Galicaftor (ABBV-2222; GLPG-2222) is a potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. Galicaftor can be used for cystic fibrosis research[1].
Atibuclimab, is a chimeric monoclonal antibody directed against CD14 and is composed of murine variable and human IgG4 Fc regions. Atibuclimab can be used for the research of amyotrophic lateral sclerosis[1]. Atibuclimab attenuates LPS-induced symptoms and strongly inhibits LPS-induced proinflammatory cytokine release, while only delaying the release of the anti-inflammatory cytokines soluble TNF receptor type I and IL-1 receptor antagonist[2].
Arachidonic acid is an essential fatty acid and a major constituent of biomembranes.
L-693612 hydrochloride (Compd 1) is an orally active and topical carbonic anhydrase inhibitor[1].
Fibronectin, a glycoprotein (~500 kDa) present in blood as well as in cells, is a biomarker of tissue injury. Fibronectin binds to membrane-spanning receptor proteins called integrins. Fibronectin also binds to other extracellular matrix proteins such as collagen, fibrin, and heparan sulfate proteoglycans[1].
Cyclobuxine D is a steroidal alkaloid extracted from Buxus microphylla. Cyclobuxine D has a significant bradycardic effect in the rat heart and an inhibitory action on acetylcholine and Ba++−induced contraction of the longitudinal muscle isolated from the rabbit jejunum[1][2].
APX-115 (Ewha-18278) 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. APX-115 can protect ovariectomy-induced osteoporosis and type 2 diabetes-induced renal injury. APX-115 effectively prevents kidney injury such as albuminuria, glomerular hypertrophy, tubular injury, podocyte injury, fibrosis, and inflammation as well as oxidative stress in diabetic mice[1].
BPK-21, an active acrylamide, suppresses T cell activation through blockade of ERCC3 function. BPK-21 specifically targets C342 in the helicase ERCC3[1].
Ebselen is a small-molecule capsid Inhibitor of HIV-1 replication.Target:Ebselen is an organoselenium compound, as an inhibitor of HIV-1 capsid CTD dimerization. Ebselen inhibits early viral postentry events of the HIV-1 life cycle by impairing the incoming capsid uncoating process. [1] Ebselen is a non-toxic seleno-organic drug with anti-inflammatory and antioxidant properties. Ebselen is an inhibitor of inositol monophosphatase (IMPase). Ebselen permeates the blood-brain barrier and inhibits endogenous inositol monophosphatase in mouse brain. [2]
Benralizumab (MEDI-563) is an interleukin-5 receptor α (IL-5Rα)-directed cytolytic monoclonal antibody that induces direct, rapid and nearly complete depletion of eosinophils via enhanced antibody-dependent cell-mediated cytotoxicity. Benralizumab can be used to treat severe eosinophilic asthma[1].
SIRT5 Inhibitor 6 is a potent, substrate-competitive and selective SIRT5 inhibitor with an IC50 of 3.0 μM. SIRT5 Inhibitor6 has a therapeutic potential against septic AKI in vivo[1].
Tormentic acid, a triterpene isolated from Rosa rugosa, exerts anti-inflammatory, antihyperlipidemic, and anti-atherogenic properties[1][2].
Tavilermide is a selective, partial agonist of TrkA, or a nerve growth factor (NGF) mimetic.
CGI-1746 is a potent and highly selective inhibitor of the Btk with IC50 of 1.9 nM.
c-FMS inhibitor is a novel c-Fms kinase inhibitor with a potential as anti-inflammatory agent and antirheumatic agent.IC50 value:Target: c-Fms
RIPK2 inhibitor OD36 is a potent, specific, ATP-competitive inhibitor of RIPK2 with IC50 of 5.3 nM, inhibits Tyr and Ser/Thr-directed activities of RIPK2; inhibits both RIPK2 tyrosine autophosphorylation as well as downstream NF-κB and MAPK signaling induced by MDP, downregulates a panel of RIPK2 kinase-dependent genes; reduces cellular infiltration in an in vivo MDP-induced peritonitis model; also shows high affinity for cyclin G-associated kinase (GAK) with Ki of 3.8 nM.
