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CK2 inhibitor 2

Catalog No. T35557 CAS 2641079-92-5

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 [1].

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CK2 inhibitor 2, CAS 2641079-92-5

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Purity: 98%

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Description	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 [1].
Targets&IC50	CK2:0.66 nM, Clk2/CK2:32.69 nM
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 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) 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 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.

Molecular Weight	392.84
Formula	C21H17ClN4O2
CAS No.	2641079-92-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 50 mg/mL (127.28 mM), ultrasonic and warming and heat to 60°C

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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Keywords

CK2 inhibitor 2 2641079-92-5 代谢干细胞 Casein Kinase CK-2 inhibitor 2 Inhibitor inhibitor inhibit

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