YU252 (YU239252) is a small molecule SPAK inhibitor with IC50 of 8.23 uM in in vitro SPAK ELISA assay at 10 uM ATP.
YU252 decreases ion co-transporter activity and inhibits migration in glioblastoma cells by reducing both NKCC1 and KCC phosphorylation, inhibits glioblastoma proliferation and tumor growth in mice.
YU252 can potentially be used to inhibit the WNK/SPAK-OSR1 network in GBM and limit tumorigenesis in vivo.
