TPh A

TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a K_i of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells^[1]. In Vitro: The Pirin is a nuclear protein with the nuclear factor I/CCAAT box transcription factor (NFI/CTF). Pirin proteins are highly conserved between mammals, plants, fungi, and prokaryotic organisms and are considered to belong to the cupin superfamily.
TPh A (20 μM; 5 hours) reduces the amount of pirin-bound Bcl3 and inhibits the interaction between pirin and Bcl3 in HEK293T cells in a glutathione S-transferase (GST) pulldown assay (HEK293T cells are transfected with vectors that encoded bcl3-Myc and pirin-His6 for 43 h of transfection)^[1].
TPh A (0-100 μM; 48 hours) does not exert any potent cytotoxic activity against many human cancer cell lines, it against MCF7, MDA-MB231, HeLa, DU145, HepG2, A549, HT1080, WM266-4, and SK-MEL-28 cells with IC₅₀ values >50 μM, and exhibits IC₅₀ values of 27 μM, 20 μM and 26 μM for PC3 HL60 and HT29 cells, respectively^[1].
TPhA (0-50 μM; 48 hours) inhibits cell migration in WM266-4 cells, SK-MEL-28 cell in a concentration-dependent manner^[1].