Potent and selective PIKfyve inhibitor
Apilimod dimesylate is a potent and selective PIKfyve inhibitor (IC50 = 14 nM). Exhibits no significant activity at other lipid kinases and protein kinases, including PIP4K, PIP5K, mTOR, PI3K and PI4K. Inhibits cellular entry by SARS-CoV-2, MERS-CoV and MHV S pseudovirions. Reduces number of SARS-CoV-2-infected hiPSC-derived pneumocyte-like cells by 85% and inhibits SARS-CoV-2 replication in donor lung tissue. Also exhibits selective cytotoxicity in B-cell non-Hodgkin lymphoma compared with normal cells. Inhibits production of IL-12 and IL-23. Anti-inflammatory. Water-soluble.
| Marque | Tocris |
|---|---|
| Réf. B-LABO | BL-RE-124711 |
| Réf. fabricant | 18799956 |
| Nom chimique ou matériau | 4-(6-(2-(3-Methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine dimethanesulfonate |
| CAS | 870087-36-8 |
| Quantité | 5 mg |
| Cible | PIKFyve/PIP5K3 |
| Formule moléculaire | C<sub>23</sub>H<sub>26</sub>N<sub>6</sub>O<sub>2</sub>0.2 CH<sub>3</sub>SO<sub>3</sub>H |
| Pureté | 0.98 |
