LOC14

Tocris Bioscience | Catalog # 5606

High affinity protein disulfide isomerase (PDI) modulator
Tocris Bioscience
Discontinued Product
5606 has been discontinued. View all Protein Disulphide Isomerase Inhibitors products.

Key Product Details

Description

High affinity protein disulfide isomerase (PDI) modulator

Product Description

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).

Product Specifications for LOC14

Molecular Weight

317.41

Formula

C16H19N3O2S

Storage

Store at +4°C

Purity

≥98% (HPLC)

Chemical Name

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

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.

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Solubility

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

Preparing Stock Solutions for LOC14

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.15 mL 15.75 mL 31.50 mL
5 mM 0.63 mL 3.15 mL 6.30 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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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 20 publications citing the usage of this product.

Product Documents for LOC14

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for LOC14

For research use only

Customer Reviews for LOC14 (1)

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  • PDI inhibitor LOC14 inhibits platelet spreading over fibrinogen
    Name: Renato Gaspar
    Species: Human
    Assay Type: Ex Vivo
    Cell Line/Tissue: Platelets
    Verified Customer | Posted 05/11/2019
    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.
    LOC14 5606

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