Potent and selective SphK1 inhibitor
PF 543 hydrochloride is a potent and selective SphK1 inhibitor (IC50 = 2 nM; Ki = 3.6 nM). Exhibits >100-fold selectivity for Sphk1 over Sphk2. Also exhibits >5,000 fold selectivity over S1P1-5 receptors and 48 protein and lipid kinases. Attenuates proliferation and induces necrosis in human colorectal cancer cells
in vitro
. Suppresses HCT-116 tumor xenograft growth in mice. Also reduces sickling, hemolysis and inflammation in a transgenic mouse model of sickle cell disease.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-151121 |
| Réf. fabricant | 18751829 |
| Nom chimique ou matériau | (2R)-1-[[(4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride |
| CAS | 1706522-79-3 |
| Quantité | 50 mg |
| Cible | Sphingosine Kinase Inhibitors |
| Formule moléculaire | C<sub>27</sub>H<sub>31</sub>NO<sub>4</sub>S.HCl |
| Poids de la formule | 502.07 |
| Pureté | >98% |
