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SB 216763 is a potent and selective ATP-competitive inhibitor of the serine/threonine protein kinase glycogen synthase kinase-3 (GSK-3) α and β isozymes. Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli including insulin, growth factors, cell specification factors, and cell adhesion. SB 216763 displays similar potency for GSK-3β with 96% inhibition at 10 μM while exhibiting minimal activity against 24 other protein kinases (IC50 >10 μM). SB 216763 stimulates glycogen synthesis in Chang human liver cells with an EC50 value of 3.6 µM and induces expression of a β-catenin-LEF/TCF regulated reporter gene in HEK293 cells. SB 216763 treatment at 25-50 μM reduces cell viability in a dose-dependent manner, and leads to significant increase in apoptosis by 50% at 72 hours due to the specific down regulation of GSK-3β. Administration of SB 216763 at 20 mg/kg significantly prevents lung inflammation and the subsequent fibrosis in bleomycin (BLM)-induced pulmonary inflammation and fibrosis model in mice by significantly blocking the production of inflammatory cytokines MCP-1 and TNF-α by macrophages.
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SB 216763 purchased from AbMole
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Source | PLoS One (2012). Figure 1. SB 216763 |
| Method | dual luciferase reporter activity | |
| Cell Lines | HEK293 cells | |
| Concentrations | 10 μM | |
| Incubation Time | 24 h | |
| Results | "As expected, HEK293 cells treated with 1–20 μM SB-216763 exhibited a dose-dependent increase in Super TOPFlash activity" |
| Cell Experiment | |
|---|---|
| Cell lines | BXPC-3 cells and MIA-PaCa2 cells |
| Preparation method | BXPC-3 cells were treated with DMSO or the indicated concentration of GSK-3β inhibitors (AR-A014418 and SB216763) over the indicated time course. Relative cell viability was measured using the colorimetric 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium assay. B, MIA-PaCa2 cells and the normal human mammary epithelial cell line HMEC, and embryonic lung fibroblast cell line WI38 were treated with DMSO or the indicated GSK-3β inhibitor (25 μmol/L). |
| Concentrations | 1, 10, 25, 50µM |
| Incubation time | 24, 48 or 72h |
| Animal Experiment | |
|---|---|
| Animal models | saline induced pulmonary fibrosis model of C57BL/6N mice (12 weeks old) |
| Formulation | 25% dimethyl sulfoxide, 25% polyethylene glycol, and 50% saline |
| Dosages | 20 mg/kg |
| Administration | intravenously twice a week until day 28 |
| Molecular Weight | 371.22 |
| Formula | C19H12Cl2N2O2 |
| CAS Number | 280744-09-4 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related GSK-3 Products |
|---|
| CHIR-99021
CHIR-99021 (CT99021) is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively. |
| CHIR-99021 HCl
CHIR-99021 HCl (Laduviglusib; CT99021) is a hydrochloride of CHIR-99021, with IC50 of 10 nM and 6.7 nM for GSK-3α and GSK-3β, respectively. |
| AZD2858
AZD2858 is a potent, orally bioactive inhibitor of GSK-3 with an IC50 of 68 nM. |
| Indirubin
Indirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of ~75 nM and 0.19 μM. |
| TWS119
TWS119 is a GSK-3β inhibitor with IC50 of 30 nM. |
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