VRK1/CK1-IN-1
Based on 1 Customer Validation
VRK1/CK1-IN-1 (compound 36) is a dual VRK1 and CK1 family inhibitor, with a Ki of 37.9 nM against human VRK1, 8.3 nM against human CK1δ, and 7.8 nM against human CK1ε. VRK1/CK1-IN-1 exhibits extremely low activity against VRK2. VRK1/CK1-IN-1 can be used in studies related to p53-deficient tumors.
For research use only. We do not sell to patients.
- Purity: 98.69%
- CAS No.: 3050772-20-5
- Formula: C19H18F2N6O3
- Molecular Weight:416.38
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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VRK1 37.9 nM (Ki) |
VRK1/CK1-IN-1 (compound 36) (30 μM to 1.8 nM; 1 h at 30 °C) potently inhibits purified human VRK1 kinase activity with a Ki of 37.9 nM[1].
VRK1/CK1-IN-1 acts as a potent dual inhibitor of human CK1δ (Ki = 8.3 nM) and CK1ε (Ki = 7.8 nM) kinases[1].
VRK1/CK1-IN-1 (30 μM; 40 min) engages directly with VRK1 in intact, live human HEK293 cells[1].
VRK1/CK1-IN-1 (15 μM; 24 h) induces reversible p53-dependent G0/G1 cell cycle arrest in p53-proficient human RPE1 cells, with no equivalent arrest in p53-deficient cells[1].
VRK1/CK1-IN-1 (1.5-30 μM; 24 h) in p53-proficient human RPE1 cells, dose-dependently upregulates p53 and p21 expression, and reduces phosphorylated H2AX levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:p53-proficient (p53+/+) human retinal pigment epithelial (RPE1) cells, p53-deficient (p53-/-) human retinal pigment epithelial (RPE1) cells
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Concentration:15 μM
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Incubation Time:24 h
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Result:Induced p53-dependent G0/G1 phase arrest, with >80% of p53-proficient RPE1 cells arrested in G0/G1 phase; no equivalent arrest was observed in p53-deficient RPE1 cells.
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Cell Line:p53-proficient human RPE1 cells
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Concentration:1.5-30 μM
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Incubation Time:24 h
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Result:Dose-dependently upregulated expression of p53 and its cell cycle target p21, and reduced levels of phosphorylated histone H2AX (S139).
Chemical Information
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CAS No. 3050772-20-5
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Appearance Solid
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Molecular Weight 416.38
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Formula C19H18F2N6O3
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Color Off-white to gray
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SMILES
O=C1N(CC2=CC(C)=NO2)C3=CN=C(NC4=CC(F)=C(O)C(F)=C4)N=C3N(C)[C@H]1C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (240.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (12.01 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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 (protect from light). 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 | 2.4017 mL | 12.0083 mL | 24.0165 mL | 60.0413 mL |
| 5 mM | 0.4803 mL | 2.4017 mL | 4.8033 mL | 12.0083 mL | |
| 10 mM | 0.2402 mL | 1.2008 mL | 2.4017 mL | 6.0041 mL | |
| 15 mM | 0.1601 mL | 0.8006 mL | 1.6011 mL | 4.0028 mL | |
| 20 mM | 0.1201 mL | 0.6004 mL | 1.2008 mL | 3.0021 mL | |
| 25 mM | 0.0961 mL | 0.4803 mL | 0.9607 mL | 2.4017 mL | |
| 30 mM | 0.0801 mL | 0.4003 mL | 0.8006 mL | 2.0014 mL | |
| 40 mM | 0.0600 mL | 0.3002 mL | 0.6004 mL | 1.5010 mL | |
| 50 mM | 0.0480 mL | 0.2402 mL | 0.4803 mL | 1.2008 mL | |
| 60 mM | 0.0400 mL | 0.2001 mL | 0.4003 mL | 1.0007 mL | |
| 80 mM | 0.0300 mL | 0.1501 mL | 0.3002 mL | 0.7505 mL | |
| 100 mM | 0.0240 mL | 0.1201 mL | 0.2402 mL | 0.6004 mL |
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