ISO-1 is a macrophage migration inhibitory factor (MIF) antagonist with an IC50 of 7 μM.
Auraptene is the most abundant naturally occurring geranyloxycoumarin. Auraptene is primarily isolated from plants in the Rutaceae family, such as citrus fruits. Auraptene decreases the secretion of matrix metalloproteinase 2 (MMP-2) as well as key inflammatory mediators, including IL-6, IL-8, and chemokine (C-C motif) ligand-5(CCL5)[1].
Fmoc-Thr[GalNAc(Ac)3-α-D]-OH i a building block in the development of cancer vaccine.
JAK-IN-28 (Compound 111) is a JAK inhibitor. JAK-IN-28 can be used for research of cancer or inflammatory diseases[1].
HAMI3379 (HAMI-3379) is a potent and selective antagonist of cysteinyl leukotriene 2 (CysLT(2)) receptor, inhibits LTD4- and LTC4-induced intracellular calcium mobilization withIC50 of 3.8 nM and 4.4 nM respectively; exhibits very low potency on a recombinant CysLT(1) receptors (IC50>10 uM), does not exhibit any agonistic activity on both CysLT receptors; concentration-dependently inhibits and reverses the LTC(4)-induced perfusion pressure increase and contractility decrease in isolated Langendorff-perfused guinea pig hearts, protects against acute brain injury after focal cerebral ischemia in rats.
BN201 promotes neuronal differentiation, the differentiation of precursor cells to mature oligodendrocytes (EC50 of 6.3 μM) in vitro, and the myelination of new axons (EC50 of 16.6 μM). BN201 is able to cross the blood-brain barrier by active transport and activate pathways (IGF-1 pathway) associated with the response to stress and neuron survival. BN201 has potently neuroprotective effects[1].
4-Thiouridine 5′-triphosphate (4-Thio-UTP) tetralithium is a potent P2Y2 and P2Y4 receptor agonist, with EC50s of 35 and 350 nM for hP2Y2 and hP2Y4, respectively. 4-Thiouridine 5′-triphosphate tetralithium can be used in the study of crosslinking experiments, labeling of transcriptional complex[1][2].
MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively.
Seco-DUBA hydrochloride is a toxin for ADC drug SYD985[1].
Sotatercept (ACE-011) is a soluble activin receptor 2A (ACVR2A) type IgG Fc fusion protein. Sotatercept combines activin and growth differentiation factor to try to restore the balance between growth promotion and growth inhibition signal pathways. Sotatercept has potential application in pulmonary arterial hypertension, anemia, bone loss, erythropoiesis, multiple myeloma (MM) osteolytic lesions[1][2][3][4][5].
Cortisone is a 21-carbon steroid hormone. Cortisone is one of the main hormones released by the adrenal gland in response to stress. Target： In chemical structure, it is a corticosteroid closely related to cortisol. It is used to treat a variety of ailments and can be administered intravenously, orally,intraarticularly (into a joint), or transcutaneously. Cortisone suppresses the immune system, thus reducing inflammation and attendant pain and swelling at the site of the injury. Risks exist, in particular in the long-term use of cortisone. Cortisone, a glucocorticoid, and adrenaline are the main hormones released by the body as a reaction to stress. They elevate blood pressure and prepare the body for a fight or flight response.
Tabalumab (LY2127399) is a humanised anti-BAFF (B-cell activating factor) monoclonal antibody (IgG4 type) with neutralising activity against membrane bound and soluble BAFF. Tabalumab can be used in studies of autoimmune diseases such as rheumatoid arthritis, renal failure and systemic lupus erythematosus[1].
Vulpinic acid, a lichen metabolite, decreases H2O2-induced ROS production, oxidative stress and oxidative stress-related damages in human umbilical vein endothelial cells (HUVEC). Vulpinic acid is active against staphylococci, enterococci, and anaerobic bacteria.Vulpinic acid has the potential for atherosclerosis research[1][2].
EP4-IN-1 is a potent prostanoid EP4 receptor inhibitor. EP4-IN-1 is extracted from patent WO2023025270 (example 1), and exhibits prospect in tumor immunity and anti-inflammatory analgesia research[1].