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CAS No.: 486424-20-8

AZD2858 Catalog No. CSN13894

Synonyms: AZD2858

AZD2858 is an inhibitor of GSK-3 with IC50 of 68 nM that can inhibit the tau phosphorylation of S396 site and activate Wnt signaling pathway.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 GSK-3

IC50:68nM
描述Glycogen synthase kinase 3 is a serine/threonine protein kinase that mediates the addition of phosphate molecules onto serine and threonine amino acid residues. In mammals GSK-3 is encoded by two paralogous genes, GSK-3α and GSK-3β. GSK-3 is active in a number of central intracellular signaling pathways, including cellular proliferation, migration, glucose regulation, and apoptosis^[3]. AZD-2858, known as a GSK-3 inhibitor, had potency at both GSK-3β and GSK-3α enzymes with K_i value of 5nMand IC₅₀ value of 0.9nM, respectively, both of which were measured by ATP assay ^[4]. In vitro, treatment of primary isolated human osteoblast-like cells with 1μM AZD2858 for 12h showed a significant increase of β-catenin, and the IC₅₀ is 68nM for inhibition of tau phosphorylation by AZD2858 in 4-repeat-tau 3T3 cells ^[5]. Moreover, Western blotting result demonstrated that AZD-2858 inhibited tau phosphorylation in the transfected 3T3 fibroblasts in a dose-dependent fashion with increasing concentrations (100 nM to 50 μM) , exhibiting IC₅₀ value of 76nM ^[6]. Both the relative protein expression of the osteogenic markers TAZ and osterix following treatment with 6 nM to 20 μM of AZD2858 for 18h were increased in hADSC, demonstrating inhibition of GSK-3 stimulated osteoblastogenesis by AZD-2858. In addition, incubation of hADSC with 200nM AZD2858 for 26 days led to a marked increase in osteogenic mineralisation relative to DMSO vehicle control, indicating that inhibition of GSK-3 enhances osteogenic differentiation of hADSC^[4]. One In vivo study showed that oral gavage with AZD2858 (30 μmol/kg/day) produced time-dependent changes in serum bone turnover biomarkers and increased bone mass over 28 days exposure both in Female Han Wistar and Sprague–Dawley rats^[4], while the other one suggested that oral administration with AZD2858 to female Sprague Dawley rats caused a dose-dependent increase in trabecular bone mass compared to control group after a two-week treatment with a maximum effect at a dose of 20 mg/kg once daily ^[7]. Both in vivo studies revealed that AZD2858 may prove effective as an anabolic strategy in the treatment of diseases characterized by low bone mass.
作用机制AZD2858 binds to GSK-3 kinase to inhibit the formation of axin/GSK-3/APC-complex in Wnt-signaling pathway thereby stabilizing β-catenin to accumulate in the cytoplasm and translocate into the nucleus where it activates transcription ^[5].
动物研究
剂量
Rat: 0.2 mg/kg - 20 mg/kg^[3] (p.o.) Mice: 30 mg/kg^[4] (s.c., BID)

给药途径
p.o., s.c.
参考文献

动物研究
剂量	Rat: 0.2 mg/kg - 20 mg/kg^[3] (p.o.) Mice: 30 mg/kg^[4] (s.c., BID)
给药途径	p.o., s.c.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2050 mL
- 11.0249 mL
- 22.0499 mL
- 5 mM
- 0.4410 mL
- 2.2050 mL
- 4.4100 mL
- 10 mM
- 0.2205 mL
- 1.1025 mL
- 2.2050 mL

技术信息

CAS号

486424-20-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H23N7O3S

运输

蓝冰

分子量

453.52

别名

AZD2858

溶解度

DMSO	7.0 mg/mL (15.4 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

30% PEG400+0.5% Tween80+5% propylene glycol+water

30 mg/mL

suspension

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