A 1070722

SKU: orb1310035

Description

A 1070722 is a potent, selective, and brain-penetrant dual inhibitor of GSK-3α/β (Ki = 0.6 nM). Its ability to cross the blood-brain barrier makes it a valuable chemical tool for in vitro biochemical assays and in vivo research, including potential development as a PET tracer for CNS target engagement studies.

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1384424-80-9
• MW: 362.31
• Purity: 99.90% (May vary between batches)
• Formula: C₁₇H₁₃F₃N₄O₂
• SMILES: COc1ccc2c(NC(=O)Nc3cccc(n3)C(F)(F)F)ccnc2c1
• Target: GSK-3
• Solubility: DMSO:83.33 mg/mL (230 mM)

Bioactivity

• Target IC50:
  GSK-3α:0.6 nM (ki)|GSK-3β:0.6 nM (ki)
• In Vivo:
  PET imaging experiments in anesthetized vervet/African green monkey exhibited that A 1070722 penetrated the blood-brain barrier (BBB) and accumulated in brain regions, with highest radioactivity binding in frontal cortex followed by parietal cortex and anterior cingulate, and with the lowest bindings found in caudate, putamen, and thalamus, similarly to the known distribution of GSK-3 in human brain.
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Storage & Handling

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

Alternative Names

inhibit, Glycogen synthase kinase 3, Glycogen synthase kinase-3, GSK-3β, GSK-3α, GSK3, GSK-3, Inhibitor, A 1070722, A1070722, A-1070722

Compound Identifiers

PubChem CID

49830684