PIKfyve-IN-1
Based on 1 Customer Validation
PIKfyve-IN-1 is a highly potent and cell-active chemical probe that inhibits phosphatidylinositol-3phosphate 5-kinase (PIKfyve) with IC50 value of 6.9 nM. PIKfyve-IN-1 can be used for the research of PIKfyve in virology. PIKfyve-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
For research use only. We do not sell to patients.
- Purity: 99.64%
- CAS No.: 2857982-26-2
- Formula: C20H21N5
- Molecular Weight:331.41
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
IC50: 6.9 nM (PIKfyve)[1]
PIKfyve-IN-1 inhibits PIKfyve in PIKfyve enzymatic assay and PIKfyve NanoBRET assay with IC50 values of 6.9 nM and 4.01 nM, respectively[1].
PIKfyve-IN-1 (0-10 μM) disrupts multiple phases of the lifecycle of coronaviruses: viral replication and viral entry[1].
PIKfyve-IN-1 inhibits MHV replication and SARS-CoV-2 replication with IC50 values of 23.5 nM and 19.5 nM, respectively[1].
PIKfyve-IN-1 (5 μM) impacts lysosomal homeostasis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Calu-3 cells
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Concentration:1 μM
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Incubation Time:1 h
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Result:Inhibited the uptake of lentivirus pseudotyped with the SARS-CoV-2 spike glycoprotein.
Chemical Information
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CAS No. 2857982-26-2
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Appearance Solid
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Molecular Weight 331.41
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Formula C20H21N5
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Color Off-white to yellow
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SMILES
NC1=NC=C(CCC2)C(C3=C2NC4=C3C=C(C#CCN(C)C)C=C4)=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (301.74 mM; ultrasonic and warming and heat to 80°C; 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. 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. 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: 2.5 mg/mL (7.54 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
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 (276 KB)
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SDS (555 KB)
- English - EN (555 KB)
- Français - FR (555 KB)
- Deutsch - DE (555 KB)
- Norwegian - NO (555 KB)
- Español - ES (555 KB)
- Swedish - SV (555 KB)
- Italian - IT (555 KB)
- Korean - KR (555 KB)
- Portuguese - PT (555 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. 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 | 3.0174 mL | 15.0871 mL | 30.1741 mL | 75.4353 mL |
| 5 mM | 0.6035 mL | 3.0174 mL | 6.0348 mL | 15.0871 mL | |
| 10 mM | 0.3017 mL | 1.5087 mL | 3.0174 mL | 7.5435 mL | |
| 15 mM | 0.2012 mL | 1.0058 mL | 2.0116 mL | 5.0290 mL | |
| 20 mM | 0.1509 mL | 0.7544 mL | 1.5087 mL | 3.7718 mL | |
| 25 mM | 0.1207 mL | 0.6035 mL | 1.2070 mL | 3.0174 mL | |
| 30 mM | 0.1006 mL | 0.5029 mL | 1.0058 mL | 2.5145 mL | |
| 40 mM | 0.0754 mL | 0.3772 mL | 0.7544 mL | 1.8859 mL | |
| 50 mM | 0.0603 mL | 0.3017 mL | 0.6035 mL | 1.5087 mL | |
| 60 mM | 0.0503 mL | 0.2515 mL | 0.5029 mL | 1.2573 mL | |
| 80 mM | 0.0377 mL | 0.1886 mL | 0.3772 mL | 0.9429 mL | |
| 100 mM | 0.0302 mL | 0.1509 mL | 0.3017 mL | 0.7544 mL |