Art. -Nr.: HY-132175

CK2 inhibitor 2

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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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Reinheit: 98.51%
CAS. Nr.: 2641079-92-5
Formel: C₂₁H₁₇ClN₄O₂
Molecular Weight:392.84

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

CK2 inhibitor 2 Chemical Structure

CAS. Nr.: 2641079-92-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CK2

0.66 nM (IC₅₀)

Alle Casein Kinase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	3.07 μM Compound: 1c	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33834781]
HT-29	IC₅₀	5.18 μM Compound: 1c	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33834781]
L02	IC₅₀	96.68 μM Compound: 1c	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33834781]
MCF7	IC₅₀	7.5 μM Compound: 1c	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33834781]
PC-3	IC₅₀	4.53 μM Compound: 1c	Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33834781]
T-24	IC₅₀	6.1 μM Compound: 1c	Cytotoxicity against human T24 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human T24 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33834781]

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-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 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-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].

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:

C_max=7017.8 ng/mL, t_1/2=6.67 h, CL=0.60 L/h/kg.

Chemical Information

CAS. Nr. 2641079-92-5
Appearance Solid
Molecular Weight 392.84
Formel C₂₁H₁₇ClN₄O₂
Color White to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5456 mL

12.7278 mL

25.4557 mL

5 mM

0.5091 mL

2.5456 mL

5.0911 mL

10 mM

0.2546 mL

1.2728 mL

2.5456 mL

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.

Molaritätsrechner

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

Mass

Konzentration

Volumen

Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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CK2 inhibitor 2

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Casein Kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CK2 inhibitor 2

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Casein Kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CK2 inhibitor 2 Related Classifications

Art. -Nr.: HY-132175