LOC14

LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding[1]. LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells[3].

Product Specifications

CAS Number

[877963-94-5]

UNSPSC

12352005

Hazard Statement

H302

Target

PDI

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/loc14.html

Purity

98.0

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C(C=CC=C1)=C1S2)N2CN3CCN(C(C4CC4)=O)CC3

Molecular Formula

C16H19N3O2S

Molecular Weight

317.41

Precautions

H302

References & Citations

[1]Kaplan A, et al. Small molecule-induced oxidation of protein disulfide isomerase is neuroprotective. Proc Natl Acad Sci U S A. 2015 Apr 28;112 (17) :E2245-52.|[2]Chamberlain N, et al. Lung epithelial protein disulfide isomerase A3 (PDIA3) plays an important role in influenza infection, inflammation, and airway mechanics. Redox Biol. 2019 Apr;22:101129.|[3]Zhou X, et al. 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. 2018 May 1;27 (9) :1545-1555.