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Description: Highly potent GSK-3 inhibitor; inhibits tau phosphorylation
Chemical Name: 3-Amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-2-pyrazinecarboxamide
Purity: ≥98% (HPLC)
Biological Activity for AZD 2858
AZD 2858 is a potent glycogen synthase kinase-3 (GSK-3) inhibitor (IC50 values are 0.9 and 5 nM for GSK-3α and GSK-3β, respectively). AZD 2858 inhibits tau phosphorylation in vitro (IC50 = 76 nM), improves fracture healing and increases bone mass in rodent models of bone fracture. Also activates Wnt signaling in vitro and in vivo. Brain permeable and orally bioavailable.
Technical Data for AZD 2858
| M. Wt | 453.52 |
| Formula | C21H23N7O3S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 486424-20-8 |
| PubChem ID | 10138980 |
| InChI Key | FHCSBLWRGCOVPT-UHFFFAOYSA-N |
| Smiles | O=C(NC=1C=NC=CC1)C=2N=C(C=NC2N)C3=CC=C(C=C3)S(=O)(=O)N4CCN(C)CC4 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AZD 2858
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 4.54 | 10 |
Preparing Stock Solutions for AZD 2858
The following data is based on the product molecular weight 453.52. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 22.05 mL | 110.25 mL | 220.5 mL |
| 0.5 mM | 4.41 mL | 22.05 mL | 44.1 mL |
| 1 mM | 2.2 mL | 11.02 mL | 22.05 mL |
| 5 mM | 0.44 mL | 2.2 mL | 4.41 mL |
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Product Datasheets for AZD 2858
References for AZD 2858
References are publications that support the biological activity of the product.
Sisask et al (2013) Rats treated with AZD2858, a GSK3 inhibitor, heal fractures rapidly without endochondral bone formation. Bone 54 126 PMID: 23337038
Berg et al (2012) Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines. J.Med.Chem. 55 9107 PMID: 22489897
Cook et al (2014) Wnt-dependent osteogenic commitment of bone marrow stromal cells using a novel GSK3β inhibitor. Stem Cell Res. 12 415 PMID: 24382458
If you know of a relevant reference for AZD 2858, please let us know.
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Keywords: AZD 2858, AZD 2858 supplier, AZD2858, AR28, glycogen, synthases, kinases, 3a, 3b, 3alpha, 3beta, inhibitors, inhibits, alzheimers, tau, phosphorylation, wnt, signaling, signalling, Glycogen, Synthase, Kinase, 3, Other, Wnt, Signaling, 7650, Tocris Bioscience
Citations for AZD 2858
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Pathways for AZD 2858
