Catalog No.: PC-24524Not For Human Use, Lab Use Only.
GS143 is a specific small molecule inhibitor of E3 ligase β-TrCP, exhibits potent latency reversing agent (LRA) activity, also is a NF-kappaB signaling inhibitor, inhibits IκBα ubiquitylation (IC50=5.2 uM).
GS143 is a specific small molecule inhibitor of E3 ligase β-TrCP, exhibits potent latency reversing agent (LRA) activity, also is a NF-kappaB signaling inhibitor, inhibits IκBα ubiquitylation (IC50=5.2 uM). GS143 selectively inhibits IκBα ubiquitination inhibitor withIC50 of 5.2 uM for SCF βTrCP1-mediated IκBα ubiquitylation. GS143 displays potent LRA activity in a primary cell model of HIV-1 latency. GS143 triggers a novel signaling pathway to reactivate latent HIV-1 that leads to the unconventional activation of NFκB p65, by initiating the noncanonical signaling via NIK, followed by activation of IKK leading to phosphorylation of p65 on S536 and its nuclear translocation.
