Centhaquine (Centhaquin; PMZ-2010) is a novel agent has the potential for treatment of haemorrhagic shock. Centhaquine (Centhaquin; PMZ-2010) can augment cardiac output, reduce systemic vascular resistance in haemorrhagic models[1][2].
Methylophiopogonanone A, a major homoisoflavonoid in Ophiopogon japonicas, has both anti-oxidative and anti-inflammatory properties[1].
AMG-47a is a potent inhibitor of Lck and T cell proliferation; exhibits anti-inflammatory activity (ED50 = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice.IC50 value: Target: Lck inhibitorIn several other in vitro assays, AMG-47a displays subnanomolar inhibition against Lck, and low (<10 nM) inhibition against other hard to inhibit kinases such as KDR and SRC and MAPK α (p38α). In addition, at slightly higher doses but well under 10 μM, AMG-47a effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2 μM. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.
Anifrolumab is a type I interferon (IFN) receptor antagonist, a human monoclonal antibody. Anifrolumab blocks the activity of type I interferon. Anifrolumab can be used in systemic lupus erythematosus (SLE) research[1][2].
Cimpuciclib is a cyclin-dependent kinase(CDK) inhibitor and antineoplastic[1].
Bempikibart (ADX-914) is a human anti-IL-7Rα antibody. Bempikibart can be used for the research of anti-inflammatory[1].
EO 1428 is a highly specific inhibitor of p38 of the aminobenzophenone class. EO 1428 (1 μM ) markedly attenuates LPS-induced tumor necrosis factor α-converting enzyme (TACE) activity up-regulation[1].
Caffeic acid is an inhibitor of both TRPV1 ion channel and 5-Lipoxygenase (5-LO).
Marstenacisside F1 (compound 1) is a polyoxypregnanoside with anti-inflammatory activity isolated from Marsdenia tenacissima. Marstenacisside F1 inhibits lipopolysaccharide-induced nitric oxide (NO) production in RAW 264.7 cells and is a derivative of Tenacigenin B.
(-)-Dihydroguaiaretic acid is a Lipoxygenase inhibitor that has antioxidant activity. (-)-Dihydroguaiaretic acid inhibits the oxidation of unsaturated fatty acids and removes free radicals. (-)-Dihydroguaiaretic acid also has anticancer activity with an IC50 value of 7.49 μM (A549 cells)[1][2].
(3S,4R)-Tofacitinib is an enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
ZD8321 is a potent inhibitor of human Neutrophil elastase (NE) with a Ki of 13±1.7 nM.
GW9578 is a subtype-selective PPARα agonist (EC50s of 5 and 50 nM for murine and human PPAR-α) with potent lipid-lowering activity[1][2].
EJMC-1 is a moderately potent TNF-α inhibitor with an IC50 value of 42 μM[1].
α-Demethylnaproxen is the major metabolite of Nabumetone (HY-B0559), Nabumetone is an orally active COX-2 inhibitor with anti-inflammatory activity[1][2].
ML 145 is a selective GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM, but not for the related GPR55 orphan receptor[1]. GPR35 is expressed by various cells of the immune system and it may has potential as a therapeutic target in inflammatory disease[2].
Dehydroperilloxin is a natural compound isolated from the dichloromethane extract of the stems of Perilla frutescens var. acuta. Dehydroperilloxin possesses inhibitory activity against cyclooxygenase-1, with the IC50 value of 30.4 μM[1].
Magnolol, a natural lignan isolated from the stem bark of Magnolia officinalis, is a dual agonist of both RXRα and PPARγ, with EC50 values of 10.4 µM and 17.7 µM, respectively.
Flurbiprofen axetil is a non-selective cyclooxygenase (COX) inhibitor. Flurbiprofen axetil has anti-inflammatory effect[1].
Z-DEVD-CMK is an irreversible inhibitor of most of the cathepsins in vitro[1].
D-Panthenol is the biologically-active alcohol of pantothenic acid, which leads to an elevation in the amount of coenzyme A in the cell.
Mongersen is a 21-mer phosphorothioate antisense oligonucleotide targeting the mRNA of the Smad7 protein, thus leading to suppression of TGF-β1 pathways and remission of Crohn's disease.
Tazarotene is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris.
CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist[1]. CRTh2 antagonist 3 (compound 4) also enhances the activity of PDK1 toward a short peptide substrate, with an EC50 of 2 μM and a Kd of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation[2].
Pogostone is isolated from patchouli with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 µg/ml [2]. Pogostone induces cell apoptosis and autophagy[2].
Wilfortrine is a bioactive sesquiterpene alkaloid. Wilfortrine exhibits immunosuppresive effects. Wilfortrine also can inhibit leukaemia cell growth in mice and shows anti-HIV activity[1].
CK-636 is a cell permeable inhibitor of Arp2/3 complex, that could inhibit actin polymerization, with IC50 values of 4 μM, 24 μM and 32 μM for human, fission yeast and bovine, respectively.
JAK3/BTK-IN-2 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-2 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 004)[1]
Anti-inflammatory agent 55 (compound 9j) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 0.8 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model[1].
COX-2-IN-20 (Compound 5d) is a selective and orally active COX-2 inhibitor with an IC50 of 17.9 nM. COX-2-IN-20 shows anti-inflammatory activity[1].