TXS-8 is a specific, small molecule binder of Rpn-6 with KD of 14 uM, Rpn-6 is a subunit of the 19S regulatory particle (RP) of 26s proteasome.
TXS-8 showed binding affinity towards Rpn-6 in biochemical and cell-based assays.
TXS-8 was also preferentially cytotoxic to cancer cell lines that require significant 26S proteasome activity for survival (MM.1R and Ramos B-cells, IC50=14 uM).
TXS-8 exhibited no appreciable binding against other 19S RP subunit, including Rpn-13. a useful tool to further elucidate the role of Rpn-6.
Rpn-6 is a proteasome-associated protein that makes critical contacts with the 19S regulatory particle (19S RP)and the 20S core particle (20S CP) of the proteasome.
