A potent inhibitor of GSK3α and GSK3β
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AZD 1080

Item No. 16676

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-hydroxy-3-[5-(4-morpholinylmethyl)-2-pyridinyl]-1H-indole-5-carbonitrile
CAS Number
612487-72-6
Molecular Formula
C19H18N4O2
Formula Weight
334.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 0.25 mg/ml
λmax
233, 255, 302, 347, 430 nm
SMILES
OC(NC1=C2C=C(C#N)C=C1)=C2C3=NC=C(CN4CCOCC4)C=C3
InChi Code
InChI=1S/C19H18N4O2/c20-10-13-1-3-16-15(9-13)18(19(24)22-16)17-4-2-14(11-21-17)12-23-5-7-25-8-6-23/h1-4,9,11,22,24H,5-8,12H2
InChi Key
BLTVBQXJFVRPFK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $32

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    5 mg

    $113

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    10 mg

    $160

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    25 mg

    $359

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    Product Description

    AZD 1080 is a potent, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively).1,2 It shows >14-fold selectivity against several kinases, receptors, enzymes, and ion channels.1 AZD 1080 inhibits tau phosphorylation in cells.1 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).1 In humans, oral AZD 1080 inhibits GSK3 activity in peripheral blood lymphocytes following an initial delay in response.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Georgievska, B., Sandin, J., Doherty, J., et al. AZD1080, a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans. J. Neurochem. 125(3), 446-456 (2013).

    2. Eldar-Finkelman, H., and Martinez, A. GSK-3 inhibitors: Preclinical and clinical focus on CNS. Front. Mol. Neurosci. 4, 32 (2011).

    Product Citations

    Alavi, M.V. Tau phosphorylation and OPA1 proteolysis are unrelated events: Implications for Alzheimer’s Disease. Biochim. Biophys. Acta Mol. Cell Res. 1868(12), 119116 (2021).