生物活性

• 描述The Kruppel-like factors (KLFs) are a family of transcription factors that contain zinc finger, which could regulate various cellular processes including proliferation, differentiation, development and apoptosis ^[1] . ML264 is an inhibitor of one of the KLF member, the KLF5, with IC50 value of 29 nM ^[2] .
  The DLD-1 and HCT116 cells were treated with 10 μmol/L of ML264. For the cell proliferation experiment, a significant decrease in proliferation of both cells lines was observed within 24 hours of incubation. Western blot analysis showed that the protein levels of ERK and KLF5 were decreased in both DLD-1 and HCT116 cells after 72 hours of ML264 treatment. Both cell lines showed a reduction in the level of the transcription factor early growth response 1 (EGR1) which is a direct activator of KLF5 expression. ^[3] . Similar results could be seen on HCT116 and MDA-MB-468 cell lines ^[4] .
  In DLD-1 tumor xenografts nude mice model, the ML264 was injected intraperitoneally for 10 days with 10 mg/kg or 25 mg/kg twice per day, and the tumor growth was significantly inhibited. The expression of the KLF5 and EGR1 in the xenografts from mice was significantly reduced after the ML264 treatment measured by IHC and western blot analysis ^[3] .

• 动物研究
  剂量	Mice: 10 mg/kg, 25 mg/kg[3] (i.p.)
  给药途径	i.p.