FSC231

SKU: orb2566213

Description

FSC231 is a small molecule inhibitor of protein kinase Cα-interacting protein 1 (PICK1). It demonstrates analgesic efficacy in paclitaxel-induced neuropathic pain models by inhibiting PICK1, which modulates downstream targets including GSK-3β and ERK1/2. This compound is a valuable research tool for studying neuropathic pain mechanisms in both in vitro and in vivo settings.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1215849-96-9
• MW: 313.14
• Formula: C₁₃H₁₀Cl₂N₂O₃
• SMILES: C(=C(/C(NC(OCC)=O)=O)\C#N)\C1=CC(Cl)=C(Cl)C=C1
• Target: iGluR,Others
• Solubility: 10% DMSO+90% Corn Oil:2 mg/mL (6.39 mM);DMSO:40 mg/mL (127.74 mM)

Bioactivity

• In Vivo:
  Methods: The expression level of PICK1 in rat dorsal root ganglia (DRG) was altered by vector plasmids, and the effect of PICK1 on paclitaxel (PTL)-induced neuropathic pain in rats was observed in combination with FSC231 (78.40 μg/kg, intraperitoneal injection). The possible molecular mechanisms were explored by quantitative real-time polymerase chain reaction (qRT-PCR), Western Blot and co-immunoprecipitation (Co-IP) techniques. Results: PTL treatment significantly reduced the mechanical withdrawal threshold (MWT) and thermal withdrawal latency (TWL) of rats, promoted DRG inflammation and the release of substance P (SP), stimulated PICK1 expression, reduced the level of α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid receptor 2 (AMPAR, GluA2), and increased the phosphorylation of rat glycogen synthase kinase-3β (GSK-3β) and extracellular regulated protein kinase 1/2 (ERK1/2), while FSC231 treatment could alleviate the above effects induced by PTL and alleviate the effects of PTL-induced neuropathic pain in rats. In addition, PICK1 overexpression could counteract the decreased PICK1 level, increased GluA2 level, and decreased phosphorylation of GSK-3β and ERK1/2 caused by FSC231 treatment. The results of Co-IP confirmed the interaction between PICK1 and GluA2. Both FSC231 treatment and PICK1 silencing improved PTL-induced MWT reduction, TWL shortening, inflammation, SP release, and related gene expression changes, with cumulative effects.
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• In Vitro:
  FSC231 (50 μM) treatment inhibits COS7 cells and blocks the interaction between GluR2 and PICK1 in cells . Methods: FSC231 (50 μM) was used to treat CA1 neurons in acute slices to observe its effect on LTP expression in neurons. Results: FSC231 can significantly reduce LTP expression.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Compound Identifiers

PubChem CID

45100309