Reagenzien und Instrumente für die Immunologie Zellbiologie und Molekularbiologie
 
> Apilimod [541550-19-0]

Apilimod [541550-19-0]

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Katalog-Nummer HY-14644-10mg

Size : 10mg

Marke : MedChemExpress


Beschreibung

Apilimod (STA 5326) is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively[1]. Apilimod is a potent and highly selective PIKfyve inhibitor.

IC50 & Target[1][2]

IL-4

 

IL-5

 

IL-8

 

IL-12

 

IL-23

 

Cellular Effect
Cell Line Type Value Description References
HeLa IC50
0.14 μM
Compound: Apilimod
Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability incubated for 24 hrs by CCK8 assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability incubated for 24 hrs by CCK8 assay
[PMID: 38117948]
MDA-MB-231 IC50
0.1 μM
Compound: Apilimod
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 24 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 24 hrs by CCK8 assay
[PMID: 38117948]
VCaP IC50
1188 nM
Compound: 1
Antiproliferative activity against human VCaP cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by culturing in compound-free medium for 2 weeks by crystal violet staining based analysis
Antiproliferative activity against human VCaP cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by culturing in compound-free medium for 2 weeks by crystal violet staining based analysis
[PMID: 37605297]
VCaP IC50
253.6 nM
Compound: 1
Antiproliferative activity against human VCaP cells assessed as inhibition of cell proliferation incubated for 2 weeks by crystal violet staining based analysis
Antiproliferative activity against human VCaP cells assessed as inhibition of cell proliferation incubated for 2 weeks by crystal violet staining based analysis
[PMID: 37605297]
Vero C1008 CC50
>1 μM
Compound: 14; STA-5326, LAM-002A
Cytotoxicity against African green monkey Vero E6 cells
Cytotoxicity against African green monkey Vero E6 cells
[PMID: 33539089]
Vero C1008 EC50
0.023 μM
Compound: Apilimod
Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs
Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs
[PMID: 32511357]
Vero C1008 EC50
0.023 μM
Compound: Apilimod
Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs
Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs
10.1101/2020.04.16.044016
In Vitro

Apilimod inhibits IFN-γ production induced by either IFN-γ/SAC or SAC in human PBMCs, with an IC50 of approximately 20 nM. Apilimod show some inhibition against IFN-γ/SAC-induced TNF-α and ConA-induced IL-5 from human PBMCs at high concentrations, but no suppressive effect against IL-1β, IL-2, IL-4, IL-8, and IL-18 in all cultures tested. The p35 and p40 promoter-driven luciferase activities are significantly induced after stimulation with IFN-γ/LPS or IFN-γ/SAC, and are completely suppressed by 100 nM Apilimod[1].

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

Apilimod Related Antibodies

Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 100 mg/mL (238.95 mM; Need ultrasonic; 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 2.3895 mL 11.9477 mL 23.8954 mL
5 mM 0.4779 mL 2.3895 mL 4.7791 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, 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.

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 (5.97 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 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.97 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  0.5% CMC-Na/saline water

    Solubility: 3.33 mg/mL (7.96 mM); Suspended solution; Need ultrasonic
Reinheit & Dokumentation
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