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. Apilimod is a potent and highly selective PIKfyve inhibitor.
For research use only. We do not sell to patients.
Apilimod Chemical Structure
CAS No. : 541550-19-0
This product is a controlled substance and not for sale in your territory.
Based on 28 publication(s) in Google Scholar
Other Forms of Apilimod:
Apilimod mesylate
In-stock
Apilimod purchased from MedChemExpress. Usage Cited in:
Cell Mol Life Sci. 2016 Dec;73(24):4717-4737.
[Abstract]
PIKfyve inhibition affects the autophagy pathway. Cellular LC3-II levels are measured by Western blot after cells are treated with or without concanamycin A (50 nM) during the last 4 h of the preincubation step with Apilimod.
Powered by Bioz
See more details on Bioz
View All Interleukin Related Isoform Specific Products:
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
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
In Vivo
Apilimod (10 mg/kg, p.o.) is effective not only when administered throughout the entire experiment, but also when administration is initiated on day 30 when disease is clearly measurable but not maximal. TA-5326 causes a significant reduction in cell number only in the Th1 model, with an average percentage of inhibition of 51%±8% relative to the vehicle control. Apilimod treatment has no effect in the Th2 setting[1]. Apilimod (5 or 20 mg/kg, p.o.) reduces the level of IL-12 p40 in serum without altering body weight in EAU mice. Oral administration of Apilimod reduces the severity of experimental autoimmune uveoretinitis (EAU) by clinical and histopathological analysis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Room temperature in continental US; may vary elsewhere.
Storage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
2 years
-20°C
1 year
Solvent & Solubility
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
ConcentrationSolventMass
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
10 mM
0.2390 mL
1.1948 mL
2.3895 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.
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.
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO 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 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn 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
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.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
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.
[1]. Wada Y, et al. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood. 2007 Feb 1;109(3):1156-64.
[Content Brief]
[2]. Keino H, et al. Therapeutic effect of the potent IL-12/IL-23 inhibitor STA-5326 on experimental autoimmune uveoretinitis. Arthritis Res Ther. 2008;10(5):R122.
[Content Brief]
Cell Assay
[2]
Cervical lymph node cells obtained from immunized mice on day 18 (2×105 cells/well) arecultured in 0.2 mL RPMI 1640 containing 10 mM HEPES, 0.1 mM nonessential amino acid, 1 mM sodium pyruvate, 1×10-5 M 2-mercaptoethanol, 10% FCS, and 10 μg/mL IRBP1-20. For cytokine assay, supernatants are collected after 72 hours and analysed for IFN-γ, IL-4 and IL-17 by quantitative capture ELISA using quantikine ELISA kits and mouse IL-17 ELISA Ready-SET-Go kits. Cell proliferation is evaluated using a cell proliferation assay.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]
In most experiments, 5 mg/kg or 20 mg/kg Apilimod or vehicle only (0.5% carboxyl methyl cellulose) is orally administered once a day for six days a week from day 0 to day 14 after immunization. In the effector phase experiments, 20 mg/kg Apilimod or vehicle is orally administered once a day, from day 9 to day 14 after immunization.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
[1]. Wada Y, et al. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood. 2007 Feb 1;109(3):1156-64.
[Content Brief]
[2]. Keino H, et al. Therapeutic effect of the potent IL-12/IL-23 inhibitor STA-5326 on experimental autoimmune uveoretinitis. Arthritis Res Ther. 2008;10(5):R122.
[Content Brief]
[1]. Wada Y, et al. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood. 2007 Feb 1;109(3):1156-64.
[2]. Keino H, et al. Therapeutic effect of the potent IL-12/IL-23 inhibitor STA-5326 on experimental autoimmune uveoretinitis. Arthritis Res Ther. 2008;10(5):R122.
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.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
2.3895 mL
11.9477 mL
23.8954 mL
59.7386 mL
5 mM
0.4779 mL
2.3895 mL
4.7791 mL
11.9477 mL
10 mM
0.2390 mL
1.1948 mL
2.3895 mL
5.9739 mL
15 mM
0.1593 mL
0.7965 mL
1.5930 mL
3.9826 mL
20 mM
0.1195 mL
0.5974 mL
1.1948 mL
2.9869 mL
25 mM
0.0956 mL
0.4779 mL
0.9558 mL
2.3895 mL
30 mM
0.0797 mL
0.3983 mL
0.7965 mL
1.9913 mL
40 mM
0.0597 mL
0.2987 mL
0.5974 mL
1.4935 mL
50 mM
0.0478 mL
0.2390 mL
0.4779 mL
1.1948 mL
60 mM
0.0398 mL
0.1991 mL
0.3983 mL
0.9956 mL
80 mM
0.0299 mL
0.1493 mL
0.2987 mL
0.7467 mL
100 mM
0.0239 mL
0.1195 mL
0.2390 mL
0.5974 mL
Apilimod Related Classifications
Immunology/InflammationPI3K/Akt/mTOR
Interleukin RelatedPIKfyve
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.
