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AZD1080

Cat No.
CEI-1228
Description
AZD1080 is a selective, orally active, brain permeable inhibitor of GSK3 with Ki values of 6.9 nM and 31 nM for human GSK3α and GSK3β, respectively.
Product Overview
AZD1080 is a novel, potent and selective inhibitor of Glycogen synthase kinase-3β (GSK3β) with the Ki values of 6.9 nM and 31 nM, respectively. AZD1080 has been reported to inhibit GSK3β by binding within the ATP pocket by means of the high resolution X-ray crystal structure. In addition, AZD1080 has been noted to suppression recombinant human GSK3α and GSK3β with the Ki values of 6.9 nM and 31 nM, respectively. AZD1080 has also shown the selectivity against other kinases with the Ki values of 1150nM, 429nM,1980nM and >10μM for cdk2, cdk5, cdk2 and Erk2, respectively. Furthermore, AZD1080 has been revealed to concentration-dependently inhibit tauphosphorylation with the IC50 value of 324nM in 3T3 cell lines. Besides, AZD1080 has exhibited the good oral bioavailability the high blood-brain barrier permeability values of 8 × 10^-3cm/min in rat.
CAS No.
612487-72-6
Molecular Weight
334.37
Purity
0.9991
Storage
Store at-20°C
Targets
GSK-3α; GSK-3β
IC50
6.9 nM (Ki); 31 nM (Ki)
Molecular Formula
C19H18N4O2
Chemical Name
3-[5-(morpholin-4-ylmethyl)-1H-pyridin-2-ylidene]-2-oxo-1H-indole-5-carbonitrile
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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