level without affecting mRNA or intracellular mediator concentrations. This compound is useful for research on inflammatory responses and the regulation of cytokine secretion in intestinal models. -
Pro-inflammatory Mediator Inhibitor
Heparin disaccharide I-H (trisodium) is a heparin-derived disaccharide that acts as a pro-inflammatory mediator inhibitor. This compound effectively blocks the spontaneous secretion of IL-8 and IL-1β in intestinal epithelial cells at the post-translational level, while leaving mRNA expression levels and intracellular contents unaffected. Demonstrating dose-dependent anti-inflammatory activity, Heparin disaccharide I-H (trisodium) is valuable for research applications targeting intestinal inflammation and associated signaling pathways. -
Cyclophilin Inhibitor
RN-0001 is a potent inhibitor of cyclophilins, specifically demonstrating Ki values of 4.1 nM and 12.0 nM against Cyclophilin A (CypA) and Cyclophilin D (CypD), respectively. By directly binding to CypD, RN-0001 effectively inhibits its peptidyl-prolyl cis-trans isomerase activity, preventing mitochondrial permeability transition pore opening. This compound enhances mitochondrial function, diminishes reactive oxygen species (ROS) production, and downregulates lipogenic marker expression. Additionally, RN-0001 inhibits NF-κB p65 nuclear translocation and reduces the release of activated caspase-3 and cytochrome c, making it a valuable tool for investigating alcohol-associated liver disease. -
CXCR5 Inhibitor
YU241279 is a selective inhibitor of CXCR5, targeting the CXCL13-mediated signaling pathways. It effectively inhibits Gαq-dependent calcium influx and Gαi2-dependent cAMP reduction in CXCR5-expressing cells, leading to reduced proliferation of lymphoma cells. In preclinical studies, YU241279 demonstrated a significant reduction in tumor burden within the peripheral blood and bone marrow of mice with lymphoma. This compound is suitable for research into angioimmunoblastic T-cell lymphoma and Burkitt B-cell lymphoma. -
Ecto-5'-Nucleotidase Inhibitor
2,4-Dinitrobenzenesulfonic acid is an ecto-5'-nucleotidase (CD73) inhibitor with a Ki value of 63 μM for human enzymes and 144 μM for rat enzymes. This compound effectively inhibits the hydrolysis of adenosine monophosphate (AMP), preventing the production of adenosine. It is primarily utilized in cancer research to study the role of ecto-5'-nucleotidase in tumor biology and therapeutic resistance. -
COX Inhibitor
Methylhydroquinone is a potent COX inhibitor with noted activity against ovine COX-1 and human recombinant COX-2, exhibiting IC50 values of 480.7 μM and 52.2 μM, respectively. This compound demonstrates anti-inflammatory properties primarily through the inhibition of prostaglandin synthesis. Additionally, it has been associated with potential DNA-damaging effects, including the induction of DNA single-strand breaks. Methylhydroquinone functions by competitively binding to the active sites of COX-1, engaging in non-covalent interactions to exert its biological activities.
