p-selectin inhibitor

PSI-697 (P-Selectin Inhibitor) is an orally active P-selectin inhibitor with anti-inflammatory and anti-thrombotic effects, useful for studying cardiovascular diseases such as atherosclerosis.

1. Glaucocalyxin A (Leukamenin F)-SBE-β-CD could be useful with a better solubility and sustained function in drug delivery. 2. Glaucocalyxin A activates caspase-3, decreases BAD phosphorylation, and reduces the expression of X-linked inhibitor of apoptosis protein. 3. Glaucocalyxin A inhibits Akt phosphorylation, suppresses proliferation, and promotes apoptosis in a dose-dependent manner, but not in normal glial cells. 4. Glaucocalyxin A inhibits collagen-stimulated tyrosine phosphorylation of Syk, LAT, and phospholipase Cγ2, the signaling events in collagen receptor GPⅥ pathway. 5. Glaucocalyxin A could potentially be developed as an antiplatelet and antithrombotic agent, can inhibit platelet p-selectin secretion and integrin activation by convulxin, is a GPVI selective ligand.

Parmodulin 2 (ML 161) is the inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50: 0.26 μM for the inhibition of platelet P-selectin expression on human platelets). It also inhibits thrombin-induced platelet activation.

1. N-trans-Feruloyltyramine (Feruloyltyramine)(NTF) has hepatoprotective effect. 2. NTF has antioxidative activity against Aβ(1-42)-induced neuronal death. 3. NTF is likely to inhibit COX enzymes, thereby suppressing P-selectin expression on platelets, is a platelet aggregation inhibitor. 4. NTF inhibits melanogenesis in a dose-dependent manner, NTF induces downregulation of tyrosinase resulted in suppression of melanin biosynthesis in murine B16 melanoma cells.

Bimosiamose disodium has anti-inflammatory effects[1]. Bimosiamose disodium (TBC-1269Z) is a nonoligosaccharide pan-selectin inhibitor with IC50s of 88 μM, 20 μM, and 86 μM for E-selectin, P-selectin, and L-selectin, respectively.

Cylexin is a P-selectin inhibitor.

Cotransin, a Sec61 translocation inhibitor, selectively prevents the stable insertion of certain nascent chains into the Sec61 translocation channel, exhibiting signal-sequence discrimination. This compound also inhibits the expression of VCAM-1 and p-selectin proteins by blocking their co-translational translocation across endoplasmic reticulum (ER) membranes (IC 50 =0.5-5 µM). Cotransin's role extends to potential applications in inflammation and immunity research [1] [2].

KF38789 is a selective inhibitor of P-selectin-mediated cell adhesion and P-selectin immunoglobulin G chimeric protein (IgG).

Odatroltide is a nanoscale P-selectin inhibitor that serves as a nano-delivery system for 6,7-dihydroxyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid and KPAK to specifically target the thrombus.

HMCEF is a P-selectin inhibitor that acts by intercalating into calf thymus DNA, cutting off DNA pBR22. It also inhibits the proliferation of cancer cells.