β-Aminoarteether (SM934 free base) is an Artemisinin derivative with orally active. β-Aminoarteether can be used for inflammation and autoimmune disease research, such as lupus diseases[1].
PI3K-IN-38 (compound 123) is an orally active PI3K inhibitor with IC50 of 0.541 µM (PI3K-α). PI3K-IN-38 shows activities of anticancer and anti-inflammatory, which inhibis tumor growth in vivo[1].
Simeton-acetic acid is an immunizing hapten that can be coupled with bovine serum albumin. Simeton-acetic acid-BSA can produce PcAbs obtained with titer 1.0×103[1].
c-Fms-IN-12 is a c-Fms inhibitor extracted from patent WO2011079076A1, Compound Example 65, has an IC50 of 93.6-283.7 nM[1].
MS417 is a BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM).
Larazotide acetate is a synthetic peptide that functions as a tight junction regulator and reverses leaky junctions to their normally closed state.
Concanavalin A is a Ca2+/Mn2+-dependent and mannose/glucose-binding plant lectin that can be found in jack bean. Concanavalin A can induce programmed cell death[1].
Anumigilimab (CSL-324) is an humanized IgG2a mAb against human granulocyte colony-stimulating factor (G-CSF) receptor. Anumigilimab can be used for increasing numbers of neutrophils at sites of inflammation[1][2].
RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1) with an IC50 of 13 nM.
SPL-410 is an orally active, highly potent and selective hydroxyethylamine based SPPL2a (Signal Peptide Peptidase Like 2a) inhibitor, with an IC50 of 9 nM[1].
Perakine is an indole alkaloid isolated from Alstonia yunnanensis. Anti-inflammatory activities[1].
7-Deoxy-trans-dihydronarciclasine, an alkaloid, is a tobacco mosaic virus (TMV) inhibitor (IC50: 1.80 μM). 7-Deoxy-trans-dihydronarciclasine is an anti-neuroinflammatory agent. 7-Deoxy-trans-dihydronarciclasine decreases the Aβ and APP levels in the cerebral cortex of Tg2576 mice[1][2][3].
hPGDS-IN-1 is a hPGDS inhibitor ,with IC50 of 12 nM in the Fluorescence Polarization Assay or the EIA assay.IC50 value: 12 nMTarget: hPGDSThe detailed information please refer to WO2011044307A1 and WO2010080563A2
Licofelone-d4 (ML-3000-d4) is the deuterium labeled Licofelone. Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[1][2][3].
DiMNF (3',4'-Dimethoxy-αNF) is a selective aryl hydrocarbon receptor (AHR) modulator. DiMNF is a competitive AHR ligand (IC50 = 21 nM) with apparent antagonistic activity. DiMNF can be used as an anti-inflammatory agent[1].
Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα. Highly effective in inhibiting IFNγ production in a rat pharmacodynamics model and fully efficacious in a rat adjuvant arthritis model[1].
MAPK-IN-1 (Compound 2) is a MAPK signaling pathway inhibitor. MAPK-IN-1 exhibits AChE inhibitory activity with an IC50 of 23.84 μM. MAPK-IN-1 shows anti-neuroinflammatory and neuroprotective activity and can be used for Alzheimer's disease research[1].
Tamuzimod is a potent immunomodulator. Tamuzimod has S1P Receptor modulatory activity with EC50s <1 μM[1][2].
SBFI-26 is a selective and competitive inhibitor of fatty acid binding proteins FABP5 and FABP7, with Kis of 0.9 µM and 0.4 µM for FABP5 and FABP7, respectively. SBFI-26 produces anti-nociceptive and anti-inflammatory effects[1][2].
Saponins are a class of chemical compounds of glycosides found in particular abundance in various plant species. In plants, saponins may serve as anti-feedants, and to protect the plant against microbes and fungi[1].
Talizumab (TNX 901) is an anti-IgE humanized IgG1 monoclonal antibody[1].
Tibulizumab (LY 3090106) is a tetravalent bispecific monoclonal antibody targeting B-cell activating factor (BAFF) and IL-17A with Kd values of 60 pM and 14 pM, respectively. Tibulizumab can be used for autoimmune disease research[1].
Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1 inhibitor with an IC50 of 1.44 nM. Mofezolac shows weak inhibitory activity on COX-2 (IC50 of 447 nM). Mofezolac can relieve pain and has anti-inflammatory activities[1].
Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4][5].
GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3[1].
12R-LOX-IN-1 (Compound 4a) is a 12R-LOX inhibitor (IC50: 28.25 μM). 12R-LOX-IN-1 inhibits the hyper-proliferative state and colony forming potential of Imiquimod (HY-B0180)-induced psoriatic keratinocytes. 12R-LOX-IN-1 inhibits reactive oxygen species, Ki67, IL-17A, TNF-α and IL-6 production. 12R-LOX-IN-1 can be used for antipsoriatic research[1].
(2S)-2'-Methoxykurarinone, a compound isolated from the roots of Sophora flavescens, has anti-inflammatory, antipyretic, antidiabetic, and antineoplastic effects. (2S)-2'-Methoxykurarinone (MK) inhibits osteoclastogenesis and bone resorption through down-regulation of RANKL signaling. (2S)-2'-Methoxykurarinone (MK) displays cytotoxic activity against human myeloid leukemia HL-60 cells[1][2].
Soyasaponin II is a saponin with antiviral activity. Soyasaponin II inhibits the replication of HSV-1, HCMV, influenza virus, and HIV-1. Soyasaponin II shows potent inhibition on HSV-1 replication. Soyasaponin II serves as a inhibitor for YB-1 phosphorylation and NLRP3 inflammasome priming and could protect mice against LPS/GalN induced acute liver failure[1][2].
W-54011 is a potent, specific, and orally active CD88 (C5a receptor) antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM.IC50 value: 2.2 nM (Ki)Target: CD88 (C5a receptor)in vitro: W-54011 also inhibits C5a-induced intracellular Ca2+ mobilization, chemotaxis, and generation of reactive super oxide species in human neutrophils with IC50 alues of 3.1, 2.7, and 1.6 nM, respectively. In C5a-induced intracellular Ca2+ obilization assay with human neutrophils, W-54011 does not show agonistic activity at up to 10 μM and shifts rightward the concentration-response curves to C5a without depressing the maximal responses. in vivo: Examination on the species specificity of W-54011 reveals that it was able to inhibit C5a-induced intracellular Ca2+ mobilization in neutrophils of cynomolgus monkeys and gerbils but not mice, rats, guinea pigs, rabbits, and dogs. In gerbils, oral administration of W-54011 (3-30 mg/kg) inhibits C5a-induced neutropenia in a dose-dependent manner. The present report is the first description of an orally active non-peptide C5a receptor antagonist that could contribute to the treatment of inflammatory diseases mediated by C5a.
Neocryptotanshinone, a fatty diterpenoids from Salvia Miltiorrhiza, inhibits lipopolysaccharide-induced inflammation by suppression of NF-κB and iNOS signaling pathways[1][2].