CX-4945, CK2 (Casein Kinase 2) Inhibitor

Bioss

CX-4945, CK2 (Casein Kinase 2) Inhibitor

16

Research Use Only

98.0

CX-4945 (Silmitasertib) is a potent, selective and bioavailable CK2 (Casein Kinase 2) Inhibitor with IC50 of 1 nM. It only inhibits 7 of the 238 kinases by more than 90% at concentration of 0.5 microM, which is 500-fold selectivity over CK2. Although in cell-free systems CX-4945 inhibits FLT3, PIM1, and CDK1 with IC50 of 35 nM, 46 nM, and 56 nM, respectively, but it is inactive against FLT3, PIM1, and CDK1 in cell-based functional assays at 10 microM. CX-4945 exhibits a broad spectrum of antiproliferative activity, correlates with CK2alpha mRNA and protein levels but not the CK2alpha catalytic subunit, the regulatory CK2beta subunit, and the PI3K/Akt or PTEN mutational status. Combined inhibition of EGFR and CK2 augments the attenuation of PI3K-Akt-mTOR signaling and the killing of cancer cells. CX-4945 can potentiate senescence by blocking tumour progression in Ptenpc -/- mice. Now CX-4945 is in phase I/II clinical trials to treat cancer.

-20°C

51202000