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A PDI inhibitor
LOC14 is an inhibitor of protein disulfide isomerase (PDI; Kd = 62 nM).1 It inhibits PDI chaperone activity in an insulin aggregation assay when used at a concentration of 75 ?M. LOC14 reduces PC12 cell death induced by the misfolded huntingtin protein mHTTQ103 (EC50 = 500 nM). It reduces medium spiny neuron (MSN) degeneration in a rat postnatal cortical brain slice model of mHTTQ73-induced Huntington’s disease.
1.Kaplan, A., Gaschler, M.M., Dunn, D.E., et al.Small molecule-induced oxidation of protein disulfide isomerase is neuroprotectiveProc. Natl. Acad. Sci. USA112(17)E2245-E2252(2015)
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