Dazcapistat is a potent calpain inhibitor, with IC50s of <3 μM for calpain 1, calpain 2 and calpain 9, respectively (patent WO2018064119A1, compound 405)[1].
TLR4-IN-C34-C2-COO is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis[1].
Handle region peptide, rat is a prorenin receptor antagonist, suppresses the progression of diabetic nephropathy and has anti-inflammatory in the eye.
Verbascoside is isolated from Lantana camara, acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 µM, and has antitumor, anti-inflammatory and antineuropathic pain activity.
(Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation[1].
Orismilast (LEO-32731) is a PDE4 inhibitor used for the research of inflammatory diseases[1].
Priliximab (CEN 000029) is an anti-CD4 humanized monoclonal antibody. Priliximab binds to CD4 on the surface of T cells, resulting in a significant and sustained reduction in circulating CD4+ T cells. Priliximab can be used in research of rheumatoid arthritis (RA)[1].
PG106 is a potent and selective human melanocortin 3 (hMC3) receptor antagonist (IC50=210 nM) and has noactivity at hMC4 receptors (EC50=9900 nM) and hMC5 receptor[1].
4-Hydroxybenzyl alcohol is a phenolic compound widely distributed in various kinds of plants. Anti-inflammatory, anti-oxidant, anti-nociceptive activity. Neuroprotective effect. Inhibitor of tumor angiogenesis and growth[1][2][3][4].
Saponarin is a natural flavonoid isolated from Gypsophila trichotoma, with antioxidant, anti-inflammatory and hepatoprotective activities. Saponarin activates AMPK in a calcium-dependent manner, thus regulating gluconeogenesis and glucose uptake[1][2][3].
MRS4620 is a potent CD73 inhibitor, with a Ki of 0.436 nM. MRS4620 can be use for the research of cancer immunotherapy[1].
Cannflavin B is a prenylated flavone, which can be isolated from Cannabis sativa L. Cannflavin B has anti-inflammatory activity[1].
JAK3/BTK-IN-1 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-1 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 002)[1].
Aurantiamide is an orally active constituent of Portulaca oleracea L and has various biological activities, including antioxidant, antiplatelet, anti-inflammatory, and antitumor activities[1].
UCB-35440, a 5-lipoxygenase inhibitor and a histamine H1 receptor antagonist, is used potentially for the treatment of dermatitis.
SR121566A is a novel non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, which can inhibit ADP-, arachidonic acid- and collagen-induced human platelet aggregation with IC50s of 46±7.5, 56±6 and 42±3 nM, respectively.
CTCE-0214 is a chemokine CXC receptor 4 (CXCR4) agonist, SDF-1α (stromal cell-derived factor-1α) peptide analog. CTCE-0214 shows anti-inflammatory activity, and can be used in inflammation sepsis and systemic inflammatory syndromes research[1][2][3].
Vanilloid receptor antagonist 1 is a potent vanilloid receptor TRPV1 antagonist extracted from patent US8349852B2, compound B8[1].
GSK-199 hydrochloride is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 250 nM in FP binding assay (0.2 mM Ca), 200 nM in PAD4 NH3 release inhibition assay; shows high specificity for PAD4 over PAD1/2/3/6; affects cellular citrullination and mimic the deficiency in NET production in mice; significantly decreases in complement C3 deposition in both synovium and cartilage in mice.
(Rac)-Etodolac-d3 ((Rac)-AY-24236-d3) is a labelled racemic Etodolac. Etodolac (AY-24236) is a non-steroidal anti-inflammatory compound that is a non-selective inhibitor of COX (IC50=53.5 nM)
KCL-440 is a CNS-penetrated PARP inhibitor, with an IC50 of 68 nM. KCL-440 has strong inhibition of PARP-1[1][2].
DHODH-IN-13 (Compound 7a) is a hydroxyfurazan analog of A771726. DHODH-IN-13 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 4.3 μM for rat liver DHODH. DHODH-IN-13 can be used for rheumatoid arthritis[1].
c-Fms-IN-13 (compound 14) is a potent FMS kinase inhibitor with an IC50 value of 17 nM. c-Fms-IN-13 can be used as an anti-inflammatory agent[1].
Citral is a monoterpene found in Cymbopogon citratus essential oil, with antihyperalgesic, anti-nociceptive and anti-inflammatory effects[1].
RCGD423 is a gp130 modulator, which prevents articular cartilage degeneration and promotes repair.
Resolvin D1 (RvD1), an endogenous pro-resolving mediator of inflammation, is derived from omega-3 docosahexaenoic acid during the resolution phase of acute inflammation. Resolvin D1 blocks proinflammatory neutrophil migration by regulating actin polymerization, reduces TNF-α–mediated inflammation in macrophages, and enhances phagocytosis of apoptotic cells by macrophages[1][2].
ARN 077 is a potent and selective N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 7 nM for human NAAA[1]. ARN 077 significantly increases palmitoyl ethanolamine (PEA) levels within the CNS and has broad antinociceptive activity in mice and rats[2].
Prednisone (Adasone) is a synthetic corticosteroid agent that is particularly effective as an immunosuppressant compound.Target: OthersPrednisone is a synthetic corticosteroid drug that is particularly effective as an immunosuppressant drug. It is used to treat certain inflammatory diseases (such as moderate allergic reactions) and (at higher doses) some types of cancer, but has significant adverse effects. Because it suppresses the immune system, it leaves patients more susceptible to infections.Prednisone can also be used in the treatment of decompensated heart failure to potentiate renal responsiveness to diuretics, especially in heart failure patients with refractory diuretic resistance with large dose of loop diuretics. The mechanism is prednisone, as a glucocorticoid, can improve renal responsiveness to atrial natriuretic peptide by increasing the density of natriuretic peptide receptor type A in the renal inner medullary collecting duct, inducing a potent diuresis.
4-CPPC is the first reversible and selective inhibitor of pro-inflammatory protein macrophage migration inhibitory factor-2 (MIF-2) with Ki of 33 uM, 13-fold selectivity for human MIF-2 versus human MIF-1.
κ-Carrageenan is a natural polymer which predominantly available in red seaweeds. κ-Carrageenan is an effective drug carrier to deliver curcumin in cancer cells and to induce apoptosis. κ-carrageenan serves as a potential inflammatory agent that magnifies existing intestinal inflammation[1][2].