Catalog # Availability Size / Price Qty
LOC14 | CAS No. 877963-94-5 | Protein Disulphide Isomerase Inhibitors
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Description: High affinity protein disulfide isomerase (PDI) modulator

Chemical Name: 2-[[4-(Cyclopropylcarbonyl)-1-piperazinyl]methyl]-1,2-benzisothiazol-3(2H)-one

Purity: ≥98%

Product Details
Citations (1)
Reviews (1)

Biological Activity

LOC14 is a high affinity protein disulfide isomerase (PDI) modulator (Kd = 62 nM). Forces PDI to adopt an oxidized conformation and suppresses its activity. Neuroprotective.

Technical Data

Soluble to 100 mM in DMSO
Store at +4°C

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.

Background References

  1. Small molecule-induced oxidation of protein disulfide isomerase is neuroprotective.
    Kaplan et al.
    Proc.Natl.Acad.Sci.U.S.A., 2015;112:E2245

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Citation for LOC14

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PDI inhibitor LOC14 inhibits platelet spreading over fibrinogen
By Renato Gaspar on 05/11/2019
Application: Species: Human

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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