5.06074
PP2A Activating Ligand, ITH12246
Synonym(s):
PP2A Activating Ligand, ITH12246
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About This Item
Empirical Formula (Hill Notation):
C16H19N3O2 · xHCl
CAS Number:
Molecular Weight:
285.34 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77
Assay
≥98% (HPLC)
Quality Level
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
General description
A cell-permeable, relatively non-toxic, 1,8-naphthyridine derived compound that blocks the inhibitory effect of protein phosphatase inhibitors, such as okadaic acid, on protein phosphatase 2A (PP2A). Exhibits blood-brain barrier permeability. Protects neurons against β-amyloid peptides (Ab1-42) toxicity and okadaic acid (Cat. No. 459620)-induced tau hyperphosphorylation. Also protects against rotenone and oligomycin A induced neurotoxicity in SH-SY5Y neuroblastoma cells (at ~300 nM). Prevents the development of glutamate-induced neuronal lesions in rat hippocampal slices by up-regulating PP2A (~ 3.0 µM). Shown to reverse the scopolamine-induced memory loss in mice (~10 mg/kg i.p) and significantly reduces the infarct volume in an animal model of stroke (~2.5 mg/kg). Also acts as an inhibitor of acetylcholinesterase activity in Electrophorus electricus (IC50 = 60 nM) and human erythrocytes (IC50 = 780 nM).
Biochem/physiol Actions
Primary Target
PP2A
PP2A
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Lorrio, S., et al. 2013. ACS Chem. Neurosci.4,1267.
de Los Rios, C., et al. 2010. J. Med. Chem.53,5129.
de Los Rios, C., et al. 2010. J. Med. Chem.53,5129.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Certificates of Analysis (COA)
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