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Chemical Structure : LFS-829
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.
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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.
| M.Wt | 373.331 | |
| Formula | C13H9F6NOS2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Xibao Tian, et al. J Med Chem. 2020 Apr 23;63(8):3881-3895.
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