Description
SB 216763 can potently and selectively inhibit GSK-3alpha with IC50 of 34.3 nM.
Storage
2 years at -20 centigrade
Molecular Formula
C19H12N2O2Cl2
Chemical Name
3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Solubility
DSMO 23 mg/mL Water
In vitro
SB 216763 displays similar potency for GSK-3beta with 96% inhibition at 10 uM while exhibiting minimal activity against 24 other protein kinases including PKBalpha and PDK1 with IC50 of >10 uM. SB 216763 at 3 uM also completely prevents death of chicken dorsal root ganglion sensory neurones induced by LY-294002 regardless of NGF.
In vivo
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-alpha by macrophages, and significantly improves the survival of BLM-treated mice.
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