Catalog No.: PC-60898Not For Human Use, Lab Use Only.
Rpn11 inhibitor 3021 is a derivative of 8TQ, and potent and specific inhibitor of proteasome isopeptidase Rpn11 (PSMD14) with IC50 of 0.34 uM, >7-fold improved potency over 8TQ (quinoline-8-thiol).
Rpn11 inhibitor 3021 is a derivative of 8TQ, and potent and specific inhibitor of proteasome isopeptidase Rpn11 (PSMD14) with IC50 of 0.34 uM, >7-fold improved potency over 8TQ (quinoline-8-thiol).
Rpn11 inhibitor 3021 shows >5-fold selectivity for Rpn11 over the related JAMM proteases and >2 logs less activity towards metalloenzymes (HDAC6, MMP2, MMP12, and carbonic anhydrase II).
Rpn11 inhibitor 3021 stabilizes proteasome substrates, induced an unfolded protein response, and blocks proliferation of cancer cells (HCT116 GI50=2.0 uM), including bortezomib-resistant retinal pigment epithelial cells.
