化学性质:
规格 | 10mM (in 1mL DMSO) 5mg 10mg 25mg 50mg 100mg |
CAS | 612487-72-6 |
别名 |
|
化学名 | 3-[5-(morpholin-4-ylmethyl)-1H-pyridin-2-ylidene]-2-oxo-1H-indole-5-carbonitrile |
分子式 | C19H18N4O2 |
分子量 | 334.37 |
溶解度 | ≥ 16.7mg/mL in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
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 [1].
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 tau phosphorylation 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 [1].
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标签:AZD1080
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