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Submit ReviewAZD 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.
分子量 | 453.52 |
公式 | C21H23N7O3S |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 4.54 | 10 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: 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
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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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.