1. Cell Cycle/DNA Damage Stem Cell/Wnt
  2. Casein Kinase
  3. CK2 inhibitor 2

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.

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CK2 inhibitor 2 Chemical Structure

CK2 inhibitor 2 Chemical Structure

CAS No. : 2641079-92-5

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10 mM * 1 mL in DMSO
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Description

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].

IC50 & Target[1]

CK2

0.66 nM (IC50)

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[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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-Akt1S129 and p-Cdc37S13 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 Cmax (7017.8 ng/mL), elimination half-life (t1/2=6.67 h), and CL (0.60 L/h/kg) in SD rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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: Cmax=7017.8 ng/mL, t1/2=6.67 h, CL=0.60 L/h/kg.
Molecular Weight

392.84

Formula

C21H17ClN4O2

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=CC2=C(C3=CN=CC=C3C(NC4=CC(Cl)=CC=C4)=N2)C=C1)NCCO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (127.28 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5456 mL 12.7278 mL 25.4557 mL
5 mM 0.5091 mL 2.5456 mL 5.0911 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.08 mg/mL (5.29 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.08 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5456 mL 12.7278 mL 25.4557 mL 63.6391 mL
5 mM 0.5091 mL 2.5456 mL 5.0911 mL 12.7278 mL
10 mM 0.2546 mL 1.2728 mL 2.5456 mL 6.3639 mL
15 mM 0.1697 mL 0.8485 mL 1.6970 mL 4.2426 mL
20 mM 0.1273 mL 0.6364 mL 1.2728 mL 3.1820 mL
25 mM 0.1018 mL 0.5091 mL 1.0182 mL 2.5456 mL
30 mM 0.0849 mL 0.4243 mL 0.8485 mL 2.1213 mL
40 mM 0.0636 mL 0.3182 mL 0.6364 mL 1.5910 mL
50 mM 0.0509 mL 0.2546 mL 0.5091 mL 1.2728 mL
60 mM 0.0424 mL 0.2121 mL 0.4243 mL 1.0607 mL
80 mM 0.0318 mL 0.1591 mL 0.3182 mL 0.7955 mL
100 mM 0.0255 mL 0.1273 mL 0.2546 mL 0.6364 mL
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CK2 inhibitor 2 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CK2 inhibitor 2
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