Morachalcone A is a naturally-occurring aromatase inhibitor (IC50=4.6 mM). Morachalcone A is also a plants metabolite with potential anti-inflammatory and anticancer activity. Morachalcone A inhibits Lipopolysaccharide (HY-D1056)-induced nitric oxide production[1][2][3].
Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation[1].
Phenacetin is a non-opioid analgesic without anti-inflammatory properties, inhibits COX-3 activity.Target: COXPhenacetin is a pain-relieving and fever-reducing drug, Phenacetin was withdrawn from the Canadian market in June 1973 due to concerns regarding nephropathy. the clinical and laboratory data were compatible with "phenacetin nephritis" as described in Europe and Australia and recently in the United States and Canada. This report evaluates the findings in the 23 cases and cautions against the use of phenacetin, particularly in patients with impaired renal function [1]. Phenacetin has been linked to renal papillary necrosis in human beings [2, 3].
BAY-3153 is a selective CCR1 (C-C motif chemokine receptor 1) antagonist (human IC50=3 nM; rat IC50=11 nM; mice IC50=81 nM)[1].
APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P2 in the presence of in the presence of [33P]ATP with an IC50 of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.
Factor D inhibitor 6 is a potent and selective, orally bioavailable inhibitor of Factor D with IC50 of 30 nM; is highly selective for human FD, showing no inhibition of factor B; efficiently block alternative pathway activation and prevent both C3 deposition onto, and lysis of, PNH erythrocytes; inhibits lipopolysaccharide-induced AP activation in FD-humanized mice.
Etofenamate-d4 is the deuterium labeled Etofenamate. Etofenamate, a non-steroid anti-inflammatory drug (NSAID) and a non-selective COX inhibitor, possesses analgesic, anti-rheumatic, antipyretic and anti-inflammatory properties. Etofenamate is used in the research for osteoarthritis, arthritis and other inflammatory diseases[1][2][3].
Guaiacol-d3 (2-Methoxyphenol-d3) is the deuterium labeled Guaiacol. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Guaiacol has an anti-inflammatory activity[1].
ST 2825 is a MyD88 dimerization inhibitor.
Betazole (Ametazole) dihydrochloride, a pyrazole analogue of histamine, is an orally active H2 receptor agonist. Betazole dihydrochloride induces gastric acid secretion, and causes an immediate and significant increase in common bile duct pressure. Betazole dihydrochloride has been used as a diagnostic agent known as histalog, for investigating gastric acid secretory capacity[1][2][3].
Phanginin A is a potent and orally active SIK1 (salt-induced kinase 1) activator. Phanginin A inhibited gluconeogenesis. Phanginin A increases the expression of p-SIK1 and decreases the expression of p-CREB. Phanginin A reduces blood glucose levels and improves glucose tolerance and dyslipidemia. Phanginin A has the potential for the research of type 2 diabetes[1].
BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC50 of 5.1 nM) and potent functional antagonism (calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM)[1][2].
GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for the treatment of asthma[1].
A novel potent, selective CDK8 inhibitor with IC50 of 0.5 uM against recombinant Cyclin C/CDK8 complex; displays no activity against several CDKs involved in cell cycle including CDK19 (IC50>30 uM); inhibits IFNγ-induced phosphorylation of STAT1 at Ser 727 site in BMDCs, selectively upregulates IL-10 with EC50 of 1 uM.
Sirukumab (CNTO-136) is a humanized monoclonal anti-IL6 (Interleukin Related) IgG1κ antibody. Sirukumab has the potential for active lupus nephritis research[1].
Dazostinag (TAK-676 free base) is an agonist of stimulator of interferon genes (STING) protein with antineoplastic activity. Dazostinag can serve as a playload to synthesis Antibody-Drug Conjugates (ADCs)[1][2].
Metamizole sodium is a non-opioid compound with excellent analgesic and antipyretic effects. Metamizole (sodium) is a cyclooxygenase-3 (COX-3) inhibitor[1][2].
Chloranthalactone B, a lindenane-type sesquiterpenoid, is a nature product that could be isolated from Chinese medicinal herb Sarcandra glabra. Chloranthalactone B inhibits the production of inflammatory mediators by inhibiting the AP-1 and p38 MAPK pathways[1].
MR2938 is a potent AChE inhibitor, with an IC50 of 5.04 μM. MR2938 also suppresses NO production obviously (IC50 = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research[1].
Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes[1].
Tagitanlimab (HBM-9167) is a humanized anti-PD-L1 antibody (IgG1κ type). Tagitanlimab selectively blocks the interaction of PD-L1 and PD-1. Tagitanlimab has the potential to be studied in recurrent or metastatic nasopharyngeal carcinoma (NPC)[1][2].
Balstilimab (AGEN2034) is a fully human monoclonal IgG4 antibody against PD-1[1].
(Z)-Lafutidine ((Z)-FRG-8813) is a potent histamine H2 receptor antagonist. (Z)-Lafutidine shows anti-secretory and gastroprotective activities[1].
Cyclosporin A-d3 is the d3-labeled Cyclosporin A (HY-B0579)[1].
Episappanol is a natural compound isolated from Caesalpinia sappan heartwood with anti-inflammatory activity. Episappanol significantly inhibits the IL-6 and TNF-α secretion[1].
Robenacoxib is a nonsteroidal anti-inflammatory and analgesic agent. Robenacoxib is a selective COX-2 inhibitor[1][2].
Dimenhydrinate is an anti-emetic and anti-histamine commonly available over-the-counter as a motion sickness remedy.
IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1].
(±)-Naproxen-13C,d3 is the deuterium and 13C labeled (±)-Naproxen[1]. (±)-Naproxen ((Rac)-Naproxen) is a racemate of Naproxen (HY-15030). Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively.