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WP 1130
- Degrasyn
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C19H18BrN3O
- MW: 384.27
Description
WP 1130 is a small-molecule deubiquitinase (DUB) inhibitor also known as Degrasyn.
DUBs regulate ubiquitinated protein turnover, proteasome signaling and survival pathways. WP 1130 is used to study accumulation of ubiquitinated proteins, stress signaling and DUB-dependent oncogenic pathway regulation.
Key Features
- Small-molecule inhibitor of deubiquitinase activity
- Modulates ubiquitin-proteasome pathway signaling
- Promotes accumulation of ubiquitinated proteins in reported models
- Useful tool for DUB-dependent survival pathway studies
Applications
- Deubiquitinase inhibitor assays
- Ubiquitin-proteasome system research
- Cancer cell stress and apoptosis models
- Protein turnover and signaling pathway studies
More Information
| Parent CAS No. | 856243-80-6 |
|---|---|
| Chemical Name | (S,E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylbutyl)acrylamide |
| SMILES | C(N[C@H](C1=CC=CC=C1)CCC)(=O)/C(/C#N)=C/C1=NC(Br)=CC=C1 |&1:2,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C19H18BrN3O/c1-2-7-17(14-8-4-3-5-9-14)23-19(24)15(13-21)12-16-10-6-11-18(20)22-16/h3-6,8-12,17H,2,7H2,1H3,(H,23,24)/b15-12+/t17-/m0/s1 |
| InChiKey | LIDOPKHSVQTSJY-VMEIHUARSA-N |
| CID | 11222830 |
| Short Description | DUB inhibitor |
References
- V Kapuria et al. A novel small molecule deubiquitinase inhibitor blocks Jak2 signaling through Jak2 ubiquitination. Cell Signal. 2011, 23(12), 2076-2085.
- V Kapuria et al. Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis. Cancer Res. 2010, 70(22), 9265-9276.
- LV Pham et al. Degrasyn Potentiates the Antitumor Effects of Bortezomib in Mantle Cell Lymphoma Cells In vitro and In vivo: Therapeutic Implications. Mol Cancer Ther July 2010 9; 2026.
- GA Bartholomeusz et al. Activation of a novel Bcr/Abl destruction pathway by WP1130 induces apoptosis of chronic myelogenous leukemia cells. Blood. 2007, 109(8), 3470-3478.
- GA Bartholomeusz et al. Degrasyn activates proteasomal-dependent degradation of c-Myc. Cancer Res. 2007, 67(8), 3912-3918.
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