Aspartyl-alanyl-diketopiperazine (DA-DKP) is an immunomodulatory molecule generated by cleavage and cyclization from the N-terminus of human albumin and can modulate the inflammatory immune response through a molecular pathway implicated in T- lymphocyte anergy[1][2].
Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects[1].
hDDAH-1-IN-1 TFA (compound 8a) is a potent and selective non-amino acid catalytic site inhibitor of human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1), with a Ki of 18 µM[1].
2-Hydroxycinnamaldehyde is a phenylpropanoid that can be isolated from the bark of Cinnamomum cassia. 2-Hydroxycinnamaldehyde inhibits Wnt/β-catenin, STAT3 signaling. 2-Hydroxycinnamaldehyde induces cell apoptosis 2-Hydroxycinnamaldehyde has antitumor and anti-inflammation activities[1][2][3].
Lysostaphin is an antistaphylococcal agent. Lysostaphin has activities of three enzymes namely, glycylglycine endopeptidase, endo-β-N-acetyl glucosamidase and N-acteyl muramyl-L-alanine amidase[1].
MLN 3897 is a potent, specific and orally active antagonist of CCR1 with IC50 of 0.8 nM in competition binding assays, 500-fold selectivity over CCR5; inhibits osteoclastogenesis and OC activity by impairing multinucleation and by down-regulation of c-fos signaling, inhibits osteoclastogenesis and OC activity by impairing multinucleation and by down-regulation of c-Fos signaling; demonstrates potential for the treatment of multiple sclerosis and rheumatoid arthritis. Multiple Sclerosis Phase 1 Discontinued
Guanosine 5'-diphosphate-15N5 (GDP-15N5) dilithium is 15N labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K+ channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
COX-1/2-IN-3 (Compound 7a) is a COX-1 and COX-2 inhibitor. COX-2-IN-15 shows anti-inflammatory activity with low toxicity[1].
Pseudo-β-D-mannopyranose is a hapten that can be coupled with mannose[1].
Pasiniazid is an anti-TB and anti-leprosy drug, used to treat various types of TB and leprosy.
Emavusertib (CA-4948) hydrochloride is a selective, potent and orally active IRAK4/FLT3 inhibitor. Emavusertib hydrochloride has an IC50 of 57 nM for IRAK4 in a FRET kinase assay. Emavusertib hydrochloride shows anti-tumor activity[1][2][3].
FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect[1][2].
RORγt modulator 3 (Compound 23) is a modulator of retinoid-related orphan receptor γt (RORγt). RORγt modulator 3 can be used for the research of RORyt mediated diseases such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer[1].
4-Methylesculetin is an orally active natural coumarin derivative, with potent anti-oxidant and anti-inflammatory activities. 4-Methylesculetin inhibits myeloperoxidase activity and reduces IL-6 level[1].
Caraphenol A is a resveratrol trimer and is able to transiently reduce interferon-induced transmembrane (IFITM) protein expression. Caraphenol A safely enhances lentiviral vector gene delivery to hematopoietic stem and progenitor cells[1]. Caraphenol A also inhibits human cystathionine β-synthase (hCBS) and human cystathionine γ- lyase (hCSE) with IC50s of 5.9 μM and 12.1 μM, respectively[2].
COX-2-IN-23 (compound 9a) is a selective COX-2 inhibitor with IC50 values of 0.28 and 20.14 μM for COX-2 and COX-1. COX-2-IN-23 has anti-inflammatory activity and low ulcerogenic activity.
Firzacorvir is a cyclic sulfamide compound and modulates HBV core protein. Firzacorvir has anti-HBV activity with EC50 < 1 μΜ[1].
Pratol is a potent inhibitor of NF-κB. Pratol significantly reduces NO and prostaglandin PGE2 production without any cytotoxic in LPS-stimulated RAW 264.7 cells. Pratol reduces proinflammatory cytokines. Pratol can be used in study inflammatory diseases and cancer[1].
Carboxy-PTIO is a potent nitric oxide (NO) scavenger that can make a quick reaction with NO to produce NO2. Carboxy-PTIO can prevent hypotension and endotoxic shock through the direct scavenging action against NO in lipopolysaccharide-stimulated rat model[1][2][3].
BRD4-IN-2 is a bromodomain BRD4 inhibitor with an IC50 value of 9.9 nM.
SN50 is a cell permeable inhibitor of NF-κB translocation. Sequence: Ala-Ala-Val-Ala-Leu-Leu-Pro-Ala-Val-Leu-Leu-Ala-Leu-Leu-Ala-Pro-Val-Gln-Arg-Lys-Arg-Gln-Lys-Leu-Met-Pro;AAVALLPAVLALLAPVQRKRQKLMP.
DSTYSLSSTLTLSK is a generic human peptide and can be used for infliximab quantitative detection[1]. Infliximab (Avakine) is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α.
Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation[1][2][3][4].
Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC50 value of 0.28 μM.
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H+/K+-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor[1][2].
MSX-122 is a partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM; MSX-122 has anti-inflammatory and anti-metastatic activity.
DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration[1].
Defibrotide sodium is a complex mixture of single stranded polydeoxyribonucleotides. Defibrotide sodium has liver protection, anti-inflammatory, antithrombotic, profibrinolytic, and anti-ischemic properties. Defibrotide sodium can be used for sinusoidal obstruction syndrome (SOS)/veno-occlusive disease (VOD) research[1].
Amebucort is a synthetic glucocorticoid corticosteroid, may used for the research of inflammatory disorders.
Dexamethasone phosphate (Dexamethasone 21-phosphate) is a biologically inactive compound which undergoes dephosphorylation by intra-erythrocyte enzymes. The active metabolite, dexamethasone, is then released into the circulation by simple passive diffusion through cell membranes. Dexamethasone phosphate-encapsulated erythrocyte has the potential for steroid-dependent ulcerative colitis research[1].