LOC14

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Cat.No. 5606 - LOC14 | C16H19N3O2S | CAS No. 877963-94-5
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)
Datasheet
Citations (1)
Reviews (1)
Literature

Biological Activity

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

Technical Data

M. Wt 317.41
Formula C16H19N3O2S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 877963-94-5
PubChem ID 9117962
InChI Key YVBSNHLFRIVWFQ-UHFFFAOYSA-N
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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 31.74 100

Preparing Stock Solutions

The following data is based on the product molecular weight 317.41. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.15 mL 15.75 mL 31.5 mL
5 mM 0.63 mL 3.15 mL 6.3 mL
10 mM 0.32 mL 1.58 mL 3.15 mL
50 mM 0.06 mL 0.32 mL 0.63 mL

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References

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


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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

1 Citation 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


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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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