A PDI inhibitor
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LOC14

Item No. 17766

Technical Information
Formal Name
2-[[4-(cyclopropylcarbonyl)-1-piperazinyl]methyl]-1,2-benzisothiazol-3(2H)-one
CAS Number
877963-94-5
Molecular Formula
C16H19N3O2S
Formula Weight
Purity
≥90%
Formulation
A crystalline solid
DMF: 10mg/mLDMF:PBS (pH 7.2) (1:1): 0.5mg/mLDMSO: 3mg/mLEthanol: 3mg/mLEthanol:PBS (pH 7.2) (1:6): 0.14mg/mL
λmax
224, 317 nm
SMILES
O=C(C1CC1)N(CC2)CCN2CN3C(C(C=CC=C4)=C4S3)=O
InChi Code
InChI=1S/C16H19N3O2S/c20-15(12-5-6-12)18-9-7-17(8-10-18)11-19-16(21)13-3-1-2-4-14(13)22-19/h1-4,12H,5-11H2
InChi Key
YVBSNHLFRIVWFQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    LOC14 is an inhibitor of protein disulfide isomerase (PDI; Kd = 62 nM).1 It inhibits PDI chaperone activity in an insulin aggregation assay when used at a concentration of 75 µM. LOC14 reduces PC12 cell death induced by the misfolded huntingtin protein mHTTQ103 (EC50 = 500 nM). It reduces medium spiny neuron (MSN) degeneration in a rat postnatal cortical brain slice model of mHTTQ73-induced Huntington’s disease.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kaplan, A., Gaschler, M.M., Dunn, D.E., et alSmall molecule-induced oxidation of protein disulfide isomerase is neuroprotective. Proc. Natl. Acad. Sci. USA 112(17), E2245-E2252 (2015).