CK2 inhibitor 2 是一种有效的，选择性和具有口服活性的 CK2 抑制剂，IC₅₀ 值为 0.66 nM。CK2 inhibitor 2 对 Clk2 (IC₅₀=32.69 nM)/CK2 显示出高选择性。 CK2 inhibitor 2 具有良好的抗增殖和抗肿瘤活性。

CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC 50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC 50 =32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activity.

Solid

CK2 0.66 nM (IC50)

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.
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 and p-Cdc37 in HCT-116 cells.
CK2 inhibitor 2 (1-500 nM) dose-dependently inhibits exogenous ALDH1A1 enzyme activity, with an IC50 of 0.10 μM.
CK2 inhibitor 2 (5-20 μM; 24 h) inhibits the transcription and protein expression of ALDH1A1 in HCT-116 cells. has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；In solvent -80°C 6 months

[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.

In Vitro: DMSO : 50 mg/mL (127.28 mM; ultrasonic and warming and heat to 60°C)配制储备液