Home Immunology & Inflammation Interleukins inhibitor - PIKfyve inhibitor Apilimod mesylate For research use only.

Apilimod mesylate

Synonyms: STA-5326 mesylate

Apilimod mesylate 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 mesylate (STA-5326 mesylate) 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 mesylate (STA-5326 mesylate) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.

Apilimod mesylate Chemical Structure

Apilimod mesylate Chemical Structure

CAS No. 870087-36-8

Purity & Quality Control

Apilimod mesylate Related Products

Biological Activity

Description Apilimod mesylate 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 mesylate (STA-5326 mesylate) 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 mesylate (STA-5326 mesylate) 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 [2]
(Cell-free assay)
1 nM 1 nM 2 nM 14 nM
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 610.7 Formula

C25H34N6O8S2
CAS No. 870087-36-8 SDF --
Smiles CC1=CC(=CC=C1)C=NNC2=CC(=NC(=N2)OCCC3=CC=CC=N3)N4CCOCC4.CS(=O)(=O)O.CS(=O)(=O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

Water : 33 mg/mL

DMSO : 20 mg/mL ( (32.74 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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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.

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