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
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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 | |
| 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 |
| Molecular Formula | C18H11Cl2N3O3S3 |
|---|---|
| Molecular Weight | 484.39900 |
| Exact Mass | 482.93400 |
| PSA | 165.33000 |
| LogP | 6.59338 |
| Precursor 5 | |
|---|---|
| DownStream 0 | |