MP-A08 是高度选择性和 ATP 竞争性的 SPHK1 抑制剂。

MP-A08 is a highly selective ATP competitive inhibitor of sphingosine kinase (SPHK1) that targets both SphK1 and SphK2 (Ki: 6.9 ± 0.8 μM and 27 ± 3 μM, respectively).

MP-A08 inhibit SphK2, cause a decrease in EC barrier integrity in vitro in both cell type. MP-A08 blocks pro-proliferative signaling pathways causes mitochondrial-associated apoptosis in an SK-dependent manner. It also reduces the growth of human lung adenocarcinoma tumours in a mouse xenograft model by both inducing tumour cell apoptosis and inhibiting tumour angiogenesis [2]

MP-A08 inhibits the growth of human lung tumour xenografts in mice.

219832-49-2

C27H25N3O4S2

519.64

H2O:insoluble
DMSO:50 mg/mL (96.22 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years