AZD 2858

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Cat.No. 7650 - AZD 2858 | C21H23N7O3S | CAS No. 486424-20-8
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)
Datasheet
Citations
Reviews
Literature (8)
Pathways (1)

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.

Select a batch to recalculate based on the batch molecular weight:
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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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.

View Related Products by Product Action

View all Glycogen Synthase Kinase 3 Inhibitors

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

Citations are publications that use Tocris products.

Currently there are no citations for AZD 2858. Do you know of a great paper that uses AZD 2858 from Tocris? Please let us know.

Reviews for AZD 2858

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer Research Product Guide

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

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Kinases Product Listing

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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  • MAPK Signaling
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Neurodegeneration Product Guide

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  • Alzheimer's disease
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Stem Cell Research Product Guide

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Stem Cells Scientific Review

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Alzheimer's Poster

Alzheimer's Poster

Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.

Schizophrenia Poster

Schizophrenia Poster

Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.

Stem Cells Poster

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.

Pathways for AZD 2858

Wnt Signaling Pathway

Wnt Signaling Pathway

The Wnt pathway is involved in cellular differentiation and proliferation in adult tissues and also during embryogenesis. Disturbances within the pathway may lead to the formation of tumors and promote metastasis.