GSK-3α/β-IN-1 is a selective inhibitor of glycogen synthase kinase-3 alpha and beta (GSK-3α/β), demonstrating IC50 values of 0.265 μM for GSK-3α and 0.255 μM for GSK-3β. Additionally, GSK-3α/β-IN-1 exhibits PKA inhibition with an IC50 of 0.188 μM. This compound effectively reduces cell viability in several glioblastoma (GBM) cell lines, with IC50 values ranging from 3 to 6 μM over 72 hours, while displaying minimal toxicity to human astrocytes. GSK-3α/β-IN-1 also shows promising central nervous system activity in human blood-brain barrier models of GBM, supporting its potential as a therapeutic agent in cancer research.
GSK-3α/β-IN-1 is a selective inhibitor of glycogen synthase kinase-3 alpha and beta (GSK-3α/β), demonstrating IC50 values of 0.265 μM for GSK-3α and 0.255 μM for GSK-3β. Additionally, GSK-3α/β-IN-1 exhibits PKA inhibition with an IC50 of 0.188 μM. This compound effectively reduces cell viability in several glioblastoma (GBM) cell lines, with IC50 values ranging from 3 to 6 μM over 72 hours, while displaying minimal toxicity to human astrocytes. GSK-3α/β-IN-1 also shows promising central nervous system activity in human blood-brain barrier models of GBM, supporting its potential as a therapeutic agent in cancer research.
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