LFS-829 | CRM1 inhibitor | Probechem Biochemicals

Chemical Structure : LFS-829

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LFS-829 (LFS829)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	373.331
分子式	C13H9F6NOS2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S,E)-1-((4-isothiocyanatobut-1-en-1-yl)sulfinyl)-3,5-bis(trifluoromethyl)benzene

参考文献

1. Xibao Tian, et al. J Med Chem. 2020 Apr 23;63(8):3881-3895.

LFS-829 (LFS829)

生物&药学活性

物理化学性质&存储条件

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LFS-829 (LFS829)

生物&药学活性

物理化学性质&存储条件

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