Art. -Nr.: HY-14644A

Apilimod mesylate

(Synonyms: STA 5326 mesylate; LAM-002A; AIT-101 mesylate)

44 Cited Publications

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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.

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Reinheit: 99.58%
CAS. Nr.: 870087-36-8
Formel: C₂₅H₃₄N₆O₈S₂
Molecular Weight:610.70

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Apilimod mesylate Chemical Structure

CAS. Nr.: 870087-36-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (44)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]. Apilimod is a potent and highly selective PIKfyve inhibitor.

IC₅₀ & Target^[1]^[2]

IL-4

IL-5

IL-8

IL-12

IL-23

Alle Interleukin Related Isoform-spezifische Produkte anzeigen :

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.

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. Apilimod 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.

Chemical Information

CAS. Nr. 870087-36-8
Appearance Solid
Molecular Weight 610.70
Formel C₂₅H₃₄N₆O₈S₂
Color White to off-white
SMILES

CC1=CC=CC(/C=N/NC2=CC(N3CCOCC3)=NC(OCCC4=CC=CC=N4)=N2)=C1.CS(=O)(O)=O.CS(=O)(O)=O
Synonyms

STA 5326 mesylate; LAM-002A; AIT-101 mesylate
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (44)

All WBBio/Physico-chemical AssayRT-PCR

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Journal Impact Factor

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

WNK1 mediates M-CSF-induced macropinocytosis to enforce macrophage lineage fidelity. [Abstract]

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.
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.
Theranostics

IL-23, but not IL-12, plays a critical role in inflammation-mediated bone disorders. [Abstract]

2020 Mar 4;10(9):3925-3938. PMID: 32226529
Exp Mol Med

A dual inhibitor of PIP5K1C and PIKfyve prevents SARS-CoV-2 entry into cells. [Abstract]

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

Measles and Nipah virus assembly: Specific lipid binding drives matrix polymerization. [Abstract]

2022 Jul 22;8(29):eabn1440. PMID: 35857835
Cancer Lett

LW-213 induces immunogenic tumor cell death via ER stress mediated by lysosomal TRPML1. [Abstract]

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

PIKfyve inhibition increases exosome release and induces secretory autophagy. [Abstract]

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).
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

Manganese is a potent inducer of lysosomal activity that inhibits de novo HBV infection. [Abstract]

2025 Jan 2;21(1):e1012800. PMID: 39746094
PLoS Pathog

HBZ upregulates myoferlin expression to facilitate HTLV-1 infection. [Abstract]

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

Septins regulate kinase-inhibitor induced micron-scale vacuolation. [Abstract]

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

PP2A-dependent TFEB activation is blocked by PIKfyve-induced mTORC1 activity. [Abstract]

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

Phosphoinositide kinase PIKfyve inhibitor apilimod blocks hepatitis E virus infection. [Abstract]

2026 Mar 31;4(1):e100348. PMID: 41948149
bioRxiv

2025 Dec 18.
bioRxiv

Tau seeding in neurons enabled by transient endolysosomal perforations are confined within endolysosomes. [Abstract]

2025 Nov 3:2025.11.02.686178. PMID: 41278722
bioRxiv

2025 June 02.
bioRxiv

2025 March 19.
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
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

WNK1 enforces macrophage lineage fidelity. [Abstract]

2023 Apr 28:2023.04.26.538482. PMID: 37383948
bioRxiv

Inhibition of PIKfyve kinase prevents infection by Zaire ebolavirus and SARS-CoV-2. [Abstract]

2020 Jun 15:2020.04.21.053058. PMID: 32511398

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6375 mL

8.1873 mL

16.3747 mL

5 mM

0.3275 mL

1.6375 mL

3.2749 mL

10 mM

0.1637 mL

0.8187 mL

1.6375 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.25 mg/mL (2.05 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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: PBS

Solubility: 100 mg/mL (163.75 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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.

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) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

Apilimod mesylate

44 Cited Publications

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Apilimod mesylate

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Publications Citing Use of MedChemExpress (MCE) Apilimod mesylate

Alle Interleukin Related Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (44)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Apilimod mesylate Related Classifications

HY-14644A Related Classifications