Home PI3K/Akt/mTOR PIKfyve inhibitor - Interleukins inhibitor Apilimod For research use only.

Apilimod

Synonyms: STA-5326

Apilimod is a potent and orally-available inhibitor of the cytokines interleukin-12 (IL-12) and interleukin-23 (IL-23) with the potential to treat certain autoimmune and inflammatory diseases. Apilimod (STA-5326) inhibits IL-12 with IC50 of 1 nM, 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs, human monocytes and mouse PBMCs, respectively. Apilimod (STA-5326) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.

Apilimod Chemical Structure

Apilimod Chemical Structure

CAS No. 541550-19-0

Purity & Quality Control

Apilimod Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description Apilimod is a potent and orally-available inhibitor of the cytokines interleukin-12 (IL-12) and interleukin-23 (IL-23) with the potential to treat certain autoimmune and inflammatory diseases. Apilimod (STA-5326) inhibits IL-12 with IC50 of 1 nM, 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs, human monocytes and mouse PBMCs, respectively. Apilimod (STA-5326) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.
Targets
IL-12 [1]
( in IFN-γ/SAC-stimulated human PBMCs)		 IL-12 [1]
(in human monocytes)		 IL-12 [1]
(in mouse PBMCs)		 PIKfyve [1]
1 nM 1 nM 2 nM 14 nM
In vitro
In vitro

Apilimod selectively inhibits TLR-induced cytokine expression. It selectively inhibits the production of IL12p40, whereas it has little effect on IL8 production in THP-1 cells[1].

Apilimod reduces not only PtdIns(3,5)P2 production but also that of PtdIns5P in intact cells[2].
Cell Research Cell lines HeLa cells
Concentrations 10 nM and 1 μM
Incubation Time 120 min
Method

HeLa cells are metabolically labeled with [3H]inositol for 72 hr and treated with two doses of apilimod or the inactive analog API09 for 120 min. Lipids are extracted, deacetylated, and analyzed by HPLC.
In Vivo
In vivo

Apilimod is a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma.
Animal Research Animal Models Mice
Dosages 50 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00234741 Completed
Crohn''s Disease
Synta Pharmaceuticals Corp.|National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health (NIH)
 November 2005 Phase 2

Chemical Information & Solubility

Molecular Weight 418.49 Formula

C23H26N6O2
CAS No. 541550-19-0 SDF --
Smiles CC1=CC(=CC=C1)C=NNC2=CC(=NC(=N2)OCCC3=CC=CC=N3)N4CCOCC4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 84 mg/mL ( (200.72 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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