Catalog No.: PC-43474Not For Human Use, Lab Use Only.
PYR-41 is a selective, cell-permeable inhibitor of ubiquitin-activating enzyme (E1), blocks loading of immobilized His6-tagged E1 with ubiquitin with IC50 of <10 uM.
PYR-41 is a selective, cell-permeable inhibitor of ubiquitin-activating enzyme (E1), blocks loading of immobilized His6-tagged E1 with ubiquitin with IC50 of <10 uM.
PYR-41 does not affect the transfer of ubiquitin to E2 from E1, directly inhibits E1, but not E2.
In addition to blocking ubiquitylation, PYR-41 increases total sumoylation in cells, attenuates cytokine-mediated nuclear factor-kappaB activation and inhibits nonproteasomal (Lys-63) ubiquitylation of TRAF6, also prevents the downstream ubiquitylation and proteasomal degradation of IκBα。
PYR-41 inhibits degradation of p53 and activates the p53 transcriptional activity, demonstrates anti-tumor activity in animal studies.
