Identification | More | [Name]
Degrasyn (WP1130) | [CAS]
856243-80-6 | [Synonyms]
WP1130 Degrasyn Degrasyn (WP1130) WP1130 ( Degrasyn ) (S,E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylbutyl)acrylamide (2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide (2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide Degrasyn (WP1130) | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C19H18BrN3O | [MDL Number]
MFCD18839228 | [MOL File]
856243-80-6.mol | [Molecular Weight]
384.27 |
Chemical Properties | Back Directory | [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. |
Hazard Information | Back Directory | [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. | [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 |
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NCE Biomedical Co.,Ltd.
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