Apilimod mesylate
Based on 44 publication(s) in Google Scholar
Apilimod (STA 5326) mesylate 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.
- Purity: 99.58%
- CAS No.: 870087-36-8
- Formula: C25H34N6O8S2
- Molecular Weight:610.70
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Publications Citing Use of MedChemExpress (MCE) Apilimod mesylate
More- Nat Commun. 2026 May 27;17(1):4602. [Abstract]
- Nat Commun. 2025 May 28;16(1):4945. [Abstract]
- Nat Commun. 2020 Mar 27;11(1):1620. [Abstract]
- Theranostics. 2020 Mar 4;10(9):3925-3938. [Abstract]
- Exp Mol Med. 2024 Aug;56(8):1736-1749. [Abstract]
- Biomaterials. 2022 Jun;285:121509. [Abstract]
- Sci Adv. 2026 Jun 12;12(24):eaed2731. [Abstract]
- Sci Adv. 2023 Oct 13;9(41):eadh1134. [Abstract]
- Sci Adv. 2022 Jul 22;8(29):eabn1440. [Abstract]
- Cancer Lett. 2023 Nov 28:577:216435. [Abstract]
- Proc Natl Acad Sci U S A. 2024 May 21;121(21):e2403685121. [Abstract]
- Proc Natl Acad Sci U S A. 2023 Dec 26;120(52):e2307423120. [Abstract]
- Phytomedicine. 2026 May:154:158011. [Abstract]
- Br J Cancer. 2020 Aug;123(4):542-555. [Abstract]
- J Cell Biol. 2025 Feb 3;224(2):e202401136. [Abstract]
- Cell Mol Life Sci. 2016 Dec;73(24):4717-4737. [Abstract]
- Commun Biol. 2025 Aug 6;8(1):1169. [Abstract]
- Commun Biol. 2022 Mar 24;5(1):262. [Abstract]
- PLoS Pathog. 2025 Jan 2;21(1):e1012800. [Abstract]
- PLoS Pathog. 2023 Feb 24;19(2):e1011202. [Abstract]
- J Biol Chem. 2023 Jan;299(1):102775. [Abstract]
- J Virol. 2021 Oct 13;95(21):e0097521. [Abstract]
- Exp Cell Res. 2026 Aug 1;461(1):115103. [Abstract]
- Vaccine. 2025 Jul 23:62:127537. [Abstract]
- Viruses. 2023 Jun 12;15(6):1353. [Abstract]
- Viruses. 2021 Jun 28;13(7):1255. [Abstract]
- Biotechnol J. 2023 Feb;18(2):e2200147. [Abstract]
- Mol Cell Biol. 2025;45(3):99-115. [Abstract]
- Mol Biol Cell. 2022 Mar 1;33(3):ar26. [Abstract]
- bioRxiv. 2026 May 13:2026.05.11.724403. [Abstract]
- eGastroenterology. 2026 Mar 31;4(1):e100348. [Abstract]
- bioRxiv. 2025 Dec 18.
- bioRxiv. 2025 Nov 3:2025.11.02.686178. [Abstract]
- bioRxiv. 2025 June 02.
- bioRxiv. 2025 March 19.
- bioRxiv. 2023 Oct 20:2023.10.19.563158. [Abstract]
- biorxiv. 2024 May 27.
- bioRxiv. 2024 May 10.
- bioRxiv. 2024 Jan 23.
- SSRN. 2024 Jan 26.
- bioRxiv. 2023 Aug 12.
- bioRxiv. 2023 Aug 28.
- bioRxiv. 2023 Apr 28:2023.04.26.538482. [Abstract]
- bioRxiv. 2020 Jun 15:2020.04.21.053058. [Abstract]
Customer Validation & Images
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WB
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Bio/Physico-chemical Assay
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RT-PCR
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Bio/Physico-chemical Assay
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Biological Activity
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IL-4 |
IL-5 |
IL-8 |
IL-12 |
IL-23 |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 870087-36-8
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Appearance Solid
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Molecular Weight 610.70
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Formula C25H34N6O8S2
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Color White to off-white
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SMILES
CC1=CC=CC(/C=N/NC2=CC(N3CCOCC3)=NC(OCCC4=CC=CC=N4)=N2)=C1.CS(=O)(O)=O.CS(=O)(O)=O
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Synonyms
STA 5326 mesylate; LAM-002A; AIT-101 mesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (44)
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Journal Impact Factor
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Most Recent
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Nat Commun
A PI(3,5)P2/CHMP4B axis on lysosomes is essential for microautophagic degradation of STING. [Abstract]2026 May 27;17(1):4602. PMID: 42203786 -
Nat Commun
2025 May 28;16(1):4945. PMID: 40436823
Apilimod mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 28;16(1):4945. [Abstract]
M-CSF-stimulated macropinocytosis induces phosphorylation of the WNK1 kinase region in bone marrow myeloid progenitors. Mouse myeloid progenitors were isolated from the bone marrow and stimulated with M-CSF in the presence of vehicle, WNK463, or indicated macropinocytosis inhibitors EIPA, Apilimod (10 μM), and LY294002. Cells were harvested after 1 h, then assayed for WNK1 phosphorylation.
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Nat Commun
Characterization of spike glycoprotein of SARS-CoV-2 on virus entry and its immune cross-reactivity with SARS-CoV. [Abstract]2020 Mar 27;11(1):1620. PMID: 32221306
Apilimod mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Mar 27;11(1):1620. [Abstract]
Inhibition of entry of SARS-CoV, MERS-CoV, and MHV S pseudovirions by a PIKfyve inhibitor apilimod. HeLa/mCEACAM, 293/hACE2, HeLa/hDPP4 cells were pretreated with different concentrations of Apilimod (0-1 μM; 1 h) and transduced with MHV S, SARS-CoV S, MERS-CoV S pseudovirions, respectively. The luciferase activity was measured 40 h post transduction. VSV-G pseudovirions were used as a control.
Apilimod mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Mar 27;11(1):1620. [Abstract]
Inhibition of MHV A59 infection by apilimod. The 17Cl.1 cells were pretreated with 3, 10, 30, 100, 300 nM apilimod for 30 min and infected by MHV A59 at MOI = 0.01. Viral infection and cell viability were determined by using qPCR and MTT assay, respectively.
Apilimod mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Mar 27;11(1):1620. [Abstract]
HEK 293/hACE2 cells were pretreated with apimod (1–300 nM; 1 h) and then inoculated with SARS-CoV-2 S protein pseudovirus in the presence of the drug. Luciferase activity was measured 40 hours after transfection.
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Theranostics
2020 Mar 4;10(9):3925-3938. PMID: 32226529 -
Exp Mol Med
2024 Aug;56(8):1736-1749. PMID: 39085352 -
Biomaterials
Protease inhibitor Camostat Mesyalte blocks wild type SARS-CoV-2 and D614G viral entry in human engineered miniature lungs. [Abstract]2022 Jun;285:121509. PMID: 35533440 -
Sci Adv
Quantitative prediction of siRNA complexation by ionizable drugs enables their codelivery in nanoparticles. [Abstract]2026 Jun 12;12(24):eaed2731. PMID: 42284421 -
Sci Adv
A noncanonical function of SKP1 regulates the switch between autophagy and unconventional secretion. [Abstract]2023 Oct 13;9(41):eadh1134. PMID: 37831778 -
Sci Adv
2022 Jul 22;8(29):eabn1440. PMID: 35857835 -
Cancer Lett
2023 Nov 28:577:216435. PMID: 37806516 -
Proc Natl Acad Sci U S A
Genome-wide CRISPR screens in spheroid culture reveal that the tumor suppressor LKB1 inhibits growth via the PIKFYVE lipid kinase. [Abstract]2024 May 21;121(21):e2403685121. PMID: 38743625 -
Proc Natl Acad Sci U S A
A genome-wide CRISPR/Cas9 screen identifies a role for Rab5A and early endosomes in hepatitis E virus replication. [Abstract]2023 Dec 26;120(52):e2307423120. PMID: 38109552 -
Phytomedicine
Targeting GRB2 with Polyphyllin H overcomes PIKFYVE inhibitor resistance in bladder cancer by blocking Akt-SREBP1-SCD1 pathway. [Abstract]2026 May:154:158011. PMID: 41795291 -
Br J Cancer
A systematic molecular and pharmacologic evaluation of AKT inhibitors reveals new insight into their biological activity. [Abstract]2020 Aug;123(4):542-555. PMID: 32439931 -
J Cell Biol
Neuronal constitutive endolysosomal perforations enable α-synuclein aggregation by internalized PFFs. [Abstract]2025 Feb 3;224(2):e202401136. PMID: 39714357 -
Cell Mol Life Sci
2016 Dec;73(24):4717-4737. PMID: 27438886
Apilimod mesylate 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(0.5 μM; 21 h).
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Commun Biol
HSP90 deficiency promotes cholesteryl ester accumulation in lipid droplets via endocytosis of low-density lipoprotein. [Abstract]2025 Aug 6;8(1):1169. PMID: 40770403 -
Commun Biol
Antibody-dependent enhancement (ADE) of SARS-CoV-2 pseudoviral infection requires FcγRIIB and virus-antibody complex with bivalent interaction. [Abstract]2022 Mar 24;5(1):262. PMID: 35332252 -
PLoS Pathog
2025 Jan 2;21(1):e1012800. PMID: 39746094 -
PLoS Pathog
2023 Feb 24;19(2):e1011202. PMID: 36827461 -
J Biol Chem
Phosphatidylinositol (3,5)-bisphosphate machinery regulates neurite thickness through neuron-specific endosomal protein NSG1/NEEP21. [Abstract]2023 Jan;299(1):102775. PMID: 36493904 -
J Virol
Synergistic Block of SARS-CoV-2 Infection by Combined Drug Inhibition of the Host Entry Factors PIKfyve Kinase and TMPRSS2 Protease. [Abstract]2021 Oct 13;95(21):e0097521. PMID: 34406858 -
Exp Cell Res
2026 Aug 1;461(1):115103. PMID: 42276196 -
Vaccine
Long-term antibody responses to the Ebola virus and the vaccine vector after rVSV-ZEBOV vaccination in DRC. [Abstract]2025 Jul 23:62:127537. PMID: 40706506 -
Viruses
CD40 Signaling in Mice Elicits a Broad Antiviral Response Early during Acute Infection with RNA Viruses. [Abstract]2023 Jun 12;15(6):1353. PMID: 37376652 -
Viruses
Screening and Identification of Lujo Virus Inhibitors Using a Recombinant Reporter Virus Platform. [Abstract]2021 Jun 28;13(7):1255. PMID: 34203149 -
Biotechnol J
Apilimod enhances specific productivity in recombinant CHO cells through cell cycle arrest and mediation of autophagy. [Abstract]2023 Feb;18(2):e2200147. PMID: 36478399 -
Mol Cell Biol
Kinase Inhibitor-Induced Cell-Type Specific Vacuole Formation in the Absence of Canonical ATG5-Dependent Autophagy Initiation Pathway. [Abstract]2025;45(3):99-115. PMID: 39895059 -
Mol Biol Cell
2022 Mar 1;33(3):ar26. PMID: 35020443 -
bioRxiv
Naked antisense oligonucleotides remain endolysosomally sequestered despite induced membrane damage. [Abstract]2026 May 13:2026.05.11.724403. PMID: 42182263 -
eGastroenterology
2026 Mar 31;4(1):e100348. PMID: 41948149 -
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bioRxiv
Tau seeding in neurons enabled by transient endolysosomal perforations are confined within endolysosomes. [Abstract]2025 Nov 3:2025.11.02.686178. PMID: 41278722 -
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bioRxiv
LKB1 suppresses growth and promotes the internalization of EGFR through the PIKFYVE lipid kinase. [Abstract]2023 Oct 20:2023.10.19.563158. PMID: 37904985 -
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bioRxiv
2023 Apr 28:2023.04.26.538482. PMID: 37383948 -
bioRxiv
2020 Jun 15:2020.04.21.053058. PMID: 32511398
Solvent & Solubility
H2O : 100 mg/mL (163.75 mM; Need ultrasonic)
DMSO : 12.5 mg/mL (20.47 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 1.25 mg/mL (2.05 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.05 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (163.75 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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]. Billich A. Drug evaluation: apilimod, an oral IL-12/IL-23 inhibitor for the treatment of autoimmune diseases and common variable immunodeficiency.IDrugs. 2007 Jan;10(1):53-9. [Content Brief]
[3]. 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]
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 (sealed storage, away from moisture). 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 / H2O | 1 mM | 1.6375 mL | 8.1873 mL | 16.3747 mL | 40.9366 mL |
| 5 mM | 0.3275 mL | 1.6375 mL | 3.2749 mL | 8.1873 mL | |
| 10 mM | 0.1637 mL | 0.8187 mL | 1.6375 mL | 4.0937 mL | |
| 15 mM | 0.1092 mL | 0.5458 mL | 1.0916 mL | 2.7291 mL | |
| 20 mM | 0.0819 mL | 0.4094 mL | 0.8187 mL | 2.0468 mL | |
| H2O | 25 mM | 0.0655 mL | 0.3275 mL | 0.6550 mL | 1.6375 mL |
| 30 mM | 0.0546 mL | 0.2729 mL | 0.5458 mL | 1.3646 mL | |
| 40 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0234 mL | |
| 50 mM | 0.0327 mL | 0.1637 mL | 0.3275 mL | 0.8187 mL | |
| 60 mM | 0.0273 mL | 0.1365 mL | 0.2729 mL | 0.6823 mL | |
| 80 mM | 0.0205 mL | 0.1023 mL | 0.2047 mL | 0.5117 mL | |
| 100 mM | 0.0164 mL | 0.0819 mL | 0.1637 mL | 0.4094 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Apilimod mesylate Related Classifications
HY-14644A Related Classifications
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