Apilimod
Based on 44 publication(s) in Google Scholar
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.80%
- CAS 番号: 541550-19-0
- 分子式: C23H26N6O2
- 分子量:418.49
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Apilimod
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]
- Exp Mol Med. 2024 Aug;56(8):1736-1749. [Abstract]
- Theranostics. 2020 Mar 4;10(9):3925-3938. [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]
- Biomaterials. 2022 Jun;285:121509. [Abstract]
- Cancer Lett. 2023 Nov 28:577:216435. [Abstract]
- Phytomedicine. 2026 May:154:158011. [Abstract]
- eGastroenterology. 2026 Mar 31;4(1):e100348. [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]
- Br J Cancer. 2020 Aug;123(4):542-555. [Abstract]
- Cell Mol Life Sci. 2016 Dec;73(24):4717-4737. [Abstract]
- J Cell Biol. 2025 Feb 3;224(2):e202401136. [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]
- Viruses. 2023 Jun 12;15(6):1353. [Abstract]
- Viruses. 2021 Jun 28;13(7):1255. [Abstract]
- Biotechnol J. 2023 Feb;18(2):e2200147. [Abstract]
- Exp Cell Res. 2026 Aug 1;461(1):115103. [Abstract]
- Vaccine. 2025 Aug 30:62:127537. [Abstract]
- Mol Biol Cell. 2022 Mar 1;33(3):ar26. [Abstract]
- Mol Cell Biol. 2025;45(3):99-115. [Abstract]
- bioRxiv. 2026 May 13:2026.05.11.724403. [Abstract]
- bioRxiv. 2025 Dec 18.
- bioRxiv. 2025 Nov 3:2025.11.02.686178. [Abstract]
- bioRxiv. 2025 June 02.
- bioRxiv. 2025 March 19.
- biorxiv. 2024 May 27.
- bioRxiv. 2024 May 10.
- bioRxiv. 2024 Jan 23.
- SSRN. 2024 Jan 26.
- bioRxiv. 2023 Oct 20:2023.10.19.563158. [Abstract]
- 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
-
WB
-
Bio/Physico-chemical Assay
-
RT-PCR
-
Bio/Physico-chemical Assay
-
WB
生物活性
|
IL-4 |
IL-5 |
IL-8 |
IL-12 |
IL-23 |
|
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 |
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 541550-19-0
-
性状 Solid
-
分子量 418.49
-
分子式 C23H26N6O2
-
Color White to off-white
-
SMILES
CC1=CC=CC(/C=N/NC2=CC(N3CCOCC3)=NC(OCCC4=CC=CC=N4)=N2)=C1
-
別名
STA 5326; LAM-002A (free base); AIT-101
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (44)
-
Journal Impact Factor
-
Most Recent
-
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 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 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 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 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.
-
Exp Mol Med
2024 Aug;56(8):1736-1749. PMID: 39085352 -
Theranostics
2020 Mar 4;10(9):3925-3938. PMID: 32226529 -
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 -
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 -
Cancer Lett
2023 Nov 28:577:216435. PMID: 37806516 -
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 -
eGastroenterology
2026 Mar 31;4(1):e100348. PMID: 41948149 -
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 -
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 -
Cell Mol Life Sci
2016 Dec;73(24):4717-4737. PMID: 27438886
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(0.5 μM; 21 h).
-
J Cell Biol
Neuronal constitutive endolysosomal perforations enable α-synuclein aggregation by internalized PFFs. [Abstract]2025 Feb 3;224(2):e202401136. PMID: 39714357 -
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 -
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 -
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 Aug 30:62:127537. PMID: 40706506 -
Mol Biol Cell
2022 Mar 1;33(3):ar26. PMID: 35020443 -
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 -
bioRxiv
Naked antisense oligonucleotides remain endolysosomally sequestered despite induced membrane damage. [Abstract]2026 May 13:2026.05.11.724403. PMID: 42182263 -
-
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
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
2023 Apr 28:2023.04.26.538482. PMID: 37383948 -
bioRxiv
2020 Jun 15:2020.04.21.053058. PMID: 32511398
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 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.
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: 0.5% CMC-Na/saline water
Solubility: 3.33 mg/mL (7.96 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
プロトコル
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
-
データシート (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)
-
取扱説明書 (2659 KB)
参考文献
[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]
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 | Concentration Solvent Mass | 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 関連分類
HY-14644 関連分類
Powered by Bioz