FT827 |
| Katalog-Nr.GC32917 |
FT827 ist ein selektiver und kovalenter Inhibitor der Ubiquitin-spezifischen Protease 7 (USP7) (Ki=4,2 ?M). FT827 bindet an die katalytische Domäne von USP7 (USP7CD; Aminosäuren 208-560) mit einem scheinbaren Kd-Wert von 7,8 ?M.
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Cas No.: 1959537-86-0
Sample solution is provided at 25 µL, 10mM.
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FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 52 nM.
FT827 features a vinylsulfonamide moiety that covalently modifies the catalytic Cys223 of USP7 and inhibits the enzyme with Ki and Kd of 7.8 and 4.2 μM, respectively. FT827 exclusively inhibit USP7 in a panel of 38 deubiquitinases (DUBs) from diverse families. FT827 inhibits USP7 probe reactivity with IC50s of 0.1-2 µM, confirming 10 to 100-fold higher potency as compared to P22077 in crude cell extracts or with intact MCF7 breast cancer cells, followed by incubation with the ubiquitin active site suicide probe haemagglutinin (HA)-tagged ubiquitin bromoethyl (HA-UbC2Br)[1].
[1]. Turnbull AP, et al. Molecular basis of USP7 inhibition by selective small-molecule inhibitors. Nature. 2017 Oct 26;550(7677):481-486.
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