Discontinued Product

LOC14 (Cat. No. 5606) has been withdrawn from sale for commercial reasons.
Description: High affinity protein disulfide isomerase (PDI) modulator
Chemical Name: 2-[[4-(Cyclopropylcarbonyl)-1-piperazinyl]methyl]-1,2-benzisothiazol-3(2H)-one
Purity: ≥98% (HPLC)
Citations (2)
Reviews (1)
Literature (1)

Biological Activity for LOC14

LOC14 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).

Technical Data for LOC14

M. Wt 317.41
Formula C16H19N3O2S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 877963-94-5
PubChem ID 9117962
Smiles O=C1C2=CC=CC=C2SN1CN3CCN(C(C4CC4)=O)CC3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

References for LOC14

References are publications that support the biological activity of the product.

Kaplan et al (2015) Small molecule-induced oxidation of protein disulfide isomerase is neuroprotective. Proc.Natl.Acad.Sci.U.S.A. 112 E2245 PMID: 25848045

Zhou et al (2018) Small molecule modulator of protein disulfide isomerase attenuates mutant huntingtin toxicity and inhibits endoplasmic reticulum stress in a mouse model of Huntington's disease. Hum.Mol.Genet. 27 1545 PMID: 29462355

Chamberlain et al (2019) Lung epithelial protein disulfide isomerase A3 (PDIA3) plays an important role in influenza infection, inflammation, and airway mechanics. Redox.Biol. 22 PMID: 30735910

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Keywords: LOC14, LOC14 supplier, LOC14, High, affinity, protein, disulfide, isomerase, PDI, allosteric, modulator, Huntington, disease, Protein, Disulfide, Isomerase, 5606, Tocris Bioscience

2 Citations for LOC14

Citations are publications that use Tocris products. Selected citations for LOC14 include:

Chamberlain et al (2019) Lung epithelial protein disulfide isomerase A3 (PDIA3) plays an important role in influenza infection, inflammation, and airway mechanics. Redox Biol 22 101129 PMID: 30735910

Vikas et al (2022) Protein Disulfide Isomerase A3 Regulates Influenza Neuraminidase Activity and Influenza Burden in the Lung. Int J Mol Sci 23 PMID: 35162999

Reviews for LOC14

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PDI inhibitor LOC14 inhibits platelet spreading over fibrinogen.
By Renato Gaspar on 05/11/2019
Assay Type: Ex Vivo
Species: Human
Cell Line/Tissue: Platelets

Washed platelets (2 x 10ˆ7 platelets/mL) were incubated in absence or presence of LOC14 (0.1, 1 and 10 µM) for 10 minutes at 37°C, then 300 µL of the solution was dispensed on a fibrinogen (100 µg/mL)-coated coverslip for 45 minutes at 37°C. Non-adhered platelets were removed and the coverslip washed three times with PBS. Adhered platelets were fixed using 0.2% paraformaldehyde for 10 minutes. This solution was then removed and coverslips washed three times with PBS before the addition of 0.1% (v/v) Triton-X to permeabilise the cells. After removal of Triton-X and further washes using PBS, platelets were stained with Alexa Fluor 488-conjugated phalloidin (1:1000 v/v) for 1 hour in the dark at room temperature. Coverslips were mounted onto microscope glass slides and imaged using a 100x oil immersion lens on a Nikon A1-R Confocal microscope.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Gut Hormones Poster

Gut Hormones Poster

The gastrointestinal tract is the largest endocrine gland in the human body, secreting hormones that affect digestion, appetite and energy expenditure. Neuropeptide modulators and gut hormones that influence appetite are reviewed in this poster.