PRL inhibitor Cmpd-43 is a specific small molecule inhibitor and detrimerizer of phosphatase of regenerating liver (PRL), significantly decreases PRL1 trimer formation inside the cell.
PRL inhibitor Cmpd-43 (20 uM) does not inhibit the phosphatase activity of PRL1 as well as a large panel of PTPs including receptor-like PTPs, PTPμ, PTPε, LAR, PTPσ and PTPγ, cytosolic PTPs, PTP1B, Lyp, SHP1, PTPH1, HePTP, STEP, and PEZ, the dual specificity phosphatase VHR, VHZ, MKP5, CDC14A, and the low molecular weight PTP.
Cmpd-43 (0.1-50 uM) inhibits PRL1 induced cell proliferation and migration in a dose dependent manner in PRL1 expressing HEK293 cells.
Cmpd-43 also markedly delays the wound closure induced by PRL1 overexpression.
Cmpd-43 exerts anti-proliferative activity through blocking PRL1 trimerization.
Cmpd-43 inhibits PRL1-induced ERK1/2 and Akt activation in MeWo cells by blocking PRL1 trimerization.
Cmpd-43 (30 mg/kg) suppresses melanoma xenograft growth in vivo.
Cmpd-43 phenocopies the effect of genetic deletion of Prl2 and reduces Tp53 deficiency-induced tumor growth.