| Description | 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]. |
| In vitro | CK2 inhibitor 2 (compound 1c) exhibits effective antiproliferative activities against PC-3, HCT-116, MCF-7, HT-29, T24 and LO2 cells, with IC 50 s 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-Akt1 S129 and p-Cdc37 S13 in HCT-116 cells [1]. CK2 inhibitor 2 (1-500 nM) dose-dependently inhibits exogenous ALDH1A1 enzyme activity, with an IC 50 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]. Apoptosis Analysis [1] Cell Line: HCT-116 cells Concentration: 5, 10, 20 μM Incubation Time: 24 hours Result: The apoptotic ratio reached about 55% at the concentration of 20 μM. Western Blot Analysis [1] Cell Line: HCT-116 cells Concentration: 5, 10, 20 μM Incubation Time: 24 hours Result: Inhibited the expression of p-Akt1 S129 and p-Cdc37 S13 in a dose-dependent manner. |
| In vivo | CK2 inhibitor 2 (60-90 mg/kg; p.o. twice a day for 4 weeks) significantly 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 C max (7017.8 ng/mL), elimination half-life (t 1/2 =6.67 h), and CL (0.60 L/h/kg) in SD rats [1]. Animal Model: Male BALB/c athymic nude mice (5 weeks old; 16-18 g) were injected HCT-116 cells [1] Dosage: 60, 90 mg/kg Administration: P.o. twice a day for 4 weeks Result: Inhibited the tumor growth in a dose-dependent manner. No conspicuous change in body weight. Animal Model: Sprague-Dawley (SD) rats [1] Dosage: 25 mg/kg (Pharmacokinetic Analysis) Administration: A single p.o. Result: C max =7017.8 ng/mL, t 1/2 =6.67 h, CL=0.60 L/h/kg. |
| Target activity | CK2:0.66 nM, CLK2/CK2:32.69 nM |
| molecular weight | 392.84 |
| Molecular formula | C21H17ClN4O2 |
| CAS | 2641079-92-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (127.28 mM), Sonication and heating to 60℃ are recommended. |
| References | 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. |