Catalog No.: PC-72381Not For Human Use, Lab Use Only.
HKB99 (PGAM1 allosteric inhibitor HKB99) is a novel potent, cellularly active PGAM1 (Phosphoglycerate mutase 1) allosteric inhibitor, HKB99 is noncompetitive with the substrate 3-PG with IC50 of 0.85 uM in in vitro enzyme assays.
HKB99 (PGAM1 allosteric inhibitor HKB99) is a novel potent, cellularly active PGAM1 (Phosphoglycerate mutase 1) allosteric inhibitor, HKB99 is noncompetitive with the substrate 3-PG with IC50 of 0.85 uM in in vitro enzyme assays.
HKB99 significantly inhibited the proliferation of NSCLC cells (PC9, HCC827, H1975, and A549) in a concentration-dependent manner with the IC50 of 17-67 uM.
HKB99 allosterically block conformational change of PGAM1 during catalytic process and PGAM1-ACTA2 interaction, disrupts cellular migration and induces apoptosis in NSCLC cells.
HKB99 resensitizes the erlotinib-resistant NSCLC cells to erlotinib treatment. HKB99 (100 mg/kg, i.p.) significantly suppresses tumor growth and augments the tumoricidal effect of erlotinib in mouse xenografts
