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GSK-3

Glycogen synthase kinase 3 (GSK-3) inhibitors act on GSK-3α and GSK-3β, two constitutively active kinases. The serine/threonine kinase was separated in 1980 from rabbit skeletal muscle as a kinase that phosphorylates glycogen synthase. In 1995 insulin was shown to inhibit GSK-3 through protein kinase B (PKB), also known as Akt. GSK-3 also phosphorylates β-catenin and marks it for degradation, so its inhibition activates canonical Wnt signaling. In 2008 laduviglusib, also called CHIR-99021, was combined with a second kinase inhibitor to keep mouse embryonic stem cells in a ground state of self-renewal. SB 216763, TWS119, tideglusib and AR-A 014418 are further GSK-3 inhibitors for Wnt, neuronal and metabolic studies.

2 Items

  • PROTAC GSK-3β Degrader-1
    Cat. No.
    A44084
    CAS No.
    3093409-30-1

    PROTAC GSK-3β Degrader-1

    PROTAC GSK-3β Degrader-1 is a targeted GSK-3β degrader that induces the proteasomal degradation of GSK-3β with an IC50 value of 833 nM. This compound integrates SB-216763, a known GSK-3β inhibitor, a PEG linker, and a CRBN ligand to facilitate E3 ligase-mediated degradation. It has demonstrated efficacy in reducing neurotoxicity induced by Aβ25-35 peptide and CuSO4, making it a valuable tool for researching Alzheimer's disease mechanisms and potential therapeutic interventions.

    In stock View Details
    5 mg
    $355.00
    10 mg
    $590.00
    All 3 sizes
  • PT-65
    Cat. No.
    A44087
    CAS No.
    2721998-87-2

    PT-65

    PT-65 is a PROTAC degrader targeting GSK3α and GSK3β, exhibiting DC50 values of 28.3 nM and 34.2 nM, respectively. This compound effectively inhibits excessive tau phosphorylation induced by GSK3β, amyloid-beta, and okadaic acid. PT-65 is a valuable tool for research into the pathophysiology of Alzheimer's disease, allowing for further investigation into tau-related mechanisms and potential therapeutic interventions.

    In stock View Details
    1 mg
    $265.00
    5 mg
    $675.00
    All 5 sizes

2 Items

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