1. Cell Cycle/DNA Damage
  2. Deubiquitinase
  3. FT827

FT827 

Cat. No.: HY-111350 Purity: 98.48%
Handling Instructions

FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 52 nM.

For research use only. We do not sell to patients.

FT827 Chemical Structure

FT827 Chemical Structure

CAS No. : 1959537-86-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 785 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4900 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

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Description

FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 52 nM.

IC50 & 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].

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8228 mL 9.1139 mL 18.2279 mL
5 mM 0.3646 mL 1.8228 mL 3.6456 mL
10 mM 0.1823 mL 0.9114 mL 1.8228 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.79 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.79 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.79 mM); Clear solution

References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

548.61

Formula

C₂₇H₂₈N₆O₅S

CAS No.

1959537-86-0

SMILES

C=CS(=O)(NC1=CC=CC=C1C2=CC=C(C(N3CCC(O)(CN(C=NC4=C5C=NN4C)C5=O)CC3)=O)C=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
FT827
Cat. No.:
HY-111350
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FT827

Cat. No.: HY-111350