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USP7/USP47 inhibitor

Names

[ CAS No. ]:
1247825-37-1

[ Name ]:
USP7/USP47 inhibitor

[Synonym ]:
TERT-BUTYL 4-CYANO-4-PHENYL-1-PIPERIDINECARBOXYLATE
1-BOC-4-CYANO-4-PHENYL-PIPERIDINE
4-cyano-5-((3,5-dichloropyridin-4-yl)thio)-N-(4-(methylsulfonyl)phenyl)thiophene-2-carboxamide
N-(tert-butoxycarbonyl)-4-phenyl-4-cyanopiperidine
4-cyano-4-phenyl-piperidine-1-carboxylic acid tert-butyl ester
1-N-BOC-4-PHENYLPIPERIDINE-4-CARBONITRILE
USP7-USP47 inhibitor
1-Boc-4-phenyl-4-piperidinecarbonitrile
Tert-butyl 4-cyano-4-phenyl-piperidine-1-carboxylate
USP7/USP47 inhibitor

Biological Activity

[Description]:

USP7/USP47 inhibitor is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively.

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> Deubiquitinase
Research Areas >> Cancer

[Target]

EC50: 0.42 μM (USP7), 1.0 μM (USP47)[1]


[In Vitro]

USP7/USP47 inhibitor (compound 14) is a selective inhibitor of USP7/USP47 with EC50s of 0.42 μM and 1 μM, respectively. USP7/USP47 inhibitor does not inhibit caspase 3, calpain 1, 20S proteasome, and a panel of representative USPs (USP2, USP5, USP8, USP21, and USP28; EC50 > 31.6 μM). USP7/USP47 inhibitor inhibits the growth of HCT-116 cells with an EC50 of 7.6 μM[1].

[Kinase Assay]

The cloning, expression and purification of USP21 from BL21 (DE3) bacteria are performed using standard molecular biology techniques. USP2, USP5, USP7, USP8, USP28, USP47, Ub-PLA2 (Ub-CHOP) and Ub-EKL (Ub-CHOP2) are generated. Caspase 3 and the caspase 3 substrate DEVD-Rh110 are used. Deubiquitylating enzyme, cathepsin B and 20S proteasome chymotrypsin like protease activities are measured. Caspase 3 activity is determined using a similar protocol. Briefly, dose ranges of compound (including USP7/USP47 inhibitor) are incubated with caspase 3 for 30 minutes before the addition of DEVD-Rh110 and reading on a fluorometric plate reader using excitation and emission maxima of 485 nm and 531 nm respectively. The final concentrations of caspase 3 and DEVD-Rh110 are 2 nM and 100 nM respectively[1].

[References]

[1]. Weinstock J, et al. Selective Dual Inhibitors of the Cancer-Related Deubiquitylating Proteases USP7 and USP47. ACS Med Chem Lett. 2012 Sep 11;3(10):789-92.


[Related Small Molecules]

BAY 11-7082 | P5091 | PR-619 | VLX1570 | Degrasyn(WP1130) | P 22077 | DUBs-IN-2 | ML364 | NSC 687852 | GNE-6776 | ML 323 | HBX 19818 | IU1 | LDN-57444

Chemical & Physical Properties

[ Molecular Formula ]:
C18H11Cl2N3O3S3

[ Molecular Weight ]:
484.39900

[ Exact Mass ]:
482.93400

[ PSA ]:
165.33000

[ LogP ]:
6.59338

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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