GSK-3β-IN-28 

GSK-3β inhibitor 28 is selective and non-competitivea glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC₅₀ of 14.82 nM. GSK-3β inhibitor 28 can upregulate the expression level of phosphorylated GSK-3β and downregulate the expression of p-NF-κB, P65, C-myc and Cyclin D1. GSK-3β inhibitor 28 can induce cells apoptosis, G1 phase arrest and inhibit migration. GSK-3β inhibitor 28 can be used for the research of cancer, such as colorectal cancer^[1].

GSK-3β inhibitor 28 (Compound 7f) shows strong inhibitory activity against SW480, MDA-MB-231, and A549 cells with IC₅₀ values of 14.58, 14.61, 19.15 μM, and weak activity against MoLM13 (IC₅₀ = 25.75 μM) and HepG2 (IC₅₀ = 51.51 μM) cells^[1].
GSK-3β inhibitor 28 (1 μM) exhibits good selectivity against most kinases (MAPK, EGFR, Src) except GSK-3α, showing only a moderate inhibition rate (58.0%) against GSK-3α^[1].
GSK-3β inhibitor 28 (0.78-25 μM, 72 h) shows IC₅₀ values >25μM against LX-2 (hepatic stellate cells) and MIHA (normal hepatocytes) cells^[1].
GSK-3β inhibitor 28 (5-20 μM, 24 h) inhibits migration and reduces colony numbers in SW480 cells^[1].
GSK-3β inhibitor 28 (5-20 μM, 24 h) induces apoptosis and G1 phase arrest in SW480 cells^[1].
GSK-3β inhibitor 28 (10-20 μM) upregulates p-GSK-3β expression and downregulates the expression of p-NF-κB, P65, C-myc, Cyclin D1, and XIAP proteins in SW480 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

425.89

C₂₁H₁₆ClN₃O₃S

O=C(N1CCC2=CC=CC=C2)N(C3=CC4=C(N(C(C=C)=O)C=C4Cl)C=C3)SC1=O

Room temperature in continental US; may vary elsewhere.

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• [1]. Xu J, et al. Design, synthesis, and biological evaluation of novel GSK-3β covalent inhibitors for cancer treatment. Bioorg Chem. 2025 Sep;164:108856.  [Content Brief]