MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

AZD2858

CAS No. : 486424-20-8

MCE 国际站：AZD2858

产品活性：AZD2858 是一种有效的，可口服的 GSK-3 抑制剂，可以抑制 GSK-3α 和 GSK-3β 的活性，IC₅₀ 值分别为 0.9 和 5 nM，可用于骨折愈合的研究。

研究领域：PI3K/Akt/mTOR  |  Stem Cell/Wnt

作用靶点：GSK-3

In Vitro: AZD2858 (1 μM) increases β-catenin levels after a short period of time in human osteoblast cells. AZD2858 inhibits GSK-3β dependent phosphorylation with an IC₅₀ of 68 nM. AZD2858 (10 nM) has no effect on β-catenin levels. AZD2858 increases TAZ expression and osterix expression both by 1.4-fold, with EC₅₀ of 440 nM and 1.2 μM, respectively, in hADSC. AZD2858 also induces a marked increase in osteogenic mineralisation in hADSC. AZD2858 (AR28) demonstrates from 70- to greater than 6000-fold selectivity over a panel of other kinases and an IC₅₀ of 5 nM. AR28 inhibits GSK-3 in murine cells and indicates activation of the canonical Wnt/β-catenin signaling cascade. AR28 (50, 10, and 1 nM) enhances the clonogenic ability of mesenchymal progenitors with osteogenic and adipogenic potential. AR28 (50 μM) also enhances the differentiation ability of mesenchymal progenitors to the osteogenic but not adipogenic lineage in vitro.

In Vivo: AZD2858 (20 mg/kg) causes a dose-dependent increase in trabecular bone mass compared to control after a two-week treatment with a maximum effect. AZD2858 exhibits a substantial effect on fracture healing. AZD2858 (20 mg/kg) causes an increase in cortical BMC of 9%, cortical area of 10%, and cortical thickness of 11% at 3 weeks in the non-operated right femur of rats. AZD2858 (30 μmol/kg/day) alters the biomarkers of bone turnover with statistically significant increases in P1NP and decreases in TRAcP-5b seen from 3 days of treatment and onwards. AZD2858 demonstrates significant changes in serum bone turnover markers (P1NP and TRAcP-5b) and femur bone formation after only 7 days of daily dosing. AZD2858 (AR28, 30 mg/kg, s.c.) stimulates an increase in an initial wave of mesenchymal progenitors with osteogenic and adipogenic potential and drives their differentiation to the osteogenic lineage in BALB/c mice. AR28 (30 mg/kg, s.c.) enhances the proliferation of committed hematopoietic progenitors and their differentiation to the osteoclast lineage but does not prevent an overall increase in bone mass.

相关产品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Stem Cell Signaling Compound Library  |  Wnt/Hedgehog/Notch Compound Library  |  Anti-Aging Compound Library  |  Reprogramming Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Orally Active Compound Library  |  Anti-Alzheimer's Disease Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Cancer Metabolism Compound Library  |  Neurodegenerative Disease-related Compound Library  |  Anti-Obesity Compound Library  |  Glucose Metabolism Compound Library  |  Targeted Diversity Library  |  Antidepressant Compound Library  |  Human Metabolite Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Cancer Stem Cells Compound Library  |  Membrane Protein-targeted Compound Library  |  BRD5648  |  AR-A014418  |  GSK-3β inhibitor 3  |  SAR502250  |  GSK 3 Inhibitor IX  |  K00546  |  GSK-3β inhibitor 10  |  DIF-3  |  GSK3-IN-2  |  RGB-286638  |  Laduviglusib (GMP)  |  ROCK-IN-5  |  Indirubin-3′-oxime  |  GSK-3β inhibitor 2  |  Bikinin  |  Alsterpaullone  |  GSK3 Substrate, α, β subunit  |  Indirubin-3'-monoxime  |  GSK-3 Inhibitor XIII  |  GSK-3β inhibitor 7  |  Aloisine A  |  Aloisine RP106  |  GSK-3β inhibitor 11  |  AChE/BACE1/GSK3β-IN-1  |  7BIO  |  5-Iodo-indirubin-3'-monoxime  |  6-Me-ATP trisodium  |  3F8

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。