ZINC08383544

ZINC08383544 forms a stable complex with dimeric human PKM2, with a binding free energy of -84.285 kJ/mol; it promotes the formation of tetramers from purified human PKM2; and it activates purified human PKM2 in a dose-dependent manner, increasing its activity from 6.5 U/mL to a maximum of 9.63 U/mL at 300 nM^[1].
ZINC08383544 (200 nM) blocks the nuclear translocation of PKM2, increases cytoplasmic PKM2 levels, and reduces the phosphorylation levels of nuclear histone H3-T11 and STAT3-Y705 in HeLa and HepG2 cells^[1].
ZINC08383544 (25-200 nM) dose-dependently downregulates the expression of LDHA and GLUT1 in HeLa and HepG2 cells, with a stronger effect on LDHA in HeLa cells^[1].
ZINC08383544 inhibits the viability of HeLa, HCT116, SKBR3, HepG2 and H1299 cancer cells in a dose-dependent manner (with IC₅₀ < 100 nM for HeLa and HCT116 cells), while exerting no significant effect on normal LO2 hepatocytes^[1].
ZINC08383544 (100-600 nM; 24 h) exerts antiproliferative effects on HeLa and HepG2 cells, and these effects depend on the expression of PKM2, since knockdown of PKM2 significantly reduces the inhibitory activity of this compound^[1].

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