aNDR1 (NDR1 agonist) is a specific small-molecule agonist of Nuclear Dbf2-related kinase 1 (NDR1, STK38), specifically inhibits CRPC cells and promotes kinase activity of NDR1.
aNDR1 is tumor specific, significantly inhibits growth in PCa cells with IC50 of 1.178 uM and 1.763 uM for PC3 and DU145 cells respectivel, does not display noticeable cytotoxicity in WPMY-1 cells.
aNDR1 inhibits proliferation and migration and induces apoptosis of PCa cells in vitro.
aNDR1 increases the expression of NDR1 and can directly bind to NDR1.
aNDR1 (5 mg/kg) inhibits the growth and metastasis of PCa cells in prostate cancer cell xenograft model, with no obvious toxic pathologic damage in the heart, liver, spleen, lungs, or kidneys.
NDR1, also known as STK38, belongs to the NDR (nuclear Dbf2 related) kinase family, regulating cell mitosis, embryonic development, centrosome replication and organ size.
NDR1 mainly functions as a member of the Hippo pathway by cooperating with NDR2, LATS1 and LATS2 to phosphorylate YAP and regulate its activity.