PLX314407

GSE101637: RNA-Seq analysis of the impact of a kinase NIK inhibitor (DMBP5) on the human melanoma cell line A375 (replicate 1)

• Organsim human
• Type RNASEQ
• Target gene
• Project ARCHS4

Introduction: there is growing evidence that the IFN--related cytokine signature plays a major role supporting the effect of pharmacological blockade of immune checkpoints. The expression of IFN- in cancer cells is repressed by several factors, among them a key role is played by the oncogene EZH2, which in turns is controlled by the non-canonical NF-kB pathway and its upstream kinase, NIK.; ; Methodology: we developed a series of NIK inhibitors and compared the effects on cancer cells of one of them (DMBP5) to an siRNA against NIK via transcriptomic analysis (RNA-seq).; ; Results: mRNA modifications induced by DMBP5 on A375 melanoma cells closely resemble the ones observed with siRNA against NIK.; ; Conclusions: DMBP5 is a very selective and effective non-competitive NIK inhibitor (first in class). SOURCE: Kevin LebrigandFunctional Genomics Platform of Nice-Sophia-Antipolis, France. IPMC/CNRS