Tag: Anti-Inflammatory

Epoxomicin is a Selective and Irreversible Inhibitor of Proteasome

Epoxomicin (BU-4061T) is a potent, selective and irreversible proteasome inhibitor. Epoxomicin can cross the blood-brain barrier and has strongly antitumor and anti-inflammatory activity. Proteasome is a 700 kDa, cylindrical-shaped multicatalytic protease complex. It has 28 subunits and organizes into four rings. Besides, Eukaryote 20S proteasome has three major proteolytic...

Chelerythrine is a Potent Protein kinase C Inhibitor

Chelerythrine is a natural benzo[c]phenanthridine alkaloid. It extracts from a number of plant species, such as Chelidonium majus, Macleaya cordata, Sanguinaria canadensis, etc. This compound exerts a wide spectrum of biological activities, including anti-cancer, anti-diabetes, anti-fungus, as well as a protective effect against the ethanol-induced gastric ulcer and the...

VU0359595 is a Selective PLD1 Inhibitor

Phospholipase is a member of a very complex group of enzymes that break down phospholipids into fatty acids and other compounds. Phospholipase D (PLD) is an enzyme of the phospholipase superfamily. There are two mammalian isoforms of PLD, coined PLD1 and PLD2, and despite conserved regulatory and catalytic domains....

IV-361 is an Orally Active and Selective CDK7 Inhibitor

Cyclin-dependent kinase 7 (CDK7) is a catalytic subunit of CDK activated kinase (CAK). CAK is a kinase complex that catalyzes T-ring phosphorylation and activates a variety of cyclin-related kinases, including CDK1, CDK2, CDK4, and CDK6. Importantly, CDK7 plays a role at the direct interface between important processes of cell...

Lumiracoxib is a Selective and Orally Active COX-2 Inhibitor and Nonselective NSAID

Prostaglandins play an important role in modulating both physiological and inflammatory processes. They can act as autocrine factors regulating platelet aggregation, vascular tone, and secretions. Additionally, the synthesis of prostaglandin depends on the activity of cyclooxygenase (COX). There are existing two isoforms: COX-1 and COX-2. They are highly homologous...

SB-332235 is an Orally Active CXCR2 Antagonist

Chemokines are low m.w. proteins that modulate the immune response through the chemoattraction and activation of leukocytes. These mediators have four classes. Chemokines in which the first two cysteines are separated by a  single,  nonconserved amino acid are CXC or chemokines, while those containing adjacent N-terminalcysteine residues are  CC ...