PARP1/PKM2-IN-1

PARP1/PKM2-IN-1 (compound 9f) binds to purified PKM2 protein via a conformational change binding model, with a dissociation constant K_d of 0.71 μM^[1].
PARP1/PKM2-IN-1, a mixed inhibitor against purified PKM2, has a K_i value of 481 nM^[1].
PARP1/PKM2-IN-1 (0.1-5 μM) induces a dose-dependent shift in the oligomer distribution of purified 50 nM PKM2, reducing dimers and increasing trimers and tetramers; in the presence of FBP in vitro, it reduces dimers and increases trimers without altering tetramer levels^[1].
PARP1/PKM2-IN-1 (2 μM; 24 h) exhibits a better inhibitory effect on nuclear PKM2 aggregation than Olaparib (HY-10162) in CoCl₂-stimulated 4T1 cells, and reduces the size of nuclear PAR aggregates by inhibiting PARP1 activity^[1].
PARP1/PKM2-IN-1 (0.25-0.5 μM; 24 h) reduces PKM2 mRNA expression in a dose-dependent manner in 4T1 and HCC1937 cells without affecting the level of PKM1 mRNA^[1].
PARP1/PKM2-IN-1 inhibits the proliferation of 4T1, HCC1937, MCF-7, MDA-MB-231 and PC-3 cancer cell lines in 2D culture systems, with IC₅₀ values ranging from 3.19 μM to 4.57 μM^[1].
PARP1/PKM2-IN-1 (0-12.5 μM; 72 h) inhibits the formation of 4T1 cancer spheroids with an IC₅₀ of 3.83 μM; it also inhibits the viability of pre-formed spheroids with an IC₅₀ of 4.72 μM, and a concentration of 12.5 μM completely blocks spheroid formation^[1].

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