AZD2858

SKU: orb1306981

Description

AZD2858

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 486424-20-8
• MW: 453.52
• Purity: 99.25%
• Formula: C₂₁H₂₃N₇O₃S
• SMILES: C(NC=1C=CC=NC1)(=O)C=2N=C(C=NC2N)C3=CC=C(S(=O)(=O)N4CCN(C)CC4)C=C3
• Target: GSK-3
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:7 mg/mL (15.43 mM)

Bioactivity

• Target IC50:
  PKD2:2462 nM|Aurora A:4966 nM|CDK5-p25:356 nM|PIM3:1269 nM|CDK5-p35:387 nM|DYRK2:491 nM|Haspin:366 nM|CDK2-CyclinA:810 nM|CDK2-CyclinE:3310 nM|TLK2:1381 nM|GSK-3α:0.9 nM|CDK1-CyclinB:1246 nM|GSK-3β:5 nM|GSK-3:68 nM
• In Vivo:
  AZD2858 induces β-catenin stabilization in human and rat mesenchymal stem cells, activating osteoblasts and osteogenic mineralization in vitro. Treatment with AZD2858 (1 μM, 12 hours) on primary isolated human osteoblast-like cells results in a three-fold increase in β-catenin levels.
• In Vitro:
  After three weeks of treatment with 30 μM/kg AZD2858, rats exhibited increases in bone callus mineral density (28% at 2 weeks, 38% at 3 weeks) and mineral content (81% at two weeks, 93% at three weeks). Treatment with AZD2858 for 28 days resulted in time-dependent changes in serum markers of bone turnover, along with an increase in bone density. Within 7 days of AZD2858 treatment, the bone formation marker P1NP increased, and the resorption marker TRAcP-5b decreased, indicating enhanced bone metabolism and reduced absorption in rats. Oral administration of AZD2858 for two weeks led to a dose-dependent increase in bone density compared to the control group, with the greatest efficacy observed at a daily dose of 20 mg/kg (total BMC: 172% of the control group). AZD2858 treatment expedited bone fracture healing, with the presence of a bony callus and no significant cartilage components.
• Cell Research:
  Human adipose derived stem cells and rat MSCs (isolated from bone marrow of Sprague Dawley rats at less than 8 weeks after gestation) are cultured in a basal media of DMEM containing 5% FBS and 2 mM GlutaMax. Cells are seeded in basal media into 96-well plates (3–5000 cells/well) for 18 h before treatment with AZD2858 (0.3 nM to 20 mM). After 24 h, β-catenin stabilisation is measured.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AZD 2858, AZD2858, AZD-2858, GSK3, GSK-3, Glycogen synthase kinase 3, Glycogen synthase kinase-3, Inhibitor, inhibit

Compound Identifiers

PubChem CID

10138980