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| Product Name: | WP1130 | | Synonyms: | WP1130;(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide;WP1130;WP 1130;WP-1130;CS-701;DEGRASYN; WP 1130; WP-1130;Degrasyn;Degrasyn (WP1130);WP1130 ( Degrasyn ) | | CAS: | 856243-80-6 | | MF: | C19H18BrN3O | | MW: | 384.27 | | EINECS: | 604-604-1 | | Product Categories: | Inhibitor;Inhibitors | | Mol File: | 856243-80-6.mol |  |
| | WP1130 Chemical Properties |
| density | 1.358 | | storage temp. | -20° | | solubility | Soluble in DMSO (up to 45 mg/ml), or in Ethanol (up to 25 mg/ml). | | form | solid | | color | Yellow | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| | WP1130 Usage And Synthesis |
| Description | WP1130 (856243-80-6) is a novel DUB inhibitor directly inhibiting USP9x, USP5, USP14 and UCH37 inducing rapid accumulation of polyubiquitinated proteins. Triggers tumor cell apoptosis.1 Blocks Jak2 signaling via Jak2 ubiquitination.2 WP-1130 causes ablation of the oncogenic transcription factor ERG in prostate cancer cells.3 See methyl analog WP1066. | | Uses | (2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide can be used in biological study of drug screening and proteomic and metabolomic profiling to identify drug action mechanisms of breast cancer impaired pathogenicity. | | target | DUB | | References | 1) Kapuria et al. (2010), Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis; Cancer Res., 70 9265
2) Kapuria et al. (2011), A novel small molecule deubiquitinase inhibitor blocks Jak2 signaling through Jak2 ubiquitination; Cell Signal., 23 2076
3) Wang et al. (2014), Ablation of the oncogenic transcription factor ERG by deubiquitinase inhibition in prostate cancer; Proc. Natl. Acad. Sci. USA, 111 4251 |
| | WP1130 Preparation Products And Raw materials |
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