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AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2. AZD1080,with IC50 of 324 nM, inhibits tau phosphorylation in cells expressing human tau. AZD1080 inhibits tau phosphorylation in rat brain after oral dministration, with brain/plasma exposure ratio of 0.5 – 0.8 at peak concentrations. AZD1080 reverses cognitive deficits and rescues dysfunctional synapses in mice. Acute oral treatment with AZD1080 inhibits peripheral GSK3 activity, produces a dose-dependent reduction of the phosphorylated to total glycogen synthase (GS) ratio, with a mean maximal inhibitory effect of 49% at the highest dose (10 μmol/kg) at 2 h after dosing.
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Source | Oncotarget (2016). Figure 10. AZD1080 |
| Method | cell proliferation assay | |
| Cell Lines | EC cell | |
| Concentrations | 1.0, 2.0, 4.0 μM | |
| Incubation Time | 0 h, 24 h, 48 h, and 72 h | |
| Results | The MTT assay showed a significant reduction of cell viability started from 0.5 μM when exposed to AZD1080 compared with the DMSO group, and thus the www.impactjournals.com/oncotarget 27546 Oncotarget concentration of 1.0, 2.0, 4.0μM was used for further study |
| Molecular Weight | 334.37 |
| Formula | C19H18N4O2 |
| CAS Number | 612487-72-6 |
| Solubility (25°C) | DMSO 18 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related GSK-3 Products |
|---|
| CHIR-99021
CHIR-99021 (CT99021) is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively. |
| CHIR-99021 HCl
CHIR-99021 HCl (Laduviglusib; CT99021) is a hydrochloride of CHIR-99021, with IC50 of 10 nM and 6.7 nM for GSK-3α and GSK-3β, respectively. |
| SB 216763
SB 216763 is a potent and selective, cell permeable glycogen synthase kinase-3 (GSK-3) inhibitor with an IC50 value of 34 nM for GSK-3α. |
| AZD2858
AZD2858 is a potent, orally bioactive inhibitor of GSK-3 with an IC50 of 68 nM. |
| Indirubin
Indirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of ~75 nM and 0.19 μM. |
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