It is the first and only RIPK2 inhibitor that has advanced into clinical trials. However, the trial was terminated prematurely due to non-clinical toxicity and a reduced safety margin of GSK2983559. Currently, there are no inhibitors of RIPK2 available for clinical use. Notably, the solubility ...
Using quantitative real-time polymerase chain reaction (RT-PCR), we found that transient RIPK2 overexpression in PC3 cells, RIPK2-KO in 22Rv1 cells, or RIPK2 inhibition by GSK583 (a RIPK2-selective inhibitor) at different doses and time only modestly (~10%) regulated MYC mRNA abundance (Sup...
However, no data on any clinical evaluations are currently available. As for RIPK3, diverse isoform-specific inhibitors have been characterized, such as the pioneering compounds GSK843 (5) and GSK872 (6) [34]. Later, the inhibitor HS-1371 (7) [35] as well as other compounds have been ...