Chemical Name: 2-[[4-(Cyclopropylcarbonyl)-1-piperazinyl]methyl]-1,2-benzisothiazol-3(2H)-one
Biological ActivityLOC14 is a high affinity allosteric inhibitor of protein disulfide isomerase A3 (PDIA3) modulator (Kd = 62 nM, IC50 = 5 μM). In an animal model of Huntington's disease LOC14 extends survival, improves motor function, reduces ER stress from mHTT and preserves dopamine and DARPP32 levels. LOC14 is neuroprotective and rescues medium spiny neurons from neurodegeneration. LOC14 also decreases influenza A protein production in cells (IC50 = 4.97 μM).
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Small molecule-induced oxidation of protein disulfide isomerase is neuroprotective.
Kaplan et al.
Citation for LOC14
The citations listed below are publications that use Tocris products. Selected citations for LOC14 include:
1 Citation: Showing 1 - 1
Lung epithelial protein disulfide isomerase A3 (PDIA3) plays an important role in influenza infection, inflammation, and airway mechanics.
Authors: Chamberlain Et al.
Redox Biol 2019;22:101129
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