CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS[1].
Biotin-PEG2-acid is a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Regaloside C is a glycerol glucoside isolated from the bulbs of Lilium genus with anti-inflammatory activities. Regaloside C has cardiomyocyte protective activity by protecting the mitochondria in H2O2-induced heart H9C2 cells[1].
Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.
Anti-inflammatory agent 32 (compound C3) has anti-oxidative and anti-inflammatory activity. Anti-inflammatory agent 32 can be used for skin care products research and development[1].
RXFP1 receptor agonist-4 (Example 268) is a RXFP1 receptor agonist. RXFP1 receptor agonist-4 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 4.9 nM[1].
α-Truxillic acid is form by the dimerization of two molecules of α-trans-cinnamic acid, with anti-inflammatory activities[1].
MTL-CEPBA is a small activating RNA targeting for upregulation of C/EBPα. MTL-CEPBA has anti-inflammatory and anti-cancer activity[1].
Nagarine, an alkaloid isolated from the roots of Aconitum nagarum Stapf (Ranunculaceae), is used to treat Rheumatic and neuralgic disorders[1].
Yohimbic acid is an amphoteric demethylated derivative of Yohimbine. Yohimbic acid exhibits vasodilatory action, and has the potential for osteoarthritis (OA) research[1][2][3].
Diacetoxyscirpenol (DAS) is a trichothecene mycotoxin, a secondary metabolite product of fungi. Diacetoxyscirpenol (DAS) consumption induces haematological disorders (neutropenia, aplastic anemia) in human and animals[1].
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells[1][2].
7ß,27-Dihydroxycholesterol (7β, 27-OHC) is a potent and selective activator of RORγt (Ki=120 nM). 7ß,27-Dihydroxycholesterol promotes the differentiation of mouse and human CD4+ Th17 cells. 7ß,27-Dihydroxycholesterol also increases the production of IL-17 depended on CYP27A1[1].
DSG Crosslinker is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
β-Tocotrienol is one form of vitamin E. β-Tocotrienol is a less potent antioxidant than α-tocotrienol[1].
LTB4 antagonist 3 (compound 24e) is a leukotriene B4 (LTB4) antagonist with an IC50 value of 477 nM. LTB4 antagonist 3 has anti-inflammatory activity[1].
PGN36 (Compound 18) is a selective cannabinoid CB2 receptor (CB2R) antagonist with a Ki of 0.09 µM[1].
Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
CP-195543 is a potent, selective and orally active leukotriene B4 (LTB4) receptor antagonist with IC50s of 6.8, 37.0 nM for human neutrophils and murine spleen membranes, respectively. CP-195543 blocks CD11b up-regulation. CP-195543 inhibits LTB4-mediated neutrophil infiltration[1].
Lupenone, isolated from Rhizoma Musae, belongs to lupane type triterpenoids. Lupenone shows various pharmacological activities including anti-inflammatory, anti-virus, anti-diabetes, anti-cancer, improving Chagas disease without major toxicity[1][2].
CGP 53716 is a potent protein tyrosine kinase inhibitor. CGP 53716 has selective activity of platelet-derived growth factor (PDGF) receptor. CGP 53716 can be used in the study of disease induced by abnormal cell proliferation induced by PDGF receptor activation [1].
Visnagin, an antioxidant furanocoumarin derivative, possess anti-inflammatory and analgesic properties. Visnagin has substantial potential to prevent Cerulein induced acute pancreatitis (AP). Visnagin possess promising vasodilator effects in vascular smooth muscles[1][2].
tracurium (BW-33A free acid) is a potent, competitive and non-depolarizing neuromuscular blocking agent.Atracurium also is an AChR receptor antagonist. Atracurium induces bronchoconstriction and neuromuscular blockade. Atracurium promotes astroglial differentiation[1][2][3][4][5].
AZD7986 is a Dipeptidyl peptidase 1 (DPP1) inhibitor with pIC50s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, dog and rabbit, respectively.
HCH6-1 is a competitive antagonist of Formyl peptide receptor 1 (FPR1), inhibits superoxide anion generation, elastase release, and chemotaxis in human neutrophils activated by fMLF (an FPR1 agonist). HCH6-1 can be used to treat neutrophilic inflammatory disease due to its inhibitory effects in neutrophil-like cells[1].
ASK1-IN-4 (Compound 17) is an ASK1 inhibitor (IC50=0.2 μM). ASK1-IN-4 interacts with ATP-binding site of ASK1[1].
PROTAC IRAK4 degrader-2 (Compound 9) is a PROTAC-based IRAK4 degrader that affords potent IRAK4 degradation with a DC50 in peripheral blood mononuclear cells (PBMCs) cells of 151 nM. PROTAC IRAK4 degrader-2 induce a reduction of IRAK4 protein levels with a DC50 of 36 nM in PBMC cells. PROTAC IRAK4 degrader-2 also leads to the inhibition of multiple cytokines in PBMCs[1].
PCTR1 is a potent monocyte/macrophage agonist, regulating key anti-inflammatory and pro-resolving processes during bacterial infection. PCTR1 is a member of the protectin family of specialized pro-resolving mediators (SPMs)[1].
N3-PEG3-CH2CH2COOH a PEG-based PROTAC linker can be used in the synthesis of BI-3663 (HY-111546), BI-4216 and BI-0319. Azido-PEG3-acid is also a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
A novel allosteric, noncompetitive dual CXCR1/2 inhibitor that inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 in vitro with IC50 of 0.7 nM; prevents PMN infiltration and tissue damage in several models of IR injury in vivo; abrogates motility and induces apoptosis in cultured cutaneous and uveal melanoma cells and xenografts; also prevents inflammation-mediated damage in MLD-STZ, prevents and reverses diabetes in NOD mice. Diabetes Phase 2 Clinical