Apilimod | IL-12 and 23/PIKfyve inhibitor

CAS:
541550-19-0
Catalog Number:
10-4970
Activity:
IL-12 and 23/PIKfyve inhibitor
Chemical Names:
N-[(E)-(3-Methylphenyl)methylideneamino]-6-morpholin-4-yl-2-(2-pyridin-2-ylethoxy)pyrimidin-4-amine; STA5326
Molecular Weight:
418.50
Molecular Formula:
C23H26N6O2
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
99% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$35.00
25 mg$140.00
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Apilimod (541550-19-0) is a potent (IC50 = 10 nM IFN-g/LPS-stimulated human PMBC’s; IC50 = 1 nM in IFN-g/SAC-stimulated human PMBC’s) IL-12/IL-23 inhibitor downregulating both at the transcriptional level.  Suppresses Th1 but not Th2 immune response.1  Inhibition was also observed in human monocytes, monocyte-derived dendritic cells, and THP-1 cells.  Apilimod’s mechanism of action is mediation of TLR signaling via inhibition of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve; IC50 = 14 nM).2  It displayed selective cytotoxic activity in B-cell non-Hodgkin lymphoma compared with normal cells.3  Apilimod prevented infection of VSV-ZEBOV and VSV-SARS-CoV-2 (IC50 = 50 nM) as well as SARS-CoV-2 strain 2019-nCoVB/USA-1WA/2020.4

References:

  1. Wada et al. (2007), Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL23 inhibitor; Blood 109 1156
  2. Cai et al. (2013), PIKfyve, a class III PI-kinase, is the target of the small molecule IL12/23 inhibitor apilimod and a new player in toll-like receptor signaling; Chem. Biol., 20 912
  3. Gayle et al. (2016), Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma; Blood, 129 1768
  4. Kang et al. (2020), Inhibition of PIKfyve kinase prevents infection by Zaire ebola virus and SARS-CoV-2; Proc. Natl. Acad. Sci. USA 117 20803
CAS:
541550-19-0
Catalog Number:
10-4970
Activity:
IL-12 and 23/PIKfyve inhibitor
Chemical Names:
N-[(E)-(3-Methylphenyl)methylideneamino]-6-morpholin-4-yl-2-(2-pyridin-2-ylethoxy)pyrimidin-4-amine; STA5326
Molecular Weight:
418.50
Molecular Formula:
C23H26N6O2
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
99% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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