| Name | USP7/USP47 inhibitor |
| Description | USP7/USP47 inhibitor (USP7/47 inhibitor-1) is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively. |
| 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 |
| In vitro | 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 45 mg/mL (92.9 mM)
|
| Keywords | USP-7/USP47 inhibitor | Deubiquitinase | inhibit | USP7/USP47 inhibitor | Inhibitor | DUBs |
| Inhibitors Related | P22074 | BAY 11-7082 | USP15-IN-1 | N-Ethylmaleimide | DUB-IN-1 | SJB3-019A | USP30 inhibitor 11 | Vialinin A | GRL0617 | Spautin-1 | 6-Thioguanine | USP8-IN-3 |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Ubiquitination Compound Library | HIF-1 Signaling Pathway Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
