WP-1130（Cat No.:I005136）is a small molecule inhibitor of the deubiquitinating enzyme USP14, which plays a critical role in regulating protein degradation via the ubiquitin-proteasome pathway. By inhibiting USP14, WP-1130 enhances the proteasomal degradation of specific substrates, including misfolded and damaged proteins, thereby promoting apoptosis in cancer cells. It has shown potential in preclinical studies for treating various cancers, particularly hematological malignancies. Additionally, WP-1130 may have therapeutic implications in neurodegenerative diseases by reducing the accumulation of toxic proteins. Its selectivity for USP14 makes it a promising candidate for targeted cancer therapies.
| Catalog Number | I005136 |
| CAS Number | 856243-80-6 |
| Synonyms | (E)-3-(6-bromopyridin-2-yl)-2-cyano-N-[(1S)-1-phenylbutyl]prop-2-enamide |
| Molecular Formula | C₁₉H₁₈BrN₃O |
| Purity | ≥95% |
| Target | DUB |
| Solubility | DMSO: ≥ 33 mg/mL |
| Storage | 3 years -20℃ powder |
| IUPAC Name | (E)-3-(6-bromopyridin-2-yl)-2-cyano-N-[(1S)-1-phenylbutyl]prop-2-enamide |
| 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 |
| SMILES | CCCC(C1=CC=CC=C1)NC(=O)C(=CC2=NC(=CC=C2)Br)C#N |
| Reference | </br>1:WP1130 increases cisplatin sensitivity through inhibition of <i>usp9x</i> in estrogen receptor-negative breast cancer cells. Fu P, Du F, Liu Y, Yao M, Zhang S, Zheng X, Zheng S.Am J Transl Res. 2017 Apr 15;9(4):1783-1791. eCollection 2017. PMID: 28469783 Free PMC Article</br>2:WP1130 attenuates cisplatin resistance by decreasing P53 expression in non-small cell lung carcinomas. Wang X, Bao Y, Dong Z, Chen Q, Guo H, Xiang C, Shao J.Oncotarget. 2017 Apr 7. doi: 10.18632/oncotarget.16931. [Epub ahead of print] PMID: 28446729 Free Article</br>3:Deubiquitinase inhibition by WP1130 leads to ULK1 aggregation and blockade of autophagy. Drießen S, Berleth N, Friesen O, Löffler AS, Böhler P, Hieke N, Stuhldreier F, Peter C, Schink KO, Schultz SW, Stenmark H, Holland P, Simonsen A, Wesselborg S, Stork B.Autophagy. 2015;11(9):1458-70. doi: 10.1080/15548627.2015.1067359. PMID: 26207339 Free PMC Article</br>4:WP1130 increases doxorubicin sensitivity in hepatocellular carcinoma cells through usp9x-dependent p53 degradation. Liu H, Chen W, Liang C, Chen BW, Zhi X, Zhang S, Zheng X, Bai X, Liang T.Cancer Lett. 2015 Jun 1;361(2):218-25. doi: 10.1016/j.canlet.2015.03.001. Epub 2015 Mar 5. PMID: 25749422 </br>5:Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis. Kapuria V, Peterson LF, Fang D, Bornmann WG, Talpaz M, Donato NJ.Cancer Res. 2010 Nov 15;70(22):9265-76. doi: 10.1158/0008-5472.CAN-10-1530. Epub 2010 Nov 2. PMID: 21045142 Free Article</br>6:Activation of a novel Bcr/Abl destruction pathway by WP1130 induces apoptosis of chronic myelogenous leukemia cells. Bartholomeusz GA, Talpaz M, Kapuria V, Kong LY, Wang S, Estrov Z, Priebe W, Wu J, Donato NJ.Blood. 2007 Apr 15;109(8):3470-8. Epub 2007 Jan 3. PMID: 17202319 Free PMC Article |
