SKI-178 is an in vivo active non-lipid sphingosine kinase 1 (SphK1) inhibitor (IC50 = 0.1-1.8 μM), which induces CDK1-dependent apoptosis in human acute myeloid leukemia cell lines.
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SKI-178 is a potent inhibitor of sphingosine kinase-1 (SphK1) and SphK2. It exhibits cytotoxicity with IC50 concentrations ranging from 1.8 to 0.1 μM in various cancer cell lines, including those resistant to multiple agents (i.e., MTR3, NCI-ADR, and HL60/VCR cells). SKI-178 induces apoptosis in human acute myeloid leukemia cell lines in a CDK1-dependent manner[1][2].
体内研究
SKI-178 (20 mg/kg; retro-orbital injection under isoflurane anesthesia) suppresses leukemic progression in the MLL-AF9 model[3].
体外研究
The apoptotic cell death induced by SKI-178 (5 μM; 24 hours) is associated with prolonged phosphorylation of Bcl-2[1].
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