877963-94-5
Chemical Structure
LOC14
- CAS No.: 877963-94-5
- Formula:C16H19N3O2S
- Molecular Weight:317.41
IUPAC Name: 2-((4-(cyclopropanecarbonyl)piperazin-1-yl)methyl)benzo[d]isothiazol-3(2H)-one
InChIKey: YVBSNHLFRIVWFQ-UHFFFAOYSA-N
SMILES: O=C(C(C=CC=C1)=C1S2)N2CN3CCN(C(C4CC4)=O)CC3
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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LOC14 | 98.0% | 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. LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells. | ||||||||||||||||||||
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LOC14 (Standard) | ≥98% | LOC14 (Standard) is the analytical standard of LOC14 (HY-100432). This product is intended for research and analytical applications. 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. LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
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