FLLL32 is an effective JAK2/STAT3 inhibitor (IC50 of <5 μM).

JAK2:<5 μM

在MDA-MB-231乳腺癌和PANC-1胰腺癌细胞中，FLLL32降低STAT3的磷酸化和DNA结合活性。在MDA-MB-231细胞中，FLLL32抑制了集落形成和细胞侵袭。[1] 在人类多发性骨髓瘤、胶质母细胞瘤、肝癌和结直肠癌细胞系中，FLLL32同样抑制细胞增殖并诱导caspase-3和PARP的裂解。[2]

在MDA-MB-231异种移植小鼠模型中，FLLL32（50 mg/kg，i.p.）显著降低了肿瘤负担。[1] 在带有OS-33骨肉瘤细胞的小鼠异种移植模型中，FLLL32（50 mg/kg，i.p.）通过靶向STAT3也抑制了肿瘤生长。[3]

JAK2 and other human kinase activity assays: JAK2 kinase activity was assessed with the HTScan JAK2 Kinase Assay Kit per manufacturer's protocol. The possible effects of FLLL32 on the other 10 purified human protein kinases were determined by using a Kinase Profiler Assay.

Cells are seeded in 96-well plates (3,000 per well) in triplicate and then treated with 0.5 to 5 μM of FLLL31 or FLLL32 or with 0.5 to 30 μM of curcumin for 72 h. MTT (25 μL) is added to each sample and incubated for 3.5 h. Then, 100 μL of N,N-dimethylformamide solubilization solution are added to each well. The absorbance at 450 nm is read the following day. IC50 are determined using Sigma Plot 9.0 software.(Only for Reference)