CK2 inhibitor 2

Casein Kinase

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CK2 Inhibitor 2, characterized as a potent, selective, and orally active inhibitor of CK2, demonstrates an impressive IC50 value of 0.66 nM. It exhibits high selectivity towards Clk2 with an IC50 of 32.69 nM in comparison to CK2. Furthermore, CK2 Inhibitor 2 has been shown to possess promising antiproliferative and antitumor activities [1].

CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activity[1].CK2 inhibitor 2 (compound 1c) exhibits potent antiproliferative activities against PC-3, HCT-116, MCF-7, HT-29, T24 and LO2 cells, with IC50s 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) induces apoptosis of HCT-116 cells in a dose-dependent manner. CK2 inhibitor 2 dose-dependently suppresses the expression of p-Akt1S129 and p-Cdc37S13 in HCT-116 cells[1].CK2 inhibitor 2 (1-500 nM) dose-dependently inhibits exogenous ALDH1A1 enzyme activity, with an IC50 of 0.10 μM[1].CK2 inhibitor 2 (5-20 μM; 24 h) inhibits the transcription and protein expression of ALDH1A1 in HCT-116 cells[1].CK2 inhibitor 2 (60-90 mg/kg; p.o. twice a day for 4 weeks) obviously inhibits the tumor growth dose-dependently with a maximum inhibitory rate of 69% at a dose of 90 mg/kg[1].CK2 inhibitor 2 (25 mg/kg; a single p.o.) exhibits Cmax (7017.8 ng/mL), elimination half-life (t1/2=6.67 h), and CL (0.60 L/h/kg) in SD rats[1].[1]. Wang Y, et, al. Discovery of 5-(3-Chlorophenylamino)benzo[ c][2, 6]naphthyridine Derivatives as Highly Selective CK2 Inhibitors with Potent Cancer Cell Stemness Inhibition. J Med Chem. 2021 Apr 22; 64(8):5082-5098.