1959537-86-0
1959537-86-0 structure
- Name: FT-827
- Chemical Name: FT827
- CAS Number: 1959537-86-0
- Molecular Formula: C27H28N6O5S
- Molecular Weight: 548.61
- Catalog: Signaling Pathways Cell Cycle/DNA Damage Deubiquitinase
- Create Date: 2018-08-24 23:50:31
- Modify Date: 2024-01-09 08:17:13
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FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 52 nM.
| Name | FT827 |
|---|
| Description | FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 52 nM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 52 nM (USP7)[1] |
| In Vitro | 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]. |
| Kinase Assay | To determine compound IC50s, FT827 is diluted in 100% DMSO in three-fold 12- point dilution series from 100 µM. 100 nL of 100-fold concentrated solutions are dispensed into black 384-well plate. 25 nM ubiquitin-rhodamine 110, along with recombinant USP7CD (3 nM), or USP7C-term (30-125 pM, depending on batch activity) are added and the plates incubated at room temperature for 1 h. The reaction is terminated by adding 2.5 µL citric acid to a final concentration of 10 mM prior to measuring fluorescence intensity on a Pherastar with a 485 nm excitation/520 nm emission optic module[1]. |
| References |
| Molecular Formula | C27H28N6O5S |
|---|---|
| Molecular Weight | 548.61 |
| Storage condition | 2-8℃ |