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XML generation date: 2024-09-20 06:15:04.832
Product last modified at: 2024-09-19T22:13:09.223Z
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SB216763 #13621

    Product Information

    Product Usage Information

    SB216763 is supplied as a lyophilized powder. For a 25 mM stock, reconstitute the 5 mg in 538.8 µl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 5-25 µM for 3-24 hr.

    Storage

    Store lyophilized or in solution at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

    Product Description

    Molecular Weight 371.2 g/mol
    Purity >98%
    Molecular Formula C19H12Cl2N2O2
    CAS 280744-09-4
    Solubility Soluble in DMSO at 24mg/ml.

    Background

    The maleimide derivative SB216763 is a potent and selective cell permeable inhibitor of glycogen synthase kinase 3 (GSK-3). Research studies using peptide-based protein kinase assays show that SB216763 inhibits GSK-3α in an ATP competitive manner with an IC50 of 34 nM, and is an equally effective GSK3-β inhibitor. Similar assays demonstrate that SB216763 (at concentrations up to 10 µM) does not inhibit as many as 24 other serine/threonine and tyrosine protein kinases (1). As a consequence of inhibiting GSK-3, SB216763 stimulates glycogen synthesis in human liver cells (EC50 3.6 µM) via glycogen synthase activation and induces expression of a β-catenin regulated reporter gene in HEK293 cells (1). Furthermore, SB216763 induces accumulation of β-catenin, a key downstream effector in the Wnt signaling pathway, in many cell types (2-5). Additional research indicates that SB216763 can prevent neuronal cell death induced by PI3 kinase pathway inhibition (2). Glycogen synthase kinase 3 inhibitors such as SB216763 can be important research tools in studying the functional role of GSK-3 in cell signaling pathways.
    For Research Use Only. Not For Use In Diagnostic Procedures.
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