EG1, a specific Pax2 inhibitor, directly binds the paired domain of Pax2 (Kd=1.35-1.5 μM) and inhibits Pax2-DNA interactions. EG1 can inhibit embryonic kidney development, a process directly dependent on Pax2 activity[1].
EG1 (0-12.5 μM; 48 hours) decreases viability in Pax2 positive renal cancer cell lines[1].EG1 (0-500 μM) is capable of inhibiting Pax2 mediated expression of EGFP without significant effects on Pax2 protein levels[1].
[1]. Grimley E, et al. Inhibition of Pax2 Transcription Activation with a Small Molecule that Targets the DNA Binding Domain. ACS Chem Biol. 2017;12(3):724-734.