Art. -Nr.: HY-126542

VRK-IN-1

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

VRK-IN-1 is a potent and selective inhibitor of vaccinia-related kinases 1 (VRK1), with an IC₅₀ of 150 nM. VRK1 is human Ser/Thr protein kinases associated with increased cell division and neurological disorders.

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Reinheit: 99.47%
CAS. Nr.: 2378855-09-3
Formel: C₁₈H₁₁F₄NO₂
Molecular Weight:349.28

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

VRK-IN-1 Chemical Structure

CAS. Nr.: 2378855-09-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

VRK1

150 nM (IC₅₀)

In Vitro

VRK-IN-1 binds to VRK1-FL by enthalpy-driven, with a K_d of 190 nM^[1].
VRK-IN-1 (0.4-25 μM; 24 h) slightly decreases the viability of human HeLa cells at the concentration of 3.2 μM^[1].

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

Chemical Information

CAS. Nr. 2378855-09-3
Appearance Solid
Molecular Weight 349.28
Formel C₁₈H₁₁F₄NO₂
Color White to off-white
SMILES

FC1=C(O)C(F)=CC(C2=C(C)N=CC(C3=CC(F)=C(O)C(F)=C3)=C2)=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

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Journal Impact Factor

EMBO J

The global phosphorylation landscape of mouse oocytes during meiotic maturation. [Abstract]

2024 Oct;43(20):4752-4785. PMID: 39256562
Int J Mol Sci

VRK1 Kinase Activity Modulating Histone H4K16 Acetylation Inhibited by SIRT2 and VRK-IN-1. [Abstract]

2023 Mar 3;24(5):4912. PMID: 36902348
Exp Cell Res

Inactivation of VRK1 sensitizes ovarian cancer to PARP inhibition through regulating DNA-PK stability. [Abstract]

2024 Apr 16;438(1):114036. PMID: 38614421
Epigenetics Chromatin

The pattern of histone H3 epigenetic posttranslational modifications is regulated by the VRK1 chromatin kinase. [Abstract]

2023 May 13;16(1):18. PMID: 37179361
Mol Biol Rep

VRK1 promotes DNA-induced type I interferon production. [Abstract]

2024 Mar 27;51(1):453. PMID: 38536553
bioRxiv

2026 Apr 5.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (286.30 mM; Need ultrasonic; 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

2.8630 mL

14.3152 mL

28.6303 mL

5 mM

0.5726 mL

2.8630 mL

5.7261 mL

10 mM

0.2863 mL

1.4315 mL

2.8630 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

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

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(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: ≥ 2.5 mg/mL (7.16 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals 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 (272 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 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]. Serafim RAM, et, al. Development of Pyridine-based Inhibitors for the Human Vaccinia-related Kinases 1 and 2. ACS Med Chem Lett. 2019 Aug 19;10(9):1266-1271. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8630 mL	14.3152 mL	28.6303 mL	71.5758 mL
	5 mM	0.5726 mL	2.8630 mL	5.7261 mL	14.3152 mL
	10 mM	0.2863 mL	1.4315 mL	2.8630 mL	7.1576 mL
	15 mM	0.1909 mL	0.9543 mL	1.9087 mL	4.7717 mL
	20 mM	0.1432 mL	0.7158 mL	1.4315 mL	3.5788 mL
	25 mM	0.1145 mL	0.5726 mL	1.1452 mL	2.8630 mL
	30 mM	0.0954 mL	0.4772 mL	0.9543 mL	2.3859 mL
	40 mM	0.0716 mL	0.3579 mL	0.7158 mL	1.7894 mL
	50 mM	0.0573 mL	0.2863 mL	0.5726 mL	1.4315 mL
	60 mM	0.0477 mL	0.2386 mL	0.4772 mL	1.1929 mL
	80 mM	0.0358 mL	0.1789 mL	0.3579 mL	0.8947 mL
	100 mM	0.0286 mL	0.1432 mL	0.2863 mL	0.7158 mL

Keywords

VRK-IN-1

6 Cited Publications

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VRK-IN-1

Anti-Infection Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) VRK-IN-1

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

VRK-IN-1

Anti-Infection Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) VRK-IN-1

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

VRK-IN-1 Related Classifications

Art. -Nr.: HY-126542