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The apoptotic effect of GSK-3 inhibitors: BIO and CHIR 98014 on H1975 lung cancer cells through ROS generation and mitochondrial dysfunction

Objective: GSK-3 has been reported to be upregulated in malignant diseases, including lung cancers, thus suggesting it to be a valid target for cancer treatment. The study elucidates the possible mechanism involved in the ability of GSK-3 inhibitors: BIO and CHIR 98014 to regulate proteins involved in cell death of H1975 lung cancer cells.

Results: BIO and CHIR 98014 successfully induced apoptosis at lower concentrations in H1975 cells but not in H460 lung cancer cells. Moreover, increased ROS generation and depolarization of mitochondrial membrane potential were observed in both treatments. Cleavage of caspase-3 was observed in both BIO and CHIR 98014-treated cells after 72 h with monolayer and tumorsphere cell culture models.

Conclusions: The use of GSK-3 inhibitors shows promising apoptotic abilities in clinical cancer treatments, particularly for lung cancer cells. This study is the first report to describe the significant apoptotic effects of BIO and CHIR 98014 through multiple mechanisms of H1975 NSCLC that are linked to their proliferative and migratory capacities.

Related Products

Cat.No. Product Name Information Publications Customer Product Validation
S2745 CHIR-98014 CHIR-98014 (CT98014) is a potent GSK-3α/β inhibitor with IC50 of 0.65 nM/0.58 nM in cell-free assays, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2. (31) (6)

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