SKI-178 是一种鞘氨醇激酶-1(SphK1)和SphK2抑制剂，以 CDK1 依赖性方式诱导人急性髓性白血病细胞凋亡。

SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM. It induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival Bcl-2 family members, Bcl-2 and Bcl-xl, as well as the phosphorylation and subsequent degradation of Mcl-1.

SKI-178 is a multi-targeted agent that functions both as an inhibitor of the SphKs as well as a disruptor of the microtubule network.?SKI-178 induced apoptosis arises from a synergistic interaction of these two activities.?SKI-178 is safe and effective in mouse models of AML, supporting its further development as a multi-targeted anti-cancer therapeutic agent[1].

1259484-97-3

C21H22N4O4

394.431

DMSO:50 mg/mL (126.77 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years