| Product Name | WP 1130 |
|---|---|
| Description | WP 1130, also known as degrasyn, is a cell-permeable deubiquitinase (DUB) inhibitor, able to directly inhibit the DUB activity of USP9x, USP5, USP14, and UCH37. WP 1130 has been shown to downregulate both wild-type and mutant Bcr/Abl without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells. WP 1130 can cause marked anti-proliferative activity and morphological changes in NCH644 and NCH421K glioma stem-like cells. |
| Synonyms | Degrasyn |
| Molecular Weight | 384.3 Da |
| Target | Deubiquitinating enzymes |
| Amino Acid Sequence | (2E)€‹-3-€‹(6-€‹bromo-€‹2-€‹pyridinyl)€‹-€‹2-€‹cyano-€‹N-€‹[1S-€‹phenylbutyl]€‹-2-€‹propenamide |
| Form | White solid |
| Purity | >98% by HPLC |
| Cas Number | 856243-80-6 |
| Storage | Store desiccated, frozen and in the dark |
| References |
Bartholomeusz et al (2007) Activation of a novel Bcr/Abl destruction pathway by WP1130 induces apoptosis of chronic myelogenous leukemia cells. 109(8) 3470 PMID: 17202319Bartholomeusz et al (2007) Degrasyn activates proteasomal-dependent degradation of c-Myc. Cancer Res. 67(8) 3912 PMID: 17440106Kapuria et al (2010) Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis. Cancer Res. 70(22) 9265 PMID: 21045142 Related areasAll small molecules >All deubiquitinating enzyme modulators >All cancer research categories > |
| Supplier | Isca Biochemicals Limited |
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