Catalog No.: PC-25618Not For Human Use, Lab Use Only.
APL-5125 is a highly potent, selective, ATP-competitive casein kinase 2α (CK2α) inhibitor with IC50 of 0.348 nM and Ki of 0.095 nM in ADP-GloTM Assays, >300-fold selective over CLK2 and DAPK3.
APL-5125 is a highly potent, selective, ATP-competitive casein kinase 2α (CK2α) inhibitor with IC50 of 0.348 nM and Ki of 0.095 nM in ADP-GloTM Assays, >300-fold selective over CLK2 and DAPK3.
APL-5125 shows bivalent binding mode extending to the cryptic αD pocket of CK2α.
APL-5125 has >175-fold selectivity over the nearest kinases DAPK1 and DAPK3, also shows clear selectivity against a panel of 87 enzymes, ion channels, receptors and transporters.
APL-5125 shows very potent cellular inhibition of CK2α that is >150-fold more potent than silmitasertib.
APL-5125 potently inhibits p-AKT S129 (IC50 =2 nM) in vitro in human peripheral blood mononuclear cells (PBMCs).
APL-5125 (10, 30, 100 mg/kg) inhibits p-AKT S129 in HCT116-tumors in mice following oral administration.
