LIB3S0280 is a potent TBK1 inhibitor with an IC50 value of 493.9 nM. LIB3S0280 exhibits better anticancer effects in pancreatic cancer cell lines with high TBK1 expression. LIB3S0280 inhibits TBK1 downstream signaling pathways, including PI3K/AKT and NF-κB. LIB3S0280 induces G2/M arrest, apoptosis and cellular senescence. LIB3S0280 can be used for pancreatic ductal adenocarcinoma (PDAC) research [1].
In Vitro, LIB3S0280 (72-96 h) shows significant inhibition against high TBK1-expressing pancreatic cancer cell lines with the GI50 values of 2.24 μM (MIA PaCa-2) and 4.71 μM (PANC-1), and IC50 values of 6.64 μM (MIA PaCa-2) and 10.98 μM (PANC-1) at 96 h[1]. LIB3S0280 (10-20 μM, 3 h) inhibits TBK1 downstream signaling, including the PI3K/AKT and NF-κB pathways, by effectively reducing the phosphorylation of its key targets, AKT (Ser473) and IκBα, in MIA PaCa-2 and PANC-1 cells[1]. LIB3S0280 (10-20 μM, 48-96 h) induces G₂/M arrest, apoptosis, and cellular senescence in pancreatic cancer cells (MIA PaCa-2 and PANC-1) by modulating key regulators like p-cdc2, p-MPM2, cyclin B1, and p21[1].
References:
[1]. Wan-Hsi Shih, et al. Discovery of novel TANK-Binding Kinase 1 (TBK1) inhibitor against pancreatic ductal adenocarcinoma. Int J Biol Macromol. 2024 Dec;283(Pt 1):137296.
In Vitro, LIB3S0280 (72-96 h) shows significant inhibition against high TBK1-expressing pancreatic cancer cell lines with the GI50 values of 2.24 μM (MIA PaCa-2) and 4.71 μM (PANC-1), and IC50 values of 6.64 μM (MIA PaCa-2) and 10.98 μM (PANC-1) at 96 h[1]. LIB3S0280 (10-20 μM, 3 h) inhibits TBK1 downstream signaling, including the PI3K/AKT and NF-κB pathways, by effectively reducing the phosphorylation of its key targets, AKT (Ser473) and IκBα, in MIA PaCa-2 and PANC-1 cells[1]. LIB3S0280 (10-20 μM, 48-96 h) induces G₂/M arrest, apoptosis, and cellular senescence in pancreatic cancer cells (MIA PaCa-2 and PANC-1) by modulating key regulators like p-cdc2, p-MPM2, cyclin B1, and p21[1].
References:
[1]. Wan-Hsi Shih, et al. Discovery of novel TANK-Binding Kinase 1 (TBK1) inhibitor against pancreatic ductal adenocarcinoma. Int J Biol Macromol. 2024 Dec;283(Pt 1):137296.