[CAS NO. 1245319-54-3] PI4KIIIbetainhibitor3
PRODUCTS SPECIFICATIONS [1245319-54-3]
DESCRIPTION [1245319-54-3]
Overview
| MDL | MFCD22124455 |
|---|---|
| Molecular Weight | 446.53 |
| Molecular Formula | C22H22N8OS |
| SMILES | O=C(N1CCN(C2=C3C(SC(C4=CC=CN=C4)=N3)=NC(N)=N2)CC1)NC5=CC=C(C)C=C5 |
1 Publications Citing Use of MCE
Summary
PI4KIII beta inhibitor 3 is a novel and high effective PI4KIIIβ inhibitor with IC 50 of 5.7 nM.
IC50 & Target
|
PI4KIIIβ 5.7 nM (IC 50 ) |
In Vitro
PI4KIII beta inhibitor 3 is a PI4KIII inhibitor extracted from patent WO/2013034738 A1, the compound of formula 3, has an IC 50 of 5.7 nM. PI4KIII beta inhibitor 3 exerts significant immunosuppressive activity, with IC 50 value of 3 nM in the mixed lymphocyte reaction (MLR) assay. PI4KIII beta inhibitor 3 inhibits IL2 and IFNy secretion with IC 50 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. IC 50 on IFNy and IL-2 release of Cyclosporine A are 2nM and less than 1 nM respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PI4KIII beta inhibitor 3 (40 mg/kg per day, n=12) is able to delay the onset of arthritic symptoms and also to decrease symptom severity in a preventive model of arthritis compared to a vehicle control (MC 1%, n=12). PI4KIII beta inhibitor 3 reduces the anti-CII IgG titre and histological scores in the collagen-induced arthritis mouse model. 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. No treatment is applied. The second grafts from the third party are rejected at day 8 (n=2) whereas second grafts from the same donor strain are functional for more than 90 days (n=2) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 20 mg/mL ( 44.79 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2395 mL | 11.1975 mL | 22.3949 mL |
| 5 mM | 0.4479 mL | 2.2395 mL | 4.4790 mL |
| 10 mM | 0.2239 mL | 1.1197 mL | 2.2395 mL |