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CK2 inhibitor 2

CAS No. :

MCE 站：CK2 inhibitor 2

产品活性：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。

研究领域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt

作用靶点：Casein Kinase

In Vitro: 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^S129 and p-Cdc37^S13 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.

In Vivo: 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.

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