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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Ubiquitin-activating Enzyme (E1)-UBA5 inhibitor 50
UBA5 inhibitor 50

Chemical Structure : UBA5 inhibitor 50

CAS No.:

UBA5 inhibitor 50

货号: PC-25563Not For Human Use, Lab Use Only.

UBA5 inhibitor 50 is a potent, selective and noncovalent inhibitor of E1 enzyme Ubiquitin-like modifier activating enzyme 5 (UBA5) with IC50 of 32 nM in biochemical HTRF assays, SPR KD of 0.063 uM, selectively inhibits UFMylation pathway.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

UBA5 inhibitor 50 is a potent, selective and noncovalent inhibitor of E1 enzyme Ubiquitin-like modifier activating enzyme 5 (UBA5) with IC50 of 32 nM in biochemical HTRF assays, SPR KD of 0.063 uM, selectively inhibits UFMylation pathway.
UBA5 inhibitor 50 does not inhibit ubiquitination of UBE1 or the transfer of ubiquitin from UBE1 to UbE2D2/UbcH5B, and the SUMOylation of UbE2I/UBC9, indicating selectivity for the UFMylation pathway.
UBA5 inhibitor 50 (10-25 uM) selectively inhibits UFMylation of UBA5, UFC1 and leads to a decrease in total level of UFMylated proteins in RPE1 cells, significantly decreases UFMylation of UBA5 target RPL26 and reduces total levels of protein UFMylation upon anisomycin treatment.

物理化学性质&存储条件

分子量 644.75
分子式 C35H41FN6O5
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

N-(2-(((S)-1-(5-Fluoro-7-(((3R,4R)-4-hydroxytetrahydro-2H-pyran-3-yl)carbamoyl)-1,2,3-trimethyl-1H-indol-4-yl)piperidin-3-yl)(methyl)amino)-2-oxoethyl)quinoline-5-carboxamide

参考文献

1. Mignone JJ, et al. J Med Chem. 2025 Sep 25. doi: 10.1021/acs.jmedchem.5c02305.

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