CK2 inhibitor 2, with an IC50 of 0.66 nM, is a potent, selective, and orally active inhibitor of CK2. It demonstrates high selectivity for Clk2 (IC50=32.69 nM) over CK2 and exhibits favorable antiproliferative and antitumor activity[1].
体内研究
CK2 inhibitor 2 (60-90 mg/kg; oral administration twice daily for 4 weeks) significantly inhibits tumor growth in a dose-dependent manner, achieving a maximum inhibitory rate of 69% at a dose of 90 mg/kg[1].
CK2 inhibitor 2 (25 mg/kg; administered orally once) demonstrates a maximum plasma concentration (Cmax) of 7017.8 ng/mL, an elimination half-life (t1/2) of 6.67 hours, and a clearance rate (CL) of 0.60 L/h/kg in Sprague Dawley (SD) rats[1].
体外研究
CK2 inhibitor 2 demonstrates potent antiproliferative activity against PC-3, HCT-116, MCF-7, HT-29, T24, and LO2 cells, with IC50 values of 4.53 μM, 3.07 μM, 7.50 μM, 5.18 μM, 6.10 μM, and 96.68 μM, respectively[1].
CK2 inhibitor 2 (5-20 μM; 24 h) triggers apoptosis in HCT-116 cells in a dose-dependent manner. Moreover, CK2 inhibitor 2 suppresses the expression of p-Akt1S129 and p-Cdc37S13 in HCT-116 cells in a dose-dependent fashion[1].
CK2 inhibitor 2 (1-500 nM) exhibits dose-dependent inhibition of exogenous ALDH1A1 enzyme activity, achieving an IC50 value of 0.10 μM[1].
CK2 inhibitor 2 (5-20 μM; 24 h) suppresses the transcription and protein expression of ALDH1A1 in HCT-116 cells[1].
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