Magnesium Lithospermate B is a derivative of caffeic acid tetramer and extracted from Salviae miltiorrhizae. Magnesium Lithospermate B is widely used for the research of cardiovascular diseases, and it can protect against glucose-induced intracellular oxidative damage. Magnesium Lithospermate B also suppresses neuroinflammation and attenuates neurodegeneration[1][2][3].
Nodakenin is a major coumarin glucoside in the root of Peucedanum decursivum Maxim. Nodakenin inhibits acetylcholinesterase (AChE) activity with an IC50 of 84.7 μM[1][2].
2,4,7-Trihydroxy-9,10-dihydrophenanthrene is a dihydrophenanthrene derivative that can be isolated from the air-dried whole plant of Pholidota chinensis Lindl.. 2,4,7-Trihydroxy-9,10-dihydrophenanthrene shows potent activities of IC50 at 16.2 μM in DPPH radical-scavenging assay[1].
Eltenac, a non-steroidal anti-inflammatory drug (NSAID), is a COX inhibitor. Eltenac shows IC50 of 0.03 μM for both COX-1 and COX-2 in isolated human whole blood[1].
Salicin is a natural COX inhibitor.
Sinapine hydroxide is an alkaloid isolated from seeds of the cruciferous species. Sinapine hydroxide exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine hydroxide is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease[1][2][3][4].
Astilbin, a flavonoid compound, is isolated from the rhizome of Smilax glabra. Astilbin enhances NRF2 activation. Astilbin also suppresses TNF-α expression and NF-κB activation.
Masilukast is an orally administered cysteinyl leukotriene D4 (LTD4) receptor antagonist with potential to treat asthma.
N-Glycolylneuraminic acid is a nonhuman sialic acid molecule synthesized in pigs but not in humans. N-Glycolylneuraminic acid works as a decoy receptor of N-Glycolylneuraminic acid-binding influenza A viruses (IAVs)[1].
FeTMPyP is an orally active peroxynitrite (ONOO?) scavenger. FeTMPyP reduces nitrative stress and increases autophagy. FeTMPyP reduces PARP over-activation and neuroinflammation in chronic constriction injury (CCI)-induced rats, and ameliorates functional, behavioral and biochemical deficits[1][2].
5'-Methoxynobiletin is a potent and orally active antinociceptive and anti-inflammatory agent. 5'-Methoxynobiletin is a polymethoxyflavone, that can be isolated from A. conyzoides[1][2].
p38-α MAPK-IN-4 (Compound 69) is a selective p38α MAPK inhibitor with an IC50 of 1.5 µM. p38-α MAPK-IN-4 rapidly and strongly prevents the development of mechanical allodynia (MA) in vivo[1].
I-191 is a protease-activated receptor 2 (PAR-2) signaling pathway inhibitor extracted from patent WO2015048245A1. I-191 inhibits PAR-2 activators such as SLIGKV, Trypsin, and Thrombin with IC50s of 0.0014 μM, 0.0023 μM, 0.32 μM, respectively[1].
UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent[1].
Pristane (Norphytane) is a naturally occurring hydrocarbon oil found in small quantities in many plants, in various marine organisms, and as the most active component of mineral oil[1]. Pristane is a non-antigenic adjuvant, and induces MHC class II-restricted, arthritogenic T cells in the rat[2].
α-Gliadin (43-49) is the major protein component of gluten. α-Gliadin (43-49) can be used in the immunological response to α-gliadin[1].
Emodin-1-O-β-D-glucopyranoside, isolated from medicinal plant Polygonum cuspidatum Sieb. & Zucc, is a potent and noncompetitive bacterial neuraminidase (BNA) inhibitor with an IC50 of 0.85 μM[1].
Sulfachloropyridazine-d4 is the deuterium labeled Sulfachloropyridazine. Sulfachloropyridazine is a broad spectrum sulfonamide used against both Gram-positive and Gram-negative aerobic bacteria[1].
MrgprX2 antagonist-1 is an MrgprX2 antagonist extracted from patent WO2021092264A1, example E23. MrgprX2 antagonist-1 can be used for the research of inflammatory disorders of the skin[1].
SUN 1334H is a potent, orally active, highly selective H1 receptor antagonist, with Ki of 9.7 nM.
RO1138452 is a potent and selective IP (prostacyclin) receptor antagonist. RO1138452 displays high affinity for IP receptors. In human platelets, pKi is 9.3±0.1; in a recombinant IP receptor system, pKi is 8.7±0.06.
Bumadizone is a non-steroidal anti-inflammatory drug (NSAID) and can relieve pain[1].
ML358 is a first in class, selective small molecule inhibitor of the SKN-1 pathway with IC50 of 0.24 uM; shows inactivity against Nrf2, the homologous mammalian detoxification pathway, and is not toxic to C. elegans (LC50 > 64 uM) and Fa2N-4 immortalized human hepatocytes (LC50 > 5.0 uM); sensitizes the model nematode C. elegans to oxidants and anthelmintics; exhibits good solubility, permeability, and chemical and metabolic stability in human and mouse liver microsomes; a valuable chemical probe to study regulation and function of SKN-1 in vivo.
GPR34 receptor antagonist 2 (Compound D2) is a GPR34 receptor antagonist. GPR34 receptor antagonist 2 can be used for immune diseases, inflammatory diseases research[1].
Aspirin (Acetylsalicylic Acid) lithium is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin lithium induces apoptosis. Aspirin lithium inhibits the activation of NF-κB. Aspirin lithium also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis[1][2][3][4][5][6].
Korepimedoside C (Epimedin I), a flavonol glycoside, is isolated from the aerial parts of Epimedium koreanum Nakai. Epimedium koreanum Nakai is a famous Chinese herbal medicine for the research of impotence, osteoporosis, immune suppression and cardiovascular diseases[1][2].
Ganoderenic acid K is a natural product, that can be isolated from fruiting bodies of Ganoderma lucidum. Ganoderenic acid K shows strong inhibitory activity against HMG-CoA reductase (HMGCR) with IC50 of 16.5 μM[1].
4-Methylsalicylic acid is a salicylic acid. 4-Methylsalicylic acid derivative is a selective tissue-nonspecific alkaline phosphatase (TNAP) and intestinal alkaline phosphatase (IAP) inhibitor[1].
Obafistat is a potent aldo-keto reductase AKR1C3 inhibitor with an IC50 of 1.2 nM for human AKR1C3 (patent WO2017202817A1, example 4)[1].