1247825-37-1

1247825-37-1 structure

Name: USP7/USP47 inhibitor
Chemical Name: 4-Cyano-5-[(3,5-dichloro-4-pyridinyl)sulfanyl]-N-[4-(methylsulfon yl)phenyl]-2-thiophenecarboxamide
CAS Number: 1247825-37-1
Molecular Formula: C₁₈H₁₁Cl₂N₃O₃S₃
Molecular Weight: 484.39900
Catalog: Signaling Pathways Cell Cycle/DNA Damage Deubiquitinase
Create Date: 2016-07-15 11:27:00
Modify Date: 2024-01-10 17:46:25
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.

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

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.