P2X7R antagonist-1

P2X7R antagonist-1 (Compound 17d) (3.57-50 μM) potently inhibits the formation of P2X7R macropores in HEK293T-hP2X7R cells, with an IC₅₀ value of 3.57 μM^[1].
P2X7R antagonist-1 reduces the inhibitory activity against topoisomerase II (IC₅₀ = 9.23 μM) and improves the target selectivity for P2X7R^[1].
P2X7R antagonist-1 (5 μM) exhibits broad-spectrum antiproliferative activity in MCF-7, HGC-27, MKN-45, TE-1, KYSE-150, 4T1 and B16-F10 cells, with relatively strong activity in MCF-7 cells (IC₅₀ = 0.42 μM). The inhibition rates at 5 μM are 96.3%, 92.7%, 84.7%, 90.8%, 86.5%, 86.1% and 44.3%, respectively^[1].
P2X7R antagonist-1 (50-200 nM) inhibits the invasion and migration of human breast cancer MCF-7 cells in a dose-dependent manner by downregulating the expression of FAK and MMP-9^[1].
P2X7R antagonist-1 (17d) (0.1 μM) exhibits antimetastatic activity against human breast cancer MCF-7 cells, which is mainly mediated by the inhibition of P2X7R; this is confirmed by the reduced potency observed in P2X7R-knockdown cells^[1].

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