9 products were found matching "Cay18500"!

Prostaglandin J2 (PGJ2) is a metabolite of PGD2 (Cay-12010) and an agonist of the prostaglandin D2 (PGD2) receptor subtypes DP1 and DP2/CRTH. It is formed from PGD2 by spontaneous dehydration. PGJ2 binds to DP1 and DP2/CRTH receptors (Kis = 0.9 and 6.6 nM, respectively) and either increases or inhibits the...

Delta12-Prostaglandin J2 (Delta12-PGJ2) is a decomposition product of PGD2 in aqueous media in the presence of albumin. It has antitumor and antiviral activity, inhibiting growth of cultured L1210 cells at with an IC50 value of 0.7 µg/ml. Delta12-PGJ2 is present in normal human urine with a 24 hour excretion rate of...

15-deoxy-Delta12,14-Prostaglandin J2 (15-deoxy-Delta12,14-PGJ2) is formed from PGD2 by the elimination of two molecules of water. It binds selectively to PPARgamma with an EC50 value of 2 µM in a murine chimera system. 15-deoxy-Delta12,14-PGJ2 is more potent than PGD2, Delta12-PGJ2, and PGJ2 in stimulating...

Apremilast is an inhibitor of phosphodiesterase 4 (PDE4) with an IC50 value of 74 nM when tested in U937 cell lysates with 1 mM cAMP. It is orally active, significantly decreasing epidermal thickness and epithelial cell proliferation index in a mouse model of psoriasis. Apremilast reduces both TNF-alpha and matrix...

The CC chemokine receptor-1 (CCR1), whose ligands include macrophage inflammatory protein-1alpha (MIP-1alpha), RANTES, and monocyte chemotactic protein-3 (MCP-3), has a central role in leukocyte trafficking and is highly expressed in certain autoimmune diseases. BX 471 is a nonpeptide CCR1 antagonist that has been...

The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis, particularly in response to reactive oxygen and nitrogen species. 4-amino-1,8-Naphthalimide (4-ANI) is an inhibitor of PARP (IC50 = 180 nM). It blocks radiation-induced PARP in cancer cells, potentiating the...

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs of FcRgamma chains and mediates downstream signaling related to platelet function and inflammation. R788 is a prodrug of R406 (Cay-11422), an inhibitor of Syk (Ki = 30...

Aminopeptidase B is a Zn2+-dependent exopeptidase that selectively removes arginine and/or lysine from the amino terminus of peptide substrates. This enzyme is a metalloprotease commonly found on the surface of mammalian cells, including macrophages and lymphocytes. Arphamenine B is an aminopeptidase B inhibitor...

Trelagliptin is an inhibitor of dipeptidyl peptidase 4 (DPP-4, IC50 = 4 nM). It is greater than 10,000-fold selective for DPP-4 over isopeptidases. Trelagliptin (7 mg/kg) inhibits plasma DPP-4 activity and reduces postprandial plasma insulin levels in Zucker fa/fa rats. Formulations containing trelagliptin have been...