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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-FT709
FT709

Chemical Structure : FT709

CAS No.: 2413991-74-7

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FT709 (FT-709)

货号: PC-38692Not For Human Use, Lab Use Only.

FT709 is a potent, highly selective USP9X inhibitor with IC50 of 82 nM in biochemical assays, reduces CEP55 expression in BxPC3 pancreatic cancer cells with IC50 of 131 nM.

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纯度 & COA & 质检文件 纯度: 99.8% (HPLC) Select Batch:

生物&药学活性

FT709 is a potent, highly selective USP9X inhibitor with IC50 of 82 nM in biochemical assays, reduces CEP55 expression in BxPC3 pancreatic cancer cells with IC50 of 131 nM.
FT709 is inactive across a panel of 20 deubiquitylases (DUBs) in a biochemical assay (IC50 values >25 uM), shows vastly improved specificity over the compound WP1130.
FT709 competes with an active site probe (HA-UbC2Br) with an IC50 of 0.5 uM and 5 uM when applied to MCF7 breast cancer cell extracts and to intact MCF7 cells, respectively.
Acute inhibition with FT709 recapitulates gene deletion of USP9X in HCT116 cells, depletes ZNF598 and MKRN2 protein levels, and impairs the ribosomal stalling response.
FT709 is a highly specific USP9X tool compound inhibitor will enable further enquiry into pathways previously linked to USP9X, which should now include global profiling of protein translation.

物理化学性质&存储条件

分子量 498.510
分子式 C23H22N4O7S
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)-1-(5-((2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-7-yl)sulfonyl)-3,4,5,6-tetrahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)-2-hydroxy-2-(2-methylbenzo[d]oxazol-4-yl)ethan-1-one

参考文献

1. Anne Clancy, et al. J Cell Biol. 2021 Mar 1;220(3):e202004211.

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