AZD2858
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AZD2858是一种GSK-3选择性抑制剂,IC50值为68 nM.
糖原合酶激酶3β(GSK-3β)在典型的Wnt通路中扮演重要角色,且参与多个生物学过程[1].
在人类成骨细胞中,AZD2858可短暂提高β连环蛋白水平[1].hADSC与AZD2858孵育可显著提高成骨矿化作用.这表明抑制GSK-3可提高hADSC的成骨分化[2].
大鼠口服AZD2858疗法两周后可以剂量依赖的方式增加骨小梁量.在皮质位点也有显著效果.在生物力学测试中,脊椎抗压强度和股骨骨干力量均有提高.此外,骨形成指数有显著提高,骨形成及骨吸收的血清标记均有增加[1].另外,AZD2858可驱动间充质细胞转变为成骨细胞,使得在不稳定骨折环境中发生直接骨修复[3].
参考文献:
[1]. Marsell R, Sisask G, Nilsson Y, et al. GSK-3 inhibition by an orally active small molecule increases bone mass in rats. Bone, 2012, 50(3): 619-627.
[2]. Gilmour PS, O'Shea PJ, Fagura M, et al. Human stem cell osteoblastogenesis mediated by novel glycogen synthase kinase 3 inhibitors induces bone formation and a unique bone turnover biomarker profile in rats. Toxicol Appl Pharmacol, 2013, 272(2): 399-407.
[3]. Sisask G, Marsell R, Sundgren-Andersson A, et al. Rats treated with AZD2858, a GSK3 inhibitor, heal fractures rapidly without endochondral bone formation. Bone, 2013, 54(1): 126-132.
Storage | Store at -20°C |
M.Wt | 453.52 |
Cas No. | 486424-20-8 |
Formula | C21H23N7O3S |
Solubility | insoluble in H2O; insoluble in EtOH; ≥11.35 mg/mL in DMSO |
Chemical Name | 3-amino-6-(4-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-N-(pyridin-3-yl)pyrazine-2-carboxamide |
SDF | Download SDF |
Canonical SMILES | NC1=C(C(NC2=CC=CN=C2)=O)N=C(C3=CC=C(S(=O)(N4CCN(C)CC4)=O)C=C3)C=N1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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