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Degrasyn (WP1130) is a cell-permeable tyrphostin compound that acts as a partially selective deubiquitinase (DUB) inhibitor and suppresses JAK-Stat signaling pathway. Reported to cause accumulation of polyubiquitinated p53, JAK2 and Bcr-Abl, and reduce c-Myc and MCL-1 protein levels in several tumor cells and downregulate Stat3 and NF-κB activities (IC50 <1 µM in MCL cells) leading to tumor cell apoptosis (IC50 ~1.2 µM in Z138 cells). Suggested to modify active site cysteine of DUB and inhibit USP5, UCH-L1, USP9x, USP14, and UCH37 activities (≥80% inhibition at 5 µM) without affecting 20S proteasome. Reported to exert stronger antiproliferative and antitumor properties than STAT3 Inhibitor III, WP1066 in xenograft mouse models of CML and melanoma.
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Source | Cancer Res (2010). Figure 1. WP1130 |
| Method | immunoblotting | |
| Cell Lines | HEK293T cells | |
| Concentrations | 5 μmol/L | |
| Incubation Time | 2 h | |
| Results | WP1130 displayed potent antiproliferative properties against various other tumor cell lines of myeloid and lymphoid origin as well as HEK293T cells |
| Cell Experiment | |
|---|---|
| Cell lines | CML cells |
| Preparation method | MTT (viability) assay CML cells were seeded in 96-well plates (2*104 cells/well) and WP1130, imatinib mesylate, or dasatinib (0.08-10 µ M) were added in a final volume of 100 µL medium. Plates were incubated at 37°C for 72 hours, after which 20 µL of 3-4,5-dimethylthiazolyl-2-2, 5-diphenyltetrazolium bromide (MTT) reagent (Sigma; stock 5 mg/mL) was added, and the plates were incubated at 37°C for another 2 hours. Cells were lysed with 100 L lysis buffer (20% sodium dodecyl sulfate [SDS] in 50% N, N-dimethylformamide adjusted to pH 4.7 with 80% acetic acid and 1 M hydrochloric acid; final concentration of acetic acid was 2.5% and hydrochloric acid was 2.5%) and incubated for 6 hours. The optical density of each sample at 570 nm was determined with a SPECTRA MAX M2 plate reader (Molecular Devices, Sunnyvale, CA). |
| Concentrations | 0.08-10 µ M |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | CML tumors and Bcr/Abl-expressing cells in nude mice |
| Formulation | a 0.1-mL suspension of 1:1 dimethylsulfoxide to polyethylene glycol 300 |
| Dosages | 30 mg/kg every other day for 5 injections |
| Administration | injected intraperitoneally |
| Molecular Weight | 384.3 |
| Formula | C19H18BrN3O |
| CAS Number | 856243-80-6 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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