JAS239 is a novel carbocyanine dye that binds and competitively inhibits choline kinase (ChoK) intracellularly. JAS239 attenuated choline phosphorylation and viability in a panel of human breast cancer cell lines. Antibody blockade prevented cellular retention of JAS239 indicating direct interaction with ChoKα independent of the choline transporters and catabolic choline pathways. In mice bearing orthotopic MCF7 breast xenografts, optical imaging with JAS239 distinguished tumors overexpressing ChoKα from their empty vector counterparts and delineated tumor margins.
Clathrin-IN-1 is a selective clathrin inhibitor that acts by addressing clathrin function in cell physiology with potential applications as an inhibitor of virus and pathogen entry and as a modulator of cell signaling.
TOP1362 is a Narrow Spectrum Kinase Inhibitors Demonstrate Promise for the Treatment of Dry Eye Disease and Other Ocular Inflammatory Disorders. TOP1362 strongly inhibited the kinase targets p38α, Syk, Src, and Lck, blocked the rise in p38α expression in hyperosmolar Chang cells, and potently reduced inflammatory cytokine release in cellular models of innate and adaptive immunities. In the EIU model, TOP1362 dose-dependently attenuated the LPS-induced rise in inflammatory cell infiltration and ocular cytokine levels with efficacy comparable to that of dexamethasone.
DOX−NOP1 is a molecular hybrid covalently joining doxorubicin (DOX) and NOP1. DOX−NOP1 showed similar increased toxicity toward resistant cancer cells and, in addition, lower cardiotoxicity than DOX.
1-Oleoyl-2-palmitoyl-rac-glycerol (1,2-OP) is a diacylglycerol containing oleic acid at the sn-1 position and palmitic acid at the sn-2 position. It enhances the inhibition of superoxide anion production by cytochalasin B when used at a concentration of 10 μM. The concentration of 1,2-OP decreases from 25.7 to 11.15% during the dry-curing process of Iberian ham.
1-Palmitoyl-3-oleoyl-rac-glycerol, a diacylglycerol featuring palmitic acid at the sn-1 position and oleic acid at the sn-3 position, serves as a substrate for diacylglycerol acyltransferase (DAGAT) in myotubes.