Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 2-hydroxy-3-[5-(4-morpholinylmethyl)-2-pyridinyl]-1H-indole-5-carbonitrile
Purity: ≥95%
Formula Markup: C19H18N4O2
Formula Weight: 334.4
CAS Number: 612487-72-6
Notes: The two isoforms of glycogen synthase kinase 3, GSK3α and GSK3β, constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.{19045} They also phosphorylate proteins that are relevant to Alzheimer’s disease and osteogenesis.{25567,25565,25566} AZD 1080 is a potent, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively).{27257,27258} It shows >14-fold selectivity against several kinases, receptors, enzymes, and ion channels.{27257} AZD 1080 inhibits tau phosphorylation in cells.{27257} It shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist (+)-MK-801 (Item No. 10009019).{27257} In humans, oral AZD 1080 inhibits GSK3 activity in peripheral blood lymphocytes following an initial delay in response.{27257}