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About This Item
Empirical Formula (Hill Notation):
C28H26N8O
Molecular Weight:
490.56
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze, protect from light
assay
≥95% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
pale yellow
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
General description
A cell-permeable, blood-brain-barrier-permeant, and orally available anilinopyrimidine compound that acts as a highly selective, potent, reversible, and ATP-competitive JNK inhibitor (IC50 = 67, 283, and 159 nM against JNK1, JNK2, and JNK3, respectively), exhibiting little or no activity toward a panel of more than 300 kinases, including p38 (IC50 >20 µM). Shown to inhibit c-jun phosphorylation both in STZ- (Streptozotocin, Cat. No. 572201 ) stimulated INS-1 β-pancreatic cells in vitro (IC50 = 216 nM) and in SNpc (substantia nigra pars compacta) TH- (tyrosine hydroxylase) positive neurons (by 75%; single p.o. dose of 30 mg/kg) from MPTP- (N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) treated mice in vivo. Effectively protects against SNpc TH-positive dopaminergic neuron loss in mice (46% vs. 27% loss with vehicle or 30 mg/kg SR-3306; p.o. b.i.d.) and rats (6-fold increase of vehicle control cell count; 10 mg/kg/day; s.c.) due to MPTP and 6-OHDA- (6-hydroxydopamine) intoxication, respectively, in vivo.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Chambers, J.W., et al. 2011. ACS Chem Neurosci.2, 198.
Crocker, C.E., et al. 2011. ACS Chem. Neurosci.2, 207.
Crocker, C.E., et al. 2011. ACS Chem. Neurosci.2, 207.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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