Cyanidin 3-sambubioside chloride (Cyanidin-3-O-sambubioside chloride), a major anthocyanin, a natural colorant, and is a potent NO inhibitor. Cyanidin 3-sambubioside chloride is a H274Y mutation inhibitor, and inhibits influenza neuraminidase activity with an IC50 of 72 μM. Cyanidin 3-sambubioside chloride inhibits angiotensin-converting enzyme (ACE) activity and has antioxidant, anti-angiogenic and antiviral properties[1][2][3].
Sonelokimab (ALX 0761; M 1095) is a trivalent nanobody comprised of monovalent camelid-derived nanobodies specific to human interleukin (IL)-17A, IL-17F, and human serum albumin VHHs. Sonelokimab has the potential for plaque-type psoriasis research[1][2].
ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor. ERAP1-IN-1 competitively inhibits ERAP1 activity towards a nonamer peptide representative of physiological substrates[1].
Umesolerbart (REGN5714) is a Bet v1 specific mAb. Umesolerbart (REGN5714)bind to homologous allergens in Alder, Hazel and hornbeam[1].
1,7-Diphenyl-4-hepten-3-one, isolated from Alpinia officinarum, possess bioactivities against some pests, such as T. castaneum[1].
PF06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), and used to treat diseases such as rheumatoid arthritis, lupus, and lymphomas.
Arjunolic acid is a saponin isolated from Symplocos lancifolia and has various biologial activities, including antioxidant, antimicrobial, antibacterial and anti-inflammory activities. Arjunolic acid is also a potent antioxidant and plays an important role in the protection of cells and tissues against deleterious effects of reactive oxygen species[1].
CDP-840 (GR259653X) is a potent, selective and orally active phosphodiesterase IV (PDE IV) inhibitor. CDP-840 inhibits antigen-induced early and late phase bronchoconstriction in conscious squirrel monkeys[1].
ERAP2-IN-1 (compound 61) is an uncompetitive ERAP2 inhibitor. ERAP2-IN-1 specifically inhibits the ERAP2 peptide hydrolysis activity, inhibiting Arg-AMC hydrolysis with an IC50 of 27 μM and model peptide hydrolysis with an IC50 of 44 μM[1].
cis-Clovamide, a natural phenolic compound with antioxidant, anti-inflammatory and antiapoptotic activities[1].
QH536 (Compound 29) is a potent HMGCR degrader with an EC50 of 0.22 μM. QH536 has no side-effect of inducing cholesterol accumulation in cells. QH536 shows anti-inflammatory and can be used for cardiovascular disease and nonalcoholic steatohepatitis research[1].
ODN 20844, a guanine-modified inhibitory oligonucleotide (INH-ODN), is a TLR7 and TLR9 (Toll-like receptor) inhibitor, and its parent is INH-ODN 2088. ODN 20844 disrupts TLR7- and TLR9-mediated immune cell immune responses. ODN 20844 sequence: 5'-TCCTGGCGc7GGGAAGT-3'[1].
Lansoprazole(AG 1749) is a proton pump inhibitor which prevents the stomach from producing acid.Target: Proton PumpLansoprazole, a substituted benzimidizole proton pump inhibitor, on pharmacokinetics and metabolism of theophylline has been studied in healthy adults given oral lansoprazole 30 mg once daily for 11 days. On Days 4 and 11 of 300 mg aminophylline was simultaneously administered orally and blood samples for theophylline analysis were taken over 24 h [1]. Patients in the lansoprazole group were significantly less likely to have a recurrence of ulcer complications than patients in the placebo group (P=0.008). There was no significant difference in mortality between the two groups [2]. lansoprazole (AG-1749) and omeprazole, were found to have significant activities against this organism. The activity of lansoprazole was comparable to that of bismuth citrate, with MICs ranging from 3.13 to 12.5 micrograms/ml, and fourfold more potent than that of omeprazole [3]. Clinical indications: Duodenal ulcer; Esophagitis; Gastroesophageal reflux; Gastrointestinal disease; Helicobacter pylori infection; Peptic ulcer; Stomach ulcer; Ulcer; Zollinger-Ellison syndromeFDA Approved Date: May 10, 1995Toxicity: Symptoms of overdose include abdominal pain, nausea and diarrhea.
ZL0420 is a potent, highly selective BRD4 inhibitor with IC50 of 27 and 32 nM for BRD4-BD1 and BRD4-BD2, respectively; displays selectivity over BRD2, BRD3, and BRDT (BRD2-BD1 and BRD2-BD2, IC50=803 and 1736 nM); disrupts the BRD4 complex with Pol II and histones, inhibits poly(I:C)-induced expression of innate immune genes IL6 and CIG5 in human small airway epithelial cells (hSAECs) (IC50=0.54 and 0.51 uM); blocks Poly(I:C)-induced inflammation and neutrophilia in vivo.
Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders.
Obexelimab (XmAb5871) is a humanized anti-CD19 antibody Fc-engineered for increased affinity to FcγRIIb. Obexelimab can be used in research of autoimmune[1].
Antibacterial agent 61 (example 27) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
CAY10404 is a potent and highly selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM. CAY10404 exhibits no inhibition of COX-1 (IC50>500 µM)[1]. CAY10404 is a potent inhibitor of PKB/Akt and MAPK signaling pathways and induces apoptosis in NSCLC cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities[2][3].
Rosmarinic acid racemate is the racemate of Rosmarinic acid. Rosmarinic acid inhibits MAO-A, MAO-B and COMT enzymes with IC50s of 50.1, 184.6 and 26.7 μM, respectively.
AZD-0284 is an inverse agonist of the nuclear receptor RORγ. In development for the treatment of plaque psoriasis vulgaris and respiratory tract disorders[1].
MrgprX2 antagonist-8 (example 5b) is a MrgprX2 antagonist. MrgprX2 antagonist-8 can be used for the research of inflammatory disorders[1].
Astragenol is an intermediate used for Astragenol derivative synthesis. Astragenol derivatives are promising anti-inflammatory agents for prostate cancer research[1].
Bromisoval has anti-inflammatory effects and has been used as an old sedative and hypnotic.
IL-17A modulator-3 (compound 253) is a IL-17A modulator. IL-17A modulator-3 inhibits IL-17A/A with an IC50 value ＜10 μM. IL-17A modulator-3 can be used for the research of inflammation, cancer and autoimmune disease[1].
Hispidol ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 µM.
C-Reactive Protein (CRP) 77-82 is the 77-82 fragment of C-Reactive Protein. C-Reactive Protein (CRP), the prototypic marker of inflammation, is a cardiovascular risk marker and may promote atherogenesis[1].
m-PEG8-NHS ester is a non-cleavable 8 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
Homodestcardin, a destruxinbased cyclodepsipeptide, is a immunosuppressant. Homodestcardin, a fungal metabolite, displays pronounced activities against concanavalin A (Con A) activation, with an IC50 value of 0.86 μM[1].
Lutikizumab (ABT-981) is an anti-IL-1α and IL-1β dual variable domain immunoglobulin. Lutikizumab binds and inhibits IL-1α and IL-1β. Lutikizumab can be used for the research of osteoarthritis[1].
Okicenone is a Hu protein R (HuR) inhibitor. Okicenone inhibits HuR oligomerization, interferes with HuR RNA binding, HuR trafficking, cytokine expression and T-cell activation[1].