USP7/USP47 inhibitor

Modify Date: 2024-01-10 17:46:25

USP7/USP47 inhibitor Structure
USP7/USP47 inhibitor structure
Common Name USP7/USP47 inhibitor
CAS Number 1247825-37-1 Molecular Weight 484.39900
Density N/A Boiling Point N/A
Molecular Formula C18H11Cl2N3O3S3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of USP7/USP47 inhibitor


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.

 Names

Name 4-Cyano-5-[(3,5-dichloro-4-pyridinyl)sulfanyl]-N-[4-(methylsulfon yl)phenyl]-2-thiophenecarboxamide
Synonym More Synonyms

 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
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.

 Chemical & Physical Properties

Molecular Formula C18H11Cl2N3O3S3
Molecular Weight 484.39900
Exact Mass 482.93400
PSA 165.33000
LogP 6.59338

 Synthetic Route

~31%

USP7/USP47 inhibitor Structure

USP7/USP47 inhibitor

CAS#:1247825-37-1

Literature: Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar, K. G.; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin Medicinal Chemistry letters, 2012 , vol. 3, # 10 p. 789 - 792,4 Title/Abstract Full Text Show Details Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 10 p. 789 - 792

~%

USP7/USP47 inhibitor Structure

USP7/USP47 inhibitor

CAS#:1247825-37-1

Literature: Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar, K. G.; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin Medicinal Chemistry letters, 2012 , vol. 3, # 10 p. 789 - 792,4 Title/Abstract Full Text Show Details Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 10 p. 789 - 792

~%

USP7/USP47 inhibitor Structure

USP7/USP47 inhibitor

CAS#:1247825-37-1

Literature: Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar, K. G.; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin Medicinal Chemistry letters, 2012 , vol. 3, # 10 p. 789 - 792,4 Title/Abstract Full Text Show Details Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 10 p. 789 - 792

~%

USP7/USP47 inhibitor Structure

USP7/USP47 inhibitor

CAS#:1247825-37-1

Literature: Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar, K. G.; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin Medicinal Chemistry letters, 2012 , vol. 3, # 10 p. 789 - 792,4 Title/Abstract Full Text Show Details Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 10 p. 789 - 792

~%

USP7/USP47 inhibitor Structure

USP7/USP47 inhibitor

CAS#:1247825-37-1

Literature: Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar, K. G.; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin Medicinal Chemistry letters, 2012 , vol. 3, # 10 p. 789 - 792,4 Title/Abstract Full Text Show Details Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 10 p. 789 - 792

~%

USP7/USP47 inhibitor Structure

USP7/USP47 inhibitor

CAS#:1247825-37-1

Literature: Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar, K. G.; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin Medicinal Chemistry letters, 2012 , vol. 3, # 10 p. 789 - 792,4 Title/Abstract Full Text Show Details Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 10 p. 789 - 792

 Synonyms

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
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