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FT827

Catalog No. T15351   CAS 1959537-86-0

FT827 is a selective and covalent inhibitor of ubiquitin-specific protease 7 (USP7) (Ki: 4.2 μM). FT827 binds to the USP7 catalytic domain (apparent Kd: 7.8 μM).

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FT827, CAS 1959537-86-0
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description FT827 is a selective and covalent inhibitor of ubiquitin-specific protease 7 (USP7) (Ki: 4.2 μM). FT827 binds to the USP7 catalytic domain (apparent Kd: 7.8 μM).
Targets&IC50 USP7:(kd)7.8 μM, USP7:(ki)4.2 μM
In vitro FT827 exclusively inhibits USP7 in a panel of 38 deubiquitinases (DUBs) from diverse families. FT827 features a vinyl sulfonamide moiety that covalently modifies the catalytic Cys223 of USP7. FT827 inhibits USP7 probe reactivity (IC50s: 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 bromomethyl (HA-UbC2Br).
Molecular Weight 548.61
Formula C27H28N6O5S
CAS No. 1959537-86-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 125 mg/mL (227.85 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Turnbull AP, et al. Molecular basis of USP7 inhibition by selective small-molecule inhibitors. Nature. 2017 Oct 26;550(7677):481-486.

Related Products

Related compounds with same targets
USP8-IN-2 USP8-IN-3 USP15-IN-1 IMP-1710 HBX 41108 LDN-91946 FT827 USP7-IN-6

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Keywords

FT827 1959537-86-0 DNA损伤和修复 泛素化 细胞周期 DUB FT-827 Inhibitor inhibitor inhibit