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Formula | C21H23N7O3S |
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Molecular Weight | 453.52 | CAS No. | 486424-20-8 | ||||
Solubility (25°C)* | In vitro | DMSO | 7 mg/mL (15.43 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats. | ||
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In vitro | AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, inhibits tau phosphorylation at the S396 site, activates Wnt signaling pathway. AZD2858 treatment (1 μM, 12 h) on primary isolated human osteoblast-like cells results in a 3-fold increase of β-catenin levels. [1] AZD2858 causes β-catenin stabilisation in human and rat mesenchymal stem cells, stimulates hADSC commitment towards osteoblasts and osteogenic mineralisation in vitro. [2] | ||
In vivo | In rats, oral AZD2858 treatment causes a dose-dependent increase in trabecular bone mass compared to control after a two-week treatment with a maximum effect at a dose of 20 mg/kg once daily (total BMC: 172% of control). A small but significant effect is also seen at cortical sites (total BMC: 111% of control). [1] AZD285 treatment (30 μmol/kg) on rats daily for up to 3 weeks shows an increase in both mineral density (of 28% at 2 weeks and 38% at 3 weeks) and mineral content (of 81% at 2 weeks and 93% at 3 weeks) in the calluses. AZD285 treatment makes the fractures heals more rapidly, with a bony callus without an obvious endochondral component. [3] AZD2858 produces time-dependent changes in serum bone turnover biomarkers and increases bone mass over 28 days exposure in rats. After 7 days, AZD2858 increases the bone formation biomarker P1NP, and reduces the resorption biomarker TRAcP-5b, indicating increased bone anabolism and reduced resorption in rats. [2] |
Kinase Assay:[1] |
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Cell Assay:[2] |
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Animal Study: [2] |
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Data from [Data independently produced by , , FEBS Lett, 2016, 590(11):1614-29]
Visualization strategies to aid interpretation of high-dimensional genotoxicity data [ Environ Mol Mutagen, 2024, 10.1002/em.22604] | PubMed: 38757760 |
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] | PubMed: 34997030 |
The small molecule DIPQUO promotes osteogenic differentiation via inhibition of glycogen synthase kinase 3 β signaling [ J Biol Chem, 2021, S0021-9258(21)00485-3] | PubMed: 33895139 |
A novel human colon signet-ring cell carcinoma organoid line: establishment, characterization and application [ Carcinogenesis, 2020, 41(7):993-1004] | PubMed: 31740922 |
Integrin alpha11 is an Osteolectin receptor and is required for the maintenance of adult skeletal bone mass. [ Elife, 2019, 10.7554/eLife.42274] | PubMed: 30632962 |
Predictions of genotoxic potential, mode of action, molecular targets, and potency via a tiered multiflow® assay data analysis strategy [ Environ Mol Mutagen, 2019, 60(6):513-533] | PubMed: 30702769 |
SFRP2 enhanced the adipogenic and neuronal differentiation potentials of stem cells from apical papilla. [Lin X, et al. Cell Biol Int, 2017, 41(5):534-543] | PubMed: 28244619 |
Investigating the Generalizability of the MultiFlow ® DNA Damage Assay and Several Companion Machine Learning Models With a Set of 103 Diverse Test Chemicals. [ Toxicol Sci, 2017, 162(1):146-166] | PubMed: 29106658 |
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