WebApr 7, 2024 · First of all, IPI-9119 is an orally active, selective, and irreversible FASN inhibitor with an IC 50 of 0.3 nM in vitro biochemical assay. Meanwhile, IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models. In the second place, IPI-9119 inhibits FASN in cellular occupancy assays (IC 50 ∼10nM). WebJun 15, 2024 · The search yielded nine compounds that were ordered and tested using substrate-based FASN activity assay. We found that they all inhibited FASN activity with the IC 50 values ranging from 0.5 to 2.1 µM, and approximately 56–90% inhibition of FASN activity was achieved at 1 µM final concentration (Fig. S7 and Table S3). As it is known …

Evaluation of FASN inhibitors by a versatile toolkit reveals ...

WebOct 24, 2016 · For the NF-κB activity assay, P/FASN, M3K/Sh, and their control P/Vec and M3K/Scr cells were seeded at 5 × 10 4 cells per well in 24-well plates and transfected with a PathDetect NF-κB Cis-Reporting … how many seasons of love on netflix

Mechanistic MALDI-TOF Cell-Based Assay for the Discovery of ... - PubMed

WebAug 11, 2012 · This is most likely due to the incomplete inhibition of FASN activity in H3255 and PC14 cells by 30 μM of orlistat, as determined by FASN activity assay (Fig. 1), which is due to the compensatory up-regulation of FASN expression levels in these cell lines, as determined by RT-PCR (Fig. 5b; Fig. S3 in the “Electronic Supplementary Material”). WebNational Center for Biotechnology Information WebSep 15, 2012 · FASN activity determined by [¹³C₁₆]palmitate synthesis was consistent with values obtained from β-nicotinamide adenine dinucleotide 2'-phosphate (NADPH) oxidation assays. Analysis of FASN activity from tissue extracts was not hampered by contaminating enzymes or preexisting fatty acids. Crude mammary gland and liver lysates had ... how many seasons of love