Catalog No.: PC-27800Not For Human Use, Lab Use Only.
SMALS-329 is a small-molecule activator of liver kinase B1 (LKB1, STK11) via pseudokinase STE20-related kinase adapter protein (STRAD) with EC50 of 8.5 uM (activation 541%), binds ATP pocket of STRADα to activate LKB1.
SMALS-329 is a small-molecule activator of liver kinase B1 (LKB1, STK11) via pseudokinase STE20-related kinase adapter protein (STRAD) with EC50 of 8.5 uM (activation 541%), binds ATP pocket of STRADα to activate LKB1.
SMALS-329 activates LKB1 in tumor cell lines in a target- and dose-dependent manner.
SMALS-329 not only increases the thermal stability of STRAD, as assessed by cellular thermal shift assay (CETSA), but also the stability of LKB1.
SMALS-329 (8 uM) resulted in increased phosphorylation of the known LKB1 sites on the key LKB1 effectors AMPK1/2 and SIK1-3 in LKB1WT H358 lung cancer cell line.
SMALS-329 inhibits the viability of H358 cells in a dose-dependent manner, and LKB1 knockdown by CRISPRi reduced this effect by 1.5-fold.
SMALS-329 shows a growth inhibition 50% (GI50) ≤ 15 uM for 12 multiple cancer types.
SMALS-329 enhances PI3K/AKT and KRAS inhibitor effects.
