529531
PICK1 PDZ Domain Inhibitor, FSC231
The PICK1 PDZ Domain Inhibitor, FSC231 controls the biological activity of PICK1. This small molecule/inhibitor is primarily used for Neuroscience applications.
Synonym(s):
PICK1 PDZ Domain Inhibitor, FSC231, ( E)-Ethyl-2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate, (E)-Ethyl-2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate
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About This Item
Empirical Formula (Hill Notation):
C13H10Cl2N2O3
Molecular Weight:
313.14
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 100 mg/mL
shipped in
ambient
storage temp.
2-8°C
General description
A cell-permeable acryloylcarbamate compound that selectively targets the PDZ (PSD-95/Discs-large/ZO-1 homology) domain of PICK1 (protein interacting with C kinase 1), but not PDZ domains of PSD-95 (postsynaptic density protein 95) and GRIP1 (glutamate receptor interacting protein 1), effectively competing against dopamine transporter/DAT (Ki ~10 µM in competitive binding assays), GluR2 (Ki ~10 µM in competitive binding assays), and mRluR7a (~70% inhibition by Co-IP using lysates from 50 µM FSC231-treated HEK293), c-terminus binding to PICK1 PDZ. Shown to accelerate GluR2 surface recycling after NMDR-induced internalization (t1/2 = 7.5 vs 10 min with and without 50 µM FSC231 treatment) in rat hippocampal neurons and prevent both LTD (% long-term depression = 74 vs 50 with and without 50 µM FSC231 treatment) and LTP (% long-term potentiation = 137 vs 266 with and without 50 µM FSC231 treatment) in murine hippocampal slices.
A cell-permeable acryloylcarbamate compound that selectively targets the PDZ (PSD-95/Discs-large/ZO-1 homology) domain of PICK1 (protein interacting with C kinase 1), but not those of PSD-95 (postsynaptic density protein 95) and GRIP1 (glutamate receptor interacting protein 1), effectively competing against dopamine transporter/DAT (Ki ~10 µM), GluR2 (Ki ~10 µM), and mRluR7a, c-terminus binding to PICK1 PDZ. Shown to accelerate internalized GluR2 surface recycling and suppress both long-term depression and potentiation in rat and murine hippocampal neurons.
Packaging
Packaged under inert gas
Warning
Toxicity: Regulatory Review (Z)
Reconstitution
Following reconsitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Thorsen, T.S., et al. 2010. Proc. Natl. Acad. Sci. USA107, 413.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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Qian Dou et al.
BioMed research international, 2021, 9884297-9884297 (2021-07-27)
We performed in vitro and in vivo experiments to explore the role of protein kinase C-binding protein 1 (PICK1), an intracellular transporter involved in oxidative stress-related neuronal diseases, in sepsis-related acute kidney injury (AKI). Firstly, PCR, western blotting, and immunohistochemistry
Zengyan Zhu et al.
Psychopharmacology, 240(1), 239-248 (2022-12-24)
Muscarinic acetylcholine receptors (mAChRs) have been shown to play significant roles in the regulation of normal cognitive processes in the hippocampus, and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPARs) are also involved in these processes. This study aims to explore the mAChR-mediated regulation
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