α-Spinasterol, isolated from Spinacia oleracea, has antibacterial activity[1]. α-Spinasterol is a transient receptor potential vanilloid 1 (TRPV1) antagonist, has anti-inflammatory, antidepressant, antioxidant and antinociceptive effects. α-Spinasterol inhibits COX-1 andCOX-2 activities with IC50 values of 16.17 μM and 7.76 μM, respectively[2].
Avacincaptad pegol (ARC1905) is is an anti-C5 RNA aptamer that inhibits the cleavage of complement factor 5 (C5) into C5a and C5b. Avacincaptad pegol is being used for the study of age-related macular degeneration (AMD).
BMS-1 is an inhibitor of the PD-1/PD-L1 protein/protein interaction.
CU CPT 22 is a toll-like receptor 1 and 2 (TLR1/2) inhibitor with an IC50 of 0.58 µM.
Myelopeptide-2 is a peptide originally isolated from the supernatant of porcine bone marrow cell cultures, can restore mitogenic reactivity of human T lymphocytes inhibited by HL-60 leukemia cells or measles virus conditions. Myelopeptide-2 also recover depressed interleukin-2 (IL-2) synthesis and interleukin-2 receptor (IL-2R) expression. Myelopeptide-2 involves in immunity homeostasis, is perspective to be applied in antitumor and antivirus research[1][2].
CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity[1].
PD-1/PD-L1-IN-24 is a highly potent PD-1/PD-L1 inhibitor with IC50 value of 1.57 nM. PD-1/PD-L1-IN-24 can restore T-cell function at the cellular level by significantly elevating the IFN-γ level. PD-1/PD-L1-IN-24 has low toxicity on the PBMCs[1].
5F-203 (NSC-703786) is a cytotoxic molecule that forms DNA adducts and cell cycle arrest. 5F-203 induces aryl hydrocarbon receptor (AhR) signaling and elevates expression of CYP1A1. 5F-203 also increases the levels of reactive oxygen species as well as activates JNK, ERK, and p38[1][2][3].
Mequitazine is a potent, nonsedative and long-acting histamine H1 antagonist.
Phenacetin-13C is the 13C labeled Phenacetin[1]. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[2][3][4].
AHR antagonist 3 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and an aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. AHR antagonist 3 has anti-cancer effects[1].
Indomethacin farnesil is an orally active prodrug of Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes[1][2].
Sparstolonin B acts as a selective TLR2 and TLR4 antagonist and selectively blocks TLR2- and TLR4-mediated inflammatory signaling. Sparstolonin B has anti-HIV and anticancer activities[1][2].
mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM)[1].
AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.
(Rac)-Anemonin ((Rac)-Pulsatilla camphor) is the diastereoisomer of Anemonin (HY-N0278). Anemonin (Pulsatilla camphor), a selective iNOS inhibitor, is also a PKC-θ inhibitor. Anemonin can significantly inhibit the translation or protein stability of PKC-θ protein. Anemonin also ameliorates dextran sodium sulfate-induced acute ulcerative colitis (UC) in mice. Anemonin can be used in the research of inflammation-related diseases[1][2].
Zomepirac sodium salt is a pyrrole-acetic acid structurally related to tolmetin sodium; a prostaglandin synthetase inhibitor.
Casdozokitug (SRF-388) is an IgG1κ antibody targeting IL27[1].
L-Canavanine sulfate is a selective inhibitor of inducible NO synthase.
ASP6537 is a potent and selective rhCOX-1 inhibitor with an IC50 of 0.703 nM. ASP6537 has the potential for cardiovascular disease research[1].
PROTAC IRAK4 degrader-4 is a PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-127[1].
Luteolin-4'-O-glucoside is an IL-5 inhibitor with an IC50 of 3.7 μM. Luteolin-4'-O-glucoside resists hyperuricemia and acute gouty arthritis activity. Luteolin-4'-O-glucoside shows anticancer activity[1][2][3].
TYK2-IN-12 (compound 30) is an orally active, potent and selective TYK2 (tyrosine kinase 2) inhibitor, with a Ki of 0.51 nM. TYK2-IN-12 inhibits IL-12 induced IFNγ, with IC50 values of 2.7 and 7.0 μM in human and mouse whole blood, respectively. TYK2-IN-12 can be used for psoriasis research[1].
K6PC-5, a synthetic ceramide derivative,is a direct sphingosine kinase 1(SPHK1) activator and elicites a rapid transient increase in intracellular calcium levels. K6PC-5 is used for the researches of skin diseases involving abnormal keratinocyte, neurodegeneration and virus infection[1][2][3].
Myricananin A is a colorless needle that has inhibitory effect on iNOS[1].
SU5201 is an inhibitor of interleukin-2 (IL-2) production[1].
MEG (Mercaptoethylguanidine) hemisulfate is a potent and selective inhibitor of the inducible NO synthase (iNOS), with EC50s of 11.5, 110, and 60 μM for iNOS, ecNOS, and bNOS respectively in tissue homogenates. MEG hemisulfate is also a potent scavenger of peroxynitrite and inhibits peroxynitrite-induced oxidative processes. MEG hemisulfate has a protective effect in many experimental models of inflammation, including ischemia/reperfusion injury, periodontitis, hemorrhagic shock, inflammatory bowel disease, and endotoxic and septic shock[1][2][3][4].
Peonidin chloride is an O-methylated anthocyanidin that functions as a primary plant pigment, endowing purplish-red hues to flowers such as the peony, from which it takes its name, as well as berries and vegetables. Peonidin chloride exhibits chemopreventive, as well as anti-inflammatory activities on cancer cells in vitro, blocking COX-2 expression and transformation in JB6 P+ mouse epidermal cells.
VUF 5681 dihydrobromide is a neutral antagonist of histamine H3 receptor. VUF 5681 dihydrobromide also has partial agonist function of H3 receptor. VUF 5681 dihydrobromide blocks the effects of Thioperamide (HY-12206). VUF 5681 dihydrobromide is used in central nervous system disease research[1][2].
Vixarelimab (KPL-716) is a human anti-oncostatin M (OSM) monoclonal antibody that binds to the beta chain of the OSM receptor and inhibits IL-31 and OSM signalling. Vixarelimab can be used in studies of inflammatory skin diseases such as atopic dermatitis and itchy nodular rash[1].