| Description | PI4KIII beta inhibitor 3 is a novel and high effective inhibitor of PI4KIIIβ (IC50 of 5.7 nM). |
| In vitro | PI4KIII beta inhibitor 3 is a PI4KIII inhibitor, has an IC50 of 5.7 nM. PI4KIII beta inhibitor 3 exerts significant immunosuppressive activity, with IC50 value of 3 nM in the mixed lymphocyte reaction (MLR) assay. PI4KIII beta inhibitor 3 inhibits IL2 and IFNy secretion with IC50 values of less than InM in each case. Thus, PI4KIII beta inhibitor 3 is shown to be as effective at inhibiting IL2 and IFNy secretion as conventional immunosuppressants such as cyclosporine A. IC50 on IFNy and IL-2 release of Cyclosporine A are 2nM and less than 1 nM respectively[1]. |
| In vivo | Oral administration of PI4KIII beta inhibitor 3 results in prolonged graft survival in 3 out of 6 grafts in each group at day 30. Several grafts continued beating after withdrawal of the treatment (up to 60 days), indicating the induction of a certain type of graft tolerance. To evaluate the operational tolerance phenotype, animals with functional graft at day 60 are challenged with a second graft from the same donor strain or from a third party. |
| Target activity | PI4KIIIβ:5.7 nM |
| molecular weight | 446.53 |
| Molecular formula | C22H22N8OS |
| CAS | 1245319-54-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 20 mg/mL (44.79 mM), Sonication is recommended. |
| References | 1. Jean Herman, et al. Autoimmune and inflammatory disorder therapy. From PCT Int. Appl. (2013), WO 2013034738 A1 |