FT827


Catalog No. Size PriceQuantity
M13152-2 Contact sales@xcessbio.com for quotation $100
M13152-10 Contact sales@xcessbio.com for quotation $100

Description

FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor (Ki=4.2 µM). FT827 binds to the USP7 catalytic domain (USP7CD; residues 208-560) with an apparent Kd value of 7.8 µM.

Product information

CAS Number: 1959537-86-0

Molecular Weight: 548.61

Formula: C27H28N6O5S

Chemical Name: N-{4'-[4-hydroxy-4-({1-methyl-4-oxo-1H,4H,5H-pyrazolo[3,4-d]pyrimidin-5-yl}methyl)piperidine-1-carbonyl]-[1,1'-biphenyl]-2-yl}ethene-1-sulfonamide

Smiles: CN1N=CC2=C1N=CN(CC1(O)CCN(CC1)C(=O)C1C=CC(=CC=1)C1=CC=CC=C1NS(=O)(=O)C=C)C2=O

InChiKey: GFNJQQBUZURQMA-UHFFFAOYSA-N

InChi: InChI=1S/C27H28N6O5S/c1-3-39(37,38)30-23-7-5-4-6-21(23)19-8-10-20(11-9-19)25(34)32-14-12-27(36,13-15-32)17-33-18-28-24-22(26(33)35)16-29-31(24)2/h3-11,16,18,30,36H,1,12-15,17H2,2H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

FT827 features a vinylsulfonamide moiety that covalently modifies the catalytic Cys223 of USP7 and inhibits the enzyme with Ki and Kd of 4.2 and 7.8 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).

References:

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

Products are for research use only. Not for human use.

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