2. PI3K/Akt/mTOR
  3. PIKfyve
  4. PIKfyve-IN-1

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.

PIKfyve-IN-1 Chemical Structure

PIKfyve-IN-1 Chemical Structure

CAS No. : 2857982-26-2

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5 mg USD 570 In-stock
10 mg USD 910 In-stock
25 mg USD 1800 In-stock
50 mg USD 2900 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PIKfyve-IN-1 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[1]. 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.

IC50 & Target

IC50: 6.9 nM (PIKfyve)[1]
In Vitro

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.

PIKfyve-IN-1 Related Antibodies

Immunofluorescence[1]

Cell Line: Calu-3 cells
Concentration: 1 μM
Incubation Time: 1 h
Result: Inhibited the uptake of lentivirus pseudotyped with the SARS-CoV-2 spike glycoprotein.
Molecular Weight

331.41

Formula

C20H21N5
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

NC1=NC=C(CCC2)C(C3=C2NC4=C3C=C(C#CCN(C)C)C=C4)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0174 mL 15.0871 mL 30.1741 mL
5 mM 0.6035 mL 3.0174 mL 6.0348 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
×
Volume
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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    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.
  • Protocol 2

    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.
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

Purity: 99.64%

SDS (251 KB)

COA (254 KB) HNMR (136 KB) RP-HPLC (169 KB) LCMS (383 KB)

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
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PIKfyve-IN-1 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.

Keywords:

PIKfyve-IN-12857982-26-2PIKfyveFYVE domain-containing phosphatidylinositol 3-phosphate 5-kinasePhosphatidylinositol 3-phosphate 5-kinaseFab1phosphatidylinositol-3phosphate 5-kinase (PIKfyve)cell-activechemical probevirologyInhibitorinhibitorinhibit

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