Indomethacin sodium hydrate (Indometacin sodium hydrate) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin sodium hydrate disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
Mebhydrolin napadisylate is a specific histamine H1 receptor antagonist.
Lysicamine, a natural compound, possesses antibacterial, anticancer and anti-inflammation activity[1].
Thiomandelic acid is a broad spectrum inhibitor of Zinc -lactamases[1].
Adapalene(CD-271; Differin), a synthetic retinoid, is a retinoic acid receptor agonist (RAR).Target: Retinoic acid receptor agonist (RAR)Adapalene is a third-generation topical retinoid primarily used in the treatment of mild-moderate acne and is also used (off-label) to treat keratosis pilaris as well as other skin conditions. Adapalene is possibly more effective than tretinoin 0.025% gel in the treatment of acne vulgaris [1].Thirty-six rats of either sex were divided into six groups (two control groups, and an etodolac, indomethacin, tretinoin and adapalene group) of six animals each. Each group was given different drugs or chemicals. The inhibitory activities of the drugs were determined on carrageenan-induced rat-paw oedema. The inhibition rate (53.48%) in the tretinoin group was found to be higher thanadapalene and controls (P < 0.05). Adapalene was found to have an inhibition rate of 10.28%, and when compared with the other groups, was found to have no statistically significant anti-inflammatory activity [2].
Semapimod, an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod has potential in a variety of inflammatory and autoimmune disorders[1][2][3].
Picfeltarraenin IV, a triterpenoid obtained from Picriafel-terrae Lour (P.fel-terrae), is an acetylcholinesterase (AChE) inhibitor. Picfeltarraenin IV can be used for the treatment of herpes infections, cancer and inflammation[1].
Lacto-N-neotetraose (LNnT) is an endogenous metabolite. Lacto-N-neotetraose can inhibit TNF-α induced IL-8 secretion in immature epithelial cells. Lacto-N-neotetraose has anti-inflammatory avtivity, and can improve the wound closure[1][2][4].
Anti-osteoporosis agent-1 (comp 4aa) is a potent replication protein A (RPA) inhibitor (IC50=18 µM) [1].
Ozoralizumab (ATN-103) is an anti-TNFα humanized antibody. Ozoralizumab is a humanized trivalent nanobody compound that consists of two anti-human TNFα nanobodies and an anti-human serum albumin (HSA) nanobody. Ozoralizumab can be used in research of arthritis[1].
Resveratrol analog 1 is an analog of Resveratrol (HY-16561), compound 48. Resveratrol is a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties.
CU-CPT17e is a multi-Toll-like receptor (TLR) agonist that activates TLR3, TLR8, and TLR9.
Chitohexaose hexahydrochloride is a chitosan oligosaccharide with anti-inflammatory effect. Chitohexaose binds to the active sites of TLR4 and inhibits LPS induced inflammation[1][2].
JAK3/BTK-IN-4 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-4 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147953A1, compound 003)[1]
Peiminine(Verticinone; Raddeanine) is a natural compound with anti-inflammatory activity.IC50 value:Target:Peiminine and DXS significantly reduced alveolar inflammation and pulmonary interstitial inflammation in rats with bleomycin-induced lung injury. peiminine inhibits lung inflammation and pulmonary fibrosis in a rat model of bleomycin-induced lung injury, by reducing circulating IFN-γ levels and inhibiting signal transduction pathways involving TGF-β, CTGF, ERK1/2, NF-κB and FasL.
Ketotifen-d3 (HC 20511-d3) fumarate is the deuterium labeled Ketotifen fumarate. Ketotifen (HC 20511) fumarate is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer, which is used to prevent asthma attacks[1][2].
(Rac)-Bepotastine (besilate) is the inactive isomer of Bepotastine (besilate) (HY-A0015), and can be used as an experimental control. Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research[1][2][3][4].
Melittin is a PLA2 activator, stimulates the activity of the low molecular weight PLA2, while it does not the increase activity of the high molecular weight PLA2.
Enzyme-IN-1 (compound 1) is a peptide-based inhibitor of N-terminal nucleophile (Ntn) hydrolases. Specifically, Enzyme-IN-1 inhibits the chymotrypsin-like activity (CT-L) of the 20S proteasome. Enzyme-IN-1 may has potential antiinflammatory properties[1].
TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
ABT-510 acetate is an anti-angiogenic TSP peptide (Thrombospondin-1 analogue) that induces apoptosis and inhibits ovarian tumour growth in an orthotopic, syngeneic model of epithelial ovarian cancer. ABT-510 acetate also reduces angiogenesis and inflammatory responses in a murine model of inflammatory bowel disease. ABT-510 acetate can be used in studies of cancer (particularly epithelial ovarian cancer) and inflammatory bowel disease (IBD)[1][2].
Narchinol B (Compound 4) is a sesquiter penoid compound. Narchinol B has anti-inflammatory effects. Narchinol B works by inhibiting proinflammatory mediators, including prostaglandin E2 (PGE2), inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) proteins,as well as proinflammatory cytokines, such as interleukin-1b, IL-6, and tumor necrosis factor-α (TNF-α). Narchinol B significantly inhibits LPS-induced overproduction of NO in BV2 cells (IC50=2.43 μM)[1].
Avarofloxacin (JNJ-Q2) is a broad-spectrum fluoroquinolone antibacterial drug being developed for the treatment of acute bacterial skin and skin-structure infections and community-acquired pneumonia[1]. Avarofloxacin (JNJ-Q2) is an aminoethylidenylpiperidine fluoroquinolone that demonstrates antibacterial effect against numerous Gram-positive bacteria with a mean 0.12 mg/L MIC90 value[2]. Avarofloxacin (JNJ-Q2) has potential for treatment of methicillin-resistant Staphylococcus aureus (MRSA) infections[3].
Desfluoro-atorvastatin is an impurity of Atorvastatin[1]. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, has the ability to effectively decrease blood lipids[2].
DMT1 blocker 1 is a blocker of divalent metal transporter 1 (DMT1) with an IC50 of 0.64 μM, is expected to block iron uptake by enterocytes in vivo[1].
Procyanidin A2 is a flavonoid found in cranberries and lingonberries, with anti-cancer, antioxidant, antimicrobial and anti-inflammation activity[1][2].
HA-155 is a potent and selective autotaxin (ATX) inhibitor with an IC50 of 5.7 nM[1][2][3].
Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells[1][2].
1,1-Diphenyl-4-(pyrrolidin-1-yl)but-2-yn-1-ol is an anticholinergic agent. 1,1-Diphenyl-4-(pyrrolidin-1-yl)but-2-yn-1-ol has the potential for the research of bronchial asthma[1].