Paquinimod is a S100A9 inhibitor, which prevents S100A9 binding to TLR-4.
Imvotamab (IGM-2323) is a CD20xCD3 bispecific IGM antibody with dual action mechanism. Imvotamab is used to induce physiological T cell activation to prevent over-stimulation and subsequent down-regulation of immune function. Imvotamab is currently being developed for the treatment of B-cell malignant tumors, multiple myeloma (MM) and non-Hodgkin's lymphoma (NHL)[1][2][3][4].
Org 48762-0 is a potent, orally active and selective p38 inhibitor with EC50 of 0.1 μM. Org 48762-0 reduces LPS-induced TNFα release and prevents bone damage in collagen-induced arthritis in mice[1].
B022 is a potent and selective NF-κB-inducing kinase (NIK) inhibitor with a Ki of 4.2 nM. B022 protects liver from toxin-induced inflammation, oxidative stress, and injury[1].
Tolfenamic Acid is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
BNTA is a small molecule with extracellular matrix (ECM) modulatory properties, and it facilitates cartilage structural molecule synthesis on chondrocytes by activating superoxide dismutase 3 (SOD3). BNTA is a potential therapeutic agent in osteoarthritis[1].
ODN 105870, a G-modified inhibitory oligonucleotide (INH-ODN), is a selective TLR7 inhibitor. ODN 105870 can be uesd for inflammatory immune responses research[1].
UK-432097 is a highly potent and selective A2AAR agonist with a pKi of 8.4 for human A2AAR. UK-432097 has anti-inflammatory and anti-aggregatory properties. UK-432097 has the potential for COPD (Chronic Obstructive Pulmonary Disease) research[1][2][3].
ROCK inhibitor-2 is a selective dual ROCK1 and ROCK2 inhibitor with IC50s of 17 nM and 2 nM, respectively[1].
Pam3CSK4 TFA is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2[1].
Meloxicam D4 is deuterium labeled Meloxicam. Meloxicam is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively[1].
(Rac)-Reparixin is the inactive isomer of Reparixin (HY-15251), and can be used as an experimental control. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
Chenodeoxycholic acid 3-sulfate is a bile acid. Chenodeoxycholic acid 3-sulfate level corresponds closely with the extent of hepatic dysfunction[1].
HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2[1].
MS012 is a potent and selective inhibitor of G9a-Like Protein (GLP) lysine methyltransferase with IC50 of 7 nM, shows >30-fold selectivity for GLP over G9a and other methyltransferases.
Kaempferol 3-O-sophoroside, a derivative of Kaempferol, is isolated from the leaves of cultivated mountain ginseng (Panax ginseng) with anti-inflammatory effects[1].
BMS-751324 is a novel clinical prodrug of BMS-582949, which is a highly selective p38α MAPK inhibitor with IC50 of 13 nM; BMS-751324 is effectively bioconverted into parent drug BMS-582949 in vivo by alkaline phosphatase and esterase in a stepwise manner; demonstrates similar efficacy in rat LPS-induced TNFα pharmacodynamic model and rat adjuvant arthritis model compared with BMS-582949; BMS-751324 is indeed effective in addressing the pH-dependent absorption issue associated with BMS-582949.
AY 254 is a potent PAR2 biased agonist. Selectively activates ERK1/2 signaling (EC50= 2 nM for ERK1/2 phosphorylation versus 80 nM for Ca2+release). Reduces cytoKi ne-induced caspase 3/8 activation, promotes scratch-wound healing, and induces IL-8 secretion, in human colorectal cancer (HT29) cellsin vitro.
Dipyrithione is a potent antimicrobial agent. Dipyrithione shows antifungal activity and antiproliferative activity. Dipyrithione induces apoptosis and cycle arrest at G1 phase. Dipyrithione shows anti-inflammatory activity in vivo. Dipyrithione shows anti-tumor activity. Dipyrithione has the potential for the research of dermatophytosis[1][2][3].
Ginsenoside Rk3 is present in the roots Panax notoginseng herbs. Ginsenoside Rk3 significantly inhibits TNF-α-induced NF-κB transcriptional activity, with an IC50 of 14.24±1.30 μM in HepG2 cells
(R)-L 888607 is the inactive isomer of L 888607 (HY-111271), and can be used as an experimental control. L 888607 is a potent, selective, stable and orally active CRTH2 agonist. L 888607 has high affinity for the human CRTH2 receptor with a Ki value of 4 nM. L 888607 can be used for the research of several physiological events and metabolite[1].
Chondroitin sulfate, one of five classes of glycosaminoglycans, has been widely used in the treatment of osteoarthritis. Chondroitin sulfate reduces inflammation mediators and the apoptotic process and is able to reduce protein production of inflammatory cytokines, iNOS and MMPs.
LDC1267 is a highly selective TAM(Tyro3, Axl and Mer) kinase inhibitor with IC50 of <5 nM/8 nM/29 nM for Tyro3,Axl and Mer respectively.IC50 value: <5 nM/8 nM/29 nM(Tyro3/Axl/Mer) [1]Target: TAM kinase inhibitorin vitro: LDC1267 preferentially inhibits Tyro3,Axl andMer at lownanomolarity, as determined by tracer-based binding assays. Treatment of NKG2D activated NK cells with LDC1267 indeed abolished the inhibitory effects of Gas6 stimulation;LDC1267 had no apparent additional effect in Cbl-b-deficient NK cells. in vivo: wild-type mice treated with LDC1267 showed enhanced cytotoxicity towardsRMAcells overexpressing the NKG2D ligand Rae-1 (RMA-Rae1) to the same extent as C373AKI/KI mice, but had no effect on the already enhanced NK cytotoxicity in Cbl-b-mutant mice. Challenged mice with B16F10 melanoma followedby intraperitoneal LDC1267 treatment. LDC1267 markedly reduced metastatic spreading ofmelanomas; NK1.1 depletion abolished the therapeutic benefits of LDC1267.
JPE-1375 is a complement C5a receptor 1 (C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 µM) and reduces TNF levels (EC50=4.5 µM) in mice. JPE-1375 can be used in studies of autoimmune and inflammatory diseases[1].
Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
MMG-11 is a potent and selective human TLR2 antagonist. MMG-11 inhibits both TLR2/1 and TLR2/6 signaling with an IC50 of 1.7 µM for Pam3CSK4-induced hTLR2/1 and 5.7 µM for Pam2CSK4-induced hTLR2/6 responses[1].
Evolitrine (7-Methoxydictamnine; Evolitrin) is isolated from Acronychia pedunculata and show anti-inflammatory and antifeedant activities[1].
Praeroside (Baihuaqianhuoside), a coumarin glycoside. Praeroside can be extracted from the root of Peucedanum praeruptorum and Heracleum dissectum. Praeroside shows anti-inflammatory activity in vitro. Praeroside can be used for the research of inflammation[1][2].
Rituximab (anti-CD20) is an anti-CD20 chimeric monoclonal antibody used to treat certain autoimmune diseases and types of cancer[1].