A potent

AZD 1080 – 1 mg

Brand:
Cayman
CAS:
612487-72-6
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

A potent, selective, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively); shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist (+)-MK-801

Formal name: 2-​​hydroxy-​​3-​​[5-​(4-​morpholinylmethyl)​-​2-​pyridinyl]-​1H-​indole-​​5-​carbonitrile

Synonyms: 

Molecular weight: 334.4

CAS: 612487-72-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|GSK3||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease

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