Catalog No.: PC-49183Not For Human Use, Lab Use Only.
LFS-829 (LFS829) is a potent, covalent, small-molecule antagonist of exportin-1 (CRM1) with binding Kd values of 26.95 nM in SPR assays, forms a covalent bond with the sulfur atom of Cys539 126 located in the NES binding cleft of CRM1.
LFS-829 (LFS829) is a potent, covalent, small-molecule antagonist of exportin-1 (CRM1) with binding Kd values of 26.95 nM in SPR assays, forms a covalent bond with the sulfur atom of Cys539 126 located in the NES binding cleft of CRM1.
The C528S mutation or the knockdown on exportin-1 can abolish the cellular activities of LFS-829.
Oral administration of LFS-829 (30 mg/kg) significantly ameliorates DSS-induced colitis mice as compared to 5-ASA.
LFS-829 (10 mg/kg) exerts superior efficacy than APD334 in colitis mice in one-week dosing schedule.
LFS-829 attenuates both NF-kB signaling and Nrf2 cytoprotection pathway in colitis model.
LFS-829 (30mg/kg/day, α-cyclodextrin) ameliorate DSS-induced colitis in model mice.
