PDGFR Modulator

SU-4313 is a potent protein tyrosine kinases (PTKs) modulator with IC₅₀s of 14.5 μM, 18.8 μM, 11 μM, 16.9 μM, 8.0 μM for PDGFR, FLK-1, EGFR, HER2 Kinase and IGF-1R, respectively. SU-4313 has the potential for modulating tyrosine kinase signal transduction in order to regulate abnormal cell proliferation.

Dihydroparadol is a iNOS inhibitor with an IC₅₀ of 7.24 μM, and it is found in ginger. Dihydroparadol partially inhibits the catalytic activity of iNOS, blocks the nuclear translocation of NF-κB p65, reduces NF-κB activity, and attenuates lipopolysaccharide-induced degradation of IκB-α, thereby inhibiting NF-κB-mediated iNOS gene expression and protein production. Dihydroparadol inhibits lipopolysaccharide-induced nitric oxide production in macrophages and exhibits anti-inflammatory activity. Dihydroparadol increases ABCA1 protein abundance by elevating mRNA levels and reducing proteasomal degradation, and also increases ABCG1 protein abundance by enhancing protein stability. Dihydroparadol promotes cholesterol efflux from cholesterol-loaded macrophages via apolipoprotein A1-mediated and plasma-mediated pathways. Dihydroparadol inhibits PDGF-induced vascular smooth muscle cell proliferation, shows no cytotoxicity to vascular smooth muscle cells within the tested concentration range, and does not interfere with endothelial cell proliferation. Dihydroparadol can be used in the research of inflammatory diseases, atherosclerosis and cardiovascular diseases